PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 2996557-3 1985 Omeprazole, a substituted benzimidazole, while almost completely abolishing acid production at 10(-4) M, strongly stimulated secretion of preformed and newly synthesized pepsinogen. benzimidazole 26-39 pepsin II-2/3 Oryctolagus cuniculus 170-180 6326439-1 1984 A number of acyclo nucleosides of benzimidazole derivatives has been synthesized, in which the benzimidazole ring includes substituents at C(5), C(6) and C(2). benzimidazole 34-47 complement C5 Homo sapiens 139-143 6326439-1 1984 A number of acyclo nucleosides of benzimidazole derivatives has been synthesized, in which the benzimidazole ring includes substituents at C(5), C(6) and C(2). benzimidazole 34-47 complement C6 Homo sapiens 145-149 6326439-1 1984 A number of acyclo nucleosides of benzimidazole derivatives has been synthesized, in which the benzimidazole ring includes substituents at C(5), C(6) and C(2). benzimidazole 34-47 complement C2 Homo sapiens 154-158 6326439-1 1984 A number of acyclo nucleosides of benzimidazole derivatives has been synthesized, in which the benzimidazole ring includes substituents at C(5), C(6) and C(2). benzimidazole 95-108 complement C5 Homo sapiens 139-143 6326439-1 1984 A number of acyclo nucleosides of benzimidazole derivatives has been synthesized, in which the benzimidazole ring includes substituents at C(5), C(6) and C(2). benzimidazole 95-108 complement C6 Homo sapiens 145-149 6326439-1 1984 A number of acyclo nucleosides of benzimidazole derivatives has been synthesized, in which the benzimidazole ring includes substituents at C(5), C(6) and C(2). benzimidazole 95-108 complement C2 Homo sapiens 154-158 6419624-0 1983 Effects of KCl and insulin on benzimidazole-inhibited canine gastric secretion. benzimidazole 30-43 insulin Canis lupus familiaris 19-26 7097715-2 1982 Effects of benzimidazole and related compounds on aryl hydrocarbon hydroxylase activity from phenobarbitone and 3-methylcholanthrene induced rats. benzimidazole 11-24 cytochrome P450, family 1, subfamily a, polypeptide 1 Rattus norvegicus 50-78 6825202-1 1983 A series of benzimidazole derivatives containing additional fused and non-fused aromatic groupings were effective inhibitors of aryl hydrocarbon hydroxylase (PB/AHH) and aminopyrine N-demethylase (ADPM) activities in hepatic microsomes from phenobarbitone(PB)-induced rats. benzimidazole 12-25 cytochrome P450, family 1, subfamily a, polypeptide 1 Rattus norvegicus 128-156 6825202-1 1983 A series of benzimidazole derivatives containing additional fused and non-fused aromatic groupings were effective inhibitors of aryl hydrocarbon hydroxylase (PB/AHH) and aminopyrine N-demethylase (ADPM) activities in hepatic microsomes from phenobarbitone(PB)-induced rats. benzimidazole 12-25 cytochrome P450, family 1, subfamily a, polypeptide 1 Rattus norvegicus 161-164 849331-0 1977 N-Methylation of benzimidazole by catechol-O-methyltransferase. benzimidazole 17-30 catechol-O-methyltransferase Homo sapiens 34-62 361093-6 1978 The data presented suggest that several sites of both the tubulin and ligand molecule are involved in the binding of benzimidazole compounds to fungal tubulin. benzimidazole 117-130 PEX2_027410 Penicillium expansum 58-65 361093-6 1978 The data presented suggest that several sites of both the tubulin and ligand molecule are involved in the binding of benzimidazole compounds to fungal tubulin. benzimidazole 117-130 PEX2_027410 Penicillium expansum 151-158 284380-2 1979 It is shown that analogs with methyl, amino, or methylamino substituents at position 2 of the benzimidazole ring (position 8 of the purine ring) have predominantly anti conformations, whereas analogs with chloro, aza, methoxy, or methylmercapto substituents have predominantly syn conformations. benzimidazole 94-107 synemin Homo sapiens 277-280 33979615-3 2021 Here, we show that PIF proteins control apical hook opening by regulating the expression of Budding Uninhibited by Benzimidazole 3.1 (BUB3.1) and affecting cytokinesis. benzimidazole 115-128 Transducin/WD40 repeat-like superfamily protein Arabidopsis thaliana 134-140 13653104-0 1959 [Pharmacological study of an antihistaminic from the benzimidazole series: 1-p-chlorobenzyl-2-(1-pyrrolidinylmethyl)-benzimidazole (P-48)]. benzimidazole 53-66 interferon regulatory factor 9 Homo sapiens 132-136 33789191-0 2021 Selective, pH sensitive, "turn on" fluorescence sensing of carbonate ions by a benzimidazole. benzimidazole 79-92 phenylalanine hydroxylase Homo sapiens 11-13 33789191-3 2021 A pH-sensitive & selective benzimidazole-based fluorescent sensor has been developed for rapid detection of carbonate ions which can detect carbonate ions in low nanomolar concentrations. benzimidazole 27-40 phenylalanine hydroxylase Homo sapiens 2-4 34029540-0 2021 Design, synthesis, and antitumor activity of PLGA nanoparticles incorporating a discovered benzimidazole derivative as EZH2 inhibitor. benzimidazole 91-104 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 119-123 33348096-2 2021 In this work, a novel quinoline-benzimidazole conjugate containing one carboxylic acid group (QBM) was designed, and the QBM displayed highly selective fluorescence quenching response towards Pd2+ over other metal cations in aqueous solution. benzimidazole 32-45 PAF1 homolog, Paf1/RNA polymerase II complex component Homo sapiens 192-195 33842435-0 2021 New Cationic fac-[Re(CO)3(deeb)B2]+ Complex, Where B2 Is a Benzimidazole Derivative, as a Potential New Luminescent Dye for Proteins Separated by SDS-PAGE. benzimidazole 59-72 FA complementation group C Homo sapiens 13-16 31135232-0 2021 Investigation of the toxicological and inhibitory effects of some benzimidazole agents on acetylcholinesterase and butyrylcholinesterase enzymes. benzimidazole 66-79 acetylcholinesterase (Cartwright blood group) Homo sapiens 90-110 31135232-0 2021 Investigation of the toxicological and inhibitory effects of some benzimidazole agents on acetylcholinesterase and butyrylcholinesterase enzymes. benzimidazole 66-79 butyrylcholinesterase Homo sapiens 115-136 33626870-2 2021 Here, several benzimidazole derivatives have been identified as novel agonists of the melatonin receptors MT1 and MT2. benzimidazole 14-27 metallothionein 1 Rattus norvegicus 106-109 33663368-0 2022 Synthesis of Some Novel Benzimidazole Derivatives as Anticancer Agent, and Evaluation for CDK2 Inhibition Activity. benzimidazole 24-37 cyclin dependent kinase 2 Homo sapiens 90-94 33626870-2 2021 Here, several benzimidazole derivatives have been identified as novel agonists of the melatonin receptors MT1 and MT2. benzimidazole 14-27 metallothionein 2A Rattus norvegicus 114-117 32955008-0 2021 Repurposing of Benzimidazole Scaffolds for HER-2 Positive Breast Cancer Therapy: An In-Silico Approach. benzimidazole 15-28 erb-b2 receptor tyrosine kinase 2 Homo sapiens 43-48 33738049-0 2021 Novel Benzimidazole Derivatives as Transient Receptor Potential Channel 6 (TRPC6) Inhibitors. benzimidazole 6-19 transient receptor potential cation channel subfamily C member 6 Homo sapiens 35-73 33738049-0 2021 Novel Benzimidazole Derivatives as Transient Receptor Potential Channel 6 (TRPC6) Inhibitors. benzimidazole 6-19 transient receptor potential cation channel subfamily C member 6 Homo sapiens 75-80 33535550-0 2021 Design, Synthesis, Anticancer Activity, and Solid Lipid Nanoparticle Formulation of Indole- and Benzimidazole-Based Compounds as Pro-Apoptotic Agents Targeting Bcl-2 Protein. benzimidazole 96-109 BCL2 apoptosis regulator Homo sapiens 160-165 33535550-3 2021 Within the current work, we aimed to design and synthesize a new series of benzimidazole- and indole-based derivatives as inhibitors of Bcl-2 protein. benzimidazole 75-88 BCL2 apoptosis regulator Homo sapiens 136-141 33285268-0 2021 Discovery of a benzimidazole series as the first highly potent and selective ACSL1 inhibitors. benzimidazole 15-28 acyl-CoA synthetase long-chain family member 1 Mus musculus 77-82 33285268-2 2021 Structure activity relationship studies based on HTS hit compound 1 delivered the benzimidazole series as the first selective and highly potent ACSL1 inhibitors. benzimidazole 82-95 acyl-CoA synthetase long-chain family member 1 Mus musculus 144-149 33494672-6 2021 Results and Conclusion: It was observed that structures of the GSK-3 inhibitors comprised of benzopyridine, benzthiazole, pyrazole, pyrazine, dioxolo-benzoxazin, oxadiazole, benzimidazole in the skeletal with cyclopropylamide, phenyl carbamothioate, 3-[(propan-2-yl)oxy]propan-1-amine in side chain. benzimidazole 174-187 glycogen synthase kinase 3 beta Mus musculus 63-68 33090631-1 2021 Multi ligand self-assembly to attain the AgI-NHC built hexanuclear organometallic cages of composition [Ag6(3a,b)4](PF6)6 from the reaction of benzimidazole derived tris(azolium) salts [H3-3a,b](PF6)3 with Ag2O is presented. benzimidazole 143-156 H3.3 histone A Homo sapiens 186-193 33092905-4 2021 Here we utilized the azaindole-based scaffold of FDA-approved BRAF inhibitor vemurafenib 1, which displays off-target activity on MKK4, as a starting point in our fluorescent compound design. benzimidazole 21-30 B-Raf proto-oncogene, serine/threonine kinase Homo sapiens 62-66 33092905-4 2021 Here we utilized the azaindole-based scaffold of FDA-approved BRAF inhibitor vemurafenib 1, which displays off-target activity on MKK4, as a starting point in our fluorescent compound design. benzimidazole 21-30 mitogen-activated protein kinase kinase 4 Homo sapiens 130-134 32575154-6 2020 Benzimidazole derivative having 4-methoxyphenyl substitution (compound 25) was found to be a selective MAGL inhibitor (IC50 = 9.4 nM), with an IC50 value above 50 microM against FAAH. benzimidazole 0-13 monoglyceride lipase Homo sapiens 103-107 33391284-3 2020 Utilizing a recently established TRPC3/6/7 selective, photochromic benzimidazole agonist OptoBI-1, we set out to test this concept for mast cell NFAT signaling. benzimidazole 67-80 transient receptor potential cation channel, subfamily C, member 3 Rattus norvegicus 33-42 33210922-4 2020 In this work, we present the development of a novel class of azaindole SHP2 inhibitors. benzimidazole 61-70 protein tyrosine phosphatase non-receptor type 11 Homo sapiens 71-75 33210922-6 2020 The most potent azaindole 45 inhibits SHP2 with an IC50 = 0.031 muM in an enzymatic assay and with an IC50 = 2.6 muM in human pancreas cells (HPAF-II). benzimidazole 16-25 protein tyrosine phosphatase non-receptor type 11 Homo sapiens 38-42 33174071-2 2021 Results from the in vivo and in vitro tests were compared with benzimidazole (BZ)-resistance-associated beta-tubulin allele frequencies determined using Pyrosequencing . benzimidazole 63-76 beta-tubulin Ovis aries 104-116 33174071-2 2021 Results from the in vivo and in vitro tests were compared with benzimidazole (BZ)-resistance-associated beta-tubulin allele frequencies determined using Pyrosequencing . benzimidazole 78-80 beta-tubulin Ovis aries 104-116 33174071-6 2021 Genotyping indicated that the susceptible strain had 10% BZ-resistant beta-tubulin codon 200 alleles and the resistant strain had 26% respective resistant alleles. benzimidazole 57-59 beta-tubulin Ovis aries 70-82 33391284-6 2020 Expression of any of three benzimidazole-sensitive TRPC isoforms (TRPC3/6/7) reconstituted plasma membrane TRPC conductances in RBL cells, and expression of TRPC6 or TRPC7 enabled light-mediated generation of temporally defined Ca2+ signaling patterns. benzimidazole 27-40 transient receptor potential cation channel, subfamily C, member 3 Rattus norvegicus 66-75 33391284-6 2020 Expression of any of three benzimidazole-sensitive TRPC isoforms (TRPC3/6/7) reconstituted plasma membrane TRPC conductances in RBL cells, and expression of TRPC6 or TRPC7 enabled light-mediated generation of temporally defined Ca2+ signaling patterns. benzimidazole 27-40 transient receptor potential cation channel, subfamily C, member 6 Rattus norvegicus 157-162 33391284-6 2020 Expression of any of three benzimidazole-sensitive TRPC isoforms (TRPC3/6/7) reconstituted plasma membrane TRPC conductances in RBL cells, and expression of TRPC6 or TRPC7 enabled light-mediated generation of temporally defined Ca2+ signaling patterns. benzimidazole 27-40 transient receptor potential cation channel, subfamily C, member 7 Rattus norvegicus 166-171 32575154-6 2020 Benzimidazole derivative having 4-methoxyphenyl substitution (compound 25) was found to be a selective MAGL inhibitor (IC50 = 9.4 nM), with an IC50 value above 50 microM against FAAH. benzimidazole 0-13 fatty acid amide hydrolase Homo sapiens 178-182 33207204-2 2020 A major player in determining this balance is the PP2A-B56 phosphatase, which is recruited to the kinase attachment regulatory domain (KARD) of budding uninhibited by benzimidazole 1-related 1 (BUBR1) in a phospho-dependent manner. benzimidazole 167-180 BUB1 mitotic checkpoint serine/threonine kinase B Homo sapiens 194-199 32738568-0 2020 Novel benzimidazole-triazole hybrids as apoptosis inducing agents in lung cancer: Design, synthesis, 18F-radiolabeling & galectin-1 inhibition studies. benzimidazole 6-19 galectin 1 Homo sapiens 121-131 32466633-4 2020 MeBib is an HDAC6 inhibitor derived from a benzimidazole scaffold. benzimidazole 43-56 histone deacetylase 6 Rattus norvegicus 12-17 33247742-8 2020 CONCLUSIONS: The degradation products were identified as benzimidazole (DP1) and amine N-oxide of bilastine (DP2). benzimidazole 57-70 prostaglandin D2 receptor Homo sapiens 72-75 32981322-0 2020 Design, Synthesis and Characterization of Benzimidazole Derivatives as PET Imaging Ligands for Metabotropic Glutamate Receptor 2 (mGluR2). benzimidazole 42-55 glutamate metabotropic receptor 2 Rattus norvegicus 95-128 32981322-0 2020 Design, Synthesis and Characterization of Benzimidazole Derivatives as PET Imaging Ligands for Metabotropic Glutamate Receptor 2 (mGluR2). benzimidazole 42-55 glutamate receptor, ionotropic, AMPA2 (alpha 2) Mus musculus 130-136 32981322-1 2020 Three benzimidazole derivatives (13-15) have been synthetized as potential PET imaging ligands for mGluR2 in the brain. benzimidazole 6-19 glutamate receptor, ionotropic, AMPA2 (alpha 2) Mus musculus 99-105 32881503-2 2020 The prodrug moiety is attached to a benzimidazole nitrogen via an oxymethyl linkage to allow for rapid and complete release of the drug for absorption following phosphate removal by intestinal alkaline phosphatase. benzimidazole 36-49 alkaline phosphatase, intestinal Mus musculus 182-213 32681791-0 2020 Synthesis, investigation of biological effects and in silico studies of new benzimidazole derivatives as aromatase inhibitors. benzimidazole 76-89 cytochrome P450 family 19 subfamily A member 1 Homo sapiens 105-114 32777641-2 2020 High-throughput virtual screening (HTVS) of a Maybridge small molecule library using the PARP1-benzimidazole-4-carboxamide co-crystal structure and pharmacophore model led to the identification of eleven compounds. benzimidazole 95-108 poly(ADP-ribose) polymerase 1 Homo sapiens 89-94 32738568-1 2020 In this study, we have synthesized a new series of benzimidazole-triazole hybrids as galectin-1 (gal-1) mediated apoptosis-inducing agents, and evaluated for their potential anticancer activity against a panel of human cancer cell lines viz. benzimidazole 51-64 galectin 1 Homo sapiens 85-95 32738568-1 2020 In this study, we have synthesized a new series of benzimidazole-triazole hybrids as galectin-1 (gal-1) mediated apoptosis-inducing agents, and evaluated for their potential anticancer activity against a panel of human cancer cell lines viz. benzimidazole 51-64 galectin 1 Homo sapiens 97-102 32738568-12 2020 Therefore, the novel benzimidazole-triazole hybrids as apoptosis-inducing agents in lung cancer would be potential cytotoxic and PET imaging agents via gal-1. benzimidazole 21-34 galectin 1 Homo sapiens 152-157 32874920-7 2020 Primary cultured rat and human hepatocytes were considered to be useful for the evaluation of effects of the benzimidazole compounds on their inducibility and inhibitory activities of cytochrome P450 forms. benzimidazole 109-122 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 184-199 32298535-4 2020 Inspired by the pharmacodynamics of HYL-6d and the selective PPARgamma ligand VSP-51, the benzimidazole was replaced by a carbazole or an indole core . benzimidazole 91-104 peroxisome proliferator activated receptor gamma Homo sapiens 62-71 32713342-0 2021 Design, Synthesis and invitro biological evaluation of Pyridine,thiadazole, Benzimidazole and Acetyl thiophneAnalogues as Anti tubercular Agents Targeting enzyme InhA. benzimidazole 76-89 inhibin subunit alpha Homo sapiens 162-166 32713342-4 2021 METHODS: Thus, a series of Pyridine, Thiadiazole, Benzimidazole; and Acetyl thiophene based molecules were designed and docked against crucial mtb enzyme target InhA (Enoyl Acyl Carrier Protein Reductase) Enzyme. benzimidazole 50-63 inhibin subunit alpha Homo sapiens 161-165 31382868-4 2020 An interesting benzimidazole fragment was selected from the in silico studies and presented as potential zing binding group for the development of novel HDAC6 selective inhibitors. benzimidazole 15-28 histone deacetylase 6 Homo sapiens 153-158 32344183-0 2020 Synthesis and anticancer evaluation of novel 1H-benzo[d]imidazole derivatives of dehydroabietic acid as PI3Kalpha inhibitors. benzimidazole 45-65 phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha Homo sapiens 104-113 32120825-4 2020 Here, we report efficient control of NFAT1 nuclear translocation in human embryonic kidney 293 (HEK293) cells by light, using a new photochromic TRPC benzimidazole activator (OptoBI-1) and a TRPC3 mutant with modified activator sensitivity. benzimidazole 150-163 nuclear factor of activated T cells 2 Homo sapiens 37-42 32251945-0 2020 Discovery of novel dual PPARalpha/delta agonists based on benzimidazole scaffold for the treatment of non-alcoholic fatty liver disease. benzimidazole 58-71 peroxisome proliferator activated receptor alpha Homo sapiens 24-33 32426613-7 2020 Moreover, these devices exhibited lower efficiency roll-off than the CBP-hosted device using the same emitters, which demonstrated the bipolar charge carrier property of carbazole/benzimidazole-based molecules. benzimidazole 180-193 CREB binding protein Homo sapiens 69-72 32150677-0 2020 Discovery of Highly Potent Benzimidazole Derivatives as Indoleamine 2,3-Dioxygenase-1 (IDO1) Inhibitors: From Structure-Based Virtual Screening to in Vivo Pharmacodynamic Activity. benzimidazole 27-40 indoleamine 2,3-dioxygenase 1 Homo sapiens 56-85 32150677-0 2020 Discovery of Highly Potent Benzimidazole Derivatives as Indoleamine 2,3-Dioxygenase-1 (IDO1) Inhibitors: From Structure-Based Virtual Screening to in Vivo Pharmacodynamic Activity. benzimidazole 27-40 indoleamine 2,3-dioxygenase 1 Homo sapiens 87-91 32150677-1 2020 In this study, a successful medicinal chemistry campaign that exploited virtual, biophysical, and biological investigations led to the identification of a novel class of IDO1 inhibitors based on a benzimidazole substructure. benzimidazole 197-210 indoleamine 2,3-dioxygenase 1 Homo sapiens 170-174 32307260-0 2020 Synthesis, state-of-the-art NMR-binding and molecular modeling study of new benzimidazole core derivatives as Pin1 inhibitors: Targeting breast cancer. benzimidazole 76-89 peptidylprolyl cis/trans isomerase, NIMA-interacting 1 Homo sapiens 110-114 32169404-0 2020 Interruption of Vif/Elongin C interaction: In silico and experimental elucidation of the underlying molecular mechanism of benzimidazole-based APOBEC3G stabilizers. benzimidazole 123-136 Vif Human immunodeficiency virus 1 16-19 32169404-0 2020 Interruption of Vif/Elongin C interaction: In silico and experimental elucidation of the underlying molecular mechanism of benzimidazole-based APOBEC3G stabilizers. benzimidazole 123-136 elongin C Homo sapiens 20-29 32169404-0 2020 Interruption of Vif/Elongin C interaction: In silico and experimental elucidation of the underlying molecular mechanism of benzimidazole-based APOBEC3G stabilizers. benzimidazole 123-136 apolipoprotein B mRNA editing enzyme catalytic subunit 3G Homo sapiens 143-151 32169404-1 2020 In 2014, two novel and promising benzimidazole-based APOBEC3G stabilizers MM-1 and MM-2 (MMs) were uncovered with an elusive mechanism of action. benzimidazole 33-46 apolipoprotein B mRNA editing enzyme catalytic subunit 3G Homo sapiens 53-61 32169404-1 2020 In 2014, two novel and promising benzimidazole-based APOBEC3G stabilizers MM-1 and MM-2 (MMs) were uncovered with an elusive mechanism of action. benzimidazole 33-46 plexin B2 Homo sapiens 74-78 32169404-1 2020 In 2014, two novel and promising benzimidazole-based APOBEC3G stabilizers MM-1 and MM-2 (MMs) were uncovered with an elusive mechanism of action. benzimidazole 33-46 PNMA family member 2 Homo sapiens 83-87 32014680-0 2020 Structural features and functional activities of benzimidazoles as NOD2 antagonists. benzimidazole 49-63 nucleotide binding oligomerization domain containing 2 Homo sapiens 67-71 31854124-5 2020 To circumvent legislative control measures, SCRA manufacturers have created a wide range of SCRA analogs that contain, more recently, previously unencountered azaindole, gamma-carbolinone, or carbazole heterocyclic scaffolds. benzimidazole 159-168 anillin, actin binding protein Homo sapiens 44-48 31854124-5 2020 To circumvent legislative control measures, SCRA manufacturers have created a wide range of SCRA analogs that contain, more recently, previously unencountered azaindole, gamma-carbolinone, or carbazole heterocyclic scaffolds. benzimidazole 159-168 anillin, actin binding protein Homo sapiens 92-96 31669219-0 2020 Benzimidazole-based dual dipeptidyl peptidase-4 and xanthine oxidase inhibitors. benzimidazole 0-13 dipeptidyl peptidase 4 Homo sapiens 25-47 32053964-0 2020 Targeting Receptor Tyrosine Kinase VEGFR-2 in Hepatocellular Cancer: Rational Design, Synthesis and Biological Evaluation of 1,2-Disubstituted Benzimidazoles. benzimidazole 125-157 kinase insert domain receptor Homo sapiens 35-42 32053964-3 2020 Our second objective was to further optimize the structures of the benzimidazole derivatives through elongation of the side chains at their one-position for the design of more potent type II-like VEGFR-2 inhibitors. benzimidazole 67-80 kinase insert domain receptor Homo sapiens 196-203 32053964-4 2020 The designed 1,2-disubstituted benzimidazoles demonstrated potent cytotoxic activity against the HepG2 cell line, reaching IC50 = 1.98 muM in comparison to sorafenib (IC50 = 10.99 muM). benzimidazole 31-45 latexin Homo sapiens 135-138 32053964-4 2020 The designed 1,2-disubstituted benzimidazoles demonstrated potent cytotoxic activity against the HepG2 cell line, reaching IC50 = 1.98 muM in comparison to sorafenib (IC50 = 10.99 muM). benzimidazole 31-45 latexin Homo sapiens 180-183 32053964-7 2020 Molecular docking studies of the synthesized 1,2-disubstituted benzimidazoles in the VEGFR-2 active site displayed their ability to accomplish the essential hydrogen bonding and hydrophobic interactions for optimum inhibitory activity. benzimidazole 63-77 kinase insert domain receptor Homo sapiens 85-92 31922163-1 2020 The mild and efficient palladium-catalyzed ortho C(sp2)-H diversification of (NH)-free 2-substituted benzimidazole, quinazoline, and imidazopyridine is reported using hypervalent iodine as the key reagent. benzimidazole 101-114 Sp2 transcription factor Homo sapiens 49-54 31450223-3 2020 Here, we have investigated the mechanism of interaction between AGP and potential Cu/Zn metallo-drugs of benzimidazole derived organic motifs (CuL2 and ZnL2, where L is Schiff base ligand) by applying integrated spectroscopic, biophysical techniques and computational molecular docking analyses. benzimidazole 105-118 cullin 2 Homo sapiens 143-147 31669219-3 2020 In this study a small series of benzimidazole derivatives (1-9) was evaluated for inhibitory activity against dipeptidyl peptidase-4 (DPP-4) and XO. benzimidazole 32-45 dipeptidyl peptidase 4 Homo sapiens 110-132 31669219-3 2020 In this study a small series of benzimidazole derivatives (1-9) was evaluated for inhibitory activity against dipeptidyl peptidase-4 (DPP-4) and XO. benzimidazole 32-45 dipeptidyl peptidase 4 Homo sapiens 134-139 31838286-0 2020 Synthesis and biological evaluation of new benzimidazole-1,2,3-triazole hybrids as potential alpha-glucosidase inhibitors. benzimidazole 43-71 sucrase-isomaltase Homo sapiens 93-110 31699396-0 2020 Synthesis, in vitro alpha-glucosidase inhibitory potential of benzimidazole bearing bis-Schiff bases and their molecular docking study. benzimidazole 62-75 sucrase-isomaltase Homo sapiens 20-37 31699396-5 2020 Current study deals with the synthesis and biological screening of benzimidazole bearing bis-Schiff bases (1-19) for their alpha-glucosidase inhibitory activity. benzimidazole 67-80 sucrase-isomaltase Homo sapiens 123-140 32357823-0 2020 Synthesis of Some Benzimidazole-derived Molecules and Their Effects on PARP-1 Activity and MDA-MB-231, MDA-MB-436, MDA-MB-468 Breast Cancer Cell Viability. benzimidazole 18-31 poly(ADP-ribose) polymerase 1 Homo sapiens 71-77 31838286-1 2020 In this study, a series of benzimidazole-1,2,3-triazole hybrids 8a-n as new alpha-glucosidase inhibitors were designed and synthesized. benzimidazole 27-55 sucrase-isomaltase Homo sapiens 76-93 31571509-3 2019 Several benzimidazole derivatives 5a-5g and 6a-6c containing various hydrophobic moieties were synthesised, and their inhibitory activity against FLT3 was evaluated. benzimidazole 8-21 fms related receptor tyrosine kinase 3 Homo sapiens 146-150 31408200-2 2019 Recently, anthelminthic benzimidazoles were shown to promote HIF-1alpha transcription in vitro and were proposed to activate Nurr1 via their benzimidazole group. benzimidazole 24-37 hypoxia inducible factor 1 subunit alpha Rattus norvegicus 61-71 31408200-2 2019 Recently, anthelminthic benzimidazoles were shown to promote HIF-1alpha transcription in vitro and were proposed to activate Nurr1 via their benzimidazole group. benzimidazole 24-37 nuclear receptor subfamily 4, group A, member 2 Rattus norvegicus 125-130 31915112-2 2020 The newly synthesized benzimidazole derivatives were evaluated against 4 physiologically relevant CA isoforms (hCA I, II, IX, and XII), and especially the sulfonamide-containing benzimidazoles demonstrated intriguing inhibitory activity against tumor associated CA IX and XII with KI values in the range of 5.2-29.3 nM and 9.9-41.7 nM, respectively. benzimidazole 22-35 HCA1 Homo sapiens 98-100 31915112-2 2020 The newly synthesized benzimidazole derivatives were evaluated against 4 physiologically relevant CA isoforms (hCA I, II, IX, and XII), and especially the sulfonamide-containing benzimidazoles demonstrated intriguing inhibitory activity against tumor associated CA IX and XII with KI values in the range of 5.2-29.3 nM and 9.9-41.7 nM, respectively. benzimidazole 22-35 cytochrome P450 family 24 subfamily A member 1 Homo sapiens 111-133 31915112-2 2020 The newly synthesized benzimidazole derivatives were evaluated against 4 physiologically relevant CA isoforms (hCA I, II, IX, and XII), and especially the sulfonamide-containing benzimidazoles demonstrated intriguing inhibitory activity against tumor associated CA IX and XII with KI values in the range of 5.2-29.3 nM and 9.9-41.7 nM, respectively. benzimidazole 22-35 carbonic anhydrase 9 Homo sapiens 262-267 31915112-2 2020 The newly synthesized benzimidazole derivatives were evaluated against 4 physiologically relevant CA isoforms (hCA I, II, IX, and XII), and especially the sulfonamide-containing benzimidazoles demonstrated intriguing inhibitory activity against tumor associated CA IX and XII with KI values in the range of 5.2-29.3 nM and 9.9-41.7 nM, respectively. benzimidazole 178-192 HCA1 Homo sapiens 98-100 31915112-2 2020 The newly synthesized benzimidazole derivatives were evaluated against 4 physiologically relevant CA isoforms (hCA I, II, IX, and XII), and especially the sulfonamide-containing benzimidazoles demonstrated intriguing inhibitory activity against tumor associated CA IX and XII with KI values in the range of 5.2-29.3 nM and 9.9-41.7 nM, respectively. benzimidazole 178-192 cytochrome P450 family 24 subfamily A member 1 Homo sapiens 111-133 31915112-2 2020 The newly synthesized benzimidazole derivatives were evaluated against 4 physiologically relevant CA isoforms (hCA I, II, IX, and XII), and especially the sulfonamide-containing benzimidazoles demonstrated intriguing inhibitory activity against tumor associated CA IX and XII with KI values in the range of 5.2-29.3 nM and 9.9-41.7 nM, respectively. benzimidazole 178-192 carbonic anhydrase 9 Homo sapiens 262-267 33602088-0 2020 Synthesis, Molecular Docking, and Biological Evaluation of Benzimidazole Derivatives as Selective Butyrylcholinesterase Inhibitors. benzimidazole 59-72 butyrylcholinesterase Homo sapiens 98-119 33602088-1 2020 Benzimidazole is an interesting pharmacophore, and its derivatives have been previously shown to possess cholinesterase inhibitory activity. benzimidazole 0-13 butyrylcholinesterase Homo sapiens 105-119 33602088-2 2020 In this study, benzimidazole derivatives were synthesized via a 4-step reaction scheme and screened for their acetylcholinesterase and butyrylcholinesterase inhibitory activities. benzimidazole 15-28 butyrylcholinesterase Homo sapiens 135-156 31678134-3 2020 Modeling of the interaction of new benzoxazole and benzimidazole derivatives with androgen receptor revealed the destabilization of helix 12, constituting activation function 2 (AF2) site, by mentioned compounds, similar to one induced by known antagonist galeterone. benzimidazole 51-64 androgen receptor Homo sapiens 82-99 31787052-2 2019 BubR1 (budding uninhibited by benzimidazole-related 1) is a multifaceted kinase that functions as a mitotic checkpoint. benzimidazole 30-43 BUB1B, mitotic checkpoint serine/threonine kinase Mus musculus 0-5 30422010-2 2019 A series of 6,7-dimethoxy-4-anilinoquinolines possessing benzimidazole moiety were synthesised and identified as potent inhibitors of the tyrosine kinase c-Met. benzimidazole 57-70 MET proto-oncogene, receptor tyrosine kinase Homo sapiens 154-159 31754201-7 2019 We showed that treatment with a benzimidazole derivative bearing a pyrrolidine side chain (compound 9a) inhibited the proliferation of SR cells by blocking the phosphorylation of AKT, p70S6 and the downstream molecule RPS6. benzimidazole 32-45 ribosomal protein S6 Homo sapiens 218-222 31728454-1 2019 A series of Schiff bases (3.a-f) bearing benzimidazole moiety was successfully synthesized in ethanol by refluxing Oct-2-ynoic acid (1,3-dihydrobenzimidazole-2-ylidene)amide with substituted amines. benzimidazole 41-54 POU class 2 homeobox 2 Homo sapiens 115-120 31744088-3 2019 In this study, we synthesized novel FXR agonists 1-4 possessing isoxazole and N-substituted benzimidazole moieties, and compared their effects on osteoblast differentiation with the known FXR agonists, chenodeoxycholic acid and a synthetic compound, GW4064. benzimidazole 92-105 nuclear receptor subfamily 1, group H, member 4 Mus musculus 36-39 31252306-0 2019 Design, synthesis and in vitro evaluation of 6-amide-2-aryl benzoxazole/benzimidazole derivatives against tumor cells by inhibiting VEGFR-2 kinase. benzimidazole 72-85 kinase insert domain receptor Homo sapiens 132-139 31671914-0 2019 Antiproliferative Aspect of Benzimidazole Derivatives" Activity and Their Impact on NF-kappaB Expression. benzimidazole 28-41 nuclear factor kappa B subunit 1 Homo sapiens 84-93 31252306-2 2019 A library of thirty-seven 6-amide-2-aryl benzoxazole/benzimidazole derivatives has been designed and synthesized based on the highly conserved active site of VEGFR-2. benzimidazole 53-66 kinase insert domain receptor Homo sapiens 158-165 31384837-3 2019 The selected data set of synthesized benzimidazole compounds was evaluated for its in vitro anticancer activity against cancer cell lines (HCT116 and MCF7) by sulforhodamine B (SRB) assay. benzimidazole 37-50 chaperonin containing TCP1 subunit 4 Homo sapiens 159-175 31103446-0 2019 Design, synthesis and biological evaluation of benzimidazole derivatives as novel human Pin1 inhibitors. benzimidazole 47-60 peptidylprolyl cis/trans isomerase, NIMA-interacting 1 Homo sapiens 88-92 31103446-1 2019 In this work, a series of novel benzimidazole derivatives were designed and synthesized as Pin1 inhibitors. benzimidazole 32-45 peptidylprolyl cis/trans isomerase, NIMA-interacting 1 Homo sapiens 91-95 31103446-5 2019 The structure-activity relationships of R1, R2, R3 and linker of the benzimidazole derivatives were analyzed in detail, which would help further exploration of new Pin1 inhibitors. benzimidazole 69-82 peptidylprolyl cis/trans isomerase, NIMA-interacting 1 Homo sapiens 164-168 31131561-7 2019 In general, these results indicate that these 6-arylurea-2-arylbenzoxazole/benzimidazole derivatives are promising inhibitors of VEGFR-2 kinase for potential development into anti-angiogenesis drugs. benzimidazole 75-88 kinase insert domain receptor Homo sapiens 129-136 31384837-3 2019 The selected data set of synthesized benzimidazole compounds was evaluated for its in vitro anticancer activity against cancer cell lines (HCT116 and MCF7) by sulforhodamine B (SRB) assay. benzimidazole 37-50 chaperonin containing TCP1 subunit 4 Homo sapiens 177-180 31054862-2 2019 In this study, a benzothiazole- and benzimidazole set of 1-aryl-3-(4-methoxybenzyl)ureas were synthesised as proposed Cys199-targeted covalent inhibitors of GSK-3beta, through the incorporation of an electrophilic warhead onto their ring scaffolds. benzimidazole 36-49 glycogen synthase kinase 3 alpha Homo sapiens 157-166 31009910-0 2019 Design, synthesis and docking studies of benzimidazole derivatives as potential EGFR inhibitors. benzimidazole 41-54 epidermal growth factor receptor Homo sapiens 80-84 31181622-9 2019 The results indicate the potential for repurposing the benzimidazole anthelmintics for the treatment of cancers overexpressing p53 negative regulators. benzimidazole 55-68 tumor protein p53 Homo sapiens 127-130 30798155-0 2019 A single point mutation in the TRPC3 lipid-recognition window generates supersensitivity to benzimidazole channel activators. benzimidazole 92-105 transient receptor potential cation channel subfamily C member 3 Homo sapiens 31-36 30952592-2 2019 Through a highly collaborative and iterative library design, synthesis and testing, a benzimidazole lead was rapidly and systematically advanced to a highly potent, selective and bioavailable DGAT1 inhibitor with the potential for further development. benzimidazole 86-99 diacylglycerol O-acyltransferase 1 Homo sapiens 192-197 30862488-0 2019 Drug library screen reveals benzimidazole derivatives as selective cytotoxic agents for KRAS-mutant lung cancer. benzimidazole 28-41 KRAS proto-oncogene, GTPase Homo sapiens 88-92 30862488-6 2019 The screening identified the cytotoxic effects of benzimidazole derivatives on KRAS-mutant lung cancer cells. benzimidazole 50-63 KRAS proto-oncogene, GTPase Homo sapiens 79-83 30862488-7 2019 Treatments with two benzimidazole derivatives, methiazole and fenbendazole-both of which are structurally specific-yielded significant suppression of the RAS-related signaling pathways in KRAS-mutated cells. benzimidazole 20-33 KRAS proto-oncogene, GTPase Homo sapiens 188-192 30862488-9 2019 Our study demonstrates that these benzimidazole derivatives play an important role in suppressing KRAS-mutant lung cancer cells, thus offering a novel combinatorial therapeutic approach against such cancer cells. benzimidazole 34-47 KRAS proto-oncogene, GTPase Homo sapiens 98-102 30047307-3 2019 Interestingly, the crystal structure of Eg-5 bound to benzimidazole unveils two chemically different allosteric pockets (PDB ID: 3ZCW). benzimidazole 54-67 kinesin family member 11 Homo sapiens 40-44 30926247-0 2019 Benzimidazole-based DGAT1 inhibitors with a [3.1.0] bicyclohexane carboxylic acid moiety. benzimidazole 0-13 diacylglycerol O-acyltransferase 1 Mus musculus 20-25 30926247-1 2019 Previously disclosed benzimidazole-based DGAT1 inhibitors containing a cyclohexane carboxylic acid moiety suffer from isomerization at the alpha position of the carboxylic acid group, generating active metabolites which exhibit DGAT1 inhibition comparable to the corresponding parent compounds. benzimidazole 21-34 diacylglycerol O-acyltransferase 1 Mus musculus 41-46 30926247-1 2019 Previously disclosed benzimidazole-based DGAT1 inhibitors containing a cyclohexane carboxylic acid moiety suffer from isomerization at the alpha position of the carboxylic acid group, generating active metabolites which exhibit DGAT1 inhibition comparable to the corresponding parent compounds. benzimidazole 21-34 diacylglycerol O-acyltransferase 1 Mus musculus 228-233 30926247-2 2019 In this report, we describe the design, synthesis and profiling of benzimidazole-based DGAT1 inhibitors with a [3.1.0] bicyclohexane carboxylic acid moiety. benzimidazole 67-80 diacylglycerol O-acyltransferase 1 Mus musculus 87-92 32255081-5 2019 As the plug, the beta-CD ring was initially located at the Bz position. benzimidazole 59-61 ACD shelterin complex subunit and telomerase recruitment factor Homo sapiens 17-24 32255081-6 2019 In an acidic tumor microenvironment, the pH sensitive Bz was protonated and the complex formation constant between Bz and beta-CD decreased. benzimidazole 54-56 ACD shelterin complex subunit and telomerase recruitment factor Homo sapiens 122-129 32255081-6 2019 In an acidic tumor microenvironment, the pH sensitive Bz was protonated and the complex formation constant between Bz and beta-CD decreased. benzimidazole 115-117 ACD shelterin complex subunit and telomerase recruitment factor Homo sapiens 122-129 30940396-1 2019 Indole- and azaindole-based glyoxylyl amide derivatives have been described as HIV-1 attachment inhibitors (AIs) that act by blocking the interaction between the viral gp120 coat protein and the human host cell CD4 receptor. benzimidazole 12-21 Envelope surface glycoprotein gp160, precursor Human immunodeficiency virus 1 168-173 30940396-1 2019 Indole- and azaindole-based glyoxylyl amide derivatives have been described as HIV-1 attachment inhibitors (AIs) that act by blocking the interaction between the viral gp120 coat protein and the human host cell CD4 receptor. benzimidazole 12-21 CD4 molecule Homo sapiens 211-223 31103918-11 2019 Molecular docking studies show that the amino acid residues 664-666 in the hinge region of the cytosolic domain of CSF1R to be the preferred region of binding for nitroindole and azaindole derivatives. benzimidazole 179-188 colony stimulating factor 1 receptor Homo sapiens 115-120 30714356-1 2019 Using a scaffold-hopping approach, imidazo[1,2-a]pyridine analogues of the ZSTK474 (benzimidazole) class of phosphatidylinositol 3-kinase (PI3K) inhibitors have been synthesized for biological evaluation. benzimidazole 84-97 phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta Homo sapiens 108-137 30707023-3 2019 High-throughput screening resulted in the identification of benzimidazole derivatives as novel hEP4-R antagonists. benzimidazole 60-73 prostaglandin E receptor 4 Homo sapiens 95-99 30934730-0 2019 Structure-Based Design of Novel Benzimidazole Derivatives as Pin1 Inhibitors. benzimidazole 32-45 peptidylprolyl cis/trans isomerase, NIMA-interacting 1 Homo sapiens 61-65 30934730-3 2019 Aiming to develop potent Pin1 inhibitors, a series of benzimidazole derivatives were designed and synthesized. benzimidazole 54-67 peptidylprolyl cis/trans isomerase, NIMA-interacting 1 Homo sapiens 25-29 30934730-6 2019 Taken together, these unique benzimidazole derivatives exhibited great potential to be further explored as potent Pin1 inhibitors with improved potency. benzimidazole 29-42 peptidylprolyl cis/trans isomerase, NIMA-interacting 1 Homo sapiens 114-118 29608549-3 2019 Budding uninhibited by benzimidazole-1 (Bub1) plays a role in Akt and JNK signaling, which control TF and TM, respectively. benzimidazole 23-36 BUB1, mitotic checkpoint serine/threonine kinase Mus musculus 40-44 30496702-2 2019 In this study, heat shock delayed the onset of anaphase by increasing the number of misoriented cells, accompanied by the kinetochore localization of budding uninhibited by benzimidazole-related (BubR)1 in a monopolar spindle (Mps)1-dependent manner. benzimidazole 173-186 BUB1 mitotic checkpoint serine/threonine kinase B Homo sapiens 196-202 29608549-3 2019 Budding uninhibited by benzimidazole-1 (Bub1) plays a role in Akt and JNK signaling, which control TF and TM, respectively. benzimidazole 23-36 thymoma viral proto-oncogene 1 Mus musculus 62-65 29608549-3 2019 Budding uninhibited by benzimidazole-1 (Bub1) plays a role in Akt and JNK signaling, which control TF and TM, respectively. benzimidazole 23-36 mitogen-activated protein kinase 8 Mus musculus 70-73 29608549-3 2019 Budding uninhibited by benzimidazole-1 (Bub1) plays a role in Akt and JNK signaling, which control TF and TM, respectively. benzimidazole 23-36 coagulation factor III Mus musculus 99-101 30809119-5 2019 Benzimidazole derivatives also reduced TNF-alpha expression in mice. benzimidazole 0-13 tumor necrosis factor Mus musculus 39-48 30823470-0 2019 Synthesis and AChE-Inhibitory Activity of New Benzimidazole Derivatives. benzimidazole 46-59 acetylcholinesterase (Cartwright blood group) Homo sapiens 14-18 30823470-5 2019 Among them, compounds 3d and 3h, which featured 3,4-dihydroxy substitution at the phenyl ring and 5(6)-chloro substitution at the benzimidazole ring were found to be potent inhibitors of AChE. benzimidazole 130-143 acetylcholinesterase (Cartwright blood group) Homo sapiens 187-191 30664786-2 2019 In a screen for compounds that restore radiosensitivity in p53 mutant zebrafish while tolerated in non-irradiated wild-type animals, we identified the benzimidazole anthelmintic oxfendazole. benzimidazole 151-164 tumor protein p53 Danio rerio 59-62 29777201-4 2019 Here, based on published structure and activity of GDC-0449 inhibitor class, we replaced its amide core with benzimidazole which retained bulk of the SMO-targeting activity as measured in our Hh/SMO/Gli1-reporter system. benzimidazole 109-122 smoothened, frizzled class receptor Mus musculus 150-153 29777201-4 2019 Here, based on published structure and activity of GDC-0449 inhibitor class, we replaced its amide core with benzimidazole which retained bulk of the SMO-targeting activity as measured in our Hh/SMO/Gli1-reporter system. benzimidazole 109-122 smoothened, frizzled class receptor Mus musculus 195-198 29777201-4 2019 Here, based on published structure and activity of GDC-0449 inhibitor class, we replaced its amide core with benzimidazole which retained bulk of the SMO-targeting activity as measured in our Hh/SMO/Gli1-reporter system. benzimidazole 109-122 GLI-Kruppel family member GLI1 Mus musculus 199-203 30538066-4 2019 Work reported here evaluates the benzimidazole scaffold and substituents resulting in the discovery of AC1903, a TRPC5 inhibitor that is active in multiple animal models of CKD. benzimidazole 33-46 transient receptor potential cation channel subfamily C member 5 Homo sapiens 113-118 30538065-2 2019 Core hopping from our previously reported phenylimidazole leads has allowed the identification of a novel series of benzimidazole NaV1.8 blockers. benzimidazole 116-129 sodium voltage-gated channel alpha subunit 10 Homo sapiens 130-136 29992893-2 2019 Bendamustine (Alkylating agent), Nocodazole (Mitotic inhibitor), Veliparib (PARP inhibitor), and Glasdegib (SMO inhibitor) are being clinically used as anticancer therapeutic which bear benzimidazole moiety. benzimidazole 186-199 poly(ADP-ribose) polymerase 1 Homo sapiens 76-80 30280671-0 2019 3D-QSAR and Molecular Docking Studies on Oxadiazole Substituted Benzimidazole Derivatives: Validation of Experimental Inhibitory Potencies Towards COX-2. benzimidazole 64-77 mitochondrially encoded cytochrome c oxidase II Homo sapiens 147-152 30280671-2 2019 Benzimidazole derivatives showed promising anti-inflammatory activity through the inhibition of COX-2 enzyme. benzimidazole 0-13 mitochondrially encoded cytochrome c oxidase II Homo sapiens 96-101 30727904-14 2019 The present series of 1H-benzimidazoles could be considered promising broad-spectrum antimicrobial candidates that deserve in future for preclinical antimicrobial evaluation and development of newer antimicrobial agents targeting microbial DHFR. benzimidazole 22-39 dihydrofolate reductase Homo sapiens 240-244 29992893-2 2019 Bendamustine (Alkylating agent), Nocodazole (Mitotic inhibitor), Veliparib (PARP inhibitor), and Glasdegib (SMO inhibitor) are being clinically used as anticancer therapeutic which bear benzimidazole moiety. benzimidazole 186-199 smoothened, frizzled class receptor Homo sapiens 108-111 30310908-0 2018 Acylhydrazone functionalized benzimidazole-based metallogel for the efficient detection and separation of Cr3. benzimidazole 29-42 teratocarcinoma-derived growth factor 1 pseudogene 3 Homo sapiens 106-109 30264679-3 2019 As in literature, azaindole is a very potent moiety, its derivatives displayed a number of biological activities such as kinase inhibitors, cytotoxic agents, anti-angiogenic activity, CRTh2 receptor antagonists, melanin agonists, nicotine agonists, effectiveness in alzheimer disease, cytokinin analogs, Orai inhibitors in asthma and chemokine receptor- 2 (CCR2) antagonists. benzimidazole 18-27 prostaglandin D2 receptor 2 Homo sapiens 184-189 30264679-3 2019 As in literature, azaindole is a very potent moiety, its derivatives displayed a number of biological activities such as kinase inhibitors, cytotoxic agents, anti-angiogenic activity, CRTh2 receptor antagonists, melanin agonists, nicotine agonists, effectiveness in alzheimer disease, cytokinin analogs, Orai inhibitors in asthma and chemokine receptor- 2 (CCR2) antagonists. benzimidazole 18-27 C-C motif chemokine receptor 2 Homo sapiens 334-355 30264679-3 2019 As in literature, azaindole is a very potent moiety, its derivatives displayed a number of biological activities such as kinase inhibitors, cytotoxic agents, anti-angiogenic activity, CRTh2 receptor antagonists, melanin agonists, nicotine agonists, effectiveness in alzheimer disease, cytokinin analogs, Orai inhibitors in asthma and chemokine receptor- 2 (CCR2) antagonists. benzimidazole 18-27 C-C motif chemokine receptor 2 Homo sapiens 357-361 30547095-4 2018 To extend the SAR investigation of the indole-2-carboxamide class of CB1 allosteric modulators, azaindole (pyrrolopyridine) rings were used to replace the indole ring of Org27569 analogs to explore the potential of azaindole-2-carboxamides as CB1 allosteric modulators. benzimidazole 96-105 cannabinoid receptor 1 Homo sapiens 243-246 30371063-7 2018 Furthermore, several representative privileged substructures that are essential for FXR binders, such as benzimidazole, indole, and stilbene moiety, were detected using information gain and substructure frequency analysis. benzimidazole 105-118 nuclear receptor subfamily 1 group H member 4 Homo sapiens 84-87 30500781-5 2018 The anticancer potential of the selected benzimidazole derivatives was evaluated against two selected cell lines (human colorectal cancer, HCT-116 and breast adenocarcinoma, MCF-7) using sulforhodamine B (SRB) assay. benzimidazole 41-54 chaperonin containing TCP1 subunit 4 Homo sapiens 187-203 30500781-5 2018 The anticancer potential of the selected benzimidazole derivatives was evaluated against two selected cell lines (human colorectal cancer, HCT-116 and breast adenocarcinoma, MCF-7) using sulforhodamine B (SRB) assay. benzimidazole 41-54 chaperonin containing TCP1 subunit 4 Homo sapiens 205-208 30075436-0 2018 A new multifunctional benzimidazole tagged coumarin as ratiometric fluorophore for the detection of Cd2+/F- ions and imaging in live cells. benzimidazole 22-35 CD2 molecule Homo sapiens 100-103 30310908-3 2018 A novel metallogel chemosensor (BMG-Fe) based on functionalized benzimidazole (BM) and Fe3+ was constructed, which could fluorescently detect and separate Cr3+. benzimidazole 64-77 teratocarcinoma-derived growth factor 1 pseudogene 3 Homo sapiens 155-158 30310908-3 2018 A novel metallogel chemosensor (BMG-Fe) based on functionalized benzimidazole (BM) and Fe3+ was constructed, which could fluorescently detect and separate Cr3+. benzimidazole 32-34 teratocarcinoma-derived growth factor 1 pseudogene 3 Homo sapiens 155-158 30170943-1 2018 Utilizing the already described 3,4-bi-aryl pyridine series as a starting point, incorporation of a second ring system with a hydrogen bond donor and additional hydrophobic contacts yielded the azaindole series which exhibited potent, picomolar RSK2 inhibition and the most potent in vitro target modulation seen thus far for a RSK inhibitor. benzimidazole 194-203 ribosomal protein S6 kinase A3 Homo sapiens 245-249 30270370-2 2018 Herein, we report the exploration of benzimidazole-containing aramid fibers (B-ANF) for the naked-eye detection of heavy metal ions in aqueous solution. benzimidazole 37-50 HESX homeobox 1 Homo sapiens 79-82 30270370-3 2018 Firstly, B-ANF was prepared by hydroxylation from benzimidazole-containing aramid fiber. benzimidazole 50-63 HESX homeobox 1 Homo sapiens 11-14 30411010-0 2018 Efficient Synthesis and in Silico Studies of the Benzimidazole Hybrid Scaffold with the Quinolinyloxadiazole Skeleton with Potential alpha-Glucosidase Inhibitory, Anticoagulant, and Antiplatelet Activities for Type-II Diabetes Mellitus Management and Treating Thrombotic Disorders. benzimidazole 49-62 sucrase-isomaltase Homo sapiens 133-150 30411010-4 2018 In addition, molecular docking studies revealed that benzimidazole-containing quinolinyl oxadiazoles can correctly dock into the target receptor protein of the human intestinal alpha-glucosidase, while their bioavailability/drug-likeness was predicted to be acceptable but requires further optimization. benzimidazole 53-66 sucrase-isomaltase Homo sapiens 177-194 30411010-9 2018 These findings reveal that benzimidazole-containing quinolinyl oxadiazoles act as alpha-glucosidase inhibitors to develop novel therapeutics for treating type-II diabetes mellitus and can act as lead molecules in drug discovery as potential antidiabetic and antithrombotic agents. benzimidazole 27-40 sucrase-isomaltase Homo sapiens 82-99 30277375-4 2018 The oligoethylenimine-conjugated beta-cyclodextrin (beta-CD-PEI600) and benzimidazole-modified four-arm-polycaprolactone-initiated hyperbranched polyglycerol (PCL-HPG-BM) were synthesized as the host and guest molecules, respectively, and then the co-delivery carrier of PCL-HPG-PEI600 was formed from the pH-mediated inclusion interaction between beta-CD and BM. benzimidazole 72-85 PHD finger protein 1 Homo sapiens 159-162 30277375-4 2018 The oligoethylenimine-conjugated beta-cyclodextrin (beta-CD-PEI600) and benzimidazole-modified four-arm-polycaprolactone-initiated hyperbranched polyglycerol (PCL-HPG-BM) were synthesized as the host and guest molecules, respectively, and then the co-delivery carrier of PCL-HPG-PEI600 was formed from the pH-mediated inclusion interaction between beta-CD and BM. benzimidazole 72-85 PHD finger protein 1 Homo sapiens 271-274 30170943-1 2018 Utilizing the already described 3,4-bi-aryl pyridine series as a starting point, incorporation of a second ring system with a hydrogen bond donor and additional hydrophobic contacts yielded the azaindole series which exhibited potent, picomolar RSK2 inhibition and the most potent in vitro target modulation seen thus far for a RSK inhibitor. benzimidazole 194-203 ribosomal protein S6 kinase A3 Homo sapiens 245-248 30157472-3 2018 Among the intracellular factors, age-dependent decrease of BubR1 (budding uninhibited by benzimidazole-related 1), YAP (Yes-associated protein) and SIRT1 (Sirtuin-1) have been associated to dampening of tissue reconstitution and inhibition of cell cycle genes following partial hepatectomy. benzimidazole 89-102 BUB1B, mitotic checkpoint serine/threonine kinase Mus musculus 59-64 30205005-0 2018 Discovery and Structure-Based Optimization of Benzimidazole-Derived Activators of SOS1-Mediated Nucleotide Exchange on RAS. benzimidazole 46-59 SOS Ras/Rac guanine nucleotide exchange factor 1 Homo sapiens 82-86 30205005-4 2018 Here, we describe a new series of benzimidazole-derived SOS1 agonists. benzimidazole 34-47 SOS Ras/Rac guanine nucleotide exchange factor 1 Homo sapiens 56-60 30647880-1 2018 Herein we continued our previous work on the development of CB2 ligands, reporting the design and synthesis of a series of benzimidazole-containing derivatives that were explored as selective CB2 ligands with binding affinity towards both CB1 and CB2 receptors. benzimidazole 123-136 cannabinoid receptor 2 Homo sapiens 60-63 30647880-1 2018 Herein we continued our previous work on the development of CB2 ligands, reporting the design and synthesis of a series of benzimidazole-containing derivatives that were explored as selective CB2 ligands with binding affinity towards both CB1 and CB2 receptors. benzimidazole 123-136 cannabinoid receptor 2 Homo sapiens 192-195 30647880-1 2018 Herein we continued our previous work on the development of CB2 ligands, reporting the design and synthesis of a series of benzimidazole-containing derivatives that were explored as selective CB2 ligands with binding affinity towards both CB1 and CB2 receptors. benzimidazole 123-136 cannabinoid receptor 1 Homo sapiens 239-242 30647880-1 2018 Herein we continued our previous work on the development of CB2 ligands, reporting the design and synthesis of a series of benzimidazole-containing derivatives that were explored as selective CB2 ligands with binding affinity towards both CB1 and CB2 receptors. benzimidazole 123-136 cannabinoid receptor 2 Homo sapiens 192-195 29966873-0 2018 Biological properties and structural study of new aminoalkyl derivatives of benzimidazole and benzotriazole, dual inhibitors of CK2 and PIM1 kinases. benzimidazole 76-89 Pim-1 proto-oncogene, serine/threonine kinase Homo sapiens 136-140 29864685-2 2018 In light of this, a series of benzimidazole scaffold based hybrid molecules were designed by integrating benzimidazoles (containing pharmacophoric elements for COXs and LOXs inhibitors) with phthalimide subunit of thalidomide (pharmacophore element for TNF-alpha inhibitor) under one construct via molecular hybridization strategy. benzimidazole 30-43 tumor necrosis factor Mus musculus 253-262 30396261-2 2018 Recently, the spindle checkpoint kinase budding uninhibited by benzimidazole-related 1 (BubR1) has emerged as a key determinant for age-related pathology in various tissues including brain. benzimidazole 63-76 BUB1B, mitotic checkpoint serine/threonine kinase Mus musculus 88-93 29775710-2 2018 Dual pH-sensitive supramolecular micelles were formed from beta-CD-(PDMAEMA)7 and benzimidazole modified poly(epsilon-caprolactone) (BM-PCL) through the host-guest interactions between beta-CD and benzimidazole. benzimidazole 82-95 PHD finger protein 1 Homo sapiens 136-139 29571113-0 2018 Synthesis of stable benzimidazole derivatives bearing pyrazole as anticancer and EGFR receptor inhibitors. benzimidazole 20-33 epidermal growth factor receptor Homo sapiens 81-85 29989628-2 2018 The 1H NMR and crystal structure measurements indicate that both 1 PF6 and 2 PF6 contain intramolecular pipi stacking interactions between the non-coordinated N-methylbenzoimidazole/benzimidazole unit and the tpy ligand, but there are no such pipi interactions in 3 PF6. benzimidazole 182-195 sperm associated antigen 17 Homo sapiens 67-70 28974341-1 2018 OBJECTIVES: Budding uninhibited by benzimidazole-related 1 (BubR1), a cell cycle-related protein, is an essential component of the spindle checkpoint that regulates cell division. benzimidazole 35-48 BUB1B, mitotic checkpoint serine/threonine kinase Mus musculus 60-65 29989628-2 2018 The 1H NMR and crystal structure measurements indicate that both 1 PF6 and 2 PF6 contain intramolecular pipi stacking interactions between the non-coordinated N-methylbenzoimidazole/benzimidazole unit and the tpy ligand, but there are no such pipi interactions in 3 PF6. benzimidazole 182-195 sperm associated antigen 17 Homo sapiens 77-80 29989628-2 2018 The 1H NMR and crystal structure measurements indicate that both 1 PF6 and 2 PF6 contain intramolecular pipi stacking interactions between the non-coordinated N-methylbenzoimidazole/benzimidazole unit and the tpy ligand, but there are no such pipi interactions in 3 PF6. benzimidazole 182-195 sperm associated antigen 17 Homo sapiens 77-80 28784429-8 2018 FLAP inhibitors reviewed herein are classified into four sub-classes as the first-generation FLAP inhibitors (indole and quinoline derivatives), the second-generation FLAP inhibitors (diaryl-alkanes and biaryl amino-heteroarenes), the benzimidazole-containing FLAP inhibitors and other FLAP inhibitors with polypharmacology for easiness of the reader. benzimidazole 235-248 arachidonate 5-lipoxygenase activating protein Homo sapiens 0-4 29991770-0 2018 Radiobrominated benzimidazole-quinoline derivatives as Platelet-derived growth factor receptor beta (PDGFRbeta) imaging probes. benzimidazole 16-29 platelet derived growth factor receptor beta Homo sapiens 55-99 29991770-0 2018 Radiobrominated benzimidazole-quinoline derivatives as Platelet-derived growth factor receptor beta (PDGFRbeta) imaging probes. benzimidazole 16-29 platelet derived growth factor receptor beta Homo sapiens 101-110 29748388-6 2018 We identified specific interactions of CENP-F and CENP-E with budding uninhibited by benzimidazole 1 (BUB1) and BUB1-related (BUBR1) mitotic checkpoint Ser/Thr kinases, respectively, paralogous proteins involved in mitotic checkpoint control and chromosome alignment. benzimidazole 85-98 centromere protein F Homo sapiens 39-45 29748388-6 2018 We identified specific interactions of CENP-F and CENP-E with budding uninhibited by benzimidazole 1 (BUB1) and BUB1-related (BUBR1) mitotic checkpoint Ser/Thr kinases, respectively, paralogous proteins involved in mitotic checkpoint control and chromosome alignment. benzimidazole 85-98 centromere protein E Homo sapiens 50-56 29754833-0 2018 Discovery of benzimidazole derivatives as orally active renin inhibitors: Optimization of 3,5-disubstituted piperidine to improve pharmacokinetic profile. benzimidazole 13-26 renin Rattus norvegicus 56-61 29754833-7 2018 Consequently, a series of novel benzimidazole derivatives were discovered as potent and orally bioavailable renin inhibitors. benzimidazole 32-45 renin Rattus norvegicus 108-113 29748388-6 2018 We identified specific interactions of CENP-F and CENP-E with budding uninhibited by benzimidazole 1 (BUB1) and BUB1-related (BUBR1) mitotic checkpoint Ser/Thr kinases, respectively, paralogous proteins involved in mitotic checkpoint control and chromosome alignment. benzimidazole 85-98 BUB1 mitotic checkpoint serine/threonine kinase Homo sapiens 102-106 29669921-3 2018 Herein, we describe the design, synthesis, and evaluation of a collection of N-arylated benzimidazole derivatives (BIMs), one of which (BIM1) shows unparalleled (>20-fold) selectivity for CLC-Ka over CLC-Kb, the two most closely related human CLC homologs. benzimidazole 88-101 Charcot-Leyden crystal galectin Homo sapiens 191-194 29669921-3 2018 Herein, we describe the design, synthesis, and evaluation of a collection of N-arylated benzimidazole derivatives (BIMs), one of which (BIM1) shows unparalleled (>20-fold) selectivity for CLC-Ka over CLC-Kb, the two most closely related human CLC homologs. benzimidazole 88-101 chloride voltage-gated channel Kb Homo sapiens 203-209 29669921-3 2018 Herein, we describe the design, synthesis, and evaluation of a collection of N-arylated benzimidazole derivatives (BIMs), one of which (BIM1) shows unparalleled (>20-fold) selectivity for CLC-Ka over CLC-Kb, the two most closely related human CLC homologs. benzimidazole 88-101 Charcot-Leyden crystal galectin Homo sapiens 203-206 29783777-0 2018 Preferential Inhibition of Wnt/beta-Catenin Signaling by Novel Benzimidazole Compounds in Triple-Negative Breast Cancer. benzimidazole 63-76 catenin beta 1 Homo sapiens 31-43 28585189-2 2018 The new anticoagulant dabigatran etexilate (DE) is a direct thrombin inhibitor that owns benzimidazole group, which has been proposed to activate Nurr1. benzimidazole 89-102 coagulation factor II Rattus norvegicus 60-68 28585189-2 2018 The new anticoagulant dabigatran etexilate (DE) is a direct thrombin inhibitor that owns benzimidazole group, which has been proposed to activate Nurr1. benzimidazole 89-102 nuclear receptor subfamily 4, group A, member 2 Rattus norvegicus 146-151 29731445-7 2018 Among all Angiotensin II Receptor Antagonists/Blockers (ARBs), Telmisartan, Milfasartan and many others have benzimidazole ring in their structure. benzimidazole 109-122 angiotensinogen Homo sapiens 10-24 29597170-3 2018 C (5)-substitution of the benzimidazole ring of BRP-7 by carboxylic acid and its bioisosteres provided compounds, exemplified by 57 that potently suppress LT formation (IC50 = 0.05 muM) by targeting FLAP along with inhibition of mPGES-1 (IC50 = 0.42 muM). benzimidazole 26-39 arachidonate 5-lipoxygenase activating protein Homo sapiens 199-203 29597170-3 2018 C (5)-substitution of the benzimidazole ring of BRP-7 by carboxylic acid and its bioisosteres provided compounds, exemplified by 57 that potently suppress LT formation (IC50 = 0.05 muM) by targeting FLAP along with inhibition of mPGES-1 (IC50 = 0.42 muM). benzimidazole 26-39 prostaglandin E synthase Mus musculus 229-236 29407951-0 2018 Design, synthesis and biological evaluation of novel indole-benzimidazole hybrids targeting estrogen receptor alpha (ER-alpha). benzimidazole 60-73 estrogen receptor 1 Homo sapiens 92-115 29382705-3 2018 Here, we report the discovery of the azaindole compounds BDP8900 and BDP9066 as potent and selective MRCK inhibitors that reduce substrate phosphorylation, leading to morphologic changes in cancer cells along with inhibition of their motility and invasive character. benzimidazole 37-46 CDC42 binding protein kinase alpha Homo sapiens 101-105 29174667-2 2018 The dye-labeled probe aptamer (PA) product was adsorbed onto the benzimidazole derivative-containing Cu-MOG via electrostatic incorporation and strong pi-pi stacking interactions, which significantly increased the FA value due to the enlargement of the molecular volume of the PA/Cu-MOG complex. benzimidazole 65-78 myelin oligodendrocyte glycoprotein Homo sapiens 104-107 29174667-2 2018 The dye-labeled probe aptamer (PA) product was adsorbed onto the benzimidazole derivative-containing Cu-MOG via electrostatic incorporation and strong pi-pi stacking interactions, which significantly increased the FA value due to the enlargement of the molecular volume of the PA/Cu-MOG complex. benzimidazole 65-78 myelin oligodendrocyte glycoprotein Homo sapiens 283-286 29593119-8 2018 Hydrophobic interactions between the molecules and HIF1alpha are also a key factor, especially the interactions between the hydrophobic groups (benzimidazole) of the molecules and the hydrophobic residues inside the binding cave. benzimidazole 144-157 hypoxia inducible factor 1 subunit alpha Homo sapiens 51-60 29459277-3 2018 Here, we describe the binding of benzimidazole-carbazole ligands to G-quadruplex structures formed in G-rich DNA sequences containing the promoter regions of human c-MYC, c-KIT1, c-KIT2, VEGF and BCL2 proto-oncogenes. benzimidazole 33-46 MYC proto-oncogene, bHLH transcription factor Homo sapiens 164-169 29459277-3 2018 Here, we describe the binding of benzimidazole-carbazole ligands to G-quadruplex structures formed in G-rich DNA sequences containing the promoter regions of human c-MYC, c-KIT1, c-KIT2, VEGF and BCL2 proto-oncogenes. benzimidazole 33-46 vascular endothelial growth factor A Homo sapiens 187-191 29459277-3 2018 Here, we describe the binding of benzimidazole-carbazole ligands to G-quadruplex structures formed in G-rich DNA sequences containing the promoter regions of human c-MYC, c-KIT1, c-KIT2, VEGF and BCL2 proto-oncogenes. benzimidazole 33-46 BCL2 apoptosis regulator Homo sapiens 196-200 29407951-0 2018 Design, synthesis and biological evaluation of novel indole-benzimidazole hybrids targeting estrogen receptor alpha (ER-alpha). benzimidazole 60-73 estrogen receptor 1 Homo sapiens 117-125 28638907-0 2017 Ruthenium(ii) p-cymene complexes of a benzimidazole-based ligand capable of VEGFR2 inhibition: hydrolysis, reactivity and cytotoxicity studies. benzimidazole 38-51 kinase insert domain receptor Homo sapiens 76-82 29334584-1 2018 RATIONALE: A novel benzimidazole compound ZLN005 was previously identified as a transcriptional activator of peroxisome proliferator-activated receptor gamma coactivator 1alpha (PGC-1alpha) in certain metabolic tissues. benzimidazole 19-32 PPARG coactivator 1 alpha Rattus norvegicus 109-176 29334584-1 2018 RATIONALE: A novel benzimidazole compound ZLN005 was previously identified as a transcriptional activator of peroxisome proliferator-activated receptor gamma coactivator 1alpha (PGC-1alpha) in certain metabolic tissues. benzimidazole 19-32 PPARG coactivator 1 alpha Rattus norvegicus 178-188 30338731-1 2018 AIM AND OBJECTIVE: The benzimidazole derivatives have been obtained via weightreducing aid (L-Carnitine) as a cheap catalyst. benzimidazole 23-36 activation induced cytidine deaminase Homo sapiens 87-90 29133046-3 2018 Additional Western blot analyses showed different mechanisms of cytostatic activity between compounds 10c and 11f that could be associated with the nature of aromatic substituent at 1-(1,2,3-triazolyl) and amidino moiety at C-5 position of benzimidazole ring. benzimidazole 240-253 Rho GTPase activating protein 9 Homo sapiens 102-105 29111367-0 2017 Synthesis and biological evaluation of novel radioiodinated benzimidazole derivatives for imaging alpha-synuclein aggregates. benzimidazole 60-73 synuclein alpha Homo sapiens 98-113 29111367-3 2017 In order to develop imaging probes targeting alpha-syn aggregates, we synthesized and evaluated three novel radioiodinated benzimidazole (BI) derivatives for selective imaging of alpha-syn aggregates. benzimidazole 123-136 synuclein alpha Homo sapiens 179-188 29111367-3 2017 In order to develop imaging probes targeting alpha-syn aggregates, we synthesized and evaluated three novel radioiodinated benzimidazole (BI) derivatives for selective imaging of alpha-syn aggregates. benzimidazole 138-140 synuclein alpha Homo sapiens 45-54 29111367-3 2017 In order to develop imaging probes targeting alpha-syn aggregates, we synthesized and evaluated three novel radioiodinated benzimidazole (BI) derivatives for selective imaging of alpha-syn aggregates. benzimidazole 138-140 synuclein alpha Homo sapiens 179-188 29111367-4 2017 In binding experiments, BI-2 exhibited the highest selective binding affinity for alpha-syn aggregates among the BI derivatives. benzimidazole 24-26 synuclein alpha Homo sapiens 82-91 28949377-2 2017 In this study, the antiplatelet activity of three newly synthesized saccharide based benzimidazole derivatives, M3BIM, Malto-BIM and Melibio-BIM, in collagen and thrombin-stimulated human platelets in vitro was examined. benzimidazole 85-98 coagulation factor II, thrombin Homo sapiens 162-170 28603987-7 2017 We have thus identified the novel benzimidazole derivatives 10, 21, 27, and 30, which are highly potent AC inhibitors. benzimidazole 34-47 N-acylsphingosine amidohydrolase 1 Homo sapiens 104-106 27602589-4 2017 The central benzimidazole ring, however, remained intact considering its great affinity toward AT1R and PPARgamma. benzimidazole 12-25 angiotensin II receptor type 1 Homo sapiens 95-99 27602589-4 2017 The central benzimidazole ring, however, remained intact considering its great affinity toward AT1R and PPARgamma. benzimidazole 12-25 peroxisome proliferator activated receptor gamma Homo sapiens 104-113 28638907-3 2017 In our work, we have generated a bispyrazole-containing benzimidazole ligand with potency against vascular endothelial growth factor receptor 2 (VEGFR2), which is known to have roles in vasculogenesis/angiogenesis. benzimidazole 56-69 kinase insert domain receptor Homo sapiens 98-143 28638907-3 2017 In our work, we have generated a bispyrazole-containing benzimidazole ligand with potency against vascular endothelial growth factor receptor 2 (VEGFR2), which is known to have roles in vasculogenesis/angiogenesis. benzimidazole 56-69 kinase insert domain receptor Homo sapiens 145-151 28498655-0 2017 Discovery of an Orally Bioavailable Benzimidazole Diacylglycerol Acyltransferase 1 (DGAT1) Inhibitor That Suppresses Body Weight Gain in Diet-Induced Obese Dogs and Postprandial Triglycerides in Humans. benzimidazole 36-49 diacylglycerol O-acyltransferase 1 Canis lupus familiaris 50-82 28498655-0 2017 Discovery of an Orally Bioavailable Benzimidazole Diacylglycerol Acyltransferase 1 (DGAT1) Inhibitor That Suppresses Body Weight Gain in Diet-Induced Obese Dogs and Postprandial Triglycerides in Humans. benzimidazole 36-49 diacylglycerol O-acyltransferase 1 Canis lupus familiaris 84-89 28498655-1 2017 Modification of a gut restricted class of benzimidazole DGAT1 inhibitor 1 led to 9 with good oral bioavailability. benzimidazole 42-55 diacylglycerol O-acyltransferase 1 Canis lupus familiaris 56-61 28137469-0 2017 Combined CoMFA and CoMSIA 3D-QSAR study of benzimidazole and benzothiophene derivatives with selective affinity for the CB2 cannabinoid receptor. benzimidazole 43-56 cannabinoid receptor 2 Homo sapiens 120-123 28460359-0 2017 Synthesis and biological evaluation of benzimidazole derivatives as the G9a Histone Methyltransferase inhibitors that induce autophagy and apoptosis of breast cancer cells. benzimidazole 39-52 euchromatic histone lysine methyltransferase 2 Homo sapiens 72-101 28340412-6 2017 Two co-crystal structures of compounds 11b and 15e complexed with PARP-1 were achieved and demonstrated a unique binding mode of these benzo-imidazole derivatives. benzimidazole 135-150 poly(ADP-ribose) polymerase 1 Homo sapiens 66-72 28328217-4 2017 To achieve this goal, we synthesized a series of benzimidazole-based derivatives of Cl-amidine, hypothesizing that this scaffold would allow access to a series of PAD2-selective inhibitors with enhanced cellular efficacy. benzimidazole 49-62 peptidyl arginine deiminase 2 Homo sapiens 163-167 28915607-8 2017 Moreover, the expression of the spindle checkpoint-related proteins, mitotic arrest defective 2 (Mad2), budding uninhibited in benzimidazole 1 (Bub1), and anaphase-promoting complex (APC), indicators of abnormal chromosomes and carcinogenesis, reduced in CTPE-treated BEAS-2B cells at Passage 30 compared with the vehicle control using real-time PCR and immunohistochemistry. benzimidazole 127-140 mitotic arrest deficient 2 like 1 Homo sapiens 69-95 28915607-8 2017 Moreover, the expression of the spindle checkpoint-related proteins, mitotic arrest defective 2 (Mad2), budding uninhibited in benzimidazole 1 (Bub1), and anaphase-promoting complex (APC), indicators of abnormal chromosomes and carcinogenesis, reduced in CTPE-treated BEAS-2B cells at Passage 30 compared with the vehicle control using real-time PCR and immunohistochemistry. benzimidazole 127-140 BUB1 mitotic checkpoint serine/threonine kinase Homo sapiens 144-148 28233680-0 2017 Benzimidazole inhibitors from the Niclosamide chemotype inhibit Wnt/beta-catenin signaling with selectivity over effects on ATP homeostasis. benzimidazole 0-13 catenin beta 1 Homo sapiens 68-80 28043913-3 2017 We recently identified a series of benzimidazole analogs as potent inhibitors of Wnt/beta-catenin signaling. benzimidazole 35-48 catenin beta 1 Homo sapiens 85-97 28190654-0 2017 Discovery and optimization of benzimidazole derivatives as a novel chemotype of farnesoid X receptor (FXR) antagonists. benzimidazole 30-43 xenotropic and polytropic retrovirus receptor 1 Homo sapiens 90-100 28190654-0 2017 Discovery and optimization of benzimidazole derivatives as a novel chemotype of farnesoid X receptor (FXR) antagonists. benzimidazole 30-43 nuclear receptor subfamily 1 group H member 4 Homo sapiens 102-105 28190654-1 2017 We describe here a novel chemotype with substituted benzimidazole scaffold for nonsteroidal farnesoid X receptor (FXR) antagonists starting from the identification of a screening hit, BB-4. benzimidazole 52-65 xenotropic and polytropic retrovirus receptor 1 Homo sapiens 102-112 28190654-1 2017 We describe here a novel chemotype with substituted benzimidazole scaffold for nonsteroidal farnesoid X receptor (FXR) antagonists starting from the identification of a screening hit, BB-4. benzimidazole 52-65 nuclear receptor subfamily 1 group H member 4 Homo sapiens 114-117 28086233-0 2017 A novel benzimidazole derivative, MBIC inhibits tumor growth and promotes apoptosis via activation of ROS-dependent JNK signaling pathway in hepatocellular carcinoma. benzimidazole 8-21 mitogen-activated protein kinase 8 Mus musculus 116-119 28138686-2 2017 Two modes of cycloaddition ([4 + 1] cycloaddition and [4 + 2] cycloaddition) occurred during condensation, causing the in situ generation of two benzimidazole derivative ligands (L1 and L3) and a quinoxaline derivative ligand (L2). benzimidazole 145-158 immunoglobulin kappa variable 1-16 Homo sapiens 179-188 27987485-0 2017 Design, synthesis, docking and QSAR study of substituted benzimidazole linked oxadiazole as cytotoxic agents, EGFR and erbB2 receptor inhibitors. benzimidazole 57-70 epidermal growth factor receptor Homo sapiens 110-114 27854075-0 2017 Benzimidazole derivative M084 extends the lifespan of Caenorhabditis elegans in a DAF-16/FOXO-dependent way. benzimidazole 0-13 Fork-head domain-containing protein;Forkhead box protein O Caenorhabditis elegans 82-88 28146092-0 2017 Synthesis and Biological Evaluation of Novel Benzimidazole Derivatives and Analogs Targeting the NLRP3 Inflammasome. benzimidazole 45-58 NLR family pyrin domain containing 3 Homo sapiens 97-102 27923497-6 2017 Molecular docking study showed that morpholine and oxadiazole rings linked to the benzimidazole nucleus play an important role in binding with the COX-2. benzimidazole 82-95 cytochrome c oxidase II, mitochondrial Rattus norvegicus 147-152 27987485-0 2017 Design, synthesis, docking and QSAR study of substituted benzimidazole linked oxadiazole as cytotoxic agents, EGFR and erbB2 receptor inhibitors. benzimidazole 57-70 erb-b2 receptor tyrosine kinase 2 Homo sapiens 119-124 27987485-1 2017 The synthesis of benzimidazole linked oxadiazole derivatives designed as potential EGFR and erbB2 receptor inhibitors with anticancer and apoptotic activity were studied. benzimidazole 17-30 epidermal growth factor receptor Homo sapiens 83-87 27987485-1 2017 The synthesis of benzimidazole linked oxadiazole derivatives designed as potential EGFR and erbB2 receptor inhibitors with anticancer and apoptotic activity were studied. benzimidazole 17-30 erb-b2 receptor tyrosine kinase 2 Homo sapiens 92-97 27979595-2 2017 Previously reported benzimidazole CYP11B2 inhibitors led the way for bioisosteric imidazopyridines that are both potent and selective over CYP11B1. benzimidazole 20-33 cytochrome P450 family 11 subfamily B member 2 Homo sapiens 34-41 28197323-4 2017 Substitution at the 2-position of the azaindole ring generated somewhat less potent analogues, but reduced AO-mediated metabolism. benzimidazole 38-47 aldehyde oxidase 1 Homo sapiens 107-109 27979595-2 2017 Previously reported benzimidazole CYP11B2 inhibitors led the way for bioisosteric imidazopyridines that are both potent and selective over CYP11B1. benzimidazole 20-33 cytochrome P450 family 11 subfamily B member 1 Homo sapiens 139-146 27689533-0 2016 Iodinated benzimidazole PARP radiotracer for evaluating PARP1/2 expression in vitro and in vivo. benzimidazole 10-23 poly(ADP-ribose) polymerase 1 Homo sapiens 24-28 27930648-2 2016 The benzimidazole (BZ) drugs albendazole (ABZ) and mebendazole (MBZ) are used for treatment of human STH infections and this use is increasing dramatically with massive drug donations. benzimidazole 4-17 saitohin Homo sapiens 101-104 27930648-2 2016 The benzimidazole (BZ) drugs albendazole (ABZ) and mebendazole (MBZ) are used for treatment of human STH infections and this use is increasing dramatically with massive drug donations. benzimidazole 19-21 saitohin Homo sapiens 101-104 27689533-0 2016 Iodinated benzimidazole PARP radiotracer for evaluating PARP1/2 expression in vitro and in vivo. benzimidazole 10-23 poly(ADP-ribose) polymerase family member 12 Homo sapiens 56-63 27677422-0 2016 Microwave-Assisted Syntheses of Benzimidazole-Containing Selenadiazole Derivatives That Induce Cell-Cycle Arrest and Apoptosis in Human Breast Cancer Cells by Activation of the ROS/AKT Pathway. benzimidazole 32-45 AKT serine/threonine kinase 1 Homo sapiens 181-184 27560280-0 2016 Synthesis, binding assays, cytotoxic activity and docking studies of benzimidazole and benzothiophene derivatives with selective affinity for the CB2 cannabinoid receptor. benzimidazole 69-82 cannabinoid receptor 2 Homo sapiens 146-149 27560280-2 2016 To test the hypothesis that the lack of a hydrogen bond interaction between benzimidazole and benzothiophene derivatives with Lys192 reduces their affinity for CB1 receptors (as we previously reported) and leads to CB2 selectivity, most of the tested compounds do not exhibit hydrogen bond acceptors. benzimidazole 76-89 cannabinoid receptor 1 Homo sapiens 160-163 27560280-2 2016 To test the hypothesis that the lack of a hydrogen bond interaction between benzimidazole and benzothiophene derivatives with Lys192 reduces their affinity for CB1 receptors (as we previously reported) and leads to CB2 selectivity, most of the tested compounds do not exhibit hydrogen bond acceptors. benzimidazole 76-89 cannabinoid receptor 2 Homo sapiens 215-218 27647702-2 2016 The use of benzimidazole as a bridging ligand at the meso position enables the binding of two BF2 units to provide sufficient rigidity and enhanced electron-withdrawing strength. benzimidazole 11-24 forkhead box G1 Homo sapiens 94-97 27406796-0 2016 Synthesis of benzimidazole based thiadiazole and carbohydrazide conjugates as glycogen synthase kinase-3beta inhibitors with anti-depressant activity. benzimidazole 13-26 glycogen synthase kinase 3 beta Homo sapiens 78-108 27664806-1 2016 BACKGROUND: Budding uninhibited by benzimidazole-related 1 (BubR1), a cell cycle-related protein, is an essential component of the spindle checkpoint that regulates cell division. benzimidazole 35-48 BUB1B, mitotic checkpoint serine/threonine kinase Mus musculus 60-65 27561386-2 2016 BubR1 (budding uninhibited by benzimidazole-related 1) controls chromosome mitotic segregation through the spindle assembly checkpoint, and BubR1 down-regulation promotes aging-associated phenotypes. benzimidazole 30-43 BUB1B, mitotic checkpoint serine/threonine kinase Mus musculus 0-5 27301679-3 2016 Pyridazin-4(1H)-one derivative 1 was linked with a benzimidazole group through an alkyl spacer to interact with the OH of Tyr683 and fill the PDE10A selectivity pocket. benzimidazole 51-64 phosphodiesterase 10A Homo sapiens 142-148 27301679-5 2016 The crystal structure of 16f bound to PDE10A revealed that the benzimidazole moiety was located deep within the PDE10A selectivity pocket and interacted with Tyr683. benzimidazole 63-76 phosphodiesterase 10A Homo sapiens 38-44 27301679-5 2016 The crystal structure of 16f bound to PDE10A revealed that the benzimidazole moiety was located deep within the PDE10A selectivity pocket and interacted with Tyr683. benzimidazole 63-76 phosphodiesterase 10A Homo sapiens 112-118 27572707-0 2016 A simple and efficient synthesis of novel inhibitors of alpha-glucosidase based on benzimidazole skeleton and molecular docking studies. benzimidazole 83-96 sucrase-isomaltase Homo sapiens 56-73 27406796-1 2016 A series of benzimidazole based thiadiazole and carbohydrazide conjugates have been synthesized and evaluated for inhibition of glycogen synthase kinase-3beta and anti-depressant effect. benzimidazole 12-25 glycogen synthase kinase 3 beta Homo sapiens 128-158 27406796-2 2016 Compounds 4f, 4j, 5b, 5g and 5i were found to be the most potent inhibitors of GSK-3beta in vitro amongst the twenty-five benzimidazole based thiadiazole and carbohydrazide conjugates synthesized. benzimidazole 122-135 glycogen synthase kinase 3 beta Homo sapiens 79-88 27112449-4 2016 Among these, a lead compound 6a bearing a 1H-benzimidazole motif showed comparable binding affinity to MCHR1 to the corresponding imidazopyridine derivative 1. benzimidazole 42-58 melanin-concentrating hormone receptor 1 Rattus norvegicus 103-108 27089212-4 2016 Following this approach, the interaction between triazine-benzimidazole analogues and bovine serum albumin (BSA) has been investigated with UV-Visible and fluorescence spectroscopic methods under physiological conditions. benzimidazole 58-71 albumin Homo sapiens 93-106 27261178-0 2016 Novel JAK1-selective benzimidazole inhibitors with enhanced membrane permeability. benzimidazole 21-34 Janus kinase 1 Homo sapiens 6-10 27117261-1 2016 To develop non-basic melanin-concentrating hormone receptor 1 (MCHR1) antagonists with a high probability of target selectivity and therapeutic window, we explored neutral bicyclic motifs that could replace the previously reported imidazo[1,2-a]pyridine or 1H-benzimidazole motif. benzimidazole 257-273 melanin-concentrating hormone receptor 1 Rattus norvegicus 63-68 27009905-0 2016 Plasmin inhibitors with hydrophobic amino acid-based linker between hydantoin moiety and benzimidazole scaffold enhance inhibitory activity. benzimidazole 89-102 plasminogen Homo sapiens 0-7 27058429-2 2016 Herein, we design a cRGD-polycarboxybetaine methacrylate-b-polybenzimidazole methacrylate (cRGD-PCB-b-PBBMZ) copolymer to self-assemble into smart drug-loaded nanoparticles (cRGD-PCM NPs) which can target alphavbeta3 integrin overexpressed cancer tissue by cRGD peptide unit and release drug quickly in cancer cells by protonation of benzimidazole groups. benzimidazole 63-76 pyruvate carboxylase Homo sapiens 96-99 27009905-1 2016 In this letter we report the design and synthesis of a series of plasmin inhibitors, which share the amino acid-based linker with limited free rotation between the hydantoin moiety and the benzimidazole scaffold. benzimidazole 189-202 plasminogen Homo sapiens 65-72 27096045-1 2016 To identify BCATm inhibitors suitable for in vivo study, Encoded Library Technology (ELT) was used to affinity screen a 117 million member benzimidazole based DNA encoded library, which identified an inhibitor series with both biochemical and cellular activities. benzimidazole 139-152 branched chain aminotransferase 2, mitochondrial Mus musculus 12-17 26952080-4 2016 Here, we describe a direct comparison of tetrazine ligation and strain promoted azide-alkyne cycloaddition using benzimidazole based probes to bind their known target, the gastric proton pump, ATP4A. benzimidazole 113-126 ATPase H+/K+ transporting subunit alpha Homo sapiens 193-198 26952080-6 2016 In addition, we have identified several novel binding partners of benzimidazole probes: Isoform 2 of deleted in malignant brain tumors 1 protein (DMBT1) and three uncharacterized proteins. benzimidazole 66-79 ZP domain-containing protein LOC729800-like Homo sapiens 101-144 26952080-6 2016 In addition, we have identified several novel binding partners of benzimidazole probes: Isoform 2 of deleted in malignant brain tumors 1 protein (DMBT1) and three uncharacterized proteins. benzimidazole 66-79 ZP domain-containing protein LOC729800-like Homo sapiens 146-151 26894559-1 2016 Benzimidazole analogs 1-27 were synthesized, characterized by EI-MS and (1)HNMR and their alpha-glucosidase inhibitory activities were found out experimentally. benzimidazole 0-13 sucrase-isomaltase Homo sapiens 90-107 26976506-1 2016 For finding the novel inhibitor of nuclear factor kappaB activity, a series of benzimidazole derivatives were rationally designed, synthesized and systematically studied for their in vitro activities against LPS induced NF-kappaB inhibition in RAW 264.7 cells using the SEAP assay based on the flexible chalcone JSH ((E)-1-(2-hydroxy-6-(isopentyloxy)phenyl)-3-(4-hydroxy phenyl)prop-2-en-1-one) which was previously reported. benzimidazole 79-92 toll-like receptor 4 Mus musculus 208-211 26976506-1 2016 For finding the novel inhibitor of nuclear factor kappaB activity, a series of benzimidazole derivatives were rationally designed, synthesized and systematically studied for their in vitro activities against LPS induced NF-kappaB inhibition in RAW 264.7 cells using the SEAP assay based on the flexible chalcone JSH ((E)-1-(2-hydroxy-6-(isopentyloxy)phenyl)-3-(4-hydroxy phenyl)prop-2-en-1-one) which was previously reported. benzimidazole 79-92 nuclear factor of kappa light polypeptide gene enhancer in B cells 1, p105 Mus musculus 220-229 26878127-0 2016 Design, synthesis and molecular modeling studies of few chalcone analogues of benzimidazole for epidermal growth factor receptor inhibitor in search of useful anticancer agent. benzimidazole 78-91 epidermal growth factor receptor Homo sapiens 96-128 26669310-0 2016 Mibefradil represents a new class of benzimidazole TRPM7 channel agonists. benzimidazole 37-50 transient receptor potential cation channel subfamily M member 7 Homo sapiens 51-56 26669310-8 2016 Here, we demonstrate that mibefradil and NNC 50-0396, two benzimidazole relatives of the TRPM7 inhibitor NS8593, are positive modulators of TRPM7. benzimidazole 58-71 transient receptor potential cation channel subfamily M member 7 Homo sapiens 89-94 26669310-8 2016 Here, we demonstrate that mibefradil and NNC 50-0396, two benzimidazole relatives of the TRPM7 inhibitor NS8593, are positive modulators of TRPM7. benzimidazole 58-71 transient receptor potential cation channel subfamily M member 7 Homo sapiens 140-145 26901666-5 2016 Thus, the newly designed benzimidazole 29g showed in vivo CRF1 receptor antagonistic activity and good brain penetration, indicating that it is a promising lead for CRF1 receptor antagonist drug discovery research. benzimidazole 25-38 corticotropin releasing hormone receptor 1 Mus musculus 58-71 26901666-5 2016 Thus, the newly designed benzimidazole 29g showed in vivo CRF1 receptor antagonistic activity and good brain penetration, indicating that it is a promising lead for CRF1 receptor antagonist drug discovery research. benzimidazole 25-38 corticotropin releasing hormone receptor 1 Mus musculus 165-178 26526214-1 2015 In this Letter, we report the continued optimization of the N-acyl-2-aminobenzimidazole series, focusing in particular on the N-alkyl substituent and 5-position of the benzimidazole based on the binding mode and the early SAR. benzimidazole 74-87 sarcosine dehydrogenase Homo sapiens 222-225 27194865-1 2016 BACKGROUND: Budding uninhibited by benzimidazole related 1 (BUBR1) is an important protein in the mitotic spindle assembly checkpoint. benzimidazole 35-48 BUB1 mitotic checkpoint serine/threonine kinase B Homo sapiens 60-65 26056978-2 2015 In this work benzimidazole based metal organic thin films of dichlorobis (1H-Benzimidazole) Co(II) and dichlorobis (1H-Benzimidazole) Cu(II) were deposited by chemical bath deposition method. benzimidazole 13-26 mitochondrially encoded cytochrome c oxidase II Homo sapiens 92-98 26088338-5 2015 Benzimidazole derivatives have shown a wide variety of pharmacological activities including PARP and DHODH inhibition. benzimidazole 0-13 dihydroorotate dehydrogenase (quinone) Homo sapiens 101-106 26088338-0 2015 Benzimidazole derivatives as potential dual inhibitors for PARP-1 and DHODH. benzimidazole 0-13 poly(ADP-ribose) polymerase 1 Homo sapiens 59-65 25935642-1 2015 A novel series of CXCR4 antagonists with substituted piperazines as benzimidazole replacements is described. benzimidazole 68-81 C-X-C motif chemokine receptor 4 Homo sapiens 18-23 26330080-4 2015 Three hydrazone derivatives of benzimidazole significantly increased the cellular ATP levels, reduced caspase-3 activity, reduced nitrite production and increased glucose-stimulated insulin secretion in the presence of proinflammatory cytokines. benzimidazole 31-44 caspase 3 Homo sapiens 102-111 26330080-4 2015 Three hydrazone derivatives of benzimidazole significantly increased the cellular ATP levels, reduced caspase-3 activity, reduced nitrite production and increased glucose-stimulated insulin secretion in the presence of proinflammatory cytokines. benzimidazole 31-44 insulin Homo sapiens 182-189 26370442-1 2015 A new quinazoline functionalized benzimidazole-based fluorogenic chemosensor H3L is synthesized and fully characterized by conventional techniques including single crystal X-ray analysis. benzimidazole 33-46 H3 clustered histone 2 Homo sapiens 77-80 26351728-0 2015 Benzimidazole Derivatives as Potent JAK1-Selective Inhibitors. benzimidazole 0-13 Janus kinase 1 Homo sapiens 36-40 26351728-5 2015 A clear structure-activity relationship was observed with respect to JAK1 selectivity; this highlighted the importance of hydrogen bond donors at both N(1) and R2 positions located within a specific distance from the benzimidazole core. benzimidazole 217-230 Janus kinase 1 Homo sapiens 69-73 26073618-0 2015 Synthesis of benzimidazole derivatives as potent beta-glucuronidase inhibitors. benzimidazole 13-26 glucuronidase beta Homo sapiens 49-67 26088338-0 2015 Benzimidazole derivatives as potential dual inhibitors for PARP-1 and DHODH. benzimidazole 0-13 dihydroorotate dehydrogenase (quinone) Homo sapiens 70-75 26088338-5 2015 Benzimidazole derivatives have shown a wide variety of pharmacological activities including PARP and DHODH inhibition. benzimidazole 0-13 poly(ADP-ribose) polymerase 1 Homo sapiens 92-96 26088338-6 2015 We hereby report the design, synthesis and bioactivities of a series of benzimidazole derivatives as inhibitors of both the PARP-1 and DHODH enzymes. benzimidazole 72-85 poly(ADP-ribose) polymerase 1 Homo sapiens 124-130 26088338-6 2015 We hereby report the design, synthesis and bioactivities of a series of benzimidazole derivatives as inhibitors of both the PARP-1 and DHODH enzymes. benzimidazole 72-85 dihydroorotate dehydrogenase (quinone) Homo sapiens 135-140 32689708-0 2015 Corrigendum to "Discovery of quinazolin-4-amines bearing benzimidazole fragments as dual inhibitors of c-Met and VEGFR-2" [Bioorg. benzimidazole 57-70 MET proto-oncogene, receptor tyrosine kinase Homo sapiens 103-108 32689708-0 2015 Corrigendum to "Discovery of quinazolin-4-amines bearing benzimidazole fragments as dual inhibitors of c-Met and VEGFR-2" [Bioorg. benzimidazole 57-70 kinase insert domain receptor Homo sapiens 113-120 26001340-0 2015 Novel 2,5-disubtituted-1,3,4-oxadiazoles with benzimidazole backbone: a new class of beta-glucuronidase inhibitors and in silico studies. benzimidazole 46-59 glucuronidase beta Homo sapiens 85-103 25388787-3 2015 Benzimidazole libraries were prepared using an efficient solution-phase approach and screened for inhibition of the MDM2-p53 and MDMX-p53 protein-protein interactions. benzimidazole 0-13 MDM2 proto-oncogene Homo sapiens 116-120 25388787-3 2015 Benzimidazole libraries were prepared using an efficient solution-phase approach and screened for inhibition of the MDM2-p53 and MDMX-p53 protein-protein interactions. benzimidazole 0-13 tumor protein p53 Homo sapiens 121-124 25388787-3 2015 Benzimidazole libraries were prepared using an efficient solution-phase approach and screened for inhibition of the MDM2-p53 and MDMX-p53 protein-protein interactions. benzimidazole 0-13 MDM4 regulator of p53 Homo sapiens 129-133 25388787-3 2015 Benzimidazole libraries were prepared using an efficient solution-phase approach and screened for inhibition of the MDM2-p53 and MDMX-p53 protein-protein interactions. benzimidazole 0-13 tumor protein p53 Homo sapiens 134-137 25819489-6 2015 This effort culminated in the identification of a benzimidazole, non-glycoside SGLT2 hit with an EC50 value of 0.62 muM by high-throughput screening of 41,000 compounds. benzimidazole 50-63 solute carrier family 5 member 2 Homo sapiens 79-84 27314076-3 2016 We found that DNA damage-induced PIDDosome formation is blocked by the mitotic checkpoint factor BUBR1 (budding uninhibited by benzimidazole-related 1), via a direct interaction that disrupts the PIDDosome core scaffold. benzimidazole 127-140 BUB1 mitotic checkpoint serine/threonine kinase B Homo sapiens 97-102 25921265-3 2015 The results of the former gave us pivotal information on the further optimization of the P4 moiety in plasmin inhibitors and those of the latter revealed that appropriate moieties extending from the benzimidazole scaffold engaged with S4 pocket in the active site of plasmin. benzimidazole 199-212 plasminogen Homo sapiens 102-109 25921265-3 2015 The results of the former gave us pivotal information on the further optimization of the P4 moiety in plasmin inhibitors and those of the latter revealed that appropriate moieties extending from the benzimidazole scaffold engaged with S4 pocket in the active site of plasmin. benzimidazole 199-212 plasminogen Homo sapiens 267-274 25352112-5 2015 This review will further be helpful for the researcher on the basis of substitution pattern around the nucleus with an aim to help medicinal chemists for developing an SAR on benzimidazole drugs/compounds. benzimidazole 175-188 sarcosine dehydrogenase Homo sapiens 168-171 26005536-0 2015 Discovery of Benzimidazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys. benzimidazole 13-26 cytochrome P450, family 11, subfamily b, polypeptide 2 Rattus norvegicus 27-34 26039085-1 2015 The novel field-induced single-molecule magnet based on a tetracoordinate mononuclear heteroleptic Co(II) complex involving two heterocyclic benzimidazole (bzi) and two thiocyanido ligands, [Co(bzi)2(NSC)2], (CoL4), was prepared and thoroughly characterized. benzimidazole 141-154 mitochondrially encoded cytochrome c oxidase II Homo sapiens 99-105 26039085-1 2015 The novel field-induced single-molecule magnet based on a tetracoordinate mononuclear heteroleptic Co(II) complex involving two heterocyclic benzimidazole (bzi) and two thiocyanido ligands, [Co(bzi)2(NSC)2], (CoL4), was prepared and thoroughly characterized. benzimidazole 156-159 mitochondrially encoded cytochrome c oxidase II Homo sapiens 99-105 25847768-4 2015 Here we report the screening, synthesis and SAR studies of benzimidazole derivatives as potent inhibitors against HIV-1 replication via protecting A3G protein. benzimidazole 59-72 apolipoprotein B mRNA editing enzyme catalytic subunit 3G Homo sapiens 147-150 26191374-1 2015 Benzimidazole 1 is the lead compound resulting from an antibacterial program targeting dual inhibitors of bacterial DNA gyrase and topoisomerase IV. benzimidazole 0-13 DNA topoisomerase II alpha Homo sapiens 116-126 26005536-1 2015 We report the discovery of a benzimidazole series of CYP11B2 inhibitors. benzimidazole 29-42 cytochrome P450 family 11 subfamily B member 2 Macaca mulatta 53-60 25766325-0 2015 A benzimidazole derivative exhibiting antitumor activity blocks EGFR and HER2 activity and upregulates DR5 in breast cancer cells. benzimidazole 2-15 epidermal growth factor receptor Homo sapiens 64-68 25766325-0 2015 A benzimidazole derivative exhibiting antitumor activity blocks EGFR and HER2 activity and upregulates DR5 in breast cancer cells. benzimidazole 2-15 erb-b2 receptor tyrosine kinase 2 Homo sapiens 73-77 25766325-0 2015 A benzimidazole derivative exhibiting antitumor activity blocks EGFR and HER2 activity and upregulates DR5 in breast cancer cells. benzimidazole 2-15 TNF receptor superfamily member 10b Homo sapiens 103-106 25599839-5 2015 The synthesis, biological evaluation and SAR of novel benzimidazole derivatives as KOR agonists are described. benzimidazole 54-67 sarcosine dehydrogenase Homo sapiens 41-44 25415586-3 2015 However, depending on concentration, this cationic benzimidazole derivative exhibits paradoxical positive or negative effects on the phosphorylation of Akt that are not well understood. benzimidazole 51-64 AKT serine/threonine kinase 1 Homo sapiens 152-155 25592707-0 2015 Synthesis and in vitro characterization of cinnoline and benzimidazole analogues as phosphodiesterase 10A inhibitors. benzimidazole 57-70 phosphodiesterase 10A Homo sapiens 84-105 25599839-5 2015 The synthesis, biological evaluation and SAR of novel benzimidazole derivatives as KOR agonists are described. benzimidazole 54-67 opioid receptor kappa 1 Homo sapiens 83-86 25499880-1 2015 Herein we report the identification of a highly potent and selective CB2 agonist, RQ-00202730 (40), obtained by lead optimization of the benzimidazole scaffold. benzimidazole 137-150 cannabinoid receptor 2 Rattus norvegicus 69-72 25886260-8 2015 RESULTS: A benzimidazole derivative, named MB21, was found to be the most potent in inhibiting the cloned protease (IC50 = 5.95 muM). benzimidazole 11-24 latexin Homo sapiens 128-131 25641513-4 2015 These results confirm our previously reported QSAR model on benzimidazole derivatives, providing new information for the development of small molecules with high CB1 affinity. benzimidazole 60-73 cannabinoid receptor 1 Homo sapiens 162-165 25685063-8 2015 siRNA-mediated knock-down of Noxa completely rescued benzimidazole-potentiated navitoclax activity. benzimidazole 53-66 phorbol-12-myristate-13-acetate-induced protein 1 Homo sapiens 29-33 25685063-9 2015 In addition, inhibiting caspase 3 and 9 partially rescued benzimidazole-potentiated navitoclax activity. benzimidazole 58-71 caspase 3 Homo sapiens 24-33 25748233-2 2015 identified a previously undetected participant mediating both canonical signaling, i.e., TGF-beta receptor kinase mediated, and non-canonical signaling, budding uninhibited by benzimidazole 1 (BUB1). benzimidazole 176-189 BUB1 mitotic checkpoint serine/threonine kinase Homo sapiens 193-197 25134430-0 2015 Synthesis and evaluation of benzimidazole derivatives as selective COX-2 inhibitors. benzimidazole 28-41 mitochondrially encoded cytochrome c oxidase II Homo sapiens 67-72 25415869-3 2015 Examples are a recently discovered group II PAK (PAK4, -5, -6) selective inhibitor series based on a benzimidazole core, a group I PAK selective series based on a pyrido[2,3-d]pyrimidine-7-one core, and an allosteric dibenzodiazepine PAK1 inhibitor series. benzimidazole 101-114 p21 (RAC1) activated kinase 4 Homo sapiens 44-47 25415869-3 2015 Examples are a recently discovered group II PAK (PAK4, -5, -6) selective inhibitor series based on a benzimidazole core, a group I PAK selective series based on a pyrido[2,3-d]pyrimidine-7-one core, and an allosteric dibenzodiazepine PAK1 inhibitor series. benzimidazole 101-114 p21 (RAC1) activated kinase 4 Homo sapiens 49-53 25415869-3 2015 Examples are a recently discovered group II PAK (PAK4, -5, -6) selective inhibitor series based on a benzimidazole core, a group I PAK selective series based on a pyrido[2,3-d]pyrimidine-7-one core, and an allosteric dibenzodiazepine PAK1 inhibitor series. benzimidazole 101-114 p21 (RAC1) activated kinase 4 Homo sapiens 49-52 26680714-1 2015 A molecular modeling study is performed on series of benzimidazol-based inhibitors of human dipeptidyl peptidase III (DPP III). benzimidazole 53-65 dipeptidyl peptidase 3 Homo sapiens 92-116 26680714-1 2015 A molecular modeling study is performed on series of benzimidazol-based inhibitors of human dipeptidyl peptidase III (DPP III). benzimidazole 53-65 dipeptidyl peptidase 3 Homo sapiens 118-125 26680714-3 2015 This study is aimed to elucidate the structural features of benzimidazole derivatives required for antagonism of human DPP III activity using Quantitative Structure-Activity Relationship (QSAR) analysis, and to understand the mechanism of one of the most potent inhibitor binding into the active site of this enzyme, by molecular dynamics (MD) simulations. benzimidazole 60-73 dipeptidyl peptidase 3 Homo sapiens 119-126 25303727-0 2014 Design and synthesis of benzimidazole analogs endowed with oxadiazole as selective COX-2 inhibitor. benzimidazole 24-37 mitochondrially encoded cytochrome c oxidase II Homo sapiens 83-88 25514817-0 2014 Correction to Design and Synthesis of Orally Bioavailable Benzimidazole Reverse Amides as Pan RAF Kinase Inhibitors. benzimidazole 58-71 adenosine deaminase 2 Homo sapiens 90-93 25234256-4 2014 In contrast, when the imidazole groups in L(1) are replaced with benzoimidazole groups (L(3)), L(3) also yields the 4:2 complex [(L(3))4-(Zn(2+))2] at a molar ratio of 0.50. benzimidazole 65-79 immunoglobulin kappa variable 2-14 (pseudogene) Homo sapiens 88-92 25234256-4 2014 In contrast, when the imidazole groups in L(1) are replaced with benzoimidazole groups (L(3)), L(3) also yields the 4:2 complex [(L(3))4-(Zn(2+))2] at a molar ratio of 0.50. benzimidazole 65-79 immunoglobulin kappa variable 2-14 (pseudogene) Homo sapiens 95-99 25234256-4 2014 In contrast, when the imidazole groups in L(1) are replaced with benzoimidazole groups (L(3)), L(3) also yields the 4:2 complex [(L(3))4-(Zn(2+))2] at a molar ratio of 0.50. benzimidazole 65-79 immunoglobulin kappa variable 2-14 (pseudogene) Homo sapiens 95-99 25816587-1 2014 Specifically synthesized group of benzimidazole derivatives possessing varying degrees of delocalization of the positive charge in the cation group of the molecule has been studied in order to search for potential cholinergically active compounds and to study the role of the Coulomb interaction in cholinesterase catalysis. benzimidazole 34-47 butyrylcholinesterase Homo sapiens 299-313 25349648-1 2014 We report the discovery of a novel series of DGAT1 inhibitors in the benzimidazole class with a piperdinyl-oxy-cyclohexanecarboxylic acid moiety. benzimidazole 69-82 diacylglycerol O-acyltransferase 1 Mus musculus 45-50 25255762-1 2014 The reactions of the benzimidazole nitrogen atoms and the exocyclic amino group of 2-aminobenzimidazole with CS2 in NaOH basic medium followed by methylation with methyl iodide was explored. benzimidazole 21-34 chorionic somatomammotropin hormone 2 Homo sapiens 109-112 25082515-0 2014 Discovery of quinazolin-4-amines bearing benzimidazole fragments as dual inhibitors of c-Met and VEGFR-2. benzimidazole 41-54 MET proto-oncogene, receptor tyrosine kinase Homo sapiens 87-92 25082515-0 2014 Discovery of quinazolin-4-amines bearing benzimidazole fragments as dual inhibitors of c-Met and VEGFR-2. benzimidazole 41-54 kinase insert domain receptor Homo sapiens 97-104 25082515-3 2014 Among these compounds bearing quinazoline and benzimidazole fragments, compound 7j exhibited the most potent inhibitory activity against c-Met and VEGFR-2 with IC50 of 0.05muM and 0.02muM, respectively. benzimidazole 46-59 MET proto-oncogene, receptor tyrosine kinase Homo sapiens 137-142 25082515-3 2014 Among these compounds bearing quinazoline and benzimidazole fragments, compound 7j exhibited the most potent inhibitory activity against c-Met and VEGFR-2 with IC50 of 0.05muM and 0.02muM, respectively. benzimidazole 46-59 kinase insert domain receptor Homo sapiens 147-154 24992072-1 2014 Two series of novel benzimidazole derivatives were designed, synthesized and evaluated for their SIRT1 and SIRT2 inhibitory activity. benzimidazole 20-33 sirtuin 1 Homo sapiens 97-102 24992072-1 2014 Two series of novel benzimidazole derivatives were designed, synthesized and evaluated for their SIRT1 and SIRT2 inhibitory activity. benzimidazole 20-33 sirtuin 2 Homo sapiens 107-112 25123063-6 2014 In addition, we found that a benzimidazole-based compound known to have a binding pocket on the surface of the HIV-1 capsid prevents the binding of MxB to capsid. benzimidazole 29-42 MX dynamin like GTPase 2 Homo sapiens 148-151 25221654-0 2014 Design and Synthesis of Orally Bioavailable Benzimidazole Reverse Amides as Pan RAF Kinase Inhibitors. benzimidazole 44-57 adenosine deaminase 2 Homo sapiens 76-79 25072161-0 2014 Pharmacophore modeling, 3D-QSAR and molecular docking studies of benzimidazole derivatives as potential FXR agonists. benzimidazole 65-78 nuclear receptor subfamily 1 group H member 4 Homo sapiens 104-107 25072161-2 2014 Atom-based three-dimensional quantitative structure activity relationship (3D-QSAR) models were developed for a series of 48 benzimidazole-based agonists of FXR. benzimidazole 125-138 nuclear receptor subfamily 1 group H member 4 Homo sapiens 157-160 25072161-6 2014 Furthermore, molecular docking simulation was performed to understand the binding affinity of 48 benzimidazole-based compounds against the active site of human FXR protein. benzimidazole 97-110 nuclear receptor subfamily 1 group H member 4 Homo sapiens 160-163 25072161-9 2014 Substitution effects at different positions of benzimidazole derivatives would lead to the discovery of new agonists against human FXR protein. benzimidazole 47-60 nuclear receptor subfamily 1 group H member 4 Homo sapiens 131-134 25060336-2 2014 Periodic administration of benzimidazole drugs is the mainstay for global STH control but it does not prevent re-infection, and is unlikely to interrupt transmission as a stand-alone intervention. benzimidazole 27-40 saitohin Homo sapiens 74-77 25221654-1 2014 Benzimidazole reverse amides were designed and synthesized as Pan RAF kinase inhibitors. benzimidazole 0-13 adenosine deaminase 2 Homo sapiens 62-65 24756216-1 2014 The objective of this study was to investigate the expression and clinical role of the spindle checkpoint kinase budding uninhibited by benzimidazole 1 (Bub1) in primary and metastatic advanced-stage ovarian serous carcinoma. benzimidazole 136-149 BUB1 mitotic checkpoint serine/threonine kinase Homo sapiens 153-157 24837154-0 2014 Novel benzimidazole derivatives as phosphodiesterase 10A (PDE10A) inhibitors with improved metabolic stability. benzimidazole 6-19 phosphodiesterase 10A Homo sapiens 35-56 24837154-0 2014 Novel benzimidazole derivatives as phosphodiesterase 10A (PDE10A) inhibitors with improved metabolic stability. benzimidazole 6-19 phosphodiesterase 10A Homo sapiens 58-64 24680957-5 2014 Modification of the substituents on the two 1H-benzimidazole groups of BBP resulted in analogues equipotent in anti-BVDV activity (EC50=0.7+-0.1muM), devoid of cytotoxicity (S.I.=142). benzimidazole 44-60 transmembrane protein 158 Homo sapiens 71-74 24641614-0 2014 The novel benzimidazole derivative BRP-7 inhibits leukotriene biosynthesis in vitro and in vivo by targeting 5-lipoxygenase-activating protein (FLAP). benzimidazole 10-23 arachidonate 5-lipoxygenase Homo sapiens 109-123 24641614-0 2014 The novel benzimidazole derivative BRP-7 inhibits leukotriene biosynthesis in vitro and in vivo by targeting 5-lipoxygenase-activating protein (FLAP). benzimidazole 10-23 arachidonate 5-lipoxygenase activating protein Homo sapiens 144-148 24641614-2 2014 We recently identified the benzimidazole derivative BRP-7 as chemotype for anti-LT agents by virtual screening targeting 5-LOX-activating protein (FLAP). benzimidazole 27-40 arachidonate 5-lipoxygenase activating protein Homo sapiens 147-151 23627317-1 2014 Two series of compounds (AB and APB) bearing substituted phenoxy groups at 2-position of benzimidazole nucleus through amino or phenyleneamino were synthesized and evaluated through PASS software for predicting the activity spectrum of each compound. benzimidazole 89-102 arginyl aminopeptidase Homo sapiens 32-35 24665903-0 2014 A small-molecule benzimidazole derivative that potently activates AMPK to increase glucose transport in skeletal muscle: comparison with effects of contraction and other AMPK activators. benzimidazole 17-30 protein kinase AMP-activated catalytic subunit alpha 2 Rattus norvegicus 66-70 25379167-4 2014 Furthermore, computational analysis, taken together with experimental data, provides evidence that azaindole- and indole-based attachment inhibitors bind gp120 at an accessory hydrophobic pocket beneath the CD4-binding site and can also adopt multiple unique binding modes in interacting with gp120. benzimidazole 99-108 inter-alpha-trypsin inhibitor heavy chain 4 Homo sapiens 154-159 25379167-4 2014 Furthermore, computational analysis, taken together with experimental data, provides evidence that azaindole- and indole-based attachment inhibitors bind gp120 at an accessory hydrophobic pocket beneath the CD4-binding site and can also adopt multiple unique binding modes in interacting with gp120. benzimidazole 99-108 inter-alpha-trypsin inhibitor heavy chain 4 Homo sapiens 293-298 24509821-5 2014 Among 27 lead interactions, the most avid interaction is between a benzimidazole (1) and precursor microRNA-96. benzimidazole 67-80 microRNA 96 Homo sapiens 99-110 24656800-4 2014 Aminothiazole and benzimidazole derivatives were identified as novel scaffolds that bind to the catalytic triad of sEH with good ligand efficiency. benzimidazole 18-31 epoxide hydrolase 2 Homo sapiens 115-118 24602793-7 2014 Compounds 3c &4c enhanced hPreP-mediated proteolysis of Abeta (1-42), pF1beta (2-54) and fluorogenic-substrate V. These results suggest that activation of hPreP by small benzimidazole derivatives provide a promising avenue for AD treatment. benzimidazole 170-183 prolyl endopeptidase Homo sapiens 26-31 24602793-7 2014 Compounds 3c &4c enhanced hPreP-mediated proteolysis of Abeta (1-42), pF1beta (2-54) and fluorogenic-substrate V. These results suggest that activation of hPreP by small benzimidazole derivatives provide a promising avenue for AD treatment. benzimidazole 170-183 prolyl endopeptidase Homo sapiens 155-160 25844392-10 2014 The benzimidazole microtubule/tubulin inhibitor, mebendazole complemented the anti-neoplastic cytotoxicity of gemcitabine-(C4-amide)-[anti-EGFR] in dual-combination with epirubicin-(C3-amide)-[anti-HER2/neu]. benzimidazole 4-17 epidermal growth factor receptor Homo sapiens 139-143 25844392-10 2014 The benzimidazole microtubule/tubulin inhibitor, mebendazole complemented the anti-neoplastic cytotoxicity of gemcitabine-(C4-amide)-[anti-EGFR] in dual-combination with epirubicin-(C3-amide)-[anti-HER2/neu]. benzimidazole 4-17 erb-b2 receptor tyrosine kinase 2 Homo sapiens 198-202 25844392-12 2014 The benzimidazole tubulin/microtubule inhibitor, mebendazole also possessed anti-neoplastic cytotoxicity against chemotherapeutic-resistant mammary adenocarcinoma (SKBr-3) and complemented the potency and efficacy of gemcitabine-(C4-amide)-[anti-EGFR] in dual-combination with epirubicin-(C3-amide)-[anti-HER2/neu]. benzimidazole 4-17 epidermal growth factor receptor Homo sapiens 246-250 25844392-12 2014 The benzimidazole tubulin/microtubule inhibitor, mebendazole also possessed anti-neoplastic cytotoxicity against chemotherapeutic-resistant mammary adenocarcinoma (SKBr-3) and complemented the potency and efficacy of gemcitabine-(C4-amide)-[anti-EGFR] in dual-combination with epirubicin-(C3-amide)-[anti-HER2/neu]. benzimidazole 4-17 erb-b2 receptor tyrosine kinase 2 Homo sapiens 305-309 24461289-0 2014 Benzimidazole CB2 agonists: design, synthesis and SAR. benzimidazole 0-13 cannabinoid receptor 2 Homo sapiens 14-17 24587137-4 2014 Structure-activity analysis identified a core benzimidazole-phenyl-succinamide structure as being essential to inhibition of mGPDH while modifications to the benzimidazole ring system modulated both potency and off-target effects. benzimidazole 46-59 glycerol phosphate dehydrogenase 2, mitochondrial Mus musculus 125-130 24461289-0 2014 Benzimidazole CB2 agonists: design, synthesis and SAR. benzimidazole 0-13 sarcosine dehydrogenase Homo sapiens 50-53 24461289-1 2014 A new series of CB2-selective agonists containing a benzimidazole core is reported. benzimidazole 52-65 cannabinoid receptor 2 Homo sapiens 16-19 24360999-3 2014 Compound 10 showed ten and eleven folds more activity than respective quinazoline and benzimidazole class of compounds with GI50 value of 1.64 muM. benzimidazole 86-99 latexin Homo sapiens 143-146 24387981-1 2014 A total of 15 novel benzimidazole derivatives were designed, synthesized and evaluated for their SIRT1 and SIRT2 inhibitory activity. benzimidazole 20-33 sirtuin 1 Homo sapiens 97-102 24428639-2 2014 The most potent inhibitors in this series contained a five-membered heterocycle at the 2-position of the benzimidazole, leading to highly potent and selective compounds that exploit the differences in the size of a binding pocket adjacent to the NADPH cofactor between the bacterial and human DHFR enzymes. benzimidazole 105-118 dihydrofolate reductase Homo sapiens 293-297 23356363-0 2014 Benzenesulfonamides with benzimidazole moieties as inhibitors of carbonic anhydrases I, II, VII, XII and XIII. benzimidazole 25-38 carbonic anhydrase 1 Homo sapiens 65-95 24387105-0 2014 Selective ALDH3A1 inhibition by benzimidazole analogues increase mafosfamide sensitivity in cancer cells. benzimidazole 32-45 aldehyde dehydrogenase 3 family member A1 Homo sapiens 10-17 24387981-1 2014 A total of 15 novel benzimidazole derivatives were designed, synthesized and evaluated for their SIRT1 and SIRT2 inhibitory activity. benzimidazole 20-33 sirtuin 2 Homo sapiens 107-112 24392830-0 2014 Topomer CoMFA and virtual screening studies of azaindole class renin inhibitors. benzimidazole 47-56 renin Homo sapiens 63-68 24268539-0 2014 Design, synthesis, and enzyme kinetics of novel benzimidazole and quinoxaline derivatives as methionine synthase inhibitors. benzimidazole 48-61 5-methyltetrahydrofolate-homocysteine methyltransferase Rattus norvegicus 93-112 24268539-2 2014 Benzimidazole and deazatetrahydrofolates derivatives have been shown to inhibit methionine synthase by competing with the substrate 5-methyltetrahydrofolate. benzimidazole 0-13 5-methyltetrahydrofolate-homocysteine methyltransferase Rattus norvegicus 80-99 24392830-2 2014 In this paper, a series of azaindole class renin inhibitors were subjected to 3D-QSAR study using Topomer CoMFA. benzimidazole 27-36 renin Homo sapiens 43-48 24045148-3 2013 Compound III is a benzoimidazole, which has a submicromolar IC50 in both human and rat recombinant mPGES-1. benzimidazole 18-32 prostaglandin E synthase Mus musculus 99-106 24316668-0 2014 Discovery of a benzimidazole series of ADAMTS-5 (aggrecanase-2) inhibitors by scaffold hopping. benzimidazole 15-28 ADAM metallopeptidase with thrombospondin type 1 motif 5 Homo sapiens 39-47 24316668-0 2014 Discovery of a benzimidazole series of ADAMTS-5 (aggrecanase-2) inhibitors by scaffold hopping. benzimidazole 15-28 ADAM metallopeptidase with thrombospondin type 1 motif 5 Homo sapiens 49-62 24238902-0 2013 Design and synthesis of novel benzimidazole derivatives as phosphodiesterase 10A inhibitors with reduced CYP1A2 inhibition. benzimidazole 30-43 phosphodiesterase 10A Homo sapiens 59-80 24238902-0 2013 Design and synthesis of novel benzimidazole derivatives as phosphodiesterase 10A inhibitors with reduced CYP1A2 inhibition. benzimidazole 30-43 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 105-111 24238902-2 2013 Introduction of an isopropyl group at the 2-position and a methoxy group at the 5-position of the benzimidazole ring of lead compound 1 resulted in the identification of 2-{[(2-isopropyl-5-methoxy-1-phenyl-1H-benzimidazol-6-yl)oxy]methyl}quinoline (25b), which exhibited potent PDE10A inhibitory activity with reduced CYP1A2 inhibitory activity compared to compound 1. benzimidazole 98-111 phosphodiesterase 10A Homo sapiens 278-284 24238902-2 2013 Introduction of an isopropyl group at the 2-position and a methoxy group at the 5-position of the benzimidazole ring of lead compound 1 resulted in the identification of 2-{[(2-isopropyl-5-methoxy-1-phenyl-1H-benzimidazol-6-yl)oxy]methyl}quinoline (25b), which exhibited potent PDE10A inhibitory activity with reduced CYP1A2 inhibitory activity compared to compound 1. benzimidazole 98-111 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 318-324 24533813-9 2014 In this article benzimidazole inhibitors are reported with their mechanisms of action, structure-activity relationship (SAR) and biological properties. benzimidazole 16-29 sarcosine dehydrogenase Homo sapiens 87-124 24120542-3 2013 Extensive optimization resulted in azaindole 26 (Cdc7 IC50=1.1 nM, pMCM2 IC50=32 nM) that demonstrated robust lowering of pMCM2 in a mouse pharmacodynamic (PD) model when dosed orally. benzimidazole 35-44 cell division cycle 7 (S. cerevisiae) Mus musculus 49-53 24288780-1 2013 Benzimidazole and their metal analogs that can act as multimodal agent and have non-peptidic CCK-B receptor antagonist were synthesized and characterized on the basis of spectroscopic techniques such as FT-IR, NMR, FAB-MS and also evaluated for biologic efficacy. benzimidazole 0-13 cholecystokinin B receptor Rattus norvegicus 93-107 24689236-0 2013 [Synthesis and activity evaluation of PARP-1 inhibitors with azaindole skeleton]. benzimidazole 61-70 poly(ADP-ribose) polymerase 1 Homo sapiens 38-44 24260527-10 2013 The benzylvanillin alone (Bn1) has weak anticancer activity even after it was combined with the benzimidazole (2MP), but after addition of another benzylvanillin structure (2XP), stronger activity was observed. benzimidazole 96-109 C-C motif chemokine receptor 6 Homo sapiens 26-29 24121339-0 2013 Crystal structure of a complex of human chymase with its benzimidazole derived inhibitor. benzimidazole 57-70 chymase 1 Homo sapiens 40-47 24121339-1 2013 The crystal structure of human chymase complexed with a novel benzimidazole inhibitor, TJK002, was determined at 2.8 A resolution. benzimidazole 62-75 chymase 1 Homo sapiens 31-38 24121339-2 2013 The X-ray crystallographic study shows that the benzimidazole inhibitor forms a non-covalent interaction with the catalytic domain of human chymase. benzimidazole 48-61 chymase 1 Homo sapiens 140-147 23981529-0 2013 Synthesis and antiproliferative evaluation of novel benzoimidazole-contained oxazole-bridged analogs of combretastatin A-4. benzimidazole 52-66 immunoglobulin kappa variable 1D-27 (pseudogene) Homo sapiens 119-122 24936240-1 2013 A de novo hit-to-lead effort involving the redesign of benzimidazole-containing antagonists of the CXCR4 receptor resulted in the discovery of a novel series of 1,2,3,4-tetrahydroisoquinoline (TIQ) analogues. benzimidazole 55-68 C-X-C motif chemokine receptor 4 Homo sapiens 99-104 23810496-1 2013 A series of benzimidazole derivatives with a phenylcyclohexyl acetic acid group as DGAT-1 inhibitors was developed. benzimidazole 12-25 diacylglycerol O-acyltransferase 1 Homo sapiens 83-89 23891231-0 2013 Synthesis, biological activity and molecular modeling studies on 1H-benzimidazole derivatives as acetylcholinesterase inhibitors. benzimidazole 65-81 acetylcholinesterase (Cartwright blood group) Homo sapiens 97-117 23763627-2 2013 Changing the two benzimidazole groups of the DDDD unit to triazole groups replaces two of the NH N hydrogen bonds with CH N interactions (complex [5 6]), but only reduces the association constant in CH3CN by 2 orders of magnitude (K(a) = 2.6 x 10(4) M(-1) in CH3CN; K(a) > 1 x 10(7) M(-1) in CH2Cl2). benzimidazole 17-30 single-pass membrane protein with aspartate rich tail 1 Homo sapiens 45-49 23544603-5 2013 In the present review, benzimidazole derivatives with different pharmacological activities are described on the basis of substitution pattern around the nucleus with an aim to help medicinal chemists for the development of SAR on benzimidazoles for each activity. benzimidazole 23-36 sarcosine dehydrogenase Homo sapiens 223-226 23805983-1 2013 The chlorotropy observed by NMR in this study occurred by the rapid intermolecular transfer of a chloro group between 1-chlorobenzimidazole and benzimidazole in CCl4/CH3OH/K2CO3 solution. benzimidazole 126-139 C-C motif chemokine ligand 4 Homo sapiens 161-165 23886696-0 2013 Synthesis, characterization, and molecular docking analysis of novel benzimidazole derivatives as cholinesterase inhibitors. benzimidazole 69-82 butyrylcholinesterase Homo sapiens 98-112 23886696-1 2013 Two series of novel acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitors containing benzimidazole core structure were synthesized by a four-step reaction pathway starting from 4-fluoro-3-nitrobenzoic acid as the basic compound. benzimidazole 103-116 acetylcholinesterase (Cartwright blood group) Homo sapiens 20-40 23886696-1 2013 Two series of novel acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitors containing benzimidazole core structure were synthesized by a four-step reaction pathway starting from 4-fluoro-3-nitrobenzoic acid as the basic compound. benzimidazole 103-116 acetylcholinesterase (Cartwright blood group) Homo sapiens 42-46 23886696-1 2013 Two series of novel acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitors containing benzimidazole core structure were synthesized by a four-step reaction pathway starting from 4-fluoro-3-nitrobenzoic acid as the basic compound. benzimidazole 103-116 butyrylcholinesterase Homo sapiens 52-73 23886696-1 2013 Two series of novel acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitors containing benzimidazole core structure were synthesized by a four-step reaction pathway starting from 4-fluoro-3-nitrobenzoic acid as the basic compound. benzimidazole 103-116 butyrylcholinesterase Homo sapiens 75-79 23743277-1 2013 Benzimidazole and indane are the two key fragments in our potent and selective MCH-1 receptor (MCHR1) antagonists. benzimidazole 0-13 melanin concentrating hormone receptor 1 Homo sapiens 95-100 23713567-2 2013 Using structure activity analysis, we established that the benzimidazole moiety at C-17 is essential and optimal and also that hydrophilic and heteroaromatic groups at C-3 enhance both antiproliferative (AP) and AR degrading (ARD) activities. benzimidazole 59-72 cytokine like 1 Homo sapiens 83-87 23481650-3 2013 Synthesis of focused indole and azaindole analogs yielded potent and selective 5-azaindole Cdc7 inhibitors with improved intrinsic metabolic stability (ie 36). benzimidazole 32-41 cell division cycle 7 Homo sapiens 91-95 23815580-5 2013 In the present review, benzimidazole derivatives with different pharmacological activities are described on the basis of substitution pattern around the nucleus with an aim to help medicinal chemists for the development of SAR on benzimidazoles for each activity. benzimidazole 23-36 sarcosine dehydrogenase Homo sapiens 223-226 24900745-0 2013 Potent DGAT1 Inhibitors in the Benzimidazole Class with a Pyridyl-oxy-cyclohexanecarboxylic Acid Moiety. benzimidazole 31-44 diacylglycerol O-acyltransferase 1 Mus musculus 7-12 24900745-1 2013 We report the design and synthesis of a series of novel DGAT1 inhibitors in the benzimidazole class with a pyridyl-oxy-cyclohexanecarboxylic acid moiety. benzimidazole 80-93 diacylglycerol O-acyltransferase 1 Mus musculus 56-61 23629894-0 2013 Two one-dimensional coordination polymers generated from a new benzimidazole bridging ligand and CdX2 (X = Br and I). benzimidazole 63-76 RE1 silencing transcription factor Homo sapiens 103-115 23525274-1 2013 A conceptually new and general strategy has been developed for the construction of a benzimidazole or a benzoxazole ring fused with isoquinolinone affording a diverse and unique class of small molecules as potential and novel inhibitors of PDE4. benzimidazole 85-98 phosphodiesterase 4A Homo sapiens 240-244 23392733-1 2013 BUBR1 (budding uninhibited by benzimidazole-related 1) represents the component of a controlling complex in mitosis. benzimidazole 30-43 BUB1 mitotic checkpoint serine/threonine kinase B Homo sapiens 0-5 23440991-2 2013 The budding uninhibited by benzimidazole 1 (BUB1) gene is a highly conserved protein that plays a critical role at the spindle assembly checkpoint during cell division. benzimidazole 27-40 BUB1 mitotic checkpoint serine/threonine kinase Homo sapiens 44-48 23360431-5 2013 A predictive model was developed from the initial SAR in which the potency of the analogues correlated with the ability of the substituent in the 7-position of the azaindole to adopt a coplanar conformation by either forming internal hydrogen bonds or avoiding repulsive substitution patterns. benzimidazole 164-173 sarcosine dehydrogenase Homo sapiens 50-53 22946527-0 2013 Synthesis, p38 kinase inhibitory and anti-inflammatory activity of new substituted benzimidazole derivatives. benzimidazole 83-96 mitogen-activated protein kinase 14 Homo sapiens 11-14 22812394-3 2013 In this study, we prepared a group of Co(II)-pbzim complexes that bear variable numbers of both positive charges and benzimidazole (bzim) groups. benzimidazole 117-130 mitochondrially encoded cytochrome c oxidase II Homo sapiens 38-44 22812394-3 2013 In this study, we prepared a group of Co(II)-pbzim complexes that bear variable numbers of both positive charges and benzimidazole (bzim) groups. benzimidazole 46-50 mitochondrially encoded cytochrome c oxidase II Homo sapiens 38-44 23438747-3 2013 Using a high-throughput chemical screen, we identified a benzimidazole compound, wALADin1, that selectively targets the delta-aminolevulinic acid dehydratase (ALAD) of Wolbachia (wALAD) and exhibits macrofilaricidal effects on Wolbachia-containing filarial worms in vitro. benzimidazole 57-70 aminolevulinate dehydratase Homo sapiens 120-157 23438747-3 2013 Using a high-throughput chemical screen, we identified a benzimidazole compound, wALADin1, that selectively targets the delta-aminolevulinic acid dehydratase (ALAD) of Wolbachia (wALAD) and exhibits macrofilaricidal effects on Wolbachia-containing filarial worms in vitro. benzimidazole 57-70 aminolevulinate dehydratase Homo sapiens 82-86 24900653-0 2013 Azaindole-Based Inhibitors of Cdc7 Kinase: Impact of the Pre-DFG Residue, Val 195. benzimidazole 0-9 cell division cycle 7 Homo sapiens 30-34 24900653-2 2013 X-ray cocrystallization using a surrogate protein, GSK3beta, and modeling studies confirmed the azaindole motif as the hinge binder. benzimidazole 96-105 glycogen synthase kinase 3 beta Homo sapiens 51-59 24155042-4 2012 Based on these findings, we designed and synthesized new PPARgamma ligands with a benzimidazole (agonists 4-5 and 4-6), benzothiophene (agonists 5-5 and 5-6) or benzofuran (agonists 6-5 and 6-6) moiety either at position 5 or 6 of the benzimidazole core structure. benzimidazole 82-95 peroxisome proliferator activated receptor gamma Mus musculus 57-66 23206862-0 2013 Identification of a novel benzimidazole derivative as a highly potent NPY Y5 receptor antagonist with an anti-obesity profile. benzimidazole 26-39 neuropeptide Y receptor Y5 Mus musculus 70-85 23026385-0 2012 Docking investigation and binding interaction of benzimidazole derivative with bovine serum albumin. benzimidazole 49-62 albumin Homo sapiens 86-99 23025998-0 2012 Identification of a novel and orally available benzimidazole derivative as an NPY Y5 receptor antagonist with in vivo efficacy. benzimidazole 47-60 neuropeptide Y receptor Y5 Homo sapiens 78-93 23141914-0 2012 Discovery of a novel series of benzimidazole derivatives as diacylglycerol acyltransferase inhibitors. benzimidazole 31-44 diacylglycerol O-acyltransferase 1 Homo sapiens 60-90 23141914-1 2012 A novel series of benzimidazole derivatives was prepared and evaluated for their diacylglycerol acyltransferase (DGAT) inhibitory activity using microsome from rat liver. benzimidazole 18-31 diacylglycerol O-acyltransferase 1 Rattus norvegicus 81-111 23141914-1 2012 A novel series of benzimidazole derivatives was prepared and evaluated for their diacylglycerol acyltransferase (DGAT) inhibitory activity using microsome from rat liver. benzimidazole 18-31 diacylglycerol O-acyltransferase 1 Rattus norvegicus 113-117 23058106-0 2012 Benzimidazole inhibitors of the protein kinase CHK2: clarification of the binding mode by flexible side chain docking and protein-ligand crystallography. benzimidazole 0-13 checkpoint kinase 2 Homo sapiens 47-51 23058106-1 2012 Two closely related binding modes have previously been proposed for the ATP-competitive benzimidazole class of checkpoint kinase 2 (CHK2) inhibitors; however, neither binding mode is entirely consistent with the reported SAR. benzimidazole 88-101 checkpoint kinase 2 Homo sapiens 111-130 23058106-1 2012 Two closely related binding modes have previously been proposed for the ATP-competitive benzimidazole class of checkpoint kinase 2 (CHK2) inhibitors; however, neither binding mode is entirely consistent with the reported SAR. benzimidazole 88-101 checkpoint kinase 2 Homo sapiens 132-136 23058106-1 2012 Two closely related binding modes have previously been proposed for the ATP-competitive benzimidazole class of checkpoint kinase 2 (CHK2) inhibitors; however, neither binding mode is entirely consistent with the reported SAR. benzimidazole 88-101 sarcosine dehydrogenase Homo sapiens 221-224 23058106-2 2012 Unconstrained rigid docking of benzimidazole ligands into representative CHK2 protein crystal structures reveals an alternative binding mode involving a water-mediated interaction with the hinge region; docking which incorporates protein side chain flexibility for selected residues in the ATP binding site resulted in a refinement of the water-mediated hinge binding mode that is consistent with observed SAR. benzimidazole 31-44 checkpoint kinase 2 Homo sapiens 73-77 23058106-2 2012 Unconstrained rigid docking of benzimidazole ligands into representative CHK2 protein crystal structures reveals an alternative binding mode involving a water-mediated interaction with the hinge region; docking which incorporates protein side chain flexibility for selected residues in the ATP binding site resulted in a refinement of the water-mediated hinge binding mode that is consistent with observed SAR. benzimidazole 31-44 sarcosine dehydrogenase Homo sapiens 406-409 23058106-3 2012 The flexible docking results are in good agreement with the crystal structures of four exemplar benzimidazole ligands bound to CHK2 which unambiguously confirmed the binding mode of these inhibitors, including the water-mediated interaction with the hinge region, and which is significantly different from binding modes previously postulated in the literature. benzimidazole 96-109 checkpoint kinase 2 Homo sapiens 127-131 24155042-4 2012 Based on these findings, we designed and synthesized new PPARgamma ligands with a benzimidazole (agonists 4-5 and 4-6), benzothiophene (agonists 5-5 and 5-6) or benzofuran (agonists 6-5 and 6-6) moiety either at position 5 or 6 of the benzimidazole core structure. benzimidazole 235-248 peroxisome proliferator activated receptor gamma Mus musculus 57-66 22564276-0 2012 Novel benzimidazole analogs as inhibitors of EGFR tyrosine kinase. benzimidazole 6-19 epidermal growth factor receptor Homo sapiens 45-49 22854224-0 2012 Antioxidant benzimidazole bind bovine serum albumin. benzimidazole 12-25 albumin Homo sapiens 38-51 22519452-0 2012 Modulation of PAR(1) signalling by benzimidazole compounds. benzimidazole 36-49 Prader Willi/Angelman region RNA 1 Homo sapiens 14-20 22921743-8 2012 Two inhibitors are benzimidazole-like compounds that reversibly and competitively inhibit human DDAH-1 with Ligand Efficiency values >=0.3 kcal/mol/heavy (non-hydrogen) atom, indicating their suitability for further development. benzimidazole 19-32 dimethylarginine dimethylaminohydrolase 1 Homo sapiens 96-102 22877085-2 2012 Using a structure-based design approach, we have identified a series of potent and selective benzimidazole-based inhibitors of PI3Kdelta. benzimidazole 93-106 phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta Homo sapiens 127-136 22853998-0 2012 Design, synthesis and identification of novel benzimidazole derivatives as highly potent NPY Y5 receptor antagonists with attractive in vitro ADME profiles. benzimidazole 46-59 neuropeptide Y receptor Y5 Homo sapiens 89-104 22519452-11 2012 CONCLUSIONS AND IMPLICATIONS: The Q94 and Q109 benzimidazole derivatives represent a novel scaffold for the development of new PAR(1) inhibitors and provide a starting point to develop dual signalling pathway-selective positive/negative modulators of PAR(1) . benzimidazole 47-60 Prader Willi/Angelman region RNA 1 Homo sapiens 127-133 22801646-1 2012 The lead optimization of a series of potent azaindole IKK2 inhibitors is described. benzimidazole 44-53 inhibitor of nuclear factor kappa B kinase subunit beta Homo sapiens 54-58 22519452-11 2012 CONCLUSIONS AND IMPLICATIONS: The Q94 and Q109 benzimidazole derivatives represent a novel scaffold for the development of new PAR(1) inhibitors and provide a starting point to develop dual signalling pathway-selective positive/negative modulators of PAR(1) . benzimidazole 47-60 Prader Willi/Angelman region RNA 1 Homo sapiens 252-258 22863183-0 2012 Synthesis and biological evaluation of novel benzimidazole derivatives and their binding behavior with bovine serum albumin. benzimidazole 45-58 albumin Homo sapiens 110-123 22863183-4 2012 The interaction evaluation of compound 11d with bovine serum albumin (BSA) by Fluorescence and UV-vis absorption spectroscopic method showed that BSA could generate fluorescent quenching under approximately human physiological conditions by the prepared benzimidazole compound 11d as result of the formation of ground-state compound 11d-BSA complex. benzimidazole 254-267 albumin Homo sapiens 55-68 24900520-0 2012 Substituted benzimidazole and imidazopyridine compounds useful as cyp17 modulators: patent highlight. benzimidazole 12-25 cytochrome P450 family 17 subfamily A member 1 Homo sapiens 66-71 22765895-4 2012 Through targeted SAR and structure-guided design, new imidazopyridine and imidazopyridazine scaffolds were identified that demonstrated superior inhibition of mTOR in cellular assays, selectivity over the closely related PIKK family and improved in vivo clearance over our previously reported benzimidazole series. benzimidazole 293-306 sarcosine dehydrogenase Homo sapiens 17-20 22765895-4 2012 Through targeted SAR and structure-guided design, new imidazopyridine and imidazopyridazine scaffolds were identified that demonstrated superior inhibition of mTOR in cellular assays, selectivity over the closely related PIKK family and improved in vivo clearance over our previously reported benzimidazole series. benzimidazole 293-306 mechanistic target of rapamycin kinase Homo sapiens 159-163 22357520-2 2012 To understand how telmisartan partially activates PPARgamma, we determined the ternary complex structure of PPARgamma, telmisartan, and a coactivator peptide from steroid receptor coactivator-1 at a resolution of 2.18 A. Crystallographic analysis revealed that telmisartan exhibits an unexpected binding mode in which the central benzimidazole ring is engaged in a non-canonical--and suboptimal--hydrogen-bonding network around helix 12 (H12). benzimidazole 330-343 peroxisome proliferator activated receptor gamma Homo sapiens 108-117 22481174-2 2012 The mutual interaction of this benzimidazole derivative (MBTBI) with bovine serum albumin (BSA) was investigated using solution spectral studies. benzimidazole 31-44 albumin Homo sapiens 76-95 22127612-8 2012 Concurrently, we identified several unique binding features of benzimidazole derivatives and showed that alkoxy-substituents of the benzimidazole ring are located within a FPR1 hole bounded by Thr199, Thr265, Ile268, and Leu271 or in a groove in the vicinity of Leu198, Arg201, Gly202, and Arg205. benzimidazole 63-76 formyl peptide receptor 1 Homo sapiens 172-176 22607880-0 2012 Identification of novel benzimidazole derivatives as inhibitors of leukotriene biosynthesis by virtual screening targeting 5-lipoxygenase-activating protein (FLAP). benzimidazole 24-37 arachidonate 5-lipoxygenase Homo sapiens 123-137 22607880-0 2012 Identification of novel benzimidazole derivatives as inhibitors of leukotriene biosynthesis by virtual screening targeting 5-lipoxygenase-activating protein (FLAP). benzimidazole 24-37 arachidonate 5-lipoxygenase activating protein Homo sapiens 158-162 22127612-8 2012 Concurrently, we identified several unique binding features of benzimidazole derivatives and showed that alkoxy-substituents of the benzimidazole ring are located within a FPR1 hole bounded by Thr199, Thr265, Ile268, and Leu271 or in a groove in the vicinity of Leu198, Arg201, Gly202, and Arg205. benzimidazole 132-145 formyl peptide receptor 1 Homo sapiens 172-176 22127612-9 2012 The understanding of these molecular features will likely prove beneficial in future design of novel FPR1 agonists based on the benzimidazole scaffold. benzimidazole 128-141 formyl peptide receptor 1 Homo sapiens 101-105 24900459-1 2012 A novel series of benzimidazole designed multiple ligands (DMLs) with activity at the neuronal nitric oxide synthase (nNOS) enzyme and the mu-opioid receptor was developed. benzimidazole 18-31 nitric oxide synthase 1 Homo sapiens 86-116 22464457-0 2012 In silico binding free energy predictability with pi-pi interaction energy-augmented scoring function: benzimidazole Raf inhibitors as a case study. benzimidazole 103-116 zinc fingers and homeoboxes 2 Homo sapiens 117-120 22268420-1 2012 One pharmacophore model and three quantitative structure-activity relationship models were developed on a series of benzimidazole and imidazole inhibitors of histone deacetylase 2. benzimidazole 116-129 histone deacetylase 2 Homo sapiens 158-179 22530898-0 2012 Synthesis and beta-glucuronidase inhibitory potential of benzimidazole derivatives. benzimidazole 57-70 glucuronidase beta Homo sapiens 14-32 22530898-1 2012 Benzimidazole derivatives 1-24 have been synthesized and their in vitro beta-glucuronidase inhibitory activitiy was evaluated. benzimidazole 0-13 glucuronidase beta Homo sapiens 72-90 22237832-2 2012 Benzimidazole forming ring closure was enabled under microwave irradiation in the presence of 10% TFA/DCE. benzimidazole 0-13 24-dehydrocholesterol reductase Homo sapiens 102-105 22524426-0 2012 Discovery and optimization of new benzimidazole- and benzoxazole-pyrimidone selective PI3Kbeta inhibitors for the treatment of phosphatase and TENsin homologue (PTEN)-deficient cancers. benzimidazole 34-47 phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta Homo sapiens 86-94 22524426-0 2012 Discovery and optimization of new benzimidazole- and benzoxazole-pyrimidone selective PI3Kbeta inhibitors for the treatment of phosphatase and TENsin homologue (PTEN)-deficient cancers. benzimidazole 34-47 phosphatase and tensin homolog Homo sapiens 127-159 22524426-0 2012 Discovery and optimization of new benzimidazole- and benzoxazole-pyrimidone selective PI3Kbeta inhibitors for the treatment of phosphatase and TENsin homologue (PTEN)-deficient cancers. benzimidazole 34-47 phosphatase and tensin homolog Homo sapiens 161-165 22524426-3 2012 Herein we describe the discovery and optimization of a new series of benzimidazole- and benzoxazole-pyrimidones as small molecular mass PI3Kbeta-selective inhibitors. benzimidazole 69-82 phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta Homo sapiens 136-144 22856146-3 2012 Several potential benzimidazole--plant FtsZ protein binding sites were identified. benzimidazole 18-31 Tubulin/FtsZ family protein Arabidopsis thaliana 39-43 22366657-0 2012 A novel series of benzimidazole NR2B-selective NMDA receptor antagonists. benzimidazole 18-31 glutamate ionotropic receptor NMDA type subunit 2B Homo sapiens 32-36 24900459-1 2012 A novel series of benzimidazole designed multiple ligands (DMLs) with activity at the neuronal nitric oxide synthase (nNOS) enzyme and the mu-opioid receptor was developed. benzimidazole 18-31 nitric oxide synthase 1 Homo sapiens 118-122 22204908-1 2012 The newly synthesized benzimidazole compounds were suggested to be inhibitors of Plasmodium falciparum plasmepsin II and human cathepsin D by virtual screening of an internal library of synthetic compounds. benzimidazole 22-35 cathepsin D Homo sapiens 127-138 21724404-0 2011 Discovery of benzimidazole derivatives as novel multi-target EGFR, VEGFR-2 and PDGFR kinase inhibitors. benzimidazole 13-26 epidermal growth factor receptor Homo sapiens 61-65 22119126-2 2012 The benzimidazole (L) crystallizes in the space group P2(1)/c with a = 8.6660(3) A, b = 16.6739(7) A, c = 9.8611(4) A and beta = 113.505(3) and forms an infinite chain structure with a trans-zigzag type along the crystallographic axis "a", through the intermolecular H-bond. benzimidazole 4-17 H3 histone pseudogene 16 Homo sapiens 54-59 23109848-0 2012 A combination of 3D-QSAR, molecular docking and molecular dynamics simulation studies of benzimidazole-quinolinone derivatives as iNOS inhibitors. benzimidazole 89-102 nitric oxide synthase 2 Homo sapiens 130-134 23109848-2 2012 In previous studies, a series of benzimidazole-quinolinone derivatives with high inhibitory activity against human iNOS were discovered. benzimidazole 33-46 nitric oxide synthase 2 Homo sapiens 115-119 21723881-5 2011 In contrast, several novel benzimidazole openers showed selectivity for KCNQ2/3 and KCNQ2 and retain activity at KCNQ2(W236L). benzimidazole 27-40 potassium voltage-gated channel subfamily Q member 2 Homo sapiens 72-79 21723881-5 2011 In contrast, several novel benzimidazole openers showed selectivity for KCNQ2/3 and KCNQ2 and retain activity at KCNQ2(W236L). benzimidazole 27-40 potassium voltage-gated channel subfamily Q member 2 Homo sapiens 72-77 21723881-5 2011 In contrast, several novel benzimidazole openers showed selectivity for KCNQ2/3 and KCNQ2 and retain activity at KCNQ2(W236L). benzimidazole 27-40 potassium voltage-gated channel subfamily Q member 2 Homo sapiens 84-89 21820945-0 2011 Synthesis and interaction studies of benzimidazole derivative with human serum albumin. benzimidazole 37-50 albumin Homo sapiens 73-86 21798739-0 2011 Discovery of GSK1997132B a novel centrally penetrant benzimidazole PPARgamma partial agonist. benzimidazole 53-66 peroxisome proliferator activated receptor gamma Homo sapiens 67-76 21798739-2 2011 A novel benzimidazole series of centrally penetrant PPARgamma partial agonists has been identified. benzimidazole 8-21 peroxisome proliferator activated receptor gamma Homo sapiens 52-61 21724404-0 2011 Discovery of benzimidazole derivatives as novel multi-target EGFR, VEGFR-2 and PDGFR kinase inhibitors. benzimidazole 13-26 kinase insert domain receptor Homo sapiens 67-74 21724404-0 2011 Discovery of benzimidazole derivatives as novel multi-target EGFR, VEGFR-2 and PDGFR kinase inhibitors. benzimidazole 13-26 platelet derived growth factor receptor beta Homo sapiens 79-84 21724404-2 2011 In this work, we used two virtual screening methods, support vector machines (SVM) and molecular docking, to identify a novel series of benzimidazole derivatives, 2-aryl benzimidazole compounds, as multi-target EGFR, VEGFR-2 and PDGFR inhibitors. benzimidazole 136-149 epidermal growth factor receptor Homo sapiens 211-215 21724404-2 2011 In this work, we used two virtual screening methods, support vector machines (SVM) and molecular docking, to identify a novel series of benzimidazole derivatives, 2-aryl benzimidazole compounds, as multi-target EGFR, VEGFR-2 and PDGFR inhibitors. benzimidazole 136-149 kinase insert domain receptor Homo sapiens 217-224 21724404-2 2011 In this work, we used two virtual screening methods, support vector machines (SVM) and molecular docking, to identify a novel series of benzimidazole derivatives, 2-aryl benzimidazole compounds, as multi-target EGFR, VEGFR-2 and PDGFR inhibitors. benzimidazole 136-149 platelet derived growth factor receptor beta Homo sapiens 229-234 21724404-7 2011 Our study discovered a novel series of benzimidazole derivatives as multi-target EGFR, VEGFR-2 and PDGFR kinases inhibitors. benzimidazole 39-52 epidermal growth factor receptor Homo sapiens 81-85 21724404-7 2011 Our study discovered a novel series of benzimidazole derivatives as multi-target EGFR, VEGFR-2 and PDGFR kinases inhibitors. benzimidazole 39-52 kinase insert domain receptor Homo sapiens 87-94 21724404-7 2011 Our study discovered a novel series of benzimidazole derivatives as multi-target EGFR, VEGFR-2 and PDGFR kinases inhibitors. benzimidazole 39-52 platelet derived growth factor receptor beta Homo sapiens 99-104 21319800-2 2011 The benzimidazole derivative AKT inhibitor-IV (ChemBridge 5233705) affects this pathway and exhibits potent anticancer and antiviral activity. benzimidazole 4-17 AKT serine/threonine kinase 1 Homo sapiens 29-32 21669533-1 2011 A series of benzimidazole CB(2) receptor agonists were prepared and their properties investigated. benzimidazole 12-25 cannabinoid receptor 2 Rattus norvegicus 26-40 20607332-3 2011 In this work, molecular modeling and QSAR studies of a set of 30 compounds, indole and benzimidazole derivatives, as H(4)R antagonists were performed. benzimidazole 87-100 histamine receptor H4 Homo sapiens 117-122 20697761-0 2011 3D-QSAR and molecular docking studies of azaindole derivatives as Aurora B kinase inhibitors. benzimidazole 41-50 aurora kinase B Homo sapiens 66-74 20697761-2 2011 Recently a series of azaindole derivatives with Aurora B inhibitory activities were reported. benzimidazole 21-30 aurora kinase B Homo sapiens 48-56 20697761-3 2011 To explore the relationship between the structures of substituted azaindole derivatives and their inhibition of Aurora B, 3D-QSAR and molecular docking studies were performed on a dataset of 41 compounds. benzimidazole 66-75 aurora kinase B Homo sapiens 112-120 21366329-0 2011 Benzimidazole inhibitors induce a DFG-out conformation of never in mitosis gene A-related kinase 2 (Nek2) without binding to the back pocket and reveal a nonlinear structure-activity relationship. benzimidazole 0-13 NIMA related kinase 2 Homo sapiens 100-104 21481591-0 2011 2-Arylbenzothiazole, benzoxazole and benzimidazole derivatives as fluorogenic substrates for the detection of nitroreductase and aminopeptidase activity in clinically important bacteria. benzimidazole 37-50 carboxypeptidase Q Homo sapiens 129-143 21130741-6 2011 Telmisartan has a unique binding mode to the AT1 receptor due to its distal benzimidazole portion. benzimidazole 76-89 angiotensin II receptor type 1 Homo sapiens 45-57 21269824-0 2011 Optimization of a novel class of benzimidazole-based farnesoid X receptor (FXR) agonists to improve physicochemical and ADME properties. benzimidazole 33-46 nuclear receptor subfamily 1, group H, member 4 Mus musculus 75-78 21185722-2 2011 The SAR leading to the identification of the optimal azaindole regioisomer as well as the pharmacokinetics and off-target activities of the most potent antagonists are disclosed. benzimidazole 53-62 sarcosine dehydrogenase Homo sapiens 4-7 21128593-0 2011 Design and optimization of benzimidazole-containing transient receptor potential melastatin 8 (TRPM8) antagonists. benzimidazole 27-40 transient receptor potential cation channel, subfamily M, member 8 Rattus norvegicus 52-93 21128593-0 2011 Design and optimization of benzimidazole-containing transient receptor potential melastatin 8 (TRPM8) antagonists. benzimidazole 27-40 transient receptor potential cation channel, subfamily M, member 8 Rattus norvegicus 95-100 21128593-3 2011 The design, synthesis, and optimization of a class of selective TRPM8 antagonists based on a benzimidazole scaffold is described, leading to the identification of compounds that exhibited potent antagonism of TRPM8 in cell-based functional assays for human, rat, and canine TRPM8 channels. benzimidazole 93-106 transient receptor potential cation channel subfamily M member 8 Homo sapiens 64-69 21128593-3 2011 The design, synthesis, and optimization of a class of selective TRPM8 antagonists based on a benzimidazole scaffold is described, leading to the identification of compounds that exhibited potent antagonism of TRPM8 in cell-based functional assays for human, rat, and canine TRPM8 channels. benzimidazole 93-106 transient receptor potential cation channel subfamily M member 8 Homo sapiens 209-214 21128593-3 2011 The design, synthesis, and optimization of a class of selective TRPM8 antagonists based on a benzimidazole scaffold is described, leading to the identification of compounds that exhibited potent antagonism of TRPM8 in cell-based functional assays for human, rat, and canine TRPM8 channels. benzimidazole 93-106 transient receptor potential cation channel subfamily M member 8 Canis lupus familiaris 209-214 20951033-1 2010 A novel class of benzimidazole NPY Y5 receptor antagonists was prepared exploiting a privileged spirocarbamate moiety. benzimidazole 17-30 neuropeptide Y receptor Y5 Rattus norvegicus 31-46 21144757-0 2011 Design, synthesis, and testing of an 6-O-linked series of benzimidazole based inhibitors of CDK5/p25. benzimidazole 58-71 cyclin dependent kinase 5 Homo sapiens 92-96 21144757-0 2011 Design, synthesis, and testing of an 6-O-linked series of benzimidazole based inhibitors of CDK5/p25. benzimidazole 58-71 cyclin dependent kinase 5 regulatory subunit 1 Homo sapiens 97-100 21220496-10 2011 These data suggest that benzimidazole IGF-1R/InsR inhibitors may select for upregulation and be effluxed by the ATP-binding cassette transporter, BCRP, contributing to resistance. benzimidazole 24-37 insulin like growth factor 1 receptor Homo sapiens 38-44 21220496-10 2011 These data suggest that benzimidazole IGF-1R/InsR inhibitors may select for upregulation and be effluxed by the ATP-binding cassette transporter, BCRP, contributing to resistance. benzimidazole 24-37 insulin receptor Homo sapiens 45-49 21220496-10 2011 These data suggest that benzimidazole IGF-1R/InsR inhibitors may select for upregulation and be effluxed by the ATP-binding cassette transporter, BCRP, contributing to resistance. benzimidazole 24-37 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 146-150 21220496-0 2011 Drug efflux by breast cancer resistance protein is a mechanism of resistance to the benzimidazole insulin-like growth factor receptor/insulin receptor inhibitor, BMS-536924. benzimidazole 84-97 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 15-47 21067921-0 2010 Discovery of new azaindole-based PI3Kalpha inhibitors: apoptotic and antiangiogenic effect on cancer cells. benzimidazole 17-26 phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha Homo sapiens 33-42 21067921-3 2010 By varying groups at the 3,5-positions of azaindole, we developed the SAR (Structure-activity relationship) and identified a series of potent PI3Kalpha inhibitors. benzimidazole 42-51 phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha Homo sapiens 142-151 20937029-0 2010 Substituted benzimidazole derivatives as angiotensin II-AT1 receptor antagonist: a review. benzimidazole 12-25 angiotensinogen Homo sapiens 41-55 20937029-10 2010 Research efforts for development of new molecules with similar structural features have led to the discovery of various non-peptidic Ang II receptor antagonists with different substituted heterocyclic such as imidazole (losartan) and benzimidazole (candesartan and telmisartan). benzimidazole 234-247 angiotensinogen Homo sapiens 133-139 20937029-11 2010 In this study we have critically reviewed various benzimidazole substituted compounds as Ang II-AT(1) receptor antagonists and explored other potential clinical uses for this class of compounds. benzimidazole 50-63 angiotensinogen Homo sapiens 89-95 20965737-1 2010 In a prior communication we identified a novel class of benzimidazole-based inhibitors of EGF-induced phosphorylation of ERK5. benzimidazole 56-69 mitogen-activated protein kinase 7 Homo sapiens 121-125 20933412-1 2010 A series of potent, benzimidazole-based SCD inhibitors which demonstrate selectivity for the hSCD1 enzyme over the hSCD5 isoform are described. benzimidazole 20-33 stearoyl-CoA desaturase Homo sapiens 40-43 20933412-1 2010 A series of potent, benzimidazole-based SCD inhibitors which demonstrate selectivity for the hSCD1 enzyme over the hSCD5 isoform are described. benzimidazole 20-33 stearoyl-CoA desaturase Homo sapiens 93-98 20965737-2 2010 In this paper we examine the biological activity of several 1-isopropyl-4-amino-6-ether linked benzimidazole-based compounds for their ability to selectively inhibit EGF-mediated ERK5 phosphorylation; potential utility of variation at the 6-position was indicated by the initial structural feature survey. benzimidazole 95-108 mitogen-activated protein kinase 7 Homo sapiens 179-183 20933412-1 2010 A series of potent, benzimidazole-based SCD inhibitors which demonstrate selectivity for the hSCD1 enzyme over the hSCD5 isoform are described. benzimidazole 20-33 stearoyl-CoA desaturase 5 Homo sapiens 115-120 20153189-0 2010 SAR of PXR transactivation in benzimidazole-based IGF-1R kinase inhibitors. benzimidazole 30-43 sarcosine dehydrogenase Homo sapiens 0-3 20642456-10 2010 We synthesized five elaborated benzimidazole compounds and characterized their binding to PNMT, showing for the first time how this class of inhibitors interact with the noradrenaline-binding site. benzimidazole 31-44 phenylethanolamine N-methyltransferase Homo sapiens 90-94 20660191-8 2010 Moreover, LANA associated with another kinetochore protein, Bub1 (budding uninhibited by benzimidazole 1), which is known to form a complex with CENP-F. benzimidazole 89-102 LANA Human gammaherpesvirus 8 10-14 20660191-8 2010 Moreover, LANA associated with another kinetochore protein, Bub1 (budding uninhibited by benzimidazole 1), which is known to form a complex with CENP-F. benzimidazole 89-102 BUB1 mitotic checkpoint serine/threonine kinase Homo sapiens 60-64 20660191-8 2010 Moreover, LANA associated with another kinetochore protein, Bub1 (budding uninhibited by benzimidazole 1), which is known to form a complex with CENP-F. benzimidazole 89-102 centromere protein F Homo sapiens 145-151 20724156-2 2010 The synthesis and biological evaluation of novel benzimidazole derivatives as MCHR1 antagonists are described. benzimidazole 49-62 melanin concentrating hormone receptor 1 Homo sapiens 78-83 20174844-1 2010 Novel classes of cannabinoid 2 receptor (CB2) agonists based on 1,2,3,4-tetrahydropyrrolo[3,4-b]indole and benzimidazole scaffolds have shown high binding affinity toward CB2 receptor and good selectivity over cannabinoid 1 receptor (CB1). benzimidazole 107-120 cannabinoid receptor 2 Homo sapiens 171-174 20174844-1 2010 Novel classes of cannabinoid 2 receptor (CB2) agonists based on 1,2,3,4-tetrahydropyrrolo[3,4-b]indole and benzimidazole scaffolds have shown high binding affinity toward CB2 receptor and good selectivity over cannabinoid 1 receptor (CB1). benzimidazole 107-120 cannabinoid receptor 1 Homo sapiens 210-232 20174844-1 2010 Novel classes of cannabinoid 2 receptor (CB2) agonists based on 1,2,3,4-tetrahydropyrrolo[3,4-b]indole and benzimidazole scaffolds have shown high binding affinity toward CB2 receptor and good selectivity over cannabinoid 1 receptor (CB1). benzimidazole 107-120 cannabinoid receptor 1 Homo sapiens 234-237 20649571-0 2010 2-Phenyl-5-(pyrrolidin-1-yl)-1-(3,4,5-trimethoxybenzyl)-1H-benzimidazole, a benzimidazole derivative, inhibits growth of human prostate cancer cells by affecting tubulin and c-Jun N-terminal kinase. benzimidazole 59-72 mitogen-activated protein kinase 8 Homo sapiens 174-197 20545947-1 2010 From an azaindole lead, identified in high throughput screen, a series of potent bis-azaindole inhibitors of IGF1-R have been synthesized using rational drug design and SAR based on a in silico binding mode hypothesis. benzimidazole 8-17 insulin like growth factor 1 receptor Homo sapiens 109-115 20545947-1 2010 From an azaindole lead, identified in high throughput screen, a series of potent bis-azaindole inhibitors of IGF1-R have been synthesized using rational drug design and SAR based on a in silico binding mode hypothesis. benzimidazole 8-17 sarcosine dehydrogenase Homo sapiens 169-172 20484153-0 2010 Structural requirements for inverse agonism and neutral antagonism of indole-, benzimidazole-, and thienopyrrole-derived histamine H4 receptor ligands. benzimidazole 79-92 histamine receptor H4 Homo sapiens 121-142 20875744-1 2010 In this study, the benzimidazole derivatives were synthesized and evaluated as imaging agents for the NR2B subtype of NMDA receptor. benzimidazole 19-32 glutamate receptor, ionotropic, NMDA2B (epsilon 2) Mus musculus 102-106 20828702-3 2010 Based on the chromatographic behaviors for the resolution of PPI analogues on CSP 1, a chiral recognition mechanism utilizing the sulfoxide oxygen and the benzimidazole ring nitrogen of PPIs as bidentate coordination donors to form an enantioselective ternary complex with the central Cu(II) ion and the chiral stationary bidentate ligand was proposed. benzimidazole 155-168 regulator of calcineurin 1 Homo sapiens 78-83 20174844-0 2010 CoMFA and CoMSIA analyses on 1,2,3,4-tetrahydropyrrolo[3,4-b]indole and benzimidazole derivatives as selective CB2 receptor agonists. benzimidazole 72-85 cannabinoid receptor 2 Homo sapiens 111-114 20174844-1 2010 Novel classes of cannabinoid 2 receptor (CB2) agonists based on 1,2,3,4-tetrahydropyrrolo[3,4-b]indole and benzimidazole scaffolds have shown high binding affinity toward CB2 receptor and good selectivity over cannabinoid 1 receptor (CB1). benzimidazole 107-120 cannabinoid receptor 2 Homo sapiens 17-39 20174844-1 2010 Novel classes of cannabinoid 2 receptor (CB2) agonists based on 1,2,3,4-tetrahydropyrrolo[3,4-b]indole and benzimidazole scaffolds have shown high binding affinity toward CB2 receptor and good selectivity over cannabinoid 1 receptor (CB1). benzimidazole 107-120 cannabinoid receptor 2 Homo sapiens 41-44 21579212-1 2010 In the title salt, C(18)H(19)N(4)O(+) PF(6) (-), the dihedral angle between the benzimidazolium and benzimidazole ring systems is 16.24 (2) . benzimidazole 100-113 sperm associated antigen 17 Homo sapiens 38-43 20379528-1 2010 A coordination polymer, [Co(II)(bIM)(acetate)] (bIM = benzimidazole) was synthesized using a solvothermal method; the complex has a two dimensional non-interpenetrated network structure and exhibits a spin-canted antiferromagnetic behaviour at low temperature and a high coercive field. benzimidazole 54-67 mitochondrially encoded cytochrome c oxidase II Homo sapiens 25-31 20379528-1 2010 A coordination polymer, [Co(II)(bIM)(acetate)] (bIM = benzimidazole) was synthesized using a solvothermal method; the complex has a two dimensional non-interpenetrated network structure and exhibits a spin-canted antiferromagnetic behaviour at low temperature and a high coercive field. benzimidazole 54-67 BCL2 like 11 Homo sapiens 32-35 20379528-1 2010 A coordination polymer, [Co(II)(bIM)(acetate)] (bIM = benzimidazole) was synthesized using a solvothermal method; the complex has a two dimensional non-interpenetrated network structure and exhibits a spin-canted antiferromagnetic behaviour at low temperature and a high coercive field. benzimidazole 54-67 BCL2 like 11 Homo sapiens 48-51 20185309-0 2010 Benzimidazole Thumb Pocket I finger-loop inhibitors of HCV NS5B polymerase: improved drug-like properties through C-2 SAR in three sub-series. benzimidazole 0-13 complement C2 Homo sapiens 114-117 20185309-0 2010 Benzimidazole Thumb Pocket I finger-loop inhibitors of HCV NS5B polymerase: improved drug-like properties through C-2 SAR in three sub-series. benzimidazole 0-13 sarcosine dehydrogenase Homo sapiens 118-121 20185309-1 2010 SAR at the C-2 position of benzimidazole-based Thumb Pocket I inhibitors of HCV NS5B polymerase revealed parallel activity for distinct sub-series that harbor 5-hydroxytryptophan amides, neutral thiazole isosteres or recently disclosed cinnamic acid diamides. benzimidazole 27-40 sarcosine dehydrogenase Homo sapiens 0-3 20185309-1 2010 SAR at the C-2 position of benzimidazole-based Thumb Pocket I inhibitors of HCV NS5B polymerase revealed parallel activity for distinct sub-series that harbor 5-hydroxytryptophan amides, neutral thiazole isosteres or recently disclosed cinnamic acid diamides. benzimidazole 27-40 complement C2 Homo sapiens 11-14 20153189-0 2010 SAR of PXR transactivation in benzimidazole-based IGF-1R kinase inhibitors. benzimidazole 30-43 nuclear receptor subfamily 1 group I member 2 Homo sapiens 7-10 20153189-0 2010 SAR of PXR transactivation in benzimidazole-based IGF-1R kinase inhibitors. benzimidazole 30-43 insulin like growth factor 1 receptor Homo sapiens 50-56 20078106-6 2010 This combined experimental and computational study has permitted to propose the molecular mechanisms by which the new benzimidazole derivatives act as 5-HT(6)R antagonists. benzimidazole 118-131 5-hydroxytryptamine receptor 6 Homo sapiens 151-159 20073471-2 2010 On the basis of these findings and docking pose similarity between telmisartan and rosiglitazone in PPAR gamma active site, two classes of benzimidazole derivatives were designed and synthesized as dual PPAR gamma agonist/angiotensin II antagonists for the possible treatment of metabolic syndrome. benzimidazole 139-152 peroxisome proliferator activated receptor gamma Homo sapiens 203-213 20073471-2 2010 On the basis of these findings and docking pose similarity between telmisartan and rosiglitazone in PPAR gamma active site, two classes of benzimidazole derivatives were designed and synthesized as dual PPAR gamma agonist/angiotensin II antagonists for the possible treatment of metabolic syndrome. benzimidazole 139-152 angiotensinogen Homo sapiens 222-236 20078106-0 2010 Benzimidazole derivatives as new serotonin 5-HT6 receptor antagonists. benzimidazole 0-13 5-hydroxytryptamine receptor 6 Homo sapiens 33-57 20073471-2 2010 On the basis of these findings and docking pose similarity between telmisartan and rosiglitazone in PPAR gamma active site, two classes of benzimidazole derivatives were designed and synthesized as dual PPAR gamma agonist/angiotensin II antagonists for the possible treatment of metabolic syndrome. benzimidazole 139-152 peroxisome proliferator activated receptor gamma Homo sapiens 100-110 20042333-0 2010 Benzimidazole- and indole-substituted 1,3"-bipyrrolidine benzamides as histamine H3 receptor antagonists. benzimidazole 0-13 histamine receptor H3 Homo sapiens 71-92 20055427-3 2010 Efforts to enhance the inhibitory potency of the initial purine series of fructose-1,6-bisphosphatase (FBPase) inhibitors led to the discovery of a series of benzimidazole analogues with human FBPase IC(50)s < 100 nM. benzimidazole 158-171 fructose-bisphosphatase 2 Rattus norvegicus 103-109 20055427-3 2010 Efforts to enhance the inhibitory potency of the initial purine series of fructose-1,6-bisphosphatase (FBPase) inhibitors led to the discovery of a series of benzimidazole analogues with human FBPase IC(50)s < 100 nM. benzimidazole 158-171 fructose-bisphosphatase 2 Rattus norvegicus 193-199 20082612-11 2010 CONCLUSIONS AND IMPLICATIONS: These results demonstrate that XK1 and XK2 are effective neuroprotective agents in vitro and indicate that 5-substituted benzimidazole derivatives inhibit GluN1/GluN2B receptors via direct binding to the ATD of the GluN2B subunit. benzimidazole 151-164 glutamate ionotropic receptor NMDA type subunit 1 Rattus norvegicus 185-190 20082612-11 2010 CONCLUSIONS AND IMPLICATIONS: These results demonstrate that XK1 and XK2 are effective neuroprotective agents in vitro and indicate that 5-substituted benzimidazole derivatives inhibit GluN1/GluN2B receptors via direct binding to the ATD of the GluN2B subunit. benzimidazole 151-164 glutamate ionotropic receptor NMDA type subunit 2B Rattus norvegicus 191-197 20082612-11 2010 CONCLUSIONS AND IMPLICATIONS: These results demonstrate that XK1 and XK2 are effective neuroprotective agents in vitro and indicate that 5-substituted benzimidazole derivatives inhibit GluN1/GluN2B receptors via direct binding to the ATD of the GluN2B subunit. benzimidazole 151-164 glutamate ionotropic receptor NMDA type subunit 2B Rattus norvegicus 245-251 20110603-1 2010 We describe the interactions of two benzimidazole derivatives, astemizole (AST) and lansoprazole (LNS), with anomalous aggregates of tau protein (neurofibrillary tangles). benzimidazole 36-49 microtubule associated protein tau Homo sapiens 133-136 19433063-0 2009 A novel benzimidazole analogue inhibits the hypoxia-inducible factor (HIF)-1 pathway. benzimidazole 8-21 hypoxia inducible factor 1 subunit alpha Homo sapiens 44-76 19769332-4 2009 Systematic replacement of each of the unfused carbon atoms in the phenyl ring of the indole moiety by a nitrogen atom provided four different azaindole derivatives that displayed a clear SAR for antiviral activity and all of which displayed marked improvements in pharmaceutical properties. benzimidazole 142-151 sarcosine dehydrogenase Homo sapiens 187-190 19888760-0 2009 Synthesis and evaluation of a new generation of orally efficacious benzimidazole-based poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors as anticancer agents. benzimidazole 67-80 poly (ADP-ribose) polymerase family, member 1 Mus musculus 87-116 19888760-0 2009 Synthesis and evaluation of a new generation of orally efficacious benzimidazole-based poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors as anticancer agents. benzimidazole 67-80 poly (ADP-ribose) polymerase family, member 1 Mus musculus 118-124 19888760-2 2009 As one of the strategies to expand our portfolio of PARP-1 inhibitors, we pursued unsaturated heterocycles to replace the saturated cyclic amine derivatives appended to the benzimidazole core. benzimidazole 173-186 poly (ADP-ribose) polymerase family, member 1 Mus musculus 52-58 19716296-1 2009 SAR for a wide variety of heterocyclic replacements for a benzimidazole led to the discovery of functionalized 2-pyridyl amides as novel inhibitors of the hedgehog pathway. benzimidazole 58-71 sarcosine dehydrogenase Homo sapiens 0-3 20014869-2 2009 The synthesis and characterization of a novel polycyclic azaindole based derivative is disclosed, and its binding to JAK2 is described. benzimidazole 57-66 Janus kinase 2 Homo sapiens 117-121 19632115-3 2009 Structure-based design employing an active site homology model derived from PKA led to the preparation of benzimidazole 5-substituted compounds 26 and 27 as highly potent inhibitors (K(i) <1nM) of p70S6K, with >100-fold selectivity against PKA, ROCK and GSK3. benzimidazole 106-119 ribosomal protein S6 kinase B1 Homo sapiens 200-206 19540111-2 2009 Systematic modification of benzimidazole lead 5a identified from a high-throughput screening led to the discovery of a potent and metabolically stable glucokinase activator 16p(R) with greater structural diversity from GKAs reported to date. benzimidazole 27-40 glucokinase Rattus norvegicus 151-162 19433063-2 2009 We report the novel benzimidazole analogue AC1-004, obtained from a chemical library using an HRE-dependent cell-based assay in colorectal carcinoma HCT-116 cells. benzimidazole 20-33 long intergenic non-protein coding RNA 1587 Homo sapiens 43-50 19433063-7 2009 These results suggest the benzimidazole analogue AC1-004 is a novel HIF inhibitor that targets HIF-1alpha via the Hsp90-Akt pathway, and that it can be used as a new lead in developing anticancer drugs. benzimidazole 26-39 long intergenic non-protein coding RNA 1587 Homo sapiens 49-56 19433063-7 2009 These results suggest the benzimidazole analogue AC1-004 is a novel HIF inhibitor that targets HIF-1alpha via the Hsp90-Akt pathway, and that it can be used as a new lead in developing anticancer drugs. benzimidazole 26-39 hypoxia inducible factor 1 subunit alpha Homo sapiens 95-105 19433063-7 2009 These results suggest the benzimidazole analogue AC1-004 is a novel HIF inhibitor that targets HIF-1alpha via the Hsp90-Akt pathway, and that it can be used as a new lead in developing anticancer drugs. benzimidazole 26-39 AKT serine/threonine kinase 1 Homo sapiens 120-123 19119060-1 2009 Seven transition metal complexes of benzimidazole ligand (HL) are reported and characterized based on elemental analyses, IR, solid reflectance, magnetic moment, molar conductance and thermal analyses (TGA and DTA). benzimidazole 36-49 T-box transcription factor 1 Homo sapiens 202-205 19398200-0 2009 Optimization of benzimidazole series as opioid receptor-like 1 (ORL1) antagonists: SAR study directed toward improvement of selectivity over hERG activity. benzimidazole 16-29 opioid related nociceptin receptor 1 Homo sapiens 40-62 19398200-0 2009 Optimization of benzimidazole series as opioid receptor-like 1 (ORL1) antagonists: SAR study directed toward improvement of selectivity over hERG activity. benzimidazole 16-29 opioid related nociceptin receptor 1 Homo sapiens 64-68 19398200-0 2009 Optimization of benzimidazole series as opioid receptor-like 1 (ORL1) antagonists: SAR study directed toward improvement of selectivity over hERG activity. benzimidazole 16-29 ETS transcription factor ERG Homo sapiens 141-145 19398200-1 2009 A structure-activity relationship (SAR) study on the benzimidazole series of opioid receptor-like 1 (ORL1) antagonists related to 1 is described. benzimidazole 53-66 opioid related nociceptin receptor 1 Homo sapiens 77-99 19398200-1 2009 A structure-activity relationship (SAR) study on the benzimidazole series of opioid receptor-like 1 (ORL1) antagonists related to 1 is described. benzimidazole 53-66 opioid related nociceptin receptor 1 Homo sapiens 101-105 19327988-1 2009 The indole ring systems of the cytosolic phospholipase A(2)alpha (cPLA(2)alpha) inhibitor 1-[3-(4-octylphenoxy)-2-oxopropyl]indole-5-carboxylic acid (2) and the isomeric 6-carboxylic acid (3) were replaced by benzimidazole, benzotriazole and indazole scaffolds, respectively. benzimidazole 209-222 phospholipase A2 group IVA Homo sapiens 66-78 19307115-0 2009 Discovery of potent and selective DP1 receptor antagonists in the azaindole series. benzimidazole 66-75 transcription factor Dp-1 Homo sapiens 34-37 19307115-1 2009 Azaindole based structures were evaluated as DP1 receptor antagonists. benzimidazole 0-9 transcription factor Dp-1 Homo sapiens 45-48 19929839-3 2009 Pyrazole and azaindole fragment hits with micromolar activity were rapidly progressed to nanomolar inhibitors of PKB with activity in cells using crystallographic analysis of inhibitor binding modes to guide medicinal chemistry. benzimidazole 13-22 protein tyrosine kinase 2 beta Homo sapiens 113-116 19143569-1 2009 We have developed a series of cyclic amine-containing benzimidazole carboxamide PARP inhibitors with a methyl-substituted quaternary center at the point of attachment to the benzimidazole ring system. benzimidazole 54-67 poly(ADP-ribose) polymerase 1 Homo sapiens 80-84 18586490-0 2008 Synthesis and SAR of novel, potent and orally bioavailable benzimidazole inhibitors of poly(ADP-ribose) polymerase (PARP) with a quaternary methylene-amino substituent. benzimidazole 59-72 sarcosinemia autosomal recessive Mus musculus 14-17 18574696-3 2008 An Aurora A high throughput screen revealed a promising sub-micromolar indazole-benzimidazole lead. benzimidazole 80-93 aurora kinase A Homo sapiens 3-11 18819794-0 2008 Itk kinase inhibitors: initial efforts to improve the metabolical stability and the cell activity of the benzimidazole lead. benzimidazole 105-118 IL2 inducible T cell kinase Homo sapiens 0-3 18819794-1 2008 Previously, we reported a series of novel benzimidazole based Itk inhibitors that exhibited excellent enzymatic potency and selectivity but low microsomal stability. benzimidazole 42-55 IL2 inducible T cell kinase Homo sapiens 62-65 18819799-1 2008 A series of novel potent benzimidazole based inhibitors of interleukin-2 T-cell kinase (Itk) were prepared. benzimidazole 25-38 IL2 inducible T cell kinase Homo sapiens 59-86 18819799-1 2008 A series of novel potent benzimidazole based inhibitors of interleukin-2 T-cell kinase (Itk) were prepared. benzimidazole 25-38 IL2 inducible T cell kinase Homo sapiens 88-91 18763755-1 2008 We previously reported that 1 (BMS-536924), a benzimidazole inhibitor of the insulin-like growth factor-1 receptor, had demonstrated in vivo antitumor activity. benzimidazole 46-59 insulin like growth factor 1 receptor Homo sapiens 77-114 18541433-1 2008 We have developed a series of cyclic amine-containing benzimidazole carboxamide poly(ADP-ribose)polymerase (PARP) inhibitors, with good PARP-1 enzyme potency, as well as cellular potency. benzimidazole 54-67 poly (ADP-ribose) polymerase family, member 1 Mus musculus 80-106 18541433-1 2008 We have developed a series of cyclic amine-containing benzimidazole carboxamide poly(ADP-ribose)polymerase (PARP) inhibitors, with good PARP-1 enzyme potency, as well as cellular potency. benzimidazole 54-67 poly (ADP-ribose) polymerase family, member 1 Mus musculus 108-112 18541433-1 2008 We have developed a series of cyclic amine-containing benzimidazole carboxamide poly(ADP-ribose)polymerase (PARP) inhibitors, with good PARP-1 enzyme potency, as well as cellular potency. benzimidazole 54-67 poly (ADP-ribose) polymerase family, member 1 Mus musculus 136-142 18586490-0 2008 Synthesis and SAR of novel, potent and orally bioavailable benzimidazole inhibitors of poly(ADP-ribose) polymerase (PARP) with a quaternary methylene-amino substituent. benzimidazole 59-72 poly (ADP-ribose) polymerase family, member 1 Mus musculus 87-114 18586490-0 2008 Synthesis and SAR of novel, potent and orally bioavailable benzimidazole inhibitors of poly(ADP-ribose) polymerase (PARP) with a quaternary methylene-amino substituent. benzimidazole 59-72 poly (ADP-ribose) polymerase family, member 1 Mus musculus 116-120 18976926-0 2008 Synthesis and biological activities of novel nonpeptide angiotensin II receptor antagonists based on benzimidazole derivatives bearing a heterocyclic ring. benzimidazole 101-114 angiotensinogen Homo sapiens 56-70 18006194-6 2008 Our analysis suggests that stabilizing interactions between the halogen atom at the benzimidazole ring and the Ser-122 of the D(2)-like and Trp-358 of the 5-HT(1A) receptor. benzimidazole 84-97 5-hydroxytryptamine receptor 1A Homo sapiens 155-172 18572407-0 2008 Balancing oral exposure with Cyp3A4 inhibition in benzimidazole-based IGF-IR inhibitors. benzimidazole 50-63 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 29-35 18572407-0 2008 Balancing oral exposure with Cyp3A4 inhibition in benzimidazole-based IGF-IR inhibitors. benzimidazole 50-63 insulin like growth factor 1 receptor Homo sapiens 70-76 18586490-3 2008 Utilizing a benzimidazole carboxamide scaffold in which the amide forms a key intramolecular hydrogen bond for optimal interaction with the enzyme, we have identified a novel series of PARP inhibitors containing a quaternary methylene-amino substituent at the C-2 position of the benzimidazole. benzimidazole 12-25 poly (ADP-ribose) polymerase family, member 1 Mus musculus 185-189 18522867-0 2008 Novel benzimidazole derivatives as selective CB2 agonists. benzimidazole 6-19 cannabinoid receptor 2 Homo sapiens 45-48 18539028-0 2008 Discovery of potent, orally active benzimidazole glucagon receptor antagonists. benzimidazole 35-48 glucagon receptor Mus musculus 49-66 18522867-1 2008 The preparation and evaluation of a novel class of CB2 agonists based on a benzimidazole moiety are reported. benzimidazole 75-88 cannabinoid receptor 2 Homo sapiens 51-54 18394887-1 2008 A novel series of benzimidazole CB2-receptor agonists was synthesized and the structure-activity relationship explored. benzimidazole 18-31 cannabinoid receptor 2 Rattus norvegicus 32-44 18468891-0 2008 Identification of novel benzimidazole series of potent and selective ORL1 antagonists. benzimidazole 24-37 opioid related nociceptin receptor 1 Homo sapiens 69-73 18468891-1 2008 Structure-activity studies on benzimidazole lead 1 obtained from library screening led to the discovery of potent and selective ORL1 antagonist 28, 5-chloro-2-[(1-ethyl-1-methylpropyl)thio]-6-[4-(2-hydroxyethyl)piperazin-1-yl]-1H-benzimidazole, which is structurally distinct from conventional non-peptide antagonists known to date. benzimidazole 30-43 opioid related nociceptin receptor 1 Homo sapiens 128-132 18192899-7 2008 The SNPs 200Tyr, 167Tyr in beta-tubulin isotype 1 have been described to confer benzimidazole resistance in nematodes and recently 198Ala has also been associated with benzimidazole resistance. benzimidazole 80-93 beta-tubulin Ovis aries 27-39 18346892-0 2008 Structure-based design and synthesis of benzimidazole derivatives as dipeptidyl peptidase IV inhibitors. benzimidazole 40-53 dipeptidyl peptidase 4 Homo sapiens 69-92 18346892-1 2008 A novel series of non-covalent, benzimidazole-based inhibitors of DPP-4 has been developed from a small fragment hit using structure-based drug design. benzimidazole 32-45 dipeptidyl peptidase 4 Homo sapiens 66-71 18242988-0 2008 Discovery of small molecule benzimidazole antagonists of the chemokine receptor CXCR3. benzimidazole 28-41 C-X-C motif chemokine receptor 3 Homo sapiens 80-85 18242988-2 2008 Systematic modification of the benzimidazole core and tethered acetophenone moiety established tractable SAR of analogs with improved physicochemical properties and sub-micromolar activity across both human and murine receptors. benzimidazole 31-44 sarcosine dehydrogenase Homo sapiens 105-108 18065684-4 2008 Using this system, we have screened more than 8000 compounds in the DIVERSet chemical library for repressors of a matrix metalloproteinase-9 (MMP-9) promoter and identified 5-methyl-2-(4-methylphenyl)-1H-benzimidazole (MPBD) inhibitory for MMP-9 gene expression. benzimidazole 201-217 matrix metallopeptidase 9 Homo sapiens 142-147 18207395-3 2008 N-methylation of the benzimidazole moiety within the lead structure significantly reduced P-gp susceptibility while increasing potency, giving rise to good brain penetration. benzimidazole 21-34 phosphoglycolate phosphatase Homo sapiens 90-94 18343620-2 2008 The development of high performance liquid chromatography method on amylose-based stationary phases (Chiralpak AD) has permitted to achieve the preparative enantioseparation of one benzimidazole derivative, potent-AMP-kinase (AMPK) activator with satisfactory yields. benzimidazole 181-194 protein kinase AMP-activated catalytic subunit alpha 2 Homo sapiens 207-224 18343620-2 2008 The development of high performance liquid chromatography method on amylose-based stationary phases (Chiralpak AD) has permitted to achieve the preparative enantioseparation of one benzimidazole derivative, potent-AMP-kinase (AMPK) activator with satisfactory yields. benzimidazole 181-194 protein kinase AMP-activated catalytic subunit alpha 2 Homo sapiens 226-230 18192899-7 2008 The SNPs 200Tyr, 167Tyr in beta-tubulin isotype 1 have been described to confer benzimidazole resistance in nematodes and recently 198Ala has also been associated with benzimidazole resistance. benzimidazole 168-181 beta-tubulin Ovis aries 27-39 18192899-9 2008 These genetic analyses indicate that there is a correlation between exposure and/or resistance to MLs and an increase in the frequency of the beta-tubulin alleles containing codons, which are determinant for benzimidazole resistance. benzimidazole 208-221 beta-tubulin Ovis aries 142-154 18036341-3 2008 The budding uninhibited by benzimidazole (Bub1) is a key component of mitotic checkpoint. benzimidazole 27-40 BUB1 mitotic checkpoint serine/threonine kinase Homo sapiens 42-46 17676829-3 2007 The SAR results were also supported by the X-ray crystallographic elucidation of the role of the N1 nitrogen and the urea moiety when the benzimidazole-urea compounds were bound to the VEGFR-2 enzyme. benzimidazole 138-151 kinase insert domain receptor Homo sapiens 185-192 17937984-1 2007 A series of benzimidazole compounds containing pendant alcohol and amine moieties was found to be active against checkpoint kinase Chk2. benzimidazole 12-25 checkpoint kinase 2 Homo sapiens 131-135 18791270-3 2008 METHODS: We analyzed the mRNA expression levels of the major mitotic checkpoint genes of the budding uninhibited by benzimidazole family (BUB1, BUBR1, BUB3) and of the MAD gene family (MAD1, MAD2L1, MAD2L2) by real-time quantitative PCR in 39 ccRCC and in 36 normal kidney tissue samples. benzimidazole 116-129 BUB1 mitotic checkpoint serine/threonine kinase Homo sapiens 138-142 17934515-7 2007 Only the kinases TRK und FLT3 were inhibited by azaindole 1 in the sub-micromolar range, albeit with IC50 values of 252 and 303 nM, respectively. benzimidazole 48-57 Fms related receptor tyrosine kinase 3 Rattus norvegicus 25-29 17576060-1 2007 Part 5: Optimization of benzimidazole substitution patterns towards derivatives with improved activity. benzimidazole 24-37 tankyrase Homo sapiens 0-6 17499505-0 2007 Hit-to-lead studies on benzimidazole inhibitors of ITK: discovery of a novel class of kinase inhibitors. benzimidazole 23-36 IL2 inducible T cell kinase Homo sapiens 51-54 17482821-1 2007 We have prepared a set of heterocyclic benzimidazole derivatives bearing amidino substituents at C-5 of benzimidazole ring, by introducing various heterocyclic nuclei (pyridine, N-methyl-pyrrole or imidazole) at C-2, and evaluated their antitumor and antiviral activities. benzimidazole 39-52 complement C5 Homo sapiens 97-100 17368898-1 2007 Two different benzimidazole analogues act as multimodal agent, first one as novel non-peptidic CCK-B receptor antagonist and similarly as potent anti-fungal agent, designated as [Bz-Im]. benzimidazole 14-27 cholecystokinin B receptor Rattus norvegicus 95-109 17482821-1 2007 We have prepared a set of heterocyclic benzimidazole derivatives bearing amidino substituents at C-5 of benzimidazole ring, by introducing various heterocyclic nuclei (pyridine, N-methyl-pyrrole or imidazole) at C-2, and evaluated their antitumor and antiviral activities. benzimidazole 39-52 complement C2 Homo sapiens 212-215 17482821-1 2007 We have prepared a set of heterocyclic benzimidazole derivatives bearing amidino substituents at C-5 of benzimidazole ring, by introducing various heterocyclic nuclei (pyridine, N-methyl-pyrrole or imidazole) at C-2, and evaluated their antitumor and antiviral activities. benzimidazole 104-117 complement C5 Homo sapiens 97-100 17416530-0 2007 Inhibition of monoamine oxidase B by selected benzimidazole and caffeine analogues. benzimidazole 46-59 monoamine oxidase B Homo sapiens 14-33 17416530-3 2007 In the present study, we have prepared additional caffeine and benzimidazole analogues in an attempt to identify compounds with improved MAO-B inhibition potency while still acting reversibly. benzimidazole 63-76 monoamine oxidase B Homo sapiens 137-142 17416530-5 2007 The most potent inhibitor among the benzimidazole analogues was (E)-2-(4-trifluoromethylstyryl)-1-methylbenzimidazole with a K(i) value of 430 nM. benzimidazole 36-49 cystatin 12, pseudogene Homo sapiens 64-69 17178222-0 2007 Quinazoline and benzimidazole MCH-1R antagonists. benzimidazole 16-29 melanin concentrating hormone receptor 1 Homo sapiens 30-36 17419606-3 2007 A similar, but weaker effect was also observed when using a benzimidazole-phenoxazine derivative as Pgp inhibitor. benzimidazole 60-73 phosphoglycolate phosphatase Homo sapiens 100-103 17274763-5 2007 In haptocorrin, it provides hydrophobic contacts to the benzimidazole moiety through the apolar regions of Arg357, Trp359 and Tyr362. benzimidazole 56-69 transcobalamin 1 Homo sapiens 3-14 16513356-0 2006 Synthesis and biological evaluation of benzimidazole derivatives as potent AMP-activated protein kinase activators. benzimidazole 39-52 protein kinase AMP-activated catalytic subunit alpha 2 Homo sapiens 75-103 18193694-1 2007 The following paper addresses an attempt to determine the trace levels of two benzimidazole fungicides (carbendazim, CAS 10605-21-7 and thiabendazole, CAS 148-79-8) in drinking water samples using the newly proposed linear modulated stochastic resonance algorithm. benzimidazole 78-91 BCAR1 scaffold protein, Cas family member Homo sapiens 117-120 18193694-1 2007 The following paper addresses an attempt to determine the trace levels of two benzimidazole fungicides (carbendazim, CAS 10605-21-7 and thiabendazole, CAS 148-79-8) in drinking water samples using the newly proposed linear modulated stochastic resonance algorithm. benzimidazole 78-91 BCAR1 scaffold protein, Cas family member Homo sapiens 151-154 16904318-0 2006 Novel benzimidazole-based MCH R1 antagonists. benzimidazole 6-19 melanin concentrating hormone receptor 1 Homo sapiens 26-32 16904318-1 2006 The identification of an MCH R1 antagonist screening hit led to the optimization of a class of benzimidazole-based MCH R1 antagonists. benzimidazole 95-108 melanin concentrating hormone receptor 1 Homo sapiens 25-31 16904318-1 2006 The identification of an MCH R1 antagonist screening hit led to the optimization of a class of benzimidazole-based MCH R1 antagonists. benzimidazole 95-108 melanin concentrating hormone receptor 1 Homo sapiens 115-121 16690315-2 2006 Novel benzimidazole analogues with increased chemical stability, devoid of the potential carcinogenic liability associated with a biarylamine moiety, were synthesized and evaluated to be potent MCH R1 antagonists. benzimidazole 6-19 melanin concentrating hormone receptor 1 Homo sapiens 194-200 17209555-4 2007 Analogously, adding the equivalent of N-3 to low-fidelity benzimidazole-derived bases (i.e., bases that pol alpha rapidly incorporates opposite all four natural bases) and to generate 1-deazapurines significantly strengthens the ability of pol alpha to identify the resulting 1-deazapurines as wrong. benzimidazole 58-71 DNA polymerase alpha 1, catalytic subunit Homo sapiens 104-113 17209555-4 2007 Analogously, adding the equivalent of N-3 to low-fidelity benzimidazole-derived bases (i.e., bases that pol alpha rapidly incorporates opposite all four natural bases) and to generate 1-deazapurines significantly strengthens the ability of pol alpha to identify the resulting 1-deazapurines as wrong. benzimidazole 58-71 DNA polymerase alpha 1, catalytic subunit Homo sapiens 240-249 16760428-3 2006 We show that Plk1 binds to budding uninhibited by benzimidazole 1 (Bub1) in mitotic human cells. benzimidazole 50-63 polo like kinase 1 Homo sapiens 13-17 16760428-3 2006 We show that Plk1 binds to budding uninhibited by benzimidazole 1 (Bub1) in mitotic human cells. benzimidazole 50-63 BUB1 mitotic checkpoint serine/threonine kinase Homo sapiens 67-71 16513356-1 2006 Design, synthesis and structure-activity relationships of benzimidazole derivatives as activators of the AMP-activated protein kinase (AMPK) are presented in this paper. benzimidazole 58-71 protein kinase AMP-activated catalytic subunit alpha 2 Homo sapiens 105-133 16513356-1 2006 Design, synthesis and structure-activity relationships of benzimidazole derivatives as activators of the AMP-activated protein kinase (AMPK) are presented in this paper. benzimidazole 58-71 protein kinase AMP-activated catalytic subunit alpha 2 Homo sapiens 135-139 16563760-2 2006 Benzimidazole and indazolone derivatives prepared retained good potency in vitro and indazolone 4a was identified as a novel TRPV1 receptor antagonist suitable for evaluating orally in animal models of analgesia. benzimidazole 0-13 transient receptor potential cation channel subfamily V member 1 Homo sapiens 125-130 16789735-0 2006 Potent benzimidazole sulfonamide protein tyrosine phosphatase 1B inhibitors containing the heterocyclic (S)-isothiazolidinone phosphotyrosine mimetic. benzimidazole 7-20 protein tyrosine phosphatase non-receptor type 1 Homo sapiens 33-64 16789735-2 2006 An X-ray cocrystal structure of inhibitor 46/PTP1B at 1.8 A resolution demonstrated that the benzimidazole sulfonamides form a bidentate H bond to Asp48 as designed, although the aryl group of the sulfonamide unexpectedly interacts intramolecularly in a pi-stacking manner with the benzimidazole. benzimidazole 93-106 protein tyrosine phosphatase non-receptor type 1 Homo sapiens 45-50 16700898-6 2006 Pantoprazole and tenatoprazole, a novel proton pump inhibitor which has an imidazopyridine ring in place of the benzimidazole moiety found in other proton pump inhibitors, are activated more slowly than other proton pump inhibitors but their inhibition is resistant to reversal. benzimidazole 112-125 ATPase H+/K+ transporting subunit alpha Homo sapiens 40-51 16700898-8 2006 The chemical and pharmacological characteristics of tenatoprazole give it theoretical advantages over benzimidazole-based proton pump inhibitors that should translate into improved acid control, particularly during the night. benzimidazole 102-115 ATPase H+/K+ transporting subunit alpha Homo sapiens 122-133 16039125-0 2005 Design, synthesis, and evaluation of novelly substituted benzimidazole compounds as angiotensin II receptor antagonists. benzimidazole 57-70 angiotensinogen Homo sapiens 84-98 16442290-2 2006 Chem.2005, 48, 1873], we described the discovery of a class of benzimidazole chk2 kinase inhibitors, exemplified by compound 1, which had radio-protective effects in human T-cells subjected to ionizing radiation. benzimidazole 63-76 checkpoint kinase 2 Homo sapiens 77-81 16442290-3 2006 Here, a series of non-benzimidazole analogs intended to define the scope of the SAR about this new series of inhibitor, and allow for refinement of the binding model of these compounds to the chk2 kinase is described. benzimidazole 22-35 sarcosine dehydrogenase Homo sapiens 80-83 16442290-3 2006 Here, a series of non-benzimidazole analogs intended to define the scope of the SAR about this new series of inhibitor, and allow for refinement of the binding model of these compounds to the chk2 kinase is described. benzimidazole 22-35 checkpoint kinase 2 Homo sapiens 192-196 16539403-3 2006 Benzimidazole derivative 8b was active in an in vivo target (TGF-beta RI) inhibition assay. benzimidazole 0-13 transforming growth factor beta receptor 1 Homo sapiens 61-72 16307491-3 2005 Triclabendazole, a benzimidazole derivative, has been routinely used since 1983 in veterinary medicine to control infections with Fasciola spp. benzimidazole 19-32 histocompatibility minor 13 Homo sapiens 139-142 16125538-1 2005 This is the first report of the effects of a nonthiazolidinedione activator of peroxisome proliferator-activated receptor (PPAR) gamma, that is, FK-614 (a benzimidazole derivative), on glucose metabolism in vivo. benzimidazole 155-168 peroxisome proliferator activated receptor gamma Canis lupus familiaris 79-134 15664860-0 2005 Benzimidazole derivatives as novel nonpeptide luteinizing hormone-releasing hormone (LHRH) antagonists. benzimidazole 0-13 gonadotropin releasing hormone 1 Homo sapiens 46-83 15703302-0 2005 Transport of anthelmintic benzimidazole drugs by breast cancer resistance protein (BCRP/ABCG2). benzimidazole 26-39 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 49-81 15703302-0 2005 Transport of anthelmintic benzimidazole drugs by breast cancer resistance protein (BCRP/ABCG2). benzimidazole 26-39 BCR pseudogene 1 Homo sapiens 83-87 15703302-0 2005 Transport of anthelmintic benzimidazole drugs by breast cancer resistance protein (BCRP/ABCG2). benzimidazole 26-39 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 88-93 15664860-0 2005 Benzimidazole derivatives as novel nonpeptide luteinizing hormone-releasing hormone (LHRH) antagonists. benzimidazole 0-13 gonadotropin releasing hormone 1 Homo sapiens 85-89 15099830-1 2004 Equilibrium binding dynamics is studied for a panel of benzimidazole-containing compounds at the remodeled interface between human growth hormone (hGH) and the extracellular domain of its receptor (hGHbp), engineered by mutating to glycine hot spot residues T175 from the hormone and W104 from the receptor. benzimidazole 55-68 growth hormone 1 Homo sapiens 131-145 15664861-0 2005 Benzimidazole derivatives as novel nonpeptide luteinizing hormone-releasing hormone (LHRH) antagonists. benzimidazole 0-13 gonadotropin releasing hormone 1 Homo sapiens 46-83 15664861-0 2005 Benzimidazole derivatives as novel nonpeptide luteinizing hormone-releasing hormone (LHRH) antagonists. benzimidazole 0-13 gonadotropin releasing hormone 1 Homo sapiens 85-89 15261287-0 2004 Structure-activity relationships of potent and selective factor Xa inhibitors: benzimidazole derivatives with the side chain oriented to the prime site of factor Xa. benzimidazole 79-92 coagulation factor X Homo sapiens 57-66 15261287-0 2004 Structure-activity relationships of potent and selective factor Xa inhibitors: benzimidazole derivatives with the side chain oriented to the prime site of factor Xa. benzimidazole 79-92 coagulation factor X Homo sapiens 155-164 15261287-1 2004 A series of benzimidazole derivatives with the side chain on the nitrogen atom oriented to the prime site of factor Xa (FXa) were designed and synthesized. benzimidazole 12-25 coagulation factor X Homo sapiens 109-118 15261287-1 2004 A series of benzimidazole derivatives with the side chain on the nitrogen atom oriented to the prime site of factor Xa (FXa) were designed and synthesized. benzimidazole 12-25 coagulation factor X Homo sapiens 120-123 15278126-0 2004 A study on the mimics of Cu-Zn superoxide dismutase with high activity and stability: two copper(II) complexes of 1,4,7-triazacyclononane with benzimidazole groups. benzimidazole 143-156 superoxide dismutase 1 Homo sapiens 25-51 15635167-2 2005 We previously reported that a benzoimidazole derivative, M50367, acted directly on naive Th cells to inhibit their differentiation into Th2 cells. benzimidazole 30-44 heart and neural crest derivatives expressed 2 Mus musculus 136-139 15351401-1 2004 Part 5: design and synthesis of new benzimidazole-arylpiperazine derivatives acting as mixed 5-HT1A/5-HT3 ligands. benzimidazole 36-49 tankyrase Homo sapiens 0-6 15351401-1 2004 Part 5: design and synthesis of new benzimidazole-arylpiperazine derivatives acting as mixed 5-HT1A/5-HT3 ligands. benzimidazole 36-49 5-hydroxytryptamine receptor 1A Homo sapiens 93-99 15351401-2 2004 A series of new mixed benzimidazole-arylpiperazine derivatives were designed by incorporating in general structure III the pharmacophoric elements of 5-HT(1A) and 5-HT(3) receptors. benzimidazole 22-35 5-hydroxytryptamine receptor 1A Homo sapiens 150-157 15099830-1 2004 Equilibrium binding dynamics is studied for a panel of benzimidazole-containing compounds at the remodeled interface between human growth hormone (hGH) and the extracellular domain of its receptor (hGHbp), engineered by mutating to glycine hot spot residues T175 from the hormone and W104 from the receptor. benzimidazole 55-68 growth hormone receptor Homo sapiens 198-203 15099830-3 2004 The results of simulated tempering ligand dynamics at the protein-protein interface reveals a diversity of ligand binding modes that is consistent with the structural orientation of the benzimidazole ring which closely mimics the position of the mutated W104 hot spot residue in the wild-type hGH-hGHbp complex. benzimidazole 186-199 growth hormone receptor Homo sapiens 297-302 14987951-5 2004 The mechanism of benzimidazole-mediated induction of CYP1A1 was investigated by comparison with 3-MC, a prototypical AhR ligand. benzimidazole 17-30 cytochrome P450, family 1, subfamily a, polypeptide 1 Rattus norvegicus 53-59 14691014-0 2004 A benzimidazole fungicide, benomyl, and its metabolite, carbendazim, induce aromatase activity in a human ovarian granulose-like tumor cell line (KGN). benzimidazole 2-15 cytochrome P450 family 19 subfamily A member 1 Homo sapiens 76-85 14987951-5 2004 The mechanism of benzimidazole-mediated induction of CYP1A1 was investigated by comparison with 3-MC, a prototypical AhR ligand. benzimidazole 17-30 aryl hydrocarbon receptor Rattus norvegicus 117-120 12951088-0 2003 Design and synthesis of new benzimidazole-arylpiperazine derivatives acting as mixed 5-HT1A/5-HT3 ligands. benzimidazole 28-41 5-hydroxytryptamine receptor 1A Homo sapiens 85-91 14691134-2 2003 The budding uninhibited by benzimidazole (Bub) 1, mitotic arrest-deficient (Mad) 1, and Mad2 proteins promote this checkpoint through sustained inhibition of the anaphase-promoting complex/cyclosome. benzimidazole 27-40 MAX dimerization protein 1 L homeolog Xenopus laevis 50-82 14517972-2 2003 Multiple docking simulations are conducted with the remodeled hGH-hGHbp complex for a panel of potent benzimidazole-containing inhibitors that can restore the binding affinity of the wild-type complex, and for a set of known nonactive small molecules that contain different heterocyclic motifs. benzimidazole 102-115 growth hormone receptor Homo sapiens 66-71 14517972-5 2003 Despite numerous pockets on the protein surface of the mutant hGH-hGHbp complex, the binding-site cavity presents the energetically favorable hot spot for the benzimidazole-containing inhibitors, whereas for a set of nonactive molecules, the lowest energy ligand conformations do not necessarily bind in the engineered cavity. benzimidazole 159-172 growth hormone receptor Homo sapiens 66-71 12519059-1 2003 Novel tricyclic benzimidazole carboxamide poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors have been synthesized. benzimidazole 16-29 poly(ADP-ribose) polymerase 1 Homo sapiens 42-71 14525526-4 2003 Moreover, the spindle checkpoint component budding uninhibited by benzimidazole 1 (BUB1) localizes to kinetochores and is phosphorylated until anaphase of both meiotic M phases. benzimidazole 66-79 BUB1 mitotic checkpoint serine/threonine kinase Homo sapiens 83-87 12772307-4 2003 An analogous eta(6)-arene,eta(1)-carbene complex with a benzimidazole frame 6 was isolated from an in situ reaction between [RuCl(2)(p-cymene)](2), the corresponding benzimidazolium salt and cesium carbonate. benzimidazole 56-69 endothelin receptor type A Homo sapiens 13-16 12772307-4 2003 An analogous eta(6)-arene,eta(1)-carbene complex with a benzimidazole frame 6 was isolated from an in situ reaction between [RuCl(2)(p-cymene)](2), the corresponding benzimidazolium salt and cesium carbonate. benzimidazole 56-69 endothelin receptor type A Homo sapiens 26-29 12679136-5 2003 CYP3A4 was the only CYP3A isoform that was induced by all of the four benzimidazole derivatives, while CYP3A5, CYP3A7, and CYP3A43 were unaffected or even slightly downregulated by these drugs. benzimidazole 70-83 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-6 12679136-5 2003 CYP3A4 was the only CYP3A isoform that was induced by all of the four benzimidazole derivatives, while CYP3A5, CYP3A7, and CYP3A43 were unaffected or even slightly downregulated by these drugs. benzimidazole 70-83 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-5 15317289-4 2003 Reported herein is the pharmacology of potent, low molecular weight thrombin receptor antagonists from pyrroloquinazoline, benzimidazole, and himbacine series. benzimidazole 123-136 coagulation factor II, thrombin Homo sapiens 68-76 12591101-0 2003 New benzimidazole derivatives: selective and orally active 5-HT3 receptor antagonists. benzimidazole 4-17 5-hydroxytryptamine receptor 3A Rattus norvegicus 59-73 12591101-5 2003 These benzimidazole derivatives have proved to be 5-HT(3) receptor antagonists. benzimidazole 6-19 5-hydroxytryptamine receptor 3A Rattus norvegicus 50-66 12519059-1 2003 Novel tricyclic benzimidazole carboxamide poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors have been synthesized. benzimidazole 16-29 poly(ADP-ribose) polymerase 1 Homo sapiens 73-79 12113886-5 2002 All three analogs (purine, benzimidazole, and 7-azaindole) exhibited affinity for PepT1 in binding studies, but only the purine analog (as the L-valine ester) showed PepT1-associated transcellular transport across Caco-2 cell monolayers. benzimidazole 27-40 solute carrier family 15 member 1 Homo sapiens 82-87 12113886-6 2002 The benzimidazole and 7-azaindole analogs (as their L-valine esters) were rapidly metabolized by esterase when applied to the apical surface of Caco-2 cells, which probably explains their low penetration as the intact prodrugs via PepT1. benzimidazole 4-17 solute carrier family 15 member 1 Homo sapiens 231-236 11825309-1 2001 Lansoprazole (Prevacid, TAP Pharmaceuticals, Inc.) is a substituted benzimidazole that inhibits gastric acid secretion. benzimidazole 68-81 nuclear RNA export factor 1 Homo sapiens 24-27 11965377-1 2002 A novel potent and selective aminophenol scaffold for fXa inhibitors was developed from a previously reported benzimidazole-based naphthylamidine template. benzimidazole 110-123 coagulation factor X Homo sapiens 54-57 11965378-0 2002 Benzimidazole-based fXa inhibitors with improved thrombin and trypsin selectivity. benzimidazole 0-13 coagulation factor X Homo sapiens 20-23 11965378-0 2002 Benzimidazole-based fXa inhibitors with improved thrombin and trypsin selectivity. benzimidazole 0-13 coagulation factor II, thrombin Homo sapiens 49-57 11965378-1 2002 Optimization of the benzimidazole-based fXa inhibitors for selectivity versus thrombin and trypsin was achieved by substitution on the benzimidazole ring and replacement of the naphthylamidine group. benzimidazole 20-33 coagulation factor X Homo sapiens 40-43 11965378-1 2002 Optimization of the benzimidazole-based fXa inhibitors for selectivity versus thrombin and trypsin was achieved by substitution on the benzimidazole ring and replacement of the naphthylamidine group. benzimidazole 20-33 coagulation factor II, thrombin Homo sapiens 78-86 11965378-1 2002 Optimization of the benzimidazole-based fXa inhibitors for selectivity versus thrombin and trypsin was achieved by substitution on the benzimidazole ring and replacement of the naphthylamidine group. benzimidazole 135-148 coagulation factor X Homo sapiens 40-43 11965378-1 2002 Optimization of the benzimidazole-based fXa inhibitors for selectivity versus thrombin and trypsin was achieved by substitution on the benzimidazole ring and replacement of the naphthylamidine group. benzimidazole 135-148 coagulation factor II, thrombin Homo sapiens 78-86 11965378-2 2002 Substitution of a nitro group at the 4-position on the benzimidazole improves both potency against fXa and selectivity versus thrombin. benzimidazole 55-68 coagulation factor X Homo sapiens 99-102 11965378-2 2002 Substitution of a nitro group at the 4-position on the benzimidazole improves both potency against fXa and selectivity versus thrombin. benzimidazole 55-68 coagulation factor II, thrombin Homo sapiens 126-134 11597414-1 2001 Several benzimidazole derivatives have been identified as potent thrombin receptor (PAR-1) antagonists as represented by compound 1h, which showed an IC(50) of 33 nM. benzimidazole 8-21 coagulation factor II thrombin receptor Homo sapiens 84-89 12052197-3 2002 This article will review the development of the most important classes of 5-HT(4R) antagonists with an emphasis on benzimidazole derivatives, their structure-affinity relationships, ligand-receptor interactions and pharmacological applications. benzimidazole 115-128 5-hydroxytryptamine receptor 4 Homo sapiens 74-81 11868391-4 2002 On the other hand, benzimidazole compounds can induce CYP1A1 without binding to the Ah receptor as a ligand (ligand-independent pathway). benzimidazole 19-32 cytochrome P450 family 1 subfamily A member 1 Homo sapiens 54-60 11300866-3 2001 Appropriate substitution on the benzimidazole ring, especially with small alkyl groups, led to dramatic increases in potency, both in a cellular assay of apoB secretion and especially in animal models of cholesterol lowering. benzimidazole 32-45 apolipoprotein B-100 Macaca fascicularis 154-158 11055353-0 2000 1,2-Disubstituted indole, azaindole and benzimidazole derivatives possessing amine moiety: a novel series of thrombin inhibitors. benzimidazole 26-35 coagulation factor II, thrombin Homo sapiens 109-117 11169164-3 2001 Only compound 7a, with the presence of both the pyridyl moiety bound at the ethylenic bridge in C-2 of benzimidazole and the nitro-group in the benzene ring, displays a selective antiproliferative effect against certain leukaemia cells and a good antiviral activity especially towards the Coxsackie B5 virus. benzimidazole 103-116 complement C2 Homo sapiens 96-99 11063605-2 2000 Synthesis and biological properties of benzimidazole inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase. benzimidazole 39-52 poly(ADP-ribose) polymerase 1 Gallus gallus 89-116 11055353-0 2000 1,2-Disubstituted indole, azaindole and benzimidazole derivatives possessing amine moiety: a novel series of thrombin inhibitors. benzimidazole 40-53 coagulation factor II, thrombin Homo sapiens 109-117 11055353-1 2000 A novel series of 1,2-disubstituted indole, azaindole and benzimidazole derivatives possessing an amine moiety was identified as thrombin inhibitors. benzimidazole 44-53 coagulation factor II, thrombin Homo sapiens 129-137 11055353-1 2000 A novel series of 1,2-disubstituted indole, azaindole and benzimidazole derivatives possessing an amine moiety was identified as thrombin inhibitors. benzimidazole 58-71 coagulation factor II, thrombin Homo sapiens 129-137 10103034-0 1999 Structural and mechanistic aspects of transcriptional induction of cytochrome P450 1A1 by benzimidazole derivatives in rat hepatoma H4IIE cells. benzimidazole 90-103 cytochrome P450, family 1, subfamily a, polypeptide 1 Rattus norvegicus 67-86 10853669-0 2000 Design, synthesis, and in vitro biological activity of benzimidazole based factor Xa inhibitors. benzimidazole 55-68 coagulation factor X Homo sapiens 75-84 10853669-1 2000 Inhibitors based on the benzimidazole scaffold showed subnanomolar potency against Factor Xa with 500-1000-fold selectivity against thrombin and 50-100-fold selectivity against trypsin. benzimidazole 24-37 coagulation factor X Homo sapiens 83-92 10853669-1 2000 Inhibitors based on the benzimidazole scaffold showed subnanomolar potency against Factor Xa with 500-1000-fold selectivity against thrombin and 50-100-fold selectivity against trypsin. benzimidazole 24-37 coagulation factor II, thrombin Homo sapiens 132-140 10853669-2 2000 The 2-substituent on the benzimidazole ring had a strong impact on the FXa inhibitory activity. benzimidazole 25-38 coagulation factor X Homo sapiens 71-74 11079373-3 2000 We observed a marked increase in ALP activity in the serum of rats given a benzimidazole derivative by gavage, and detected it as slow-migrating ALPs (SM-ALPs), which were mALP-like but resistant to PIPLC and n-butanol treatment on disc PAGE. benzimidazole 75-88 alopecia, recessive Mus musculus 33-36 10936227-1 2000 Thiabendazole (TBZ), an anthelmintic and fungicide benzimidazole, was recently demonstrated to be extensively metabolized by cytochrome P450 (CYP) 1A2 in man and rabbit, yielding 5-hydroxythiabendazole (5OH-TBZ), the major metabolite furtherly conjugated, and two minor unidentified metabolites (M1 and M2). benzimidazole 51-64 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 125-150 10660561-3 2000 In stably expressing HEK293 cells, the benzimidazole-reactive cysteines, Cys-321 (transmembrane helix (TM) 3), Cys-813 and Cys-822 (TM5/6), and Cys-892 (TM7/8) were mutated to the amino acids found in the SCH28080-resistant Na,K-ATPase and kinetic parameters of H,K-ATPase activity analyzed. benzimidazole 39-52 tropomyosin 3 Homo sapiens 132-135 10605056-0 1999 Synthesis of benzimidazole derivatives as antiallergic agents with 5-lipoxygenase inhibiting action. benzimidazole 13-26 arachidonate 5-lipoxygenase Rattus norvegicus 67-81 10605056-1 1999 Syntheses were conducted of novel benzimidazole derivatives that suppress histamine release from mast cells, inhibit 5-lipoxygenase, and possess antioxidative action. benzimidazole 34-47 arachidonate 5-lipoxygenase Rattus norvegicus 117-131 10572257-2 1999 We also show results extending the knowledge of the range of compounds to which FLR1 gene confers resistance to the antimitotic systemic benzimidazole fungicide benomyl and the antitumor agent methotrexate, reinforcing the concept that the FLR1 gene is a multidrug resistance (MDR) determinant. benzimidazole 137-150 Flr1p Saccharomyces cerevisiae S288C 80-84 10572257-2 1999 We also show results extending the knowledge of the range of compounds to which FLR1 gene confers resistance to the antimitotic systemic benzimidazole fungicide benomyl and the antitumor agent methotrexate, reinforcing the concept that the FLR1 gene is a multidrug resistance (MDR) determinant. benzimidazole 137-150 Flr1p Saccharomyces cerevisiae S288C 240-244 10445394-1 1999 Benzimidazole compounds, such as omeprazole and thiabendazole, are a different type of CYP1A1-inducer from Ah receptor-ligands, such as 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) and 3-methylcholanthrene. benzimidazole 0-13 cytochrome P450 family 1 subfamily A member 1 Homo sapiens 87-93 10103034-1 1999 The effect of several structurally different benzimidazole compounds on CYP1A1 expression at the transcriptional, mRNA and protein levels was investigated in the rat hepatoma H4IIE cell line. benzimidazole 45-58 cytochrome P450, family 1, subfamily a, polypeptide 1 Rattus norvegicus 72-78 9702206-4 1998 The antiproliferative activity and the maximum potency of antiviral activity correlate with the presence of both the 2-pyridyl moiety bound at the ethylenic bridge in C-2 of benzimidazole and the nitro group in the benzene ring. benzimidazole 174-187 complement C2 Homo sapiens 167-170 9990464-0 1999 Azaindole derivatives with high affinity for the dopamine D4 receptor: synthesis, ligand binding studies and comparison of molecular electrostatic potential maps. benzimidazole 0-9 dopamine receptor D4 Homo sapiens 49-69 9873696-0 1998 Benzimidazole derivatives as arginine mimetics in 1,4-benzodiazepine nonpeptide vitronectin receptor (alpha v beta 3) antagonists. benzimidazole 0-13 eukaryotic translation elongation factor 1 beta 2 pseudogene 2 Homo sapiens 102-116 9873696-1 1998 In a 3-oxo-1,4-benzodiazepine-2-acetic acid series of vitronectin receptor (alpha v beta 3) antagonists containing a benzimidazole as a novel arginine mimetic, we examined the effects of benzimidazole modifications and amide substitutions on both activity and pharmacokinetics. benzimidazole 117-130 eukaryotic translation elongation factor 1 beta 2 pseudogene 2 Homo sapiens 84-90 9784250-1 1998 Benzimidazole compounds, such as omeprazole and thiabendazole, are a different type of CYP1A1 inducer from Ah receptor-ligands, such as TCDD (2,3,7,8-tetrachlorodibenzo-p-dioxin) and 3-methylcholanthrene. benzimidazole 0-13 cytochrome P450 family 1 subfamily A member 1 Homo sapiens 87-93 9784250-1 1998 Benzimidazole compounds, such as omeprazole and thiabendazole, are a different type of CYP1A1 inducer from Ah receptor-ligands, such as TCDD (2,3,7,8-tetrachlorodibenzo-p-dioxin) and 3-methylcholanthrene. benzimidazole 0-13 aryl hydrocarbon receptor Homo sapiens 107-118 9873613-1 1998 A new family of PDE4 inhibitors based on a benzimidazole framework is described. benzimidazole 43-56 phosphodiesterase 4A Homo sapiens 16-20 9258368-8 1997 The inhibitory profile exhibited by this new class of NMT ligands is a function of the pKa of the imidazole substituent as illustrated by the benzimidazole analog 35 which is about 10-fold less potent than 31. benzimidazole 142-155 N-myristoyltransferase 1 Homo sapiens 54-57 9699220-10 1998 This points to the importance of electronic properties of substituents in position 2 of benzimidazole ring for the D2/5-HT1A affinity ratio of this type of ligands. benzimidazole 88-101 5-hydroxytryptamine receptor 1A Bos taurus 118-124 9041675-2 1997 Induction of endogenous cytochrome P4501A1 (CYP1A1) by benzimidazole derivatives has been investigated in the human hepatoma cell line HepG2. benzimidazole 55-68 cytochrome P450 family 1 subfamily A member 1 Homo sapiens 24-42 9211916-9 1997 CobT phosphoribosylated alternative base substrates including benzimidazole, 4,5-dimethyl-1,2-phenylenediamine, imidazole, histidine, adenine, and guanine in vitro. benzimidazole 62-75 nicotinate-nucleotide--dimethylbenzimidazole phosphoribosyltransferase Salmonella enterica subsp. enterica serovar Typhimurium str. LT2 0-4 9041675-0 1997 Effects of benzimidazole derivatives on cytochrome P450 1A1 expression in a human hepatoma cell line. benzimidazole 11-24 cytochrome P450 family 1 subfamily A member 1 Homo sapiens 40-59 9041675-2 1997 Induction of endogenous cytochrome P4501A1 (CYP1A1) by benzimidazole derivatives has been investigated in the human hepatoma cell line HepG2. benzimidazole 55-68 cytochrome P450 family 1 subfamily A member 1 Homo sapiens 44-50 8900397-0 1996 Differences in inducibility of CYP1A1-mRNA by benzimidazole compounds between human and mouse cells: evidences of a human-specific signal transduction pathway for CYP1A1 induction. benzimidazole 46-59 cytochrome P450 family 1 subfamily A member 1 Homo sapiens 31-37 8967990-1 1996 We identified a novel azaindole derivative, L-750,667, that has high affinity (Ki = 0.51 nM) and >2000-fold selectivity for D4 dopamine receptors compared with its activity at D2 and D3 dopamine receptors. benzimidazole 22-31 Rho GDP dissociation inhibitor beta Homo sapiens 127-129 8900397-0 1996 Differences in inducibility of CYP1A1-mRNA by benzimidazole compounds between human and mouse cells: evidences of a human-specific signal transduction pathway for CYP1A1 induction. benzimidazole 46-59 cytochrome P450 family 1 subfamily A member 1 Homo sapiens 163-169 8855719-3 1996 A number of benzimidazole derivatives were synthesized and tested for cholecystokinin A (CCK-A) receptor inhibitory activity in order to study structure-activity relationships. benzimidazole 12-25 cholecystokinin A receptor Homo sapiens 89-104 8258826-2 1993 Systemic variation of several substituents at the benzimidazole ring positions 4-7 led to the finding that substitution in position 6 with acylamino groups results in highly active AII antagonists. benzimidazole 50-63 angiotensinogen Rattus norvegicus 181-184 7733914-1 1995 Benzimidazole derivatives are potent inducers of CYP1A1 in rabbit and human hepatocytes, but apparently do not bind the AH receptor. benzimidazole 0-13 cytochrome P450 1A1 Oryctolagus cuniculus 49-55 7877171-6 1995 All H. contortus tub-1 constructs, which encoded Phe at position 200, conferred susceptibility to thiabendazole in BZ-resistant C. elegans ben-1 mutants. benzimidazole 115-117 Tubby protein homolog 1 Caenorhabditis elegans 17-22 7877171-6 1995 All H. contortus tub-1 constructs, which encoded Phe at position 200, conferred susceptibility to thiabendazole in BZ-resistant C. elegans ben-1 mutants. benzimidazole 115-117 Tubulin beta chain Caenorhabditis elegans 139-144 7710270-8 1994 Thus, while introduction of a benzimidazole group into the PR inhibitors was a successful structural modification with regard to antiviral activity in cell culture, it completely abolished oral bioavailability. benzimidazole 30-43 endogenous retrovirus group K member 25 Homo sapiens 59-61 8647108-0 1996 Induction of CYP1A1 gene by benzimidazole derivatives during Caco-2 cell differentiation. benzimidazole 28-41 cytochrome P450 family 1 subfamily A member 1 Homo sapiens 13-19 8647108-10 1996 The induction of CYP1A1 transcription by benzimidazole derivatives in Caco-2 cells occurred with no direct binding of benzimidazole derivatives to the aryl-hydrocarbon receptor, as in human hepatocytes. benzimidazole 41-54 cytochrome P450 family 1 subfamily A member 1 Homo sapiens 17-23 8647108-13 1996 These results question about the mechanism of ligand-independent activation of the aryl-hydrocarbon receptor and intracellular signaling, initiated by benzimidazole derivatives. benzimidazole 151-164 aryl hydrocarbon receptor Homo sapiens 83-108 20650191-9 1996 Different induction rates obtained with several benzimidazole drugs suggest that the sulfur atom within the molecule is critical for CYP1A1 induction. benzimidazole 48-61 cytochrome P450 1A1 Oryctolagus cuniculus 133-139 20650191-10 1996 The widely used benzimidazole anthelmintics OFZ and FBZ may exert an inducing effect through an original pathway that does not require a specific binding step to the Ah receptor. benzimidazole 16-29 aryl hydrocarbon receptor Oryctolagus cuniculus 166-177 7877171-3 1995 Functional analysis of a conserved beta-tubulin isotype (tub-1) mutation near GTP-binding domain II, which is linked to BZ resistance, was carried out in C. elegans by heterologous expression of: (1) parasite BZ-sensitive alleles; (2) BZ-resistant alleles; and (3) in vitro mutagenised beta-tubulin gene constructs. benzimidazole 120-122 Tubby protein homolog 1 Caenorhabditis elegans 57-62 7877171-3 1995 Functional analysis of a conserved beta-tubulin isotype (tub-1) mutation near GTP-binding domain II, which is linked to BZ resistance, was carried out in C. elegans by heterologous expression of: (1) parasite BZ-sensitive alleles; (2) BZ-resistant alleles; and (3) in vitro mutagenised beta-tubulin gene constructs. benzimidazole 209-211 Tubby protein homolog 1 Caenorhabditis elegans 57-62 7877171-3 1995 Functional analysis of a conserved beta-tubulin isotype (tub-1) mutation near GTP-binding domain II, which is linked to BZ resistance, was carried out in C. elegans by heterologous expression of: (1) parasite BZ-sensitive alleles; (2) BZ-resistant alleles; and (3) in vitro mutagenised beta-tubulin gene constructs. benzimidazole 209-211 Tubby protein homolog 1 Caenorhabditis elegans 57-62 8258826-4 1993 In contrast, analogous substitution of the benzimidazole moiety with basic heterocycles resulted in potent AII antagonists which were also well absorbed after oral application. benzimidazole 43-56 angiotensinogen Rattus norvegicus 107-110 8401764-4 1993 The preliminary SAR studies indicate the importance of chlorine atom at position 3 in diazine nucleus and of alkyl substituents in benzimidazole moiety for positive inotropic effects. benzimidazole 131-144 sarcosine dehydrogenase Homo sapiens 16-19 8488169-1 1993 BIBS 39 and BIBS 222 are novel, nonpeptide angiotensin II receptor antagonists with a benzimidazole structure. benzimidazole 86-99 angiotensinogen Rattus norvegicus 43-57 8487256-0 1993 Synthesis and structure-activity relationships of novel benzimidazole and imidazo[4,5-b]pyridine acid derivatives as thromboxane A2 receptor antagonists. benzimidazole 56-69 thromboxane A2 receptor Homo sapiens 117-140 1388592-1 1992 The influence of bioisosteric replacement of catechol moiety of L-Dopa and alpha-Methyldopa with benzimidazole and benzotriazole ring has been examined on dopamine beta-hydroxylase and tyrosinase, in order to evidentiate an inhibitory activity on the synthesis of catecholamines and a possible antihypertensive action. benzimidazole 97-110 tyrosinase Homo sapiens 185-195 1280125-1 1992 Omeprazole is a benzimidazole derivative which induces both P450 1A1 and 1A2 in human liver in vitro and in vivo. benzimidazole 16-29 solute carrier family 45 member 2 Homo sapiens 65-68 1886288-1 1991 Antisecretory effects of a substituted benzimidazole, (+/-)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridyl]methyl] sulfinyl]-1H-benzimidazole (AG-1749) were compared with those of a histamine H2-receptor antagonist, famotidine. benzimidazole 39-52 histamine receptor H2 Canis lupus familiaris 185-206 1748033-3 1991 Omeprazole contains a benzimidazole moiety and thus has the potential to interact with the cytochrome P-450 enzyme group. benzimidazole 22-35 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 91-107 2016714-0 1991 Receptor-based design of novel dihydrofolate reductase inhibitors: benzimidazole and indole derivatives. benzimidazole 67-80 Dihydrofolate reductase Escherichia coli 31-54 1548677-6 1992 The benzimidazole antagonists displaced AII in binding studies in vitro with IC50 values in the range 10(-5)-10(-7) M and antagonized the hypertensive effects of AII in vivo (rats) following intravenous administration with ED50 values in the range of 5-20 mg/kg. benzimidazole 4-17 angiotensinogen Rattus norvegicus 40-43 1548677-6 1992 The benzimidazole antagonists displaced AII in binding studies in vitro with IC50 values in the range 10(-5)-10(-7) M and antagonized the hypertensive effects of AII in vivo (rats) following intravenous administration with ED50 values in the range of 5-20 mg/kg. benzimidazole 4-17 angiotensinogen Rattus norvegicus 162-165 1738300-6 1992 Incubation of hookworms with some benzimidazole anthelmintics viz., mebendazole or albendazole significantly reduced the capacity of the worms to secrete cholinesterase and increase in enzyme activity within the parasite. benzimidazole 34-47 butyrylcholinesterase Homo sapiens 154-168 1738300-8 1992 These observations indicate role of microtubules in the secretion of cholinesterase by hookworms and as a target for the action of benzimidazole anthelmintics. benzimidazole 131-144 butyrylcholinesterase Homo sapiens 69-83 34931332-0 2022 Design, synthesis, biological activity, molecular docking, and molecular dynamics of novel benzimidazole derivatives as potential AChE/MAO-B dual inhibitors. benzimidazole 91-104 acetylcholinesterase (Cartwright blood group) Homo sapiens 130-134 33764593-0 2021 Theoretical Insights into Molecular Mechanism and Energy Criteria of PARP-2 Enzyme Inhibition by Benzimidazole Analogues. benzimidazole 97-110 poly(ADP-ribose) polymerase 2 Homo sapiens 69-75 34971430-2 2021 BRP-201, a novel benzimidazole-based FLAP antagonist, inhibits leukotriene biosynthesis in isolated leukocytes. benzimidazole 17-30 arachidonate 5-lipoxygenase activating protein Homo sapiens 37-41 33766769-0 2021 Exploring naltrexamine derivatives featuring azaindole moiety via nitrogen-walk approach to investigate their in vitro pharmacological profiles at the mu opioid receptor. benzimidazole 45-54 opioid receptor mu 1 Homo sapiens 151-169 34931332-0 2022 Design, synthesis, biological activity, molecular docking, and molecular dynamics of novel benzimidazole derivatives as potential AChE/MAO-B dual inhibitors. benzimidazole 91-104 monoamine oxidase B Homo sapiens 135-140 34931332-1 2022 To develop new acetylcholinesterase (AChE)-monoamine oxidase-B (MAO-B) dual inhibitors against Alzheimer"s disease, the benzimidazole ring, which has a propargyl side chain with previously proven selective MAO-B inhibitory activity, was used as the main structure. benzimidazole 120-133 acetylcholinesterase (Cartwright blood group) Homo sapiens 15-35 34931332-1 2022 To develop new acetylcholinesterase (AChE)-monoamine oxidase-B (MAO-B) dual inhibitors against Alzheimer"s disease, the benzimidazole ring, which has a propargyl side chain with previously proven selective MAO-B inhibitory activity, was used as the main structure. benzimidazole 120-133 acetylcholinesterase (Cartwright blood group) Homo sapiens 37-41 34931332-1 2022 To develop new acetylcholinesterase (AChE)-monoamine oxidase-B (MAO-B) dual inhibitors against Alzheimer"s disease, the benzimidazole ring, which has a propargyl side chain with previously proven selective MAO-B inhibitory activity, was used as the main structure. benzimidazole 120-133 monoamine oxidase B Homo sapiens 43-62 34931332-1 2022 To develop new acetylcholinesterase (AChE)-monoamine oxidase-B (MAO-B) dual inhibitors against Alzheimer"s disease, the benzimidazole ring, which has a propargyl side chain with previously proven selective MAO-B inhibitory activity, was used as the main structure. benzimidazole 120-133 monoamine oxidase B Homo sapiens 64-69 34931332-1 2022 To develop new acetylcholinesterase (AChE)-monoamine oxidase-B (MAO-B) dual inhibitors against Alzheimer"s disease, the benzimidazole ring, which has a propargyl side chain with previously proven selective MAO-B inhibitory activity, was used as the main structure. benzimidazole 120-133 monoamine oxidase B Homo sapiens 206-211 34561907-3 2021 In this study, a 1D-3D mixed-dimensional perovskite material is explored by adding an organic salt with a bulk benzimidazole cation (Bn+ ). benzimidazole 111-124 zinc finger protein of the cerebellum 3 Mus musculus 133-136 34225075-3 2021 The present study introduces Beta-cyclodextrin (beta-CD) as a novel/effective organic nano-container for Benzimidazole (BM) encapsulation to obtain reliable active protection property via a controlled-release property. benzimidazole 105-118 ACD shelterin complex subunit and telomerase recruitment factor Homo sapiens 48-55 34852738-4 2022 METHODS: About 25 articles were collected that discussed various benzimidazole derivatives and categorized them under various subheadings based on the targets such as BACE 1, JNK, MAO, choline esterase enzyme, oxidative stress, mitochondrial dysfunction in which they act. benzimidazole 65-78 beta-secretase 1 Homo sapiens 167-173 34852738-4 2022 METHODS: About 25 articles were collected that discussed various benzimidazole derivatives and categorized them under various subheadings based on the targets such as BACE 1, JNK, MAO, choline esterase enzyme, oxidative stress, mitochondrial dysfunction in which they act. benzimidazole 65-78 mitogen-activated protein kinase 8 Homo sapiens 175-178 34225075-3 2021 The present study introduces Beta-cyclodextrin (beta-CD) as a novel/effective organic nano-container for Benzimidazole (BM) encapsulation to obtain reliable active protection property via a controlled-release property. benzimidazole 120-122 ACD shelterin complex subunit and telomerase recruitment factor Homo sapiens 48-55 34225075-10 2021 The dispersion-corrected Density Functional Theory (DFT)-D explorations ascertained the inclusion capacity of benzimidazole inside the beta-CD. benzimidazole 110-123 ACD shelterin complex subunit and telomerase recruitment factor Homo sapiens 135-142 34225180-0 2021 Benzimidazole-galactosides bind selectively to the Galectin-8 N-Terminal domain: Structure-based design and optimisation. benzimidazole 0-13 galectin 8 Homo sapiens 51-61 34737234-8 2021 Using a proprietary translational technology platform, a drug library screen identified a substituted benzimidazole as a Bach1 inhibitor that was validated as a nonelectrophile. benzimidazole 102-115 BTB and CNC homology 1, basic leucine zipper transcription factor 1 Mus musculus 121-126 34225180-6 2021 Thus, the benzimidazole-derivatised galactosides represent promising compounds for studies of the pathological implications of galectin-8, as well as a starting point for the development of anti-tumour and anti-inflammatory therapeutics targeting galectin-8. benzimidazole 10-23 galectin 8 Homo sapiens 127-137 34517794-10 2022 CONCLUSION: Benzothiazole, benzoxazole, benzimidazole, and sulfhydryl derivatives stand out as TIM inhibitors. benzimidazole 40-53 triosephosphate isomerase 1 Homo sapiens 95-98 34795863-2 2021 The design, synthesis, and protein affinity evaluation of a set of C-3 substituted benzimidazole and quinoline d-galactal derivatives identified a d-galactal-benzimidazole hybrid as a selective ligand for the galectin-8 N-terminal domain (galectin-8N), with a K d of 48 muM and 15-fold selectivity over galectin-3 and even better selectivity over the other mammalian galectins. benzimidazole 83-96 galectin 8 Homo sapiens 209-219 34795863-2 2021 The design, synthesis, and protein affinity evaluation of a set of C-3 substituted benzimidazole and quinoline d-galactal derivatives identified a d-galactal-benzimidazole hybrid as a selective ligand for the galectin-8 N-terminal domain (galectin-8N), with a K d of 48 muM and 15-fold selectivity over galectin-3 and even better selectivity over the other mammalian galectins. benzimidazole 158-171 galectin 8 Homo sapiens 209-219 34795863-2 2021 The design, synthesis, and protein affinity evaluation of a set of C-3 substituted benzimidazole and quinoline d-galactal derivatives identified a d-galactal-benzimidazole hybrid as a selective ligand for the galectin-8 N-terminal domain (galectin-8N), with a K d of 48 muM and 15-fold selectivity over galectin-3 and even better selectivity over the other mammalian galectins. benzimidazole 158-171 galectin 3 Homo sapiens 303-313 34651438-0 2021 Insights into the structure and drug design of benzimidazole derivatives targeting the epidermal growth factor receptor (EGFR). benzimidazole 47-60 epidermal growth factor receptor Homo sapiens 87-119 34651438-0 2021 Insights into the structure and drug design of benzimidazole derivatives targeting the epidermal growth factor receptor (EGFR). benzimidazole 47-60 epidermal growth factor receptor Homo sapiens 121-125 34651438-5 2021 Despite numerous publications on the design, synthesis and biological assays of benzimidazole derivatives, their inhibitory activities against epidermal growth factor receptor (EGFR), a receptor tyrosine kinase (RTK), have not been specifically analysed. benzimidazole 80-93 epidermal growth factor receptor Homo sapiens 143-175 34651438-5 2021 Despite numerous publications on the design, synthesis and biological assays of benzimidazole derivatives, their inhibitory activities against epidermal growth factor receptor (EGFR), a receptor tyrosine kinase (RTK), have not been specifically analysed. benzimidazole 80-93 epidermal growth factor receptor Homo sapiens 177-181 34651438-6 2021 This review covers recent research reports on the anticancer activity of benzimidazole derivatives focusing on EGFR expression cell lines, based on their structure-activity relationship study. benzimidazole 73-86 epidermal growth factor receptor Homo sapiens 111-115 34651438-7 2021 We believe it would aid researchers to envision the challenges and explore benzimidazole"s potentials as tyrosine kinase inhibitors. benzimidazole 75-88 TXK tyrosine kinase Homo sapiens 105-120 34681742-4 2021 Following a previous lead scaffold, benzimidazole moiety was modified with various aryl groups and hydroxylation, and the resulting compounds exhibited JNK3 inhibitory activity with improved potency and selectivity. benzimidazole 36-49 mitogen activated protein kinase 10 Rattus norvegicus 152-156 34516105-1 2021 Substitution of apical halide ligands in ({Re6Sei8}Xa6)3- (X = Cl, Br) by benzimidazole (bimzH) accompanied by a self-assembly process leads to the formation of microporous Re6-based hydrogen-bonded organic frameworks (Re6-HOFs) constructed on N-H X hydrogen bonds and pi-pi-stacking interactions between bimzH ligands. benzimidazole 74-87 chromosome 12 open reading frame 73 Homo sapiens 67-69 34579637-0 2022 Inhibition of iNOS by Benzimidazole Derivatives: Synthesis, Docking, and Biological Evaluations. benzimidazole 22-35 nitric oxide synthase 2 Rattus norvegicus 14-18 34579637-3 2022 OBJECTIVE: The present work was aimed to design, synthesize and evaluate benzimidazole-coumarin coupled molecules as anti-iNOS agents through in silico and pharmacological studies. benzimidazole 73-86 nitric oxide synthase 2 Rattus norvegicus 122-126 34579637-14 2022 CONCLUSION: The newly synthesized benzimidazole-coumarin hybrids may serve as potential leads for the development of novel anti-iNOS agents. benzimidazole 34-47 nitric oxide synthase 2 Rattus norvegicus 128-132 34482215-4 2021 The study aimed to generate a homology model for the beta-tubulin of S. mansoni using the crystal structure of O visaries (Sheep) beta-tubulin (PDB ID: 3N2G D) as a template, then different beta-tubulin models were generated and two previously reported benzimidazole derivatives (NBTP-F and NBTP-OH) were docked to the generated models, the binding results indicated that both S. mansoni, S. haematobium were susceptible to the two NBTP derivatives. benzimidazole 253-266 beta-tubulin Ovis aries 53-65 34482215-7 2021 Moreover, additional seven new benzimidazole derivatives were synthesized and tested by molecular docking on the generated model binding site of S. mansoni beta-tubulin and were found to have good interaction inside the pocket. benzimidazole 31-44 beta-tubulin Ovis aries 156-168 34423556-8 2021 Finally, all atom molecular dynamics simulations determined the most energetically favorable binding mode for PQ912, in the active site of sQC, which is similar to that of LSB-09, a recently reported sQC inhibitor containing benzimidazole-6-carboxamide moiety. benzimidazole 225-238 glutaminyl-peptide cyclotransferase Homo sapiens 200-203 34722993-1 2021 A novel triazole-bridged coumarin-benzimidazole-conjugated fluorescence sensor (4) has been developed for selective detection of Cd2+ over other competitive metal ions. benzimidazole 34-47 CD2 molecule Homo sapiens 129-132 34722993-4 2021 The involvement of benzimidazole and triazole moieties in Cd2+ binding was confirmed by different spectroscopic techniques such as UV-vis, Fourier transform infrared, nuclear magnetic resonance, and ESI mass. benzimidazole 19-32 CD2 molecule Homo sapiens 58-61 34403955-0 2021 Discovery of benzimidazole derivatives as potent and selective aldehyde dehydrogenase 1A1 (ALDH1A1) inhibitors with glucose consumption improving activity. benzimidazole 13-26 aldehyde dehydrogenase 1 family member A1 Homo sapiens 63-89 34403955-0 2021 Discovery of benzimidazole derivatives as potent and selective aldehyde dehydrogenase 1A1 (ALDH1A1) inhibitors with glucose consumption improving activity. benzimidazole 13-26 aldehyde dehydrogenase 1 family member A1 Homo sapiens 91-98 34128259-0 2021 Design, synthesis, and biological evaluation of novel benzimidazole derivatives as sphingosine kinase 1 inhibitor. benzimidazole 54-67 sphingosine kinase 1 Homo sapiens 83-103 34128259-4 2021 Our design strategy is twofold: It aimed first to study the effect of replacing the 5-position of the benzimidazole ring with a polar carboxylic acid group on the SphK1-inhibitory activity and cytotoxicity. benzimidazole 102-115 sphingosine kinase 1 Homo sapiens 163-168 34128259-7 2021 The binding affinity of the benzimidazole derivatives toward SphK1 was measured by fluorescence binding and molecular docking. benzimidazole 28-41 sphingosine kinase 1 Homo sapiens 61-66 34337627-1 2021 Introduction of the propyl-sulfonic acid group at N1 of the coordinated 2-(2-pyridyl)benzimidazole ligand (L) in (RhCl(eta5-C5Me5)L)(CF3SO3) gives rise to a water-soluble complex, which can bind to the model protein lysozyme via non-covalent interactions. benzimidazole 84-98 lysozyme Homo sapiens 216-224 34586727-0 2021 Dual blocking of PI3K and mTOR signaling by DHW-221, a novel benzimidazole derivative, exerts antitumor activity in human non-small cell lung cancer. benzimidazole 61-74 mechanistic target of rapamycin kinase Homo sapiens 26-30 34153810-4 2021 The target benzimidazole 3f containing hydroxyl motif at para-position of phenyl revealed an important activity inhibitor against alpha- amylase (IC50 = 12.09 +- 0.38 microM) and alpha-glucosidase (IC50 = 11.02 +- 0.04 microM) comparable to the reference drug acarbose. benzimidazole 11-24 sucrase-isomaltase Homo sapiens 179-196 34121397-0 2021 Discovery and Characterization of Benzimidazole Derivative XY123 as a Potent, Selective, and Orally Available RORgamma Inverse Agonist. benzimidazole 34-47 RAR-related orphan receptor gamma Mus musculus 110-118 34373541-1 2021 We have recently described Pz-1, a benzimidazole-based type-2 RET and VEGFR2 inhibitor. benzimidazole 35-48 ret proto-oncogene Homo sapiens 62-65 34373541-1 2021 We have recently described Pz-1, a benzimidazole-based type-2 RET and VEGFR2 inhibitor. benzimidazole 35-48 kinase insert domain receptor Homo sapiens 70-76 34225394-2 2022 In this paper, we look for the in vitro cytotoxic capability of novel benzimidazole-based N-heterocyclic carbene (NHC) precursor (1) and its Ag(I)-NHC complex (2). benzimidazole 70-83 high mobility group nucleosomal binding domain 4 Homo sapiens 114-117 34225394-2 2022 In this paper, we look for the in vitro cytotoxic capability of novel benzimidazole-based N-heterocyclic carbene (NHC) precursor (1) and its Ag(I)-NHC complex (2). benzimidazole 70-83 high mobility group nucleosomal binding domain 4 Homo sapiens 147-150 34121397-2 2021 Herein, we report our effort on the discovery, optimization, and evaluation of benzothiazole and benzimidazole derivatives as novel inverse agonists of RORgamma. benzimidazole 97-110 RAR-related orphan receptor gamma Mus musculus 152-160 34567143-7 2021 Compound B18, a benzimidazole derivative, has an excellent binding affinity towards CRF-1 protein compared to reference molecules; hence, this compound could be a potential drug candidate for stress-dependent disorders. benzimidazole 16-29 corticotropin releasing hormone receptor 1 Homo sapiens 84-89 34101459-1 2021 The spectroscopic characterization of the benzimidazole (BIM) homodimer was carried out in a molecular beam in the ground state as well as in the cationic state using the R2PI and RIDIR methods. benzimidazole 42-55 superoxide dismutase 1 Homo sapiens 62-71 34101459-1 2021 The spectroscopic characterization of the benzimidazole (BIM) homodimer was carried out in a molecular beam in the ground state as well as in the cationic state using the R2PI and RIDIR methods. benzimidazole 57-60 superoxide dismutase 1 Homo sapiens 62-71 35569250-0 2022 Discovery of novel benzimidazole derivatives as potent p300 bromodomain inhibitors with anti-proliferative activity in multiple cancer cells. benzimidazole 19-32 E1A binding protein p300 Homo sapiens 55-59 35513222-4 2022 However, there have been few reports of direct AMPK activator with high potency for beta2-AMPK isoform, which is thought to be important for glucose homeostasis, and their chemical structure is limited to benzimidazole core. benzimidazole 205-218 protein kinase AMP-activated non-catalytic subunit beta 1 Homo sapiens 47-51 35513222-4 2022 However, there have been few reports of direct AMPK activator with high potency for beta2-AMPK isoform, which is thought to be important for glucose homeostasis, and their chemical structure is limited to benzimidazole core. benzimidazole 205-218 ATPase H+ transporting V0 subunit a2 Homo sapiens 84-89 35636123-7 2022 The benzimidazole-quinazolinone derivatives 14f,g revealed potent RAF kinases inhibitory activities on BRAF (wt), BRAF (V600E) and CRAF showing IC50 values 0.002-0.1 microM, whereas, the benzimidazole-quinazolinone derivatives 14i and 14k showed moderate VEGFR-2 inhibitory activity (IC50 = 20.60 and 6.14 microM, respectively). benzimidazole 4-17 zinc fingers and homeoboxes 2 Homo sapiens 66-69 35513222-4 2022 However, there have been few reports of direct AMPK activator with high potency for beta2-AMPK isoform, which is thought to be important for glucose homeostasis, and their chemical structure is limited to benzimidazole core. benzimidazole 205-218 protein kinase AMP-activated non-catalytic subunit beta 1 Homo sapiens 90-94 35489524-3 2022 Although most benzimidazole derivatives are commonly less toxic, their effects on SIRTs and cytochrome P450 (CYP) regulations have not been explored alongside toxicity assessments. benzimidazole 14-27 cytochrome P450, family 21, subfamily a, polypeptide 1 Mus musculus 92-107 35489524-3 2022 Although most benzimidazole derivatives are commonly less toxic, their effects on SIRTs and cytochrome P450 (CYP) regulations have not been explored alongside toxicity assessments. benzimidazole 14-27 cytochrome P450, family 21, subfamily a, polypeptide 1 Mus musculus 109-112 35595366-4 2022 In this study, we developed a fluorescent probe for the discriminative sensing of Cl- and Br- using a naphthalimide-benzimidazole conjugate-based Ag+ complex (L1-Ag+ complex) by exploiting the strong interaction between Ag+ and halide ions with selectivity control by pH variation. benzimidazole 116-129 chromosome 12 open reading frame 73 Homo sapiens 82-92 35595366-4 2022 In this study, we developed a fluorescent probe for the discriminative sensing of Cl- and Br- using a naphthalimide-benzimidazole conjugate-based Ag+ complex (L1-Ag+ complex) by exploiting the strong interaction between Ag+ and halide ions with selectivity control by pH variation. benzimidazole 116-129 S100 calcium binding protein A8 Homo sapiens 159-164 35576659-1 2022 Ligands comprising a benzimidazole rather than the imidazole ring that is common in AT2R ligands e.g. in the AT2R agonist C21, can provide both high affinity and receptor selectivity. benzimidazole 21-34 TBL1X/Y related 1 Homo sapiens 122-125 35636123-7 2022 The benzimidazole-quinazolinone derivatives 14f,g revealed potent RAF kinases inhibitory activities on BRAF (wt), BRAF (V600E) and CRAF showing IC50 values 0.002-0.1 microM, whereas, the benzimidazole-quinazolinone derivatives 14i and 14k showed moderate VEGFR-2 inhibitory activity (IC50 = 20.60 and 6.14 microM, respectively). benzimidazole 4-17 B-Raf proto-oncogene, serine/threonine kinase Homo sapiens 103-107 35636123-7 2022 The benzimidazole-quinazolinone derivatives 14f,g revealed potent RAF kinases inhibitory activities on BRAF (wt), BRAF (V600E) and CRAF showing IC50 values 0.002-0.1 microM, whereas, the benzimidazole-quinazolinone derivatives 14i and 14k showed moderate VEGFR-2 inhibitory activity (IC50 = 20.60 and 6.14 microM, respectively). benzimidazole 4-17 B-Raf proto-oncogene, serine/threonine kinase Homo sapiens 114-118 35636123-7 2022 The benzimidazole-quinazolinone derivatives 14f,g revealed potent RAF kinases inhibitory activities on BRAF (wt), BRAF (V600E) and CRAF showing IC50 values 0.002-0.1 microM, whereas, the benzimidazole-quinazolinone derivatives 14i and 14k showed moderate VEGFR-2 inhibitory activity (IC50 = 20.60 and 6.14 microM, respectively). benzimidazole 4-17 Raf-1 proto-oncogene, serine/threonine kinase Homo sapiens 131-135 35636123-7 2022 The benzimidazole-quinazolinone derivatives 14f,g revealed potent RAF kinases inhibitory activities on BRAF (wt), BRAF (V600E) and CRAF showing IC50 values 0.002-0.1 microM, whereas, the benzimidazole-quinazolinone derivatives 14i and 14k showed moderate VEGFR-2 inhibitory activity (IC50 = 20.60 and 6.14 microM, respectively). benzimidazole 187-200 B-Raf proto-oncogene, serine/threonine kinase Homo sapiens 103-107 35636123-7 2022 The benzimidazole-quinazolinone derivatives 14f,g revealed potent RAF kinases inhibitory activities on BRAF (wt), BRAF (V600E) and CRAF showing IC50 values 0.002-0.1 microM, whereas, the benzimidazole-quinazolinone derivatives 14i and 14k showed moderate VEGFR-2 inhibitory activity (IC50 = 20.60 and 6.14 microM, respectively). benzimidazole 187-200 B-Raf proto-oncogene, serine/threonine kinase Homo sapiens 114-118 35636123-7 2022 The benzimidazole-quinazolinone derivatives 14f,g revealed potent RAF kinases inhibitory activities on BRAF (wt), BRAF (V600E) and CRAF showing IC50 values 0.002-0.1 microM, whereas, the benzimidazole-quinazolinone derivatives 14i and 14k showed moderate VEGFR-2 inhibitory activity (IC50 = 20.60 and 6.14 microM, respectively). benzimidazole 187-200 Raf-1 proto-oncogene, serine/threonine kinase Homo sapiens 131-135 35636124-2 2022 Herein, to develop specific pharmacologic inhibitors of HIPK2, we designed and synthesized a series of compounds containing benzimidazole and pyrimidine scaffolds via fragment-based drug design strategy. benzimidazole 124-137 homeodomain interacting protein kinase 2 Rattus norvegicus 56-61 35557491-0 2022 Further exploration of the benzimidazole scaffold as TRPC5 inhibitors: identification of 1-alkyl-2-(pyrrolidin-1-yl)-1H-benzo(d)imidazoles as potent and selective inhibitors. benzimidazole 27-40 transient receptor potential cation channel subfamily C member 5 Homo sapiens 53-58 35438328-0 2022 Computational study reveals substituted benzimidazole derivatives" binding selectivity to PI3Kdelta and PI3Kgamma. benzimidazole 40-53 phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta Homo sapiens 90-99 35624746-0 2022 Study on the Neuroprotective, Radical-Scavenging and MAO-B Inhibiting Properties of New Benzimidazole Arylhydrazones as Potential Multi-Target Drugs for the Treatment of Parkinson"s Disease. benzimidazole 88-101 monoamine oxidase B Homo sapiens 53-58 35438328-0 2022 Computational study reveals substituted benzimidazole derivatives" binding selectivity to PI3Kdelta and PI3Kgamma. benzimidazole 40-53 phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma Homo sapiens 104-113 35438328-4 2022 Preliminary studies have obtained PI3K inhibitors bearing a benzimidazole structural motif with a certain selectivity for PI3Kdelta and PI3Kgamma subtypes. benzimidazole 60-73 phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta Homo sapiens 122-131 35438328-4 2022 Preliminary studies have obtained PI3K inhibitors bearing a benzimidazole structural motif with a certain selectivity for PI3Kdelta and PI3Kgamma subtypes. benzimidazole 60-73 phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma Homo sapiens 136-145 35033885-0 2022 Discovery of a benzimidazole-based dual FLT3/TrKA inhibitor targeting acute myeloid leukemia. benzimidazole 15-28 fms related receptor tyrosine kinase 3 Homo sapiens 40-44 35184951-1 2022 Benzimidazole 1 (BUB1) and budding uninhibited by benzimidazole 1-related 1 (BUBR1) are multidomain paralogs with key roles in chromosome alignment during mitosis and the spindle assembly checkpoint (SAC), an evolutionarily conserved signaling pathway that monitors errors in chromosome segregation during cell division in eukaryotes. benzimidazole 0-13 BUB1 mitotic checkpoint serine/threonine kinase Homo sapiens 17-21 35184951-1 2022 Benzimidazole 1 (BUB1) and budding uninhibited by benzimidazole 1-related 1 (BUBR1) are multidomain paralogs with key roles in chromosome alignment during mitosis and the spindle assembly checkpoint (SAC), an evolutionarily conserved signaling pathway that monitors errors in chromosome segregation during cell division in eukaryotes. benzimidazole 50-63 BUB1 mitotic checkpoint serine/threonine kinase B Homo sapiens 77-82 35319364-11 2022 We hope that enlightened by the previous researches, more researches of AD site should be occurred and more effective benzimidazole PARP-1 inhibitors could be designed, synthesized, and applied to clinics. benzimidazole 118-131 poly(ADP-ribose) polymerase 1 Homo sapiens 132-138 35152061-0 2022 Novel potent benzimidazole-based microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitors derived from BRP-201 that also inhibit leukotriene C4 synthase. benzimidazole 13-26 prostaglandin E synthase Mus musculus 73-80 35152061-0 2022 Novel potent benzimidazole-based microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitors derived from BRP-201 that also inhibit leukotriene C4 synthase. benzimidazole 13-26 leukotriene C4 synthase Homo sapiens 132-155 35319364-0 2022 Recent Progress of the research on the benzimidazole PARP-1 inhibitors. benzimidazole 39-52 poly(ADP-ribose) polymerase 1 Homo sapiens 53-59 35319364-5 2022 However, the commercial available benzimidazole PARP-1 inhibitors have some shortcomings such as serious toxicity in combination with chemotherapy drugs, in vivo cardiovascular side effects such as anemia. benzimidazole 34-47 poly(ADP-ribose) polymerase 1 Homo sapiens 48-54 35319364-6 2022 Therefore it"s crucial for scientists to explore more structure-activity relationships of the benzimidazole PARP-1 inhibitors and access safer and more effective PARP inhibitors. benzimidazole 94-107 poly(ADP-ribose) polymerase 1 Homo sapiens 108-114 35319364-7 2022 As the binding region of PARP-1 and the substrates is usually characterized as NI site and AD site, the modification of benzimidazoles mainly occurs on the benzimidazole skeleton (NI site), and the side chain of benzimidazole on 2-C position (AD site). benzimidazole 156-169 poly(ADP-ribose) polymerase 1 Homo sapiens 25-31 35319364-7 2022 As the binding region of PARP-1 and the substrates is usually characterized as NI site and AD site, the modification of benzimidazoles mainly occurs on the benzimidazole skeleton (NI site), and the side chain of benzimidazole on 2-C position (AD site). benzimidazole 212-225 poly(ADP-ribose) polymerase 1 Homo sapiens 25-31 35156516-3 2022 The expression level of miR-664b-3p and Budding uninhibited by benzimidazole 3 (Bub3) in colon cancer cell lines and tissues were detected and analyzed using quantitative real-time PCR and bioinformatics method. benzimidazole 63-76 BUB3 mitotic checkpoint protein Homo sapiens 80-84 35148084-0 2022 Identification of the Benzoimidazole Compound as a Selective FLT3 Inhibitor by Cell-Based High-Throughput Screening of a Diversity Library. benzimidazole 22-36 fms related receptor tyrosine kinase 3 Homo sapiens 61-65 35148084-7 2022 Our findings establish the specific activity of the benzoimidazole compound against FLT3/ITD leukemia and warrant further investigation in this subset of leukemia patients with poor prognosis. benzimidazole 52-66 fms related receptor tyrosine kinase 3 Homo sapiens 84-88 35193612-1 2022 Novel temperature and pH dual-sensitive amphiphilic micelles were fabricated exploiting the host-guest interaction between benzimidazole-terminated PHEMA-g-(PCL-BM) and beta-CD-star-PMAA-b-PNIPAM. benzimidazole 123-136 ACD shelterin complex subunit and telomerase recruitment factor Homo sapiens 169-176 35033885-0 2022 Discovery of a benzimidazole-based dual FLT3/TrKA inhibitor targeting acute myeloid leukemia. benzimidazole 15-28 neurotrophic receptor tyrosine kinase 1 Homo sapiens 45-49 35033885-4 2022 Guided by ligand-based design and structure simplification of the FLT3 inhibitor, quizartinib, we developed a benzimidazole-based small molecule, 4ACP, that exhibited nanomolar activity against wild-type FLT3, FLT3-Internal tandem duplications (FLT3-ITD), and FLT3-D835Y (FLT3-TKD) mutation (IC50 = 43.8, 97.2, and 92.5 nM respectively). benzimidazole 110-123 fms related receptor tyrosine kinase 3 Homo sapiens 66-70 35033885-4 2022 Guided by ligand-based design and structure simplification of the FLT3 inhibitor, quizartinib, we developed a benzimidazole-based small molecule, 4ACP, that exhibited nanomolar activity against wild-type FLT3, FLT3-Internal tandem duplications (FLT3-ITD), and FLT3-D835Y (FLT3-TKD) mutation (IC50 = 43.8, 97.2, and 92.5 nM respectively). benzimidazole 110-123 fms related receptor tyrosine kinase 3 Homo sapiens 204-208 35033885-4 2022 Guided by ligand-based design and structure simplification of the FLT3 inhibitor, quizartinib, we developed a benzimidazole-based small molecule, 4ACP, that exhibited nanomolar activity against wild-type FLT3, FLT3-Internal tandem duplications (FLT3-ITD), and FLT3-D835Y (FLT3-TKD) mutation (IC50 = 43.8, 97.2, and 92.5 nM respectively). benzimidazole 110-123 fms related receptor tyrosine kinase 3 Homo sapiens 210-214 35033885-4 2022 Guided by ligand-based design and structure simplification of the FLT3 inhibitor, quizartinib, we developed a benzimidazole-based small molecule, 4ACP, that exhibited nanomolar activity against wild-type FLT3, FLT3-Internal tandem duplications (FLT3-ITD), and FLT3-D835Y (FLT3-TKD) mutation (IC50 = 43.8, 97.2, and 92.5 nM respectively). benzimidazole 110-123 fms related receptor tyrosine kinase 3 Homo sapiens 245-249 35033885-4 2022 Guided by ligand-based design and structure simplification of the FLT3 inhibitor, quizartinib, we developed a benzimidazole-based small molecule, 4ACP, that exhibited nanomolar activity against wild-type FLT3, FLT3-Internal tandem duplications (FLT3-ITD), and FLT3-D835Y (FLT3-TKD) mutation (IC50 = 43.8, 97.2, and 92.5 nM respectively). benzimidazole 110-123 fms related receptor tyrosine kinase 3 Homo sapiens 260-264 35033885-4 2022 Guided by ligand-based design and structure simplification of the FLT3 inhibitor, quizartinib, we developed a benzimidazole-based small molecule, 4ACP, that exhibited nanomolar activity against wild-type FLT3, FLT3-Internal tandem duplications (FLT3-ITD), and FLT3-D835Y (FLT3-TKD) mutation (IC50 = 43.8, 97.2, and 92.5 nM respectively). benzimidazole 110-123 fms related receptor tyrosine kinase 3 Homo sapiens 272-276 2592410-7 1989 Since the deletion strains appear to be fully resistant to the drugs, the ben-1 product appears to be the only benzimidazole-sensitive beta-tubulin in C. elegans. benzimidazole 111-124 Tubulin beta chain Caenorhabditis elegans 74-79