PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 33086897-0 2020 Synthesis and biological activity of 2-cyanoacrylamide derivatives tethered to imidazopyridine as TAK1 inhibitors. imidazopyridine 79-94 mitogen-activated protein kinase kinase kinase 7 Homo sapiens 98-102 33738077-3 2021 Detailed subsequently are efforts to identify a structurally differentiated IDO1 inhibitor via the pursuit of a variety of heterocyclic isosteres, leading to the discovery of highly potent, imidazopyridine-containing IDO1 inhibitors. imidazopyridine 190-205 indoleamine 2,3-dioxygenase 1 Homo sapiens 76-80 33738077-3 2021 Detailed subsequently are efforts to identify a structurally differentiated IDO1 inhibitor via the pursuit of a variety of heterocyclic isosteres, leading to the discovery of highly potent, imidazopyridine-containing IDO1 inhibitors. imidazopyridine 190-205 indoleamine 2,3-dioxygenase 1 Homo sapiens 217-221 33391507-3 2021 W2014-S with pharmacophore structure of imidazopyridine, which was firstly reported to be utilized in STAT3 inhibitor discovery, was screened out as a potent STAT3 inhibitor from a library of small molecules. imidazopyridine 40-55 signal transducer and activator of transcription 3 Homo sapiens 102-107 33391507-3 2021 W2014-S with pharmacophore structure of imidazopyridine, which was firstly reported to be utilized in STAT3 inhibitor discovery, was screened out as a potent STAT3 inhibitor from a library of small molecules. imidazopyridine 40-55 signal transducer and activator of transcription 3 Homo sapiens 158-163 34055224-0 2021 Design, Synthesis, and Biological Evaluation of Imidazopyridines as PD-1/PD-L1 Antagonists. imidazopyridine 48-64 programmed cell death 1 Homo sapiens 68-72 34055224-0 2021 Design, Synthesis, and Biological Evaluation of Imidazopyridines as PD-1/PD-L1 Antagonists. imidazopyridine 48-64 CD274 molecule Homo sapiens 73-78 33086897-6 2020 We synthesised imidazopyridine derivatives as novel TAK1 inhibitors, which have 2-cyanoacrylamide moiety that can form reversible covalent bonding. imidazopyridine 15-30 mitogen-activated protein kinase kinase kinase 7 Homo sapiens 52-56 33116593-0 2020 A Novel Imidazopyridine Derivative Exhibits Anticancer Activity in Breast Cancer by Inhibiting Wnt/beta-catenin Signaling. imidazopyridine 8-23 catenin beta 1 Homo sapiens 99-111 33153423-1 2021 The present protocol is a simple and eco-friendly approach for the one-pot procedure by using a sonicator for the synthesis of substituted imidazopyridines ranging from important feedstock"s like styrene promoted by NBS. imidazopyridine 139-155 nibrin Homo sapiens 216-219 28800461-7 2017 The western blot assay indicated that 1i is more effective than HS-173, an imidazopyridine-based PI3Ka inhibitor, in reducing the levels of phospho-Akt. imidazopyridine 75-90 phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha Homo sapiens 97-102 32806205-2 2020 The coordination effect of Lewis acid was the dominant factor controlling the regioselective addition of silyl radical to imidazopyridines, and the corresponding C-5 silylated imidazo[1,2-a]pyridines were obtained in moderate to high yields with a broad substrate scope. imidazopyridine 122-138 complement C5 Homo sapiens 162-165 31422171-5 2019 In this study, we performed the one-step synthesis of water-dispersible ultra-small iron oxide nanoparticles (USPIONs) and combine them with an imidazopyridine based TSPO ligand and a fluorescent dye. imidazopyridine 144-159 translocator protein Homo sapiens 166-170 30261753-0 2018 Novel imidazopyridine suppresses STAT3 activation by targeting SHP-1. imidazopyridine 6-21 signal transducer and activator of transcription 3 Homo sapiens 33-38 30261753-0 2018 Novel imidazopyridine suppresses STAT3 activation by targeting SHP-1. imidazopyridine 6-21 protein tyrosine phosphatase non-receptor type 6 Homo sapiens 63-68 30261753-3 2018 Novel imidazopyridine compounds were synthesized to evaluate the inhibition of STAT3 at Y705. imidazopyridine 6-21 signal transducer and activator of transcription 3 Homo sapiens 79-84 32806205-0 2020 Selective C-5 Oxidative Radical Silylation of Imidazopyridines Promoted by Lewis Acid. imidazopyridine 46-62 complement C5 Homo sapiens 10-13 32781957-4 2020 There are several natural and synthetic FASN inhibitors reported in the literature, a few examples are GSK 2194069 (7.7 nM), imidazopyridine (16 nM), epigallocatechin-3-gallate (42.0 microg/ml) and platensimycin (300 nM) but except for TVB-2640, none of the aforementioned inhibitors have made into clinical trials. imidazopyridine 125-140 fatty acid synthase Homo sapiens 40-44 30422629-5 2018 Herein, we describe imidazopyridines represented by PF-06424439 (1) and 2 as long residence time inhibitors of DGAT2. imidazopyridine 20-36 acyl-CoA wax alcohol acyltransferase 1 Homo sapiens 111-116 30422629-9 2018 A binding assay utilizing 125I-labeled imidazopyridine demonstrated that the level of imidazopyridine binding to DGAT2 mutant enzymes, H161A and H163A, dramatically decreased to 11-17% of that of the wild-type enzyme, indicating that these residues are critical for imidazopyridines to bind to DGAT2. imidazopyridine 39-54 acyl-CoA wax alcohol acyltransferase 1 Homo sapiens 113-118 30422629-9 2018 A binding assay utilizing 125I-labeled imidazopyridine demonstrated that the level of imidazopyridine binding to DGAT2 mutant enzymes, H161A and H163A, dramatically decreased to 11-17% of that of the wild-type enzyme, indicating that these residues are critical for imidazopyridines to bind to DGAT2. imidazopyridine 86-101 acyl-CoA wax alcohol acyltransferase 1 Homo sapiens 113-118 30422629-9 2018 A binding assay utilizing 125I-labeled imidazopyridine demonstrated that the level of imidazopyridine binding to DGAT2 mutant enzymes, H161A and H163A, dramatically decreased to 11-17% of that of the wild-type enzyme, indicating that these residues are critical for imidazopyridines to bind to DGAT2. imidazopyridine 86-101 acyl-CoA wax alcohol acyltransferase 1 Homo sapiens 294-299 30422629-9 2018 A binding assay utilizing 125I-labeled imidazopyridine demonstrated that the level of imidazopyridine binding to DGAT2 mutant enzymes, H161A and H163A, dramatically decreased to 11-17% of that of the wild-type enzyme, indicating that these residues are critical for imidazopyridines to bind to DGAT2. imidazopyridine 266-282 acyl-CoA wax alcohol acyltransferase 1 Homo sapiens 113-118 30422629-10 2018 Taken together, imidazopyridines may thus represent a promising lead series for the development of DGAT2 inhibitors that display an unprecedented combination of potency, selectivity, and in vivo efficacy. imidazopyridine 16-32 acyl-CoA wax alcohol acyltransferase 1 Homo sapiens 99-104 30132331-0 2018 Visible-Light-Promoted C(sp3)-C(sp2) Cross-Dehydrogenative Coupling of Tertiary Amine with Imidazopyridine. imidazopyridine 91-106 Sp2 transcription factor Homo sapiens 30-35 30088508-0 2018 Palladium-catalyzed oxidative C-H/C-H cross-coupling of imidazopyridines with azoles. imidazopyridine 56-72 churchill domain containing 1 Homo sapiens 30-37 30088508-1 2018 An effective palladium-catalyzed oxidative C-H/C-H cross-coupling of imidazopyridines with azoles using air as the oxidant has been developed. imidazopyridine 69-85 churchill domain containing 1 Homo sapiens 43-50 29243330-0 2018 Direct, Metal-free C(sp2 )-H Chalcogenation of Indoles and Imidazopyridines with Dichalcogenides Catalysed by KIO3. imidazopyridine 59-75 Sp2 transcription factor Homo sapiens 19-24 28678513-1 2017 A hitherto unreported aminomethylation occurs at C-3 of imidazopyridines with morpholine in the presence of (diacetoxyiodo)benzene at ambient temperature in short reaction times. imidazopyridine 56-72 complement C3 Homo sapiens 49-52 28728105-0 2017 Discovery of imidazopyridines containing isoindoline-1,3-dione framework as a new class of BACE1 inhibitors: Design, synthesis and SAR analysis. imidazopyridine 13-29 beta-secretase 1 Homo sapiens 91-96 28728105-4 2017 We designed a series of imidazopyridines-based compounds bearing phthalimide moieties as inhibitors of BACE1. imidazopyridine 24-40 beta-secretase 1 Homo sapiens 103-108 28728105-6 2017 Evaluating the BACE1 inhibitory effects of the synthesized compounds revealed that introducing an aminocyclohexyl moiety in the imidazopyridine core resulted in a significant improvement in its BACE1 inhibitory potential. imidazopyridine 128-143 beta-secretase 1 Homo sapiens 15-20 28728105-6 2017 Evaluating the BACE1 inhibitory effects of the synthesized compounds revealed that introducing an aminocyclohexyl moiety in the imidazopyridine core resulted in a significant improvement in its BACE1 inhibitory potential. imidazopyridine 128-143 beta-secretase 1 Homo sapiens 194-199 28728105-8 2017 Molecular docking revealed that the nitrogen atom of imidazopyridines and the oxygen atom of the phenoxypropyl linker were involved in hydrogen bound interactions with Asp228 and Asp32 of BACE1 active site, respectively. imidazopyridine 53-69 beta-secretase 1 Homo sapiens 188-193 28830649-0 2017 Identification of an imidazopyridine scaffold to generate potent and selective TYK2 inhibitors that demonstrate activity in an in vivo psoriasis model. imidazopyridine 21-36 tyrosine kinase 2 Homo sapiens 79-83 28830649-1 2017 Herein we report identification of an imidazopyridine class of potent and selective TYK2 inhibitors, exemplified by prototype 6, through constraint of the rotatable amide bond connecting the pyridine and aryl rings of compound 1. imidazopyridine 38-53 tyrosine kinase 2 Homo sapiens 84-88 28470069-1 2017 3-Cyanomethylated imidazopyridines were synthesized via a visible light-promoted reaction of imidazopyridines with bromoacetonitrile or iodoacetonitrile catalyzed by fac-Ir(ppy)3 under mild conditions. imidazopyridine 18-34 FA complementation group C Homo sapiens 166-169 28650506-2 2017 This communication discloses an oxidative radical dual sp2/sp3 C-H thiolation strategy for the coupling of imidazopyridines with ethers or alkanes using elemental sulphur. imidazopyridine 107-123 Sp2 transcription factor Homo sapiens 55-58 28650506-2 2017 This communication discloses an oxidative radical dual sp2/sp3 C-H thiolation strategy for the coupling of imidazopyridines with ethers or alkanes using elemental sulphur. imidazopyridine 107-123 Sp3 transcription factor Homo sapiens 59-62 27992115-2 2017 This heteroarene peptide bond stacking was supported by a co-crystal structure of an imidazopyridine ligand with hCatL. imidazopyridine 87-102 cathepsin L Homo sapiens 115-120 27607364-6 2016 Moreover, bicyclic ring structures such as imidazopyridine, pyrazolopyrimidine, and phenylpurine will be highlighted as promising scaffolds for TSPO ligands. imidazopyridine 43-58 translocator protein Homo sapiens 144-148 30108796-2 2017 Herein, we report the first toxicological evaluation of imidazopyridine-based DGAT2 inhibitors and show that the arteriopathy associated with imidazopyridine 1 can be mitigated with small structural modifications, and is thus not mechanism related. imidazopyridine 56-71 acyl-CoA wax alcohol acyltransferase 1 Homo sapiens 78-83 28043720-0 2017 Discovery of imidazopyridine derivatives as novel c-Met kinase inhibitors: Synthesis, SAR study, and biological activity. imidazopyridine 13-28 MET proto-oncogene, receptor tyrosine kinase Homo sapiens 50-55 28043720-0 2017 Discovery of imidazopyridine derivatives as novel c-Met kinase inhibitors: Synthesis, SAR study, and biological activity. imidazopyridine 13-28 sarcosine dehydrogenase Homo sapiens 86-89 28043720-2 2017 A series of imidazopyridine derivatives were designed and synthesized according to the established docking studies as possible c-Met inhibitors. imidazopyridine 12-27 MET proto-oncogene, receptor tyrosine kinase Homo sapiens 127-132 28043720-3 2017 Most of these imidazopyridine derivatives displayed nanomolar potency against c-Met in both biochemical enzymatic screens and cellular pharmacology studies. imidazopyridine 14-29 MET proto-oncogene, receptor tyrosine kinase Homo sapiens 78-83 28043720-6 2017 These findings indicated that the novel imidazopyridine derivative compound 7g was a potential c-Met inhibitor deserving further investigation for cancer treatment. imidazopyridine 40-55 MET proto-oncogene, receptor tyrosine kinase Homo sapiens 95-100 27979595-2 2017 Previously reported benzimidazole CYP11B2 inhibitors led the way for bioisosteric imidazopyridines that are both potent and selective over CYP11B1. imidazopyridine 82-98 cytochrome P450 family 11 subfamily B member 2 Homo sapiens 34-41 27979595-2 2017 Previously reported benzimidazole CYP11B2 inhibitors led the way for bioisosteric imidazopyridines that are both potent and selective over CYP11B1. imidazopyridine 82-98 cytochrome P450 family 11 subfamily B member 1 Homo sapiens 139-146 27213958-0 2016 Imidazopyridine and Pyrazolopiperidine Derivatives as Novel Inhibitors of Serine Palmitoyl Transferase. imidazopyridine 0-15 alanine--glyoxylate and serine--pyruvate aminotransferase Rattus norvegicus 74-102 27399688-2 2016 In order to develop highly selective and active ligands with a high affinity for TSPO, imidazopyridine-based TSPO ligand (CB256, 3) was prepared as the precursor. imidazopyridine 87-102 translocator protein Homo sapiens 81-85 27399688-2 2016 In order to develop highly selective and active ligands with a high affinity for TSPO, imidazopyridine-based TSPO ligand (CB256, 3) was prepared as the precursor. imidazopyridine 87-102 translocator protein Homo sapiens 109-113 26856922-0 2016 Synthesis of carbon-11-labeled imidazopyridine- and purine-thioacetamide derivatives as new potential PET tracers for imaging of nucleotide pyrophosphatase/phosphodiesterase 1 (NPP1). imidazopyridine 31-46 ectonucleotide pyrophosphatase/phosphodiesterase 1 Homo sapiens 129-175 27117431-5 2016 The crystal structure illustrates that the pyrazole and imidazopyridine rings of KY-04045 are sufficient for mediating PAK4 hinge loop interaction. imidazopyridine 56-71 p21 (RAC1) activated kinase 4 Homo sapiens 119-123 26856922-0 2016 Synthesis of carbon-11-labeled imidazopyridine- and purine-thioacetamide derivatives as new potential PET tracers for imaging of nucleotide pyrophosphatase/phosphodiesterase 1 (NPP1). imidazopyridine 31-46 ectonucleotide pyrophosphatase/phosphodiesterase 1 Homo sapiens 177-181 25529740-3 2015 Further structural optimization on type II inhibitors by truncation of the imidazonaphthyridinone core and incorporation of an N-phenyl cyclopropane-1,1-dicarboxamide pharmacophore led to the discovery of novel imidazopyridine-based c-Met kinase inhibitors, displaying nanomolar enzyme inhibitory activity and improved Met kinase selectivity. imidazopyridine 211-226 MET proto-oncogene, receptor tyrosine kinase Homo sapiens 233-238 26774655-4 2016 With a hypothesis that a planar conformation between the core and the 6-heteroaryl ring will allow for the accommodation of larger 5"-substituents in a hydrophobic area under P-loop, SAR efforts focused on 5"-alkoxy heteroaryl rings at the 6-position of imidazopyridine and imidazopyridazine cores that have the same dihedral angle of zero degrees. imidazopyridine 254-269 sarcosinemia autosomal recessive Mus musculus 183-186 26490333-3 2016 The radio-iodinated imidazopyridine derivative (123)I-ABC577 was designed as a candidate for a novel amyloid-beta imaging agent. imidazopyridine 20-35 amyloid beta precursor protein Homo sapiens 101-113 26196520-3 2015 Subsequently, we performed in silico mode-of-action analysis and predicted that the synthesized imidazopyridines targets Phospholipase A2 (PLA2). imidazopyridine 96-112 phospholipase A2 group IB Homo sapiens 121-137 26196520-3 2015 Subsequently, we performed in silico mode-of-action analysis and predicted that the synthesized imidazopyridines targets Phospholipase A2 (PLA2). imidazopyridine 96-112 phospholipase A2 group IB Homo sapiens 139-143 26580609-0 2015 An Investigation of Molecular Docking and Molecular Dynamic Simulation on Imidazopyridines as B-Raf Kinase Inhibitors. imidazopyridine 74-90 B-Raf proto-oncogene, serine/threonine kinase Homo sapiens 94-99 26580609-2 2015 Nowadays, a group of imidazopyridines as B-Raf kinase inhibitors have been reported. imidazopyridine 21-37 B-Raf proto-oncogene, serine/threonine kinase Homo sapiens 41-46 26580609-8 2015 These results are expected to understand the binding between B-Raf and imidazopyridines and provide some useful information to design potential B-Raf inhibitors. imidazopyridine 71-87 B-Raf proto-oncogene, serine/threonine kinase Homo sapiens 61-66 26580609-8 2015 These results are expected to understand the binding between B-Raf and imidazopyridines and provide some useful information to design potential B-Raf inhibitors. imidazopyridine 71-87 B-Raf proto-oncogene, serine/threonine kinase Homo sapiens 144-149 26349027-0 2015 Discovery and Optimization of Imidazopyridine-Based Inhibitors of Diacylglycerol Acyltransferase 2 (DGAT2). imidazopyridine 30-45 acyl-CoA wax alcohol acyltransferase 1 Homo sapiens 66-98 26349027-0 2015 Discovery and Optimization of Imidazopyridine-Based Inhibitors of Diacylglycerol Acyltransferase 2 (DGAT2). imidazopyridine 30-45 acyl-CoA wax alcohol acyltransferase 1 Homo sapiens 100-105 26349027-1 2015 The medicinal chemistry and preclinical biology of imidazopyridine-based inhibitors of diacylglycerol acyltransferase 2 (DGAT2) is described. imidazopyridine 51-66 acyl-CoA wax alcohol acyltransferase 1 Homo sapiens 87-119 26349027-1 2015 The medicinal chemistry and preclinical biology of imidazopyridine-based inhibitors of diacylglycerol acyltransferase 2 (DGAT2) is described. imidazopyridine 51-66 acyl-CoA wax alcohol acyltransferase 1 Homo sapiens 121-126 26121643-5 2015 Imidazopyridines have recently been shown to possess Akt kinase inhibitory activity; thus in this study, we investigated the inhibitory effect of novel imidazopyridine derivatives HIMP, M-MeI, OMP, and EtOP on different human castration-resistant PCa cells. imidazopyridine 0-16 AKT serine/threonine kinase 1 Homo sapiens 53-56 26070068-2 2015 In the present study, we characterized some imidazopyridine compounds as GPR4 modulators that modify GPR4 receptor function. imidazopyridine 44-59 G protein-coupled receptor 4 Homo sapiens 73-77 26070068-2 2015 In the present study, we characterized some imidazopyridine compounds as GPR4 modulators that modify GPR4 receptor function. imidazopyridine 44-59 G protein-coupled receptor 4 Homo sapiens 101-105 26070068-4 2015 Imidazopyridine compounds inhibited the moderately acidic pH-induced SRE activity only in GPR4-expressing cells. imidazopyridine 0-15 G protein-coupled receptor 4 Homo sapiens 90-94 26070068-6 2015 We further compared the inhibition property of the imidazopyridine compound with psychosine, which has been shown to selectively inhibit actions induced by proton-sensing GPCRs, including GPR4. imidazopyridine 51-66 G protein-coupled receptor 4 Homo sapiens 188-192 26070068-8 2015 On the other hand, the imidazopyridine compound almost completely inhibited acidic pH-induced action in mutant GPR4. imidazopyridine 23-38 G protein-coupled receptor 4 Homo sapiens 111-115 26070068-9 2015 We conclude that some imidazopyridine compounds show specificity to GPR4 as negative allosteric modulators with a different action mode from psychosine, an antagonist susceptible to histidine residues, and are useful for characterizing GPR4-mediated acidic pH-induced biological actions. imidazopyridine 22-37 G protein-coupled receptor 4 Homo sapiens 68-72 26070068-9 2015 We conclude that some imidazopyridine compounds show specificity to GPR4 as negative allosteric modulators with a different action mode from psychosine, an antagonist susceptible to histidine residues, and are useful for characterizing GPR4-mediated acidic pH-induced biological actions. imidazopyridine 22-37 G protein-coupled receptor 4 Homo sapiens 236-240 25616581-1 2015 OBJECTIVE: We report synthesis of two carbon-11 labeled imidazopyridines TSPO ligands, [(11)C]CB184 and [(11)C]CB190, for PET imaging of inflammatory process along with neurodegeneration, ischemia or brain tumor. imidazopyridine 56-72 translocator protein Rattus norvegicus 73-77 25765758-0 2015 Computer aided drug discovery of highly ligand efficient, low molecular weight imidazopyridine analogs as FLT3 inhibitors. imidazopyridine 79-94 fms related receptor tyrosine kinase 3 Homo sapiens 106-110 25577039-4 2015 The SAR knowledge gleaned in the optimization of scaffolds containing benzoxazoles was parlayed toward the identification of potent NS5A inhibitors containing other heteroaromatic replacements such as indoles and imidazopyridines. imidazopyridine 213-229 sarcosine dehydrogenase Homo sapiens 4-7 25431995-4 2015 Recently, we have designed and synthesized a series of novel imidazopyridine and imidazopyrazine derivatives that inhibit Mnk1/2 kinases with a potency in the nanomolar to micromolar range. imidazopyridine 61-76 MAPK interacting serine/threonine kinase 1 Homo sapiens 122-128 24479199-0 2010 ML368 Identification of Imidazopyridines as Selective Inhibitors of the Cytochrome P450 Enzyme CYP3A4 Here we report the first highly selective CYP3A4 inhibitor optimized from an initial lead with 30-fold selectivity over CYP3A5 to yield a series of compounds with greater than 1000-fold selectivity. imidazopyridine 24-40 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 95-100 25069996-5 2014 The results of the present investigation are essential for the design of new imidazopyridine bifunctional chelate ligands targeted to TSPO. imidazopyridine 77-92 translocator protein Homo sapiens 134-138 25205195-1 2014 We report the design, synthesis, and biological evaluation of imidazopyridine-based peptidomimetics based on the substrate consensus sequence of Akt, an AGC family serine/threonine kinase hyperactivated in over 50% of human tumors. imidazopyridine 62-77 AKT serine/threonine kinase 1 Homo sapiens 145-148 24909730-0 2014 QSAR models for thiophene and imidazopyridine derivatives inhibitors of the Polo-Like Kinase 1. imidazopyridine 30-45 polo like kinase 1 Homo sapiens 76-94 25231248-1 2015 PURPOSE: The in vivo binding parameters of the novel imidazopyridine TSPO ligand [(18)F]PBR102 were assessed and compared with those of [(18)F]PBR111 in a rodent model of neuroinflammation. imidazopyridine 53-68 translocator protein Rattus norvegicus 69-73 24909730-1 2014 The inhibitory activity of 103 thiophene and 33 imidazopyridine derivatives against Polo-Like Kinase 1 (PLK1) expressed as pIC50 (-logIC50) was predicted by QSAR modeling. imidazopyridine 48-63 polo like kinase 1 Homo sapiens 84-102 24909730-1 2014 The inhibitory activity of 103 thiophene and 33 imidazopyridine derivatives against Polo-Like Kinase 1 (PLK1) expressed as pIC50 (-logIC50) was predicted by QSAR modeling. imidazopyridine 48-63 polo like kinase 1 Homo sapiens 104-108 24479199-0 2010 ML368 Identification of Imidazopyridines as Selective Inhibitors of the Cytochrome P450 Enzyme CYP3A4 Here we report the first highly selective CYP3A4 inhibitor optimized from an initial lead with 30-fold selectivity over CYP3A5 to yield a series of compounds with greater than 1000-fold selectivity. imidazopyridine 24-40 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 95-101 24479199-0 2010 ML368 Identification of Imidazopyridines as Selective Inhibitors of the Cytochrome P450 Enzyme CYP3A4 Here we report the first highly selective CYP3A4 inhibitor optimized from an initial lead with 30-fold selectivity over CYP3A5 to yield a series of compounds with greater than 1000-fold selectivity. imidazopyridine 24-40 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 223-229 24479199-1 2010 During our medicinal chemistry and biology effort pursued under our existing LRH1 inverse agonist Extended Characterization (EC) project, we identified several compounds belonging to the imidazopyridine scaffold with activity against the cytochrome enzymes. imidazopyridine 187-202 purinergic receptor P2X 5 Homo sapiens 77-81 24685494-0 2014 Synthesis of [11C]PBR170, a novel imidazopyridine, for imaging the translocator protein with PET. imidazopyridine 34-49 translocator protein Homo sapiens 67-87 24931274-0 2014 Synthesis and biological evaluation of novel radioiodinated imidazopyridine derivatives for amyloid-beta imaging in Alzheimer"s disease. imidazopyridine 60-75 amyloid beta precursor protein Homo sapiens 92-104 24922544-0 2014 Discovery and characterization of novel imidazopyridine derivative CHEQ-2 as a potent CDC25 inhibitor and promising anticancer drug candidate. imidazopyridine 40-55 cell division cycle 25C Homo sapiens 86-91 24922544-4 2014 In this article, refinement of the initial hit XDW-1 by synthesis and screening of a focused compound library led to the identification of a novel set of imidazopyridine derivatives as potent CDC25 inhibitors. imidazopyridine 154-169 cell division cycle 25C Homo sapiens 192-197 23085493-0 2013 A novel imidazopyridine derivative, HS-106, induces apoptosis of breast cancer cells and represses angiogenesis by targeting the PI3K/mTOR pathway. imidazopyridine 8-23 mechanistic target of rapamycin kinase Homo sapiens 134-138 24102269-5 2013 We herein report the design and synthesis of new imidazopyridine based potent dual inhibitors of HIF-1alpha and STAT3 pathways. imidazopyridine 49-64 hypoxia inducible factor 1 subunit alpha Homo sapiens 97-107 24102269-5 2013 We herein report the design and synthesis of new imidazopyridine based potent dual inhibitors of HIF-1alpha and STAT3 pathways. imidazopyridine 49-64 signal transducer and activator of transcription 3 Homo sapiens 112-117 24021463-3 2013 This molecule also exhibited reduced rat retinal exposures relative to a previously studied imidazo-pyridine-containing NAMPT inhibitor. imidazopyridine 92-108 nicotinamide phosphoribosyltransferase Rattus norvegicus 120-125 24021463-5 2013 The compound also exhibited only minimal effects on in vivo NAD levels in mice, and these changes were considerably less profound than those produced by an imidazo-pyridine-containing NAMPT inhibitor. imidazopyridine 156-172 nicotinamide phosphoribosyltransferase Mus musculus 184-189 23752769-1 2013 A stable Re complex containing an imidazopyridine ligand with a high affinity for TSPO has been synthesized as a model for new (99m)Tc or (188/186)Re-based radiopharmaceuticals to be used in SPECT diagnosis or in therapy, respectively. imidazopyridine 34-49 translocator protein Homo sapiens 82-86 24282133-0 2014 Combining on-chip synthesis of a focused combinatorial library with computational target prediction reveals imidazopyridine GPCR ligands. imidazopyridine 108-123 G protein-coupled receptor 166 pseudogene Homo sapiens 124-128 22929971-1 2013 We synthesized a novel imidazopyridine analogue, a PI3Kalpha inhibitor HS-173 and investigated anti-cancer capacity in human cancer cells. imidazopyridine 23-38 phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha Homo sapiens 51-60 24900571-1 2013 Potent imidazopyridine-based inhibitors of fatty acid synthase (FASN) are described. imidazopyridine 7-22 fatty acid synthase Rattus norvegicus 43-62 24900571-1 2013 Potent imidazopyridine-based inhibitors of fatty acid synthase (FASN) are described. imidazopyridine 7-22 fatty acid synthase Rattus norvegicus 64-68 22264486-0 2012 Imidazopyridines as selective CYP3A4 inhibitors. imidazopyridine 0-16 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 30-36 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. imidazopyridine 54-69 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. imidazopyridine 54-69 mechanistic target of rapamycin kinase Homo sapiens 159-163 24900520-0 2012 Substituted benzimidazole and imidazopyridine compounds useful as cyp17 modulators: patent highlight. imidazopyridine 30-45 cytochrome P450 family 17 subfamily A member 1 Homo sapiens 66-71 22672803-0 2012 Design, synthesis and biological evaluation of novel imidazopyridines as potential antidiabetic GSK3beta inhibitors. imidazopyridine 53-69 glycogen synthase kinase 3 beta Mus musculus 96-104 22672803-1 2012 Design, synthesis and biological evaluation of the imidazopyridine analogs as novel GSK3beta inhibitors for treatment of type 2 diabetes mellitus are described. imidazopyridine 51-66 glycogen synthase kinase 3 beta Mus musculus 84-92 22672803-3 2012 The structure-activity relationship (SAR) of the imidazopyridine analogs and the binding mode of analog 23 in the catalytic domain of GSK3beta, based on our X-ray crystallography study, are described. imidazopyridine 49-64 glycogen synthase kinase 3 beta Mus musculus 134-142 22155744-1 2012 Potentiation of anti-breast cancer activity of an imidazopyridine-based PI3Kalpha inhibitor, HS-104, was investigated in human breast cancer cells. imidazopyridine 50-65 phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha Homo sapiens 72-81 21420860-0 2011 Imidazopyridine CB2 agonists: optimization of CB2/CB1 selectivity and implications for in vivo analgesic efficacy. imidazopyridine 0-15 cannabinoid receptor 2 Rattus norvegicus 16-19 21420860-0 2011 Imidazopyridine CB2 agonists: optimization of CB2/CB1 selectivity and implications for in vivo analgesic efficacy. imidazopyridine 0-15 cannabinoid receptor 2 Rattus norvegicus 46-49 21420860-0 2011 Imidazopyridine CB2 agonists: optimization of CB2/CB1 selectivity and implications for in vivo analgesic efficacy. imidazopyridine 0-15 cannabinoid receptor 1 Rattus norvegicus 50-53 19539471-1 2009 A new series of DPP-4 inhibitors derived from piperidine-fused benzimidazoles and imidazopyridines is described. imidazopyridine 82-98 dipeptidyl peptidase 4 Homo sapiens 16-21 20660795-9 2010 In a small-scale screen, a series of imidazopyridine compounds was tested to identify the small molecules that modulate eIF5A-mediated phagocytic activity. imidazopyridine 37-52 eukaryotic translation initiation factor 5A Mus musculus 120-125 19589677-0 2009 Imidazopyridine derivatives as potent and selective Polo-like kinase (PLK) inhibitors. imidazopyridine 0-15 polo-like kinase 1 Rattus norvegicus 52-68 19589677-0 2009 Imidazopyridine derivatives as potent and selective Polo-like kinase (PLK) inhibitors. imidazopyridine 0-15 polo-like kinase 1 Rattus norvegicus 70-73 19589677-1 2009 A novel class of imidazopyridine derivatives was designed as PLK1 inhibitors. imidazopyridine 17-32 polo-like kinase 1 Rattus norvegicus 61-65 19952121-1 2009 CUDC-305 is a heat shock protein 90 (HSP90) inhibitor of the novel imidazopyridine class. imidazopyridine 67-82 heat shock protein 90 alpha family class A member 1 Homo sapiens 14-35 19952121-1 2009 CUDC-305 is a heat shock protein 90 (HSP90) inhibitor of the novel imidazopyridine class. imidazopyridine 67-82 heat shock protein 90 alpha family class A member 1 Homo sapiens 37-42 19539471-2 2009 Optimization of this class of DPP-4 inhibitors led to the discovery of imidazopyridine 34. imidazopyridine 71-86 dipeptidyl peptidase 4 Homo sapiens 30-35 18282708-0 2008 Potent, selective, orally bioavailable inhibitors of tumor necrosis factor-alpha converting enzyme (TACE): discovery of indole, benzofuran, imidazopyridine and pyrazolopyridine P1" substituents. imidazopyridine 140-155 ADAM metallopeptidase domain 17 Homo sapiens 53-98 19509149-1 2009 PURPOSE: We designed and synthesized CUDC-305, an HSP90 inhibitor of the novel imidazopyridine class. imidazopyridine 79-94 heat shock protein 90 alpha family class A member 1 Homo sapiens 50-55 18178668-1 2008 Imidazopyridine derivates were recently shown to be a novel class of selective and arginine-competitive inhibitors of inducible nitric-oxide synthase (iNOS), and 2-[2-(4-methoxypyridin-2-yl)-ethyl]-3H-imidazo[4,5-b]pyridine (BYK191023) was found to have very high selectivity in enzymatic and cellular models ( Mol Pharmacol 69: 328-337, 2006 ). imidazopyridine 0-15 nitric oxide synthase 2 Homo sapiens 118-149 18178668-1 2008 Imidazopyridine derivates were recently shown to be a novel class of selective and arginine-competitive inhibitors of inducible nitric-oxide synthase (iNOS), and 2-[2-(4-methoxypyridin-2-yl)-ethyl]-3H-imidazo[4,5-b]pyridine (BYK191023) was found to have very high selectivity in enzymatic and cellular models ( Mol Pharmacol 69: 328-337, 2006 ). imidazopyridine 0-15 nitric oxide synthase 2 Homo sapiens 151-155 18809672-0 2008 Imidazoquinolinone, imidazopyridine, and isoquinolindione derivatives as novel and potent inhibitors of the poly(ADP-ribose) polymerase (PARP): a comparison with standard PARP inhibitors. imidazopyridine 20-35 poly(ADP-ribose) polymerase 1 Homo sapiens 108-135 18809672-0 2008 Imidazoquinolinone, imidazopyridine, and isoquinolindione derivatives as novel and potent inhibitors of the poly(ADP-ribose) polymerase (PARP): a comparison with standard PARP inhibitors. imidazopyridine 20-35 poly(ADP-ribose) polymerase 1 Homo sapiens 137-141 19133222-4 2008 Its imidazopyridine structure interacts with CCR5 and induces a co-receptor conformation that prevents glycoproteins binding to the viral envelope. imidazopyridine 4-19 C-C motif chemokine receptor 5 Homo sapiens 45-49 18282708-0 2008 Potent, selective, orally bioavailable inhibitors of tumor necrosis factor-alpha converting enzyme (TACE): discovery of indole, benzofuran, imidazopyridine and pyrazolopyridine P1" substituents. imidazopyridine 140-155 ADAM metallopeptidase domain 17 Homo sapiens 100-104 18243692-0 2008 Imidazopyridines: a novel class of hNav1.7 channel blockers. imidazopyridine 0-16 neuron navigator 1 Homo sapiens 35-40 17722875-3 2007 For the mentioned purpose, imidazopyridine and imidazopyrimidine compounds 5-20 were synthesized, and their affinity for PBR was determined. imidazopyridine 27-42 translocator protein Homo sapiens 121-124 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. imidazopyridine 75-90 ATPase H+/K+ transporting subunit alpha Homo sapiens 40-51 16368897-0 2006 In vivo characterization of the novel imidazopyridine BYK191023 [2-[2-(4-methoxy-pyridin-2-yl)-ethyl]-3H-imidazo[4,5-b]pyridine], a potent and highly selective inhibitor of inducible nitric-oxide synthase. imidazopyridine 38-53 nitric oxide synthase 2 Rattus norvegicus 173-204 10508441-3 1999 Substitution on the imidazopyridine nucleus at position 8 with lipophilic substituents and the presence of one chlorine atom at the para position of the phenyl ring at C(2) are crucial features for high binding affinity and selectivity toward PBR. imidazopyridine 20-35 translocator protein Homo sapiens 243-246 9433391-1 1997 BACKGROUND: Zolpidem is a short-acting imidazopyridine hypnotic drug that is metabolized mainly by CYP3A4. imidazopyridine 39-54 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 99-105 8863805-1 1996 Alpidem (1), the anxiolytic imidazopyridine, has nanomolar binding affinity for both the central benzodiazepine receptor (CBR) and the peripheral benzodiazepine receptor (PBR). imidazopyridine 28-43 cannabinoid receptor 1 Homo sapiens 89-120 8863805-1 1996 Alpidem (1), the anxiolytic imidazopyridine, has nanomolar binding affinity for both the central benzodiazepine receptor (CBR) and the peripheral benzodiazepine receptor (PBR). imidazopyridine 28-43 cannabinoid receptor 1 Homo sapiens 122-125 8863805-1 1996 Alpidem (1), the anxiolytic imidazopyridine, has nanomolar binding affinity for both the central benzodiazepine receptor (CBR) and the peripheral benzodiazepine receptor (PBR). imidazopyridine 28-43 translocator protein Homo sapiens 135-169 8863805-1 1996 Alpidem (1), the anxiolytic imidazopyridine, has nanomolar binding affinity for both the central benzodiazepine receptor (CBR) and the peripheral benzodiazepine receptor (PBR). imidazopyridine 28-43 translocator protein Homo sapiens 171-174 33971490-4 2021 Series of imidazopyrazines, imidazopyridazines and imidazopyridines derivatives were synthesized and evaluated as MNK1/2 inhibitors. imidazopyridine 51-67 MAPK interacting serine/threonine kinase 1 Homo sapiens 114-120 15012992-2 2004 A variety of imidazopyridines were synthesized and potent inhibitors of KDR kinase activity were identified with good aqueous solubility. imidazopyridine 13-29 kinase insert domain receptor Homo sapiens 72-75 12688761-2 2003 Several synthetic approaches that describe the introduction of a C-3 pyrimidine substituent on the imidazopyridine core via construction of the pyrimidine or Stille coupling are outlined. imidazopyridine 99-114 complement C3 Homo sapiens 65-68 12643929-0 2003 Synthesis of imidazopyridines and purines as potent inhibitors of leukotriene A4 hydrolase. imidazopyridine 13-29 leukotriene A4 hydrolase Mus musculus 66-90 9626922-1 1998 OBJECTIVE: Zolpidem is a short-acting imidazopyridine hypnotic which is biotransformed in humans mainly by CYP3A4. imidazopyridine 38-53 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 107-113 8388468-0 1993 Cyclic nucleotide phosphodiesterase inhibition by imidazopyridines: analogues of sulmazole and isomazole as inhibitors of the cGMP specific phosphodiesterase. imidazopyridine 50-66 phosphodiesterase 3B Homo sapiens 0-35 34545902-2 2021 Under the irradiation of a blue LED, a series of C3-perfluoroalkyl-substituted imidazopyridines were synthesized from the corresponding imidazopyridines and perfluoroalkyl iodides in moderate to good yields at room temperature. imidazopyridine 136-152 small integral membrane protein 10 like 2A Homo sapiens 32-35 35424560-0 2022 A multi pathway coupled domino strategy: I2/TBHP-promoted synthesis of imidazopyridines and thiazoles via sp3, sp2 and sp C-H functionalization. imidazopyridine 71-87 Sp3 transcription factor Homo sapiens 106-109 35424560-0 2022 A multi pathway coupled domino strategy: I2/TBHP-promoted synthesis of imidazopyridines and thiazoles via sp3, sp2 and sp C-H functionalization. imidazopyridine 71-87 Sp2 transcription factor Homo sapiens 111-114