PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 9526554-1 1998 A family of sequence-related 2"-aminopyrimidine, 2"-hydroxylpurine aptamers, developed by oligonucleotide-based combinatorial chemistry, SELEX (systematic evolution of ligand by exponential enrichment) technology, binds human nonpancreatic secretory phospholipase A2 (hnps-PLA2) with nanomolar affinities and inhibits enzymatic activity. 2-aminopyrimidine 29-47 phospholipase A2 group IIA Homo sapiens 226-266 11512149-2 2001 Glivec is an aminopyrimidine derivative that interacts with the ATP-binding site within the kinase domain of ABL and several other tyrosine kinases, including c-KIT, PDGF beta receptor, and ARG. 2-aminopyrimidine 13-28 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 109-112 11512149-2 2001 Glivec is an aminopyrimidine derivative that interacts with the ATP-binding site within the kinase domain of ABL and several other tyrosine kinases, including c-KIT, PDGF beta receptor, and ARG. 2-aminopyrimidine 13-28 KIT proto-oncogene, receptor tyrosine kinase Homo sapiens 159-164 11512149-2 2001 Glivec is an aminopyrimidine derivative that interacts with the ATP-binding site within the kinase domain of ABL and several other tyrosine kinases, including c-KIT, PDGF beta receptor, and ARG. 2-aminopyrimidine 13-28 platelet derived growth factor subunit B Homo sapiens 166-175 11604388-7 2001 An aminopyrimidine, PNU 112455A, was identified in a screen for inhibitors of cdk2. 2-aminopyrimidine 3-18 cyclin dependent kinase 2 Homo sapiens 78-82 9526554-1 1998 A family of sequence-related 2"-aminopyrimidine, 2"-hydroxylpurine aptamers, developed by oligonucleotide-based combinatorial chemistry, SELEX (systematic evolution of ligand by exponential enrichment) technology, binds human nonpancreatic secretory phospholipase A2 (hnps-PLA2) with nanomolar affinities and inhibits enzymatic activity. 2-aminopyrimidine 29-47 phospholipase A2 group IIA Homo sapiens 273-277 9513604-2 1998 The structural contributions to D2/D3 and 5-HT1A receptor binding of the aminopyrimidine, cycloalkyl, and phenylpiperazine portions of the molecule were examined. 2-aminopyrimidine 73-88 immunoglobulin heavy diversity 2-15 Homo sapiens 32-48 35219044-8 2022 Our findings suggested that a 2-aminopyrimidine-based LSD1 inhibitor deserves further investigation as a treatment for LSD1-overexpressing cancer. 2-aminopyrimidine 30-47 lysine demethylase 1A Homo sapiens 54-58 34819010-4 2022 Based on our previous studies, we assumed that a hybrid of aminopyrimidine derivatives as EGFR inhibitors and benzocheromen derivatives as cytotoxic agents can induce apoptosis in EGFR positive cancer cells. 2-aminopyrimidine 59-74 epidermal growth factor receptor Homo sapiens 90-94 34819010-4 2022 Based on our previous studies, we assumed that a hybrid of aminopyrimidine derivatives as EGFR inhibitors and benzocheromen derivatives as cytotoxic agents can induce apoptosis in EGFR positive cancer cells. 2-aminopyrimidine 59-74 epidermal growth factor receptor Homo sapiens 180-184 35219044-0 2022 Design, synthesis and biological evaluation of 2-aminopyrimidine-based LSD1 inhibitors. 2-aminopyrimidine 47-64 lysine demethylase 1A Homo sapiens 71-75 35219044-3 2022 Then, a series of 2-aminopyrimidine derivatives were designed and synthesized as LSD1 inhibitors, and their structure-activity relationships were studied. 2-aminopyrimidine 18-35 lysine demethylase 1A Homo sapiens 81-85 34534838-0 2021 Design, synthesis and biological evaluation of aminopyrimidine derivatives bearing a 4,5,6,7-tetrahydrothieno (3,2-c)pyridine as potent EGFR inhibitors. 2-aminopyrimidine 47-62 epidermal growth factor receptor Homo sapiens 136-140 34534838-1 2021 To resolve the problem of drug resistance caused by epidermal growth factor receptor (EGFR) mutations in non-small cell lung cancer, we used the principle of collocation to design and synthesize a series of aminopyrimidine derivatives with 4,5,6,7-tetrahydrothieno (3,2-c)pyridine side chains (according to the binding mode of AZD9291 to EGFRT790M) for use as EGFRL858R/T790M kinase inhibitors. 2-aminopyrimidine 207-222 epidermal growth factor receptor Homo sapiens 52-84 34534838-1 2021 To resolve the problem of drug resistance caused by epidermal growth factor receptor (EGFR) mutations in non-small cell lung cancer, we used the principle of collocation to design and synthesize a series of aminopyrimidine derivatives with 4,5,6,7-tetrahydrothieno (3,2-c)pyridine side chains (according to the binding mode of AZD9291 to EGFRT790M) for use as EGFRL858R/T790M kinase inhibitors. 2-aminopyrimidine 207-222 epidermal growth factor receptor Homo sapiens 86-90 35138851-0 2022 Identification of 2-Aminopyrimidine Derivatives as FLT3 Kinase Inhibitors with High Selectivity over c-KIT. 2-aminopyrimidine 18-35 FMS-like tyrosine kinase 3 Mus musculus 51-55 35138851-0 2022 Identification of 2-Aminopyrimidine Derivatives as FLT3 Kinase Inhibitors with High Selectivity over c-KIT. 2-aminopyrimidine 18-35 KIT proto-oncogene receptor tyrosine kinase Mus musculus 101-106 33689071-4 2021 We tested the potential to inhibit the transcription of individual Oct-1 isoforms using the GSK3 kinase inhibitor CHIR, an aminopyrimidine derivative. 2-aminopyrimidine 123-138 POU class 2 homeobox 1 S homeolog Xenopus laevis 67-72 33217405-2 2021 In a recent paper, we showed the difference between the first stage of the one-substrate and the two-substrate transketolase reactions - the possibility of transfer of glycolaldehyde formed as a result of cleavage of the donor substrate from the thiazole ring of thiamine diphosphate to its aminopyrimidine ring through the tricycle formation stage, which is necessary for binding and splitting the second molecule of donor substrate [O.N. 2-aminopyrimidine 291-306 transketolase Homo sapiens 111-124 33859803-0 2021 Investigation of Covalent Warheads in the Design of 2-Aminopyrimidine-based FGFR4 Inhibitors. 2-aminopyrimidine 52-69 fibroblast growth factor receptor 4 Homo sapiens 76-81 33859803-2 2021 Herein we report a series of selective 2-aminopyrimidine-based fibroblast growth factor receptor 4 (FGFR4) inhibitors exploring different types of cysteine-targeting warheads. 2-aminopyrimidine 39-56 fibroblast growth factor receptor 4 Homo sapiens 63-98 33859803-2 2021 Herein we report a series of selective 2-aminopyrimidine-based fibroblast growth factor receptor 4 (FGFR4) inhibitors exploring different types of cysteine-targeting warheads. 2-aminopyrimidine 39-56 fibroblast growth factor receptor 4 Homo sapiens 100-105 33946516-4 2021 The current study shows that an aminopyrimidine derivative compound (CHIR99021) induces the inhibition of GSK-3beta in cultured late EPCs. 2-aminopyrimidine 32-47 glycogen synthase kinase 3 alpha Homo sapiens 106-115 33404239-3 2021 Herein, we report the discovery of a potent and novel OGA inhibitor, compound 5i, comprising an aminopyrimidine scaffold, identified by virtual screening based on multiple methodologies combining structure-based and ligand-based approaches, followed by sequential optimization with a focus on ligand lipophilicity efficiency. 2-aminopyrimidine 96-111 O-GlcNAcase Homo sapiens 54-57 33217405-6 2021 Therefore, a significant decrease in the reaction rate of the one-substrate transketolase reaction compared to the two-substrate reaction is due to the stage of transferring the first glycolaldehyde molecule from the thiazole ring to the aminopyrimidine ring of thiamine diphosphate. 2-aminopyrimidine 238-253 transketolase Homo sapiens 76-89 32574211-4 2020 We discovered an aminopyrimidine small molecule, 2062, that had no direct antimycobacterial activity, but synergized with rifampin to reduce bacterial burden in Mtb infected macrophages and mice and also dampened lung immunopathology. 2-aminopyrimidine 17-32 non-SMC condensin II complex, subunit G2 Mus musculus 161-164 32884210-0 2020 Molecular docking of C-Jun-N-Terminal Kinase (Jnk) with amino-pyrimidine derivatives. 2-aminopyrimidine 56-72 mitogen-activated protein kinase 8 Homo sapiens 21-44 32884210-0 2020 Molecular docking of C-Jun-N-Terminal Kinase (Jnk) with amino-pyrimidine derivatives. 2-aminopyrimidine 56-72 mitogen-activated protein kinase 8 Homo sapiens 46-49 32884210-1 2020 It is of interest to document the molecular docking of C-Jun-N-Terminal Kinase (Jnk) (known structure with PDB ID: 1PMN) with amino-pyrimidine derivatives in the context of Alzheimer"s Disease (AD). 2-aminopyrimidine 126-142 mitogen-activated protein kinase 8 Homo sapiens 55-78 32884210-1 2020 It is of interest to document the molecular docking of C-Jun-N-Terminal Kinase (Jnk) (known structure with PDB ID: 1PMN) with amino-pyrimidine derivatives in the context of Alzheimer"s Disease (AD). 2-aminopyrimidine 126-142 mitogen-activated protein kinase 8 Homo sapiens 80-83 32884210-2 2020 We report the optimal binding features (binding energy, interacting residues, inter atomic hydrogen bonding patterns) of 11 amino-pyrimidine derivatives with Jnk for further consideration. 2-aminopyrimidine 124-140 mitogen-activated protein kinase 8 Homo sapiens 158-161 32877741-1 2020 Hybridisation of amino-pyrimidine based SYK inhibitors (e.g. 1a) with previously reported diamine-based SYK inhibitors (e.g. TAK-659) led to the identification and optimisation of a novel pyrimidine-based series of potent and selective SYK inhibitors, where the original aminomethylene group was replaced by a 3,4-diaminotetrahydropyran group. 2-aminopyrimidine 17-33 spleen associated tyrosine kinase Homo sapiens 40-43 33142418-0 2020 Discovery and rational design of 2-aminopyrimidine-based derivatives targeting Janus kinase 2 (JAK2) and FMS-like tyrosine kinase 3 (FLT3). 2-aminopyrimidine 33-50 Janus kinase 2 Homo sapiens 79-93 33142418-0 2020 Discovery and rational design of 2-aminopyrimidine-based derivatives targeting Janus kinase 2 (JAK2) and FMS-like tyrosine kinase 3 (FLT3). 2-aminopyrimidine 33-50 Janus kinase 2 Homo sapiens 95-99 33142418-0 2020 Discovery and rational design of 2-aminopyrimidine-based derivatives targeting Janus kinase 2 (JAK2) and FMS-like tyrosine kinase 3 (FLT3). 2-aminopyrimidine 33-50 fms related receptor tyrosine kinase 3 Homo sapiens 105-131 33142418-0 2020 Discovery and rational design of 2-aminopyrimidine-based derivatives targeting Janus kinase 2 (JAK2) and FMS-like tyrosine kinase 3 (FLT3). 2-aminopyrimidine 33-50 fms related receptor tyrosine kinase 3 Homo sapiens 133-137 33142418-1 2020 Herein, with the help of computer-aided drug design (CADD), we describe the structure-based rational drug design, structure-activity relationships, and synthesis of a series of 2-aminopyrimidine derivatives that inhibit both JAK2 and FLT3 kinases. 2-aminopyrimidine 177-194 Janus kinase 2 Homo sapiens 225-229 33142418-1 2020 Herein, with the help of computer-aided drug design (CADD), we describe the structure-based rational drug design, structure-activity relationships, and synthesis of a series of 2-aminopyrimidine derivatives that inhibit both JAK2 and FLT3 kinases. 2-aminopyrimidine 177-194 fms related receptor tyrosine kinase 3 Homo sapiens 234-238 32891858-0 2020 Design and synthesis of novel desfluoroquinolone-aminopyrimidine hybrids as potent anti-MRSA agents with low hERG activity. 2-aminopyrimidine 49-64 solute carrier family 9 member A6 Homo sapiens 88-92 32891858-0 2020 Design and synthesis of novel desfluoroquinolone-aminopyrimidine hybrids as potent anti-MRSA agents with low hERG activity. 2-aminopyrimidine 49-64 ETS transcription factor ERG Homo sapiens 109-113 31303989-0 2019 Aminopyrimidine-galactose hybrids are highly selective galectin-3 inhibitors. 2-aminopyrimidine 0-15 galectin 3 Homo sapiens 55-65 31926936-1 2020 BX795, a small molecule with an aminopyrimidine backbone, is a potent ATP-competitive inhibitor of phosphoinositide-dependent kinase 1 (PDK1) and TANK-binding kinase 1 (TBK1). 2-aminopyrimidine 32-47 pyruvate dehydrogenase kinase, isoenzyme 1 Mus musculus 99-134 31926936-1 2020 BX795, a small molecule with an aminopyrimidine backbone, is a potent ATP-competitive inhibitor of phosphoinositide-dependent kinase 1 (PDK1) and TANK-binding kinase 1 (TBK1). 2-aminopyrimidine 32-47 pyruvate dehydrogenase kinase, isoenzyme 1 Mus musculus 136-140 31926936-1 2020 BX795, a small molecule with an aminopyrimidine backbone, is a potent ATP-competitive inhibitor of phosphoinositide-dependent kinase 1 (PDK1) and TANK-binding kinase 1 (TBK1). 2-aminopyrimidine 32-47 TANK-binding kinase 1 Mus musculus 146-167 31926936-1 2020 BX795, a small molecule with an aminopyrimidine backbone, is a potent ATP-competitive inhibitor of phosphoinositide-dependent kinase 1 (PDK1) and TANK-binding kinase 1 (TBK1). 2-aminopyrimidine 32-47 TANK-binding kinase 1 Mus musculus 169-173 31806538-0 2020 Structural optimization of aminopyrimidine-based CXCR4 antagonists. 2-aminopyrimidine 27-42 C-X-C motif chemokine receptor 4 Homo sapiens 49-54 31806538-1 2020 Structural optimization of aminopyrimidine-based CXCR4 antagonists is reported. 2-aminopyrimidine 27-42 C-X-C motif chemokine receptor 4 Homo sapiens 49-54 31303989-4 2019 Here, we report aminopyrimidine-derivatised galactosides as good galectin-3 inhibitors with affinities down to 1.7 muM and a more than 300-fold selectivity over galectin-1. 2-aminopyrimidine 16-31 galectin 3 Homo sapiens 65-75 31303989-4 2019 Here, we report aminopyrimidine-derivatised galactosides as good galectin-3 inhibitors with affinities down to 1.7 muM and a more than 300-fold selectivity over galectin-1. 2-aminopyrimidine 16-31 galectin 1 Homo sapiens 161-171 31303989-7 2019 Hence, combining an aminopyrimidine motif with a phenyl alpha-thiogalactoside motif offers an attractive route towards highly selective galectin-3 inhibitors. 2-aminopyrimidine 20-35 galectin 3 Homo sapiens 136-146 30667164-1 2019 A series of novel aminopyrimidine and diaminopyrimidine derivatives were designed and optimized to improve their potency and permeability relative to lead compound 1 (IC50 = 37.4 muM), which was discovered in a previous virtual screening. 2-aminopyrimidine 18-33 latexin Homo sapiens 180-183 29301478-0 2019 New substituted aminopyrimidine derivatives as BACE1 inhibitors: in silico design, synthesis and biological assays. 2-aminopyrimidine 16-31 beta-secretase 1 Homo sapiens 47-52 30646877-7 2019 An appropriate cavity and a hydrophobic nodule were also present in TKTL1/2, into which the diphosphate group fitted, and that was implicated in aminopyrimidine and thiazole ring binding in TKT, respectively. 2-aminopyrimidine 145-160 transketolase like 1 Homo sapiens 68-75 30646877-7 2019 An appropriate cavity and a hydrophobic nodule were also present in TKTL1/2, into which the diphosphate group fitted, and that was implicated in aminopyrimidine and thiazole ring binding in TKT, respectively. 2-aminopyrimidine 145-160 transketolase Homo sapiens 68-71 29301478-1 2019 We report in this work new substituted aminopyrimidine derivatives acting as inhibitors of the catalytic site of BACE1. 2-aminopyrimidine 39-54 beta-secretase 1 Homo sapiens 113-118 30204041-0 2018 Unraveling structural requirements of amino-pyrimidine T790M/L858R double mutant EGFR inhibitors: 2D and 3D QSAR study. 2-aminopyrimidine 38-54 epidermal growth factor receptor Homo sapiens 81-85 30145688-2 2018 Aim of the present study was to investigate the role of structurally related H4R ligands of the aminopyrimidine class with different efficacies and functionalities (neutral antagonist ST-994, partial agonist ST-1006, inverse agonist ST-1012, and partial inverse agonist ST-1124) on croton oil-induced ear edema and pruritus in mice. 2-aminopyrimidine 96-111 histamine receptor H4 Mus musculus 77-80 29871845-2 2018 A potent Pim kinase inhibitor 7f, derived from meridianin C, was further optimized by the replacement of 2-aminopyrimidine with substituted benzene. 2-aminopyrimidine 105-122 Pim-1 proto-oncogene, serine/threonine kinase Homo sapiens 9-12 28881253-6 2017 Replacement of ring B with a 2-amino-pyrimidine moiety led to compound 12 with an increase of affinity and selectivity for the adenosine A2A receptor. 2-aminopyrimidine 29-47 adenosine A2a receptor Rattus norvegicus 127-149 29494843-2 2018 Through scaffold hybridization of a few known CXCR4 antagonists, a series of novel aminopyrimidine derivatives was developed. 2-aminopyrimidine 83-98 C-X-C motif chemokine receptor 4 Homo sapiens 46-51 29394041-0 2018 Aminopyrimidine Class Aggregation Inhibitor Effectively Blocks Abeta-Fibrinogen Interaction and Abeta-Induced Contact System Activation. 2-aminopyrimidine 0-15 amyloid beta precursor protein Homo sapiens 63-68 28853575-4 2017 The pyrazolopyrimidine-based core differs structurally from that of aminopyrimidine-based third-generation EGFR inhibitors and therefore constitutes a new set of inhibitors that target this mechanism of drug resistance. 2-aminopyrimidine 68-83 epidermal growth factor receptor Homo sapiens 107-111 28483702-1 2017 As a part of our extensive structure-activity relationship study of anti-inflammatory heterocycles, a novel series of 67 polysubstituted 2-aminopyrimidines was prepared bearing one (at the C-4 position of the pyrimidine ring) or two (in the C-4 and C-6 positions) (hetero)aryl substituents attached directly through the C-C bond. 2-aminopyrimidine 137-155 complement C4A (Rodgers blood group) Homo sapiens 189-192 26898335-1 2016 Structure based design of a novel class of aminopyrimidine MTH1 (MutT homolog 1) inhibitors is described. 2-aminopyrimidine 43-58 nudix hydrolase 1 Homo sapiens 59-63 27517803-0 2016 Optimization and biological evaluation of aminopyrimidine-based IkappaB kinase beta inhibitors with potent anti-inflammatory effects. 2-aminopyrimidine 42-57 inhibitor of kappaB kinase beta Mus musculus 64-83 27517803-2 2016 In this study, we have successfully developed a structure-activity relationship (SAR) profile of the aminopyrimidine-based IKKbeta inhibitors through the structure-based design strategy to improve the physicochemical properties and cellular activity in terms of the anti-inflammatory effects. 2-aminopyrimidine 101-116 inhibitor of kappaB kinase beta Mus musculus 123-130 27549813-1 2016 Here is reported the development of a novel scoring function that performs remarkably well at identifying the native binding pose of a subset of HSP90 inhibitors containing aminopyrimidine or resorcinol based scaffolds. 2-aminopyrimidine 173-188 heat shock protein 90 alpha family class A member 1 Homo sapiens 145-150 27549813-5 2016 These results indicate that the specific residues considered by PocketScore are determinant to properly model the interaction between HSP90 and its subset of inhibitors containing aminopyrimidine or resorcinol based scaffolds. 2-aminopyrimidine 180-195 heat shock protein 90 alpha family class A member 1 Homo sapiens 134-139 27133739-1 2016 The present in vitro experiments demonstrate inhibitory effects of polysubstituted 2-aminopyrimidines on high output production of nitric oxide (NO) and prostaglandin E2 (PGE2) stimulated by interferon-gamma and lipopolysaccharide (LPS) in peritoneal macrophages of mouse and rat origin. 2-aminopyrimidine 83-101 interferon gamma Mus musculus 191-207 28580438-1 2017 Profiling of the kinase-binding capabilities of an aminopyrimidine analogue detected in a cellular screen of the St. Jude small-molecule collection led to the identification of a novel series of FMS-like tyrosine kinase 3 (FLT3) inhibitors. 2-aminopyrimidine 51-66 fms related receptor tyrosine kinase 3 Homo sapiens 195-221 28580438-1 2017 Profiling of the kinase-binding capabilities of an aminopyrimidine analogue detected in a cellular screen of the St. Jude small-molecule collection led to the identification of a novel series of FMS-like tyrosine kinase 3 (FLT3) inhibitors. 2-aminopyrimidine 51-66 fms related receptor tyrosine kinase 3 Homo sapiens 223-227 28523108-0 2017 2-Aminopyrimidine Derivatives as New Selective Fibroblast Growth Factor Receptor 4 (FGFR4) Inhibitors. 2-aminopyrimidine 0-17 fibroblast growth factor receptor 4 Homo sapiens 47-82 28523108-0 2017 2-Aminopyrimidine Derivatives as New Selective Fibroblast Growth Factor Receptor 4 (FGFR4) Inhibitors. 2-aminopyrimidine 0-17 fibroblast growth factor receptor 4 Homo sapiens 84-89 28523108-1 2017 A series of 2-aminopyrimidine derivatives were designed and synthesized as highly selective FGFR4 inhibitors. 2-aminopyrimidine 12-29 fibroblast growth factor receptor 4 Homo sapiens 92-97 28221788-0 2017 Substituted 2-Aminopyrimidines Selective for alpha7-Nicotinic Acetylcholine Receptor Activation and Association with Acetylcholine Binding Proteins. 2-aminopyrimidine 12-30 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 52-84 28221788-3 2017 Initial screening of a series of over 50 newly characterized 2-aminopyrimidines with affinity for AChBP showed only two to be agonists on the alpha7-nAChR below 10 muM concentration. 2-aminopyrimidine 61-79 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 149-154 27660691-2 2016 An initial hit identification campaign led to an aminopyrimidine series with an autotaxin IC50 of 500 nM. 2-aminopyrimidine 49-64 ectonucleotide pyrophosphatase/phosphodiesterase 2 Homo sapiens 80-89 26898335-1 2016 Structure based design of a novel class of aminopyrimidine MTH1 (MutT homolog 1) inhibitors is described. 2-aminopyrimidine 43-58 nudix hydrolase 1 Homo sapiens 65-79 26115573-2 2015 Previous efforts identified a series of aminopyrimidine IRAK4 inhibitors that possess good potency, but modest kinase selectivity. 2-aminopyrimidine 40-55 interleukin 1 receptor associated kinase 4 Homo sapiens 56-61 26445848-1 2015 The present study sought to determine the anti-tumor effects of OXA-11, a potent, novel small-molecule amino pyrimidine inhibitor (1.2 pM biochemical IC(50)) of focal adhesion kinase (FAK). 2-aminopyrimidine 103-119 PTK2 protein tyrosine kinase 2 Mus musculus 161-182 26445848-1 2015 The present study sought to determine the anti-tumor effects of OXA-11, a potent, novel small-molecule amino pyrimidine inhibitor (1.2 pM biochemical IC(50)) of focal adhesion kinase (FAK). 2-aminopyrimidine 103-119 PTK2 protein tyrosine kinase 2 Mus musculus 184-187 26451770-0 2015 Novel hydrazone moiety-bearing aminopyrimidines as selective inhibitors of epidermal growth factor receptor T790M mutant. 2-aminopyrimidine 31-47 epidermal growth factor receptor Homo sapiens 75-107 26451770-2 2015 Here, a series of novel aminopyrimidines bearing a hydrazone moiety were identified as potent and selective EGFR inhibitors. 2-aminopyrimidine 24-40 epidermal growth factor receptor Homo sapiens 108-112 23347159-1 2013 BACKGROUND AND PURPOSE: The recently proposed binding mode of 2-aminopyrimidines to the human (h) histamine H4 receptor suggests that the 2-amino group of these ligands interacts with glutamic acid residue E182(5.46) in the transmembrane (TM) helix 5 of this receptor. 2-aminopyrimidine 62-80 histamine receptor H4 Homo sapiens 98-119 25278747-0 2014 Drug-likeness approach of 2-aminopyrimidines as histamine H3 receptor ligands. 2-aminopyrimidine 26-44 histamine receptor H3 Homo sapiens 48-69 25317974-10 2014 Compounds with a variety of headgroups were docked into the PI3Kalpha and mTOR ATP-binding sites, and aminopyrimidine and aminopyrazine were found to make excellent phenol replacements. 2-aminopyrimidine 102-117 mechanistic target of rapamycin kinase Homo sapiens 74-78 23668417-4 2013 In the series of 2-aminopyrimidines, the introduction of an additional 2-aminopyrimidine moiety in combination with the appropriate linker lead to bispyrimidines displaying pKi values for binding the human H4R up to 8.2. 2-aminopyrimidine 17-35 histamine receptor H4 Homo sapiens 206-209 23671017-1 2013 Lead optimization of a high-throughput screening hit led to the rapid identification of aminopyrimidine ZK 304709, a multitargeted CDK and VEGF-R inhibitor that displayed a promising preclinical profile. 2-aminopyrimidine 88-103 kinase insert domain receptor Homo sapiens 139-145 23668417-4 2013 In the series of 2-aminopyrimidines, the introduction of an additional 2-aminopyrimidine moiety in combination with the appropriate linker lead to bispyrimidines displaying pKi values for binding the human H4R up to 8.2. 2-aminopyrimidine 17-34 histamine receptor H4 Homo sapiens 206-209 23352510-0 2013 Development of amino-pyrimidine inhibitors of c-Jun N-terminal kinase (JNK): kinase profiling guided optimization of a 1,2,3-benzotriazole lead. 2-aminopyrimidine 15-31 mitogen-activated protein kinase 8 Rattus norvegicus 46-69 23352510-0 2013 Development of amino-pyrimidine inhibitors of c-Jun N-terminal kinase (JNK): kinase profiling guided optimization of a 1,2,3-benzotriazole lead. 2-aminopyrimidine 15-31 mitogen-activated protein kinase 8 Rattus norvegicus 71-74 23352510-1 2013 A series of amino-pyrimidines was developed based upon an initial kinase cross-screening hit from a CDK2 program. 2-aminopyrimidine 12-29 cyclin dependent kinase 2 Rattus norvegicus 100-104 21981714-2 2011 mTOR inhibition was added to the class I PI3K inhibitor 1 (GDC-0941) scaffold primarily through the substitution of the indazole in 1 for a 2-aminopyrimidine. 2-aminopyrimidine 140-157 mechanistic target of rapamycin kinase Homo sapiens 0-4 22742537-0 2012 Ligand-based design, synthesis, and biological evaluation of 2-aminopyrimidines, a novel series of receptor for advanced glycation end products (RAGE) inhibitors. 2-aminopyrimidine 61-79 advanced glycosylation end product-specific receptor Mus musculus 99-143 22742537-0 2012 Ligand-based design, synthesis, and biological evaluation of 2-aminopyrimidines, a novel series of receptor for advanced glycation end products (RAGE) inhibitors. 2-aminopyrimidine 61-79 advanced glycosylation end product-specific receptor Mus musculus 145-149 22030027-0 2011 Discovery of new aminopyrimidine-based phosphoinositide 3-kinase beta (PI3Kbeta) inhibitors with selectivity over PI3Kalpha. 2-aminopyrimidine 17-32 phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta Homo sapiens 71-79 22030027-0 2011 Discovery of new aminopyrimidine-based phosphoinositide 3-kinase beta (PI3Kbeta) inhibitors with selectivity over PI3Kalpha. 2-aminopyrimidine 17-32 phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha Homo sapiens 114-123 22030027-3 2011 When incorporated with the phenyl ring on sulfonamide moiety, aminopyrimidine analogs showed good potency on PI3Kbeta and selectivity over PI3Kalpha. 2-aminopyrimidine 62-77 phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta Homo sapiens 109-117 22030027-3 2011 When incorporated with the phenyl ring on sulfonamide moiety, aminopyrimidine analogs showed good potency on PI3Kbeta and selectivity over PI3Kalpha. 2-aminopyrimidine 62-77 phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha Homo sapiens 139-148 22335519-3 2012 Through structure-based design, we discovered a new class of highly potent aminopyrimidine-based B-Raf inhibitors with improved solubility and pharmacokinetic profiles. 2-aminopyrimidine 75-90 Braf transforming gene Mus musculus 97-102 22290078-2 2012 Aminopyrimidines including compound 32a were identified to display good PrCP inhibitory activity (32a, IC(50)=43 nM) and impressive ability to penetrate brain in mice (brain/plasma ratio: 1.4). 2-aminopyrimidine 0-16 prolylcarboxypeptidase (angiotensinase C) Mus musculus 72-76 22202103-6 2012 Among the diverse chemical structures of the H4R antagonists described a 2-aminopyrimidine scaffold is repeatedly found. 2-aminopyrimidine 73-90 histamine receptor H4 Homo sapiens 45-48 21875802-4 2011 This approach quickly identified 2-aminotriazine and 2-aminopyrimidine derivatives as specific ligands to Hsp90 with high ligand efficiency. 2-aminopyrimidine 53-70 heat shock protein 90 alpha family class A member 1 Homo sapiens 106-111 21861543-2 2011 It is an aminopyrimidine-based, high-affinity inhibitor of the tyrosine kinase activity of BCR-ABL. 2-aminopyrimidine 9-24 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 91-98 19947601-0 2010 Synthesis, biological evaluation, X-ray structure, and pharmacokinetics of aminopyrimidine c-jun-N-terminal kinase (JNK) inhibitors. 2-aminopyrimidine 75-90 mitogen-activated protein kinase 8 Rattus norvegicus 91-114 21684737-0 2011 Discovery of a novel class of 2-aminopyrimidines as CDK1 and CDK2 inhibitors. 2-aminopyrimidine 30-48 cyclin dependent kinase 1 Homo sapiens 52-56 21684737-0 2011 Discovery of a novel class of 2-aminopyrimidines as CDK1 and CDK2 inhibitors. 2-aminopyrimidine 30-48 cyclin dependent kinase 2 Homo sapiens 61-65 20171098-0 2010 Rigidified 2-aminopyrimidines as histamine H4 receptor antagonists: effects of substitution about the rigidifying ring. 2-aminopyrimidine 11-29 histamine receptor H4 Mus musculus 33-54 20171098-1 2010 Three novel series of histamine H(4) receptor (H(4)R) antagonists containing the 2-aminopyrimidine motif are reported. 2-aminopyrimidine 81-98 histamine receptor H4 Mus musculus 22-52 21623630-3 2011 Additionally, an iodine atom or various aryl groups were introduced at the C-5 position of the 2-aminopyrimidine ring. 2-aminopyrimidine 95-112 complement C5 Homo sapiens 75-78 21666838-3 2011 To fill this void we developed an aminopyrimidine JNK inhibitor (SR-3306) that reduced the loss of dopaminergic cell bodies in the SNpc and their terminals in the striatum produced by unilateral injection of 6-hydroxydopamine (6-OHDA) into the nigrostriatal pathway. 2-aminopyrimidine 34-49 mitogen-activated protein kinase 8 Rattus norvegicus 50-53 20385788-2 2010 We have identified an aminopyrimidine derivative (CYT387), which inhibits JAK1, JAK2, and tyrosine kinase 2 (TYK2) at low nanomolar concentrations, with few additional targets. 2-aminopyrimidine 22-37 Janus kinase 1 Mus musculus 74-78 20385788-2 2010 We have identified an aminopyrimidine derivative (CYT387), which inhibits JAK1, JAK2, and tyrosine kinase 2 (TYK2) at low nanomolar concentrations, with few additional targets. 2-aminopyrimidine 22-37 Janus kinase 2 Mus musculus 80-84 20385788-2 2010 We have identified an aminopyrimidine derivative (CYT387), which inhibits JAK1, JAK2, and tyrosine kinase 2 (TYK2) at low nanomolar concentrations, with few additional targets. 2-aminopyrimidine 22-37 tyrosine kinase 2 Mus musculus 90-107 20385788-2 2010 We have identified an aminopyrimidine derivative (CYT387), which inhibits JAK1, JAK2, and tyrosine kinase 2 (TYK2) at low nanomolar concentrations, with few additional targets. 2-aminopyrimidine 22-37 tyrosine kinase 2 Mus musculus 109-113 19947601-0 2010 Synthesis, biological evaluation, X-ray structure, and pharmacokinetics of aminopyrimidine c-jun-N-terminal kinase (JNK) inhibitors. 2-aminopyrimidine 75-90 mitogen-activated protein kinase 8 Rattus norvegicus 116-119 19947601-2 2010 The structure-activity relationships (SAR) around a series of aminopyrimidines were evaluated utilizing biochemical and cell-based assays to measure JNK inhibition and brain penetration in mice. 2-aminopyrimidine 62-78 mitogen-activated protein kinase 8 Mus musculus 149-152 19920925-5 2009 The development of novel agents designed to overcome IM resistance, while still primarily targeted on BCR-ABL, led to the creation of the high affinity aminopyrimidine inhibitor, nilotinib. 2-aminopyrimidine 152-167 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 102-109 19856966-1 2009 A high-throughput screening campaign to discover small molecule leads for the treatment of bone disorders concluded with the discovery of a compound with a 2-aminopyrimidine template that targeted the Wnt beta-catenin cellular messaging system. 2-aminopyrimidine 156-173 catenin beta 1 Rattus norvegicus 205-217 19147349-0 2009 Synthesis and pharmacological evaluation of aminopyrimidine series of 5-HT1A partial agonists. 2-aminopyrimidine 44-59 5-hydroxytryptamine receptor 1A Homo sapiens 70-76 17519960-5 2007 Herein we demonstrate a dose-dependent, reversible inhibition of ABCG2-mediated Hoechst 33342 dye efflux in primary human and murine HSC by both imatinib and nilotinib (AMN107), a novel aminopyrimidine inhibitor of BCR-ABL. 2-aminopyrimidine 186-201 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 65-70 18811133-1 2008 A series of 2-aminopyrimidines was synthesized as ligands of the histamine H4 receptor (H4R). 2-aminopyrimidine 12-30 histamine receptor H4 Homo sapiens 65-86 18956997-6 2008 It represents an aminopyrimidine derivative of imatinib with approximately 30 times more potency in vitro against imatinib-sensitive BCR-ABL-expressing cell lines and activity against 32 of 33 point mutations conferring resistance to imatinib. 2-aminopyrimidine 17-32 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 133-140 18501602-0 2008 Synthesis and structure-activity relationship of aminopyrimidine IKK2 inhibitors. 2-aminopyrimidine 49-64 inhibitor of nuclear factor kappa B kinase subunit beta Homo sapiens 65-69 17613767-1 2007 The aminopyrimidine inhibitor AMN107 (Nilotinib) was rationally designed to antagonize the aberrant tyrosine kinase activity of Bcr-Abl-positive cells. 2-aminopyrimidine 4-19 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 128-135 17459703-0 2007 Synthesis and SAR of aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors. 2-aminopyrimidine 21-37 mitogen-activated protein kinase 8 Homo sapiens 47-70 17459703-0 2007 Synthesis and SAR of aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors. 2-aminopyrimidine 21-37 mitogen-activated protein kinase 8 Homo sapiens 72-75 17459703-1 2007 The development of a series of novel aminopyrimidines as inhibitors of c-Jun N-terminal kinases is described. 2-aminopyrimidine 37-53 Jun proto-oncogene, AP-1 transcription factor subunit Homo sapiens 71-76 17131463-0 2007 Macrocyclic aminopyrimidines as multitarget CDK and VEGF-R inhibitors with potent antiproliferative activities. 2-aminopyrimidine 12-28 vascular endothelial growth factor A Homo sapiens 52-56 17131463-1 2007 X-ray structures from CDK2-aminopyrimidine inhibitor complexes led to the idea to stabilize the active conformation of aminopyrimidine inhibitors by incorporating the recognition site into a macrocyclic framework. 2-aminopyrimidine 27-42 cyclin dependent kinase 2 Homo sapiens 22-26 17131463-1 2007 X-ray structures from CDK2-aminopyrimidine inhibitor complexes led to the idea to stabilize the active conformation of aminopyrimidine inhibitors by incorporating the recognition site into a macrocyclic framework. 2-aminopyrimidine 119-134 cyclin dependent kinase 2 Homo sapiens 22-26 17131463-4 2007 Macrocyclic aminopyrimidines were shown to be multitarget inhibitors of CDK1/2 and VEGF-RTKs. 2-aminopyrimidine 12-28 cyclin dependent kinase 12 Homo sapiens 72-87 16000593-0 2005 AMN107, a novel aminopyrimidine inhibitor of Bcr-Abl, has in vitro activity against imatinib-resistant chronic myeloid leukemia. 2-aminopyrimidine 16-31 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 45-52 16750629-3 2006 Among the pyrimido-pyrimidones the emergence of two sub-types of analogs-C7-amino-pyrimidines such as 24 and C7-amino-piperidines such as 42-characterized with good p38 inhibition and better off-target profiles in terms of ion channel activities was significant. 2-aminopyrimidine 76-93 mitogen-activated protein kinase 14 Homo sapiens 165-168 16078266-0 2005 AMN107, a novel aminopyrimidine inhibitor of p190 Bcr-Abl activation and of in vitro proliferation of Philadelphia-positive acute lymphoblastic leukemia cells. 2-aminopyrimidine 16-31 contactin associated protein 1 Homo sapiens 45-49 16078266-0 2005 AMN107, a novel aminopyrimidine inhibitor of p190 Bcr-Abl activation and of in vitro proliferation of Philadelphia-positive acute lymphoblastic leukemia cells. 2-aminopyrimidine 16-31 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 50-57 14625007-3 2003 Thereafter, protected amino acids were coupled iteratively by the DCC method, commencing at the amino group of the aminopyrimidine unit. 2-aminopyrimidine 115-130 DCC netrin 1 receptor Homo sapiens 66-69 14623876-8 2004 The mechanistic implications of the active site arrangement are discussed, including the potential role of the aminopyrimidine ring of the ThP2. 2-aminopyrimidine 111-126 GLI family zinc finger 2 Homo sapiens 139-143 14658877-3 2003 The structure determination of a substrate-bound DPD species, Zn2(DPD)(2-aminopyrimidine) (2), completes a set of structurally homologous zinc(II) porphyrin host and host-guest complexes, which offer a direct structural comparison for the Pacman effect upon substrate complexation. 2-aminopyrimidine 71-89 dihydropyrimidine dehydrogenase Homo sapiens 49-52 14658877-3 2003 The structure determination of a substrate-bound DPD species, Zn2(DPD)(2-aminopyrimidine) (2), completes a set of structurally homologous zinc(II) porphyrin host and host-guest complexes, which offer a direct structural comparison for the Pacman effect upon substrate complexation. 2-aminopyrimidine 71-89 dihydropyrimidine dehydrogenase Homo sapiens 66-69 12693972-8 2003 According to our hypothesis, the induced absorption band is that of the imino form of ThDP resulting from three contributing features of the ThDP binding site of transketolase: the relative hydrophobicity of this site, hydrogen bonding of the N1;-atom of the ThDP aminopyrimidine ring to Glu418, and base stacking interactions between the aminopyrimidine ring of ThDP and Phe445. 2-aminopyrimidine 264-279 transketolase Homo sapiens 162-175