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299 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
28280261 84 Non-kinase targets of protein kinase inhibitors.EBI The University of Sydney
27816515 143 Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.EBI Merck& Co.
28011202 21 Design, synthesis and biological evaluation of novel 4-(2-fluorophenoxy)quinoline derivatives as selective c-Met inhibitors.EBI Shenyang Pharmaceutical University
27490023 25 Design, synthesis and structure-activity relationships of novel 4-phenoxyquinoline derivatives containing 1,2,4-triazolone moiety as c-Met kinase inhibitors.EBI Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University)
27474925 40 Design, synthesis and biological evaluation of novel 4-arylaminopyrimidine derivatives possessing a hydrazone moiety as dual inhibitors of L1196M ALK and ROS1.EBI Shenyang Pharmaceutical University
27391135 28 3-Hydrazinoindolin-2-one derivatives: Chemical classification and investigation of their targets as anticancer agents.EBI Egyptian Russian University
27299736 37 The"Cyclopropyl Fragment" is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules.EBI St. John's University
27187857 17 Synthesis and biological evaluation of 4-(2-fluorophenoxy)-3,3'-bipyridine derivatives as potential c-met inhibitors.EBI Shenyang Pharmaceutical University
27396929 11 Synthesis and biological evaluation of Oblongifolin C derivatives as c-Met inhibitors.EBI Shanghai University of Traditional Chinese Medicine
27348537 60 Discovery of 3-(5'-Substituted)-Benzimidazole-5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazoles as Potent Fibroblast Growth Factor Receptor Inhibitors: Design, Synthesis, and Biological Evaluation.EBI East China University of Science& Technology
27131066 36 An orally available tyrosine kinase ALK and RET dual inhibitor bearing the tetracyclic benzo[b]carbazolone core.EBI Chinese Academy of Sciences
27258622 47 Novel c-Met inhibitory olive secoiridoid semisynthetic analogs for the control of invasive breast cancer.EBI University of Louisiana at Monroe
27155466 12 Discovery of a novel 6,7-disubstituted-4-(2-fluorophenoxy)quinolines bearing 1,2,3-triazole-4-carboxamide moiety as potent c-Met kinase inhibitors.EBI Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University)
27288183 130 Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors.EBI Southeast University
27068889 26 Design, synthesis and biological evaluation of 4-aminopyrimidine-5-cabaldehyde oximes as dual inhibitors of c-Met and VEGFR-2.EBI China Pharmaceutical University
27184766 5 Synthesis, antitumor evaluation and molecular docking studies of [1,2,4]triazolo[4,3-b][1,2,4,5]tetrazine derivatives.EBI Taizhou Vocational& Technical College
26555154 36 AXL Inhibitors in Cancer: A Medicinal Chemistry Perspective.EBI University of Edinburgh
27003761 120 Discovery of Entrectinib: A New 3-Aminoindazole As a Potent Anaplastic Lymphoma Kinase (ALK), c-ros Oncogene 1 Kinase (ROS1), and Pan-Tropomyosin Receptor Kinases (Pan-TRKs) inhibitor.EBI Nerviano Medical Sciences Srl
27117263 51 Discovery and optimization of 1,7-disubstituted-2,2-dimethyl-2,3-dihydroquinazolin-4(1H)-ones as potent and selective PKC┐ inhibitors.EBI Takeda Pharmaceutical Company, Ltd
27106711 87 Discovery and structure activity relationship study of novel indazole amide inhibitors for extracellular signal-regulated kinase1/2 (ERK1/2).EBI Green Valley Research Institute
27106709 92 Discovery of indirubin derivatives as new class of DRAK2 inhibitors from high throughput screening.EBI Korea Research Institute of Chemical Technology
27061987 40 Discovery of 6-(difluoro(6-(4-fluorophenyl)-[1,2,4]triazolo[4,3-b][1,2,4]triazin-3-yl)methyl)quinoline as a highly potent and selective c-Met inhibitor.EBI Chinese Academy of Sciences (CAS)
27043268 16 Design, synthesis, biological evaluation and docking studies of novel 2-substituted-4-morpholino-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidine derivatives as dual PI3Ka/mTOR inhibitors.EBI Jiangxi Science& Technology Normal University
27017548 23 Design and synthesis of novel benzo[d]oxazol-2(3H)-one derivatives bearing 7-substituted-4-enthoxyquinoline moieties as c-Met kinase inhibitors.EBI Shanghai Institute of Materia Medica
26812066 34 Discovery of (R)-6-(1-(8-Fluoro-6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)ethyl)-3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)-one (AMG 337), a Potent and Selective Inhibitor of MET with High Unbound Target Coverage and Robust In Vivo Antitumor Activity.EBI Amgen Inc
26951753 336 Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.EBI Novartis Institutes for BioMedical Research
26964675 5 Synthesis, and docking studies of phenylpyrimidine-carboxamide derivatives bearing 1H-pyrrolo[2,3-b]pyridine moiety as c-Met inhibitors.EBI Jiangxi Science& Technology Normal University
26923692 34 Discovery of novel pyrrolo[2,3-b]pyridine derivatives bearing 1,2,3-triazole moiety as c-Met kinase inhibitors.EBI Jiangxi Science and Technology Normal University
26944614 14 Synthesis and antiproliferative activity of 6,7-disubstituted-4-phenoxyquinoline derivatives bearing the 2-oxo-4-chloro-1,2-dihydroquinoline-3-carboxamide moiety.EBI Jiangxi Science and Technology Normal University
26897090 18 Design, synthesis and biological evaluation of novel 4-phenoxy-6,7-disubstituted quinolines possessing (thio)semicarbazones as c-Met kinase inhibitors.EBI Shenyang Pharmaceutical University
26717201 68 Recent advances in the development of dual VEGFR and c-Met small molecule inhibitors as anticancer drugs.EBI Shenyang Pharmaceutical University
26698536 56 Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase.EBI Chinese Academy of Sciences
26762835 342 Discovery of 2-(1H-indol-5-ylamino)-6-(2,4-difluorophenylsulfonyl)-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one (7ao) as a potent selective inhibitor of Polo like kinase 2 (PLK2).EBI Icahn School of Medicine at Mount Sinai
26526740 111 Synthesis and biological evaluation of di-aryl urea derivatives as c-Kit inhibitors.EBI Univ. Lille
26342867 52 Discovery of 6-phenylimidazo[2,1-b]thiazole derivatives as a new type of FLT3 inhibitors.EBI Sichuan University
26318067 34 Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors.EBI Hanyang University
26344595 26 Synthesis and biological evaluation of novel 7-substituted 3-(4-phenoxyphenyl)thieno[3,2-c]pyridin-4-amines as potent Bruton's tyrosine kinase (BTK) inhibitors.EBI Xi'an Jiaotong University
26243370 25 Design, synthesis and RON receptor tyrosine kinase inhibitory activity of new head groups analogs of LCRF-0004.EBI Laboratoires ChemRF Inc./ChemRF Laboratories Inc.
26112445 12 Design and synthesis of constrained analogs of LCRF-0004 as potent RON tyrosine kinase inhibitors.EBI Laboratoires ChemRF Inc. / ChemRF Laboratories Inc.
26277759 31 Discovery of thieno[3,2-c]pyridin-4-amines as novel Bruton's tyrosine kinase (BTK) inhibitors.EBI China Pharmaceutical University
26222319 192 Discovery of 2-[1-(4,4-Difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide (NMS-P118): A Potent, Orally Available, and Highly Selective PARP-1 Inhibitor for Cancer Therapy.EBI Nerviano Medical Sciences Srl
26169763 39 Design and biological evaluation of novel 4-(2-fluorophenoxy)quinoline derivatives bearing an imidazolone moiety as c-Met kinase inhibitors.EBI Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University)
25282672 18 Design and optimization of novel 4-(2-fluorophenoxy)quinoline derivatives bearing a hydrazone moiety as c-Met kinase inhibitors.EBI Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University)
25082515 44 Discovery of quinazolin-4-amines bearing benzimidazole fragments as dual inhibitors of c-Met and VEGFR-2.EBI China Pharmaceutical University
25007344 73 Optimization of potent DFG-in inhibitors of platelet derived growth factor receptor▀ (PDGF-R▀) guided by water thermodynamics.EBI Christian-Albrechts-University of Kiel
26005534 158 (R)-2-Phenylpyrrolidine Substituted Imidazopyridazines: A New Class of Potent and Selective Pan-TRK Inhibitors.EBI Genomics Institute of the Novartis Research Foundation
26005523 37 Design, Synthesis, and Biological Evaluation of Novel Imidazo[1,2-a]pyridine Derivatives as Potent c-Met Inhibitors.EBI Shanghai Institute of Materia Medica
25953155 16 Design and synthesis of close analogs of LCRF-0004, a potent and selective RON receptor tyrosine kinase inhibitor.EBI ChemRF Laboratories
25827399 52 Enhancing the cellular anti-proliferation activity of pyridazinones as c-met inhibitors using docking analysis.EBI Chinese Academy of Sciences
25699405 57 Discovery of potent and selective 8-fluorotriazolopyridine c-Met inhibitors.EBI Amgen Inc.
25827523 275 Isosteric replacements of the carboxylic acid of drug candidate VX-787: Effect of charge on antiviral potency and kinase activity of azaindole-based influenza PB2 inhibitors.EBI Vertex Pharmaceuticals Inc.
25736998 37 Identification and optimization of pyridazinones as potent and selective c-Met kinase inhibitors.EBI Merck Serono Research& Development
25461320 46 Synthesis and biological evaluation of new pyrazol-4-ylpyrimidine derivatives as potential ROS1 kinase inhibitors.EBI Korea University of Science and Technology
25537530 37 Discovery and SAR study of c-Met kinase inhibitors bearing an 3-amino-benzo[d]isoxazole or 3-aminoindazole scaffold.EBI China Pharmaceutical University
25068800 34 UNC2025, a potent and orally bioavailable MER/FLT3 dual inhibitor.EBI University of North Carolina at Chapel Hill
25036791 56 Bioisosteric replacement of an acylureido moiety attached to an indolin-2-one scaffold with a malonamido or a 2/4-pyridinoylamido moiety produces a selectively potent Aurora-B inhibitor.EBI National Taiwan University
24980703 296 Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors.EBI Nerviano Medical Sciences
24951334 34 Design, synthesis and evaluation of highly selective pyridone-based class II MET inhibitors.EBI Central China Normal University
24913714 53 Discovery of a novel series of potent MK2 non-ATP competitive inhibitors using 1,2-substituted azoles as cis-amide isosteres.EBI Merck Research Laboratories
24882675 12 Design, synthesis and biological evaluation of novel 6,7-disubstituted-4-phenoxyquinoline derivatives bearing 4-oxo-3,4-dihydrophthalazine-1-carboxamide moieties as c-Met kinase inhibitors.EBI Shenyang Pharmaceutical University
24785465 80 Discovery of novel 2,4-diarylaminopyrimidine analogues (DAAPalogues) showing potent inhibitory activities against both wild-type and mutant ALK kinases.EBI Chinese Academy of Sciences
25529740 12 Discovery of potent 1H-imidazo[4,5-b]pyridine-based c-Met kinase inhibitors via mechanism-directed structural optimization.EBI Soochow University
25438768 44 Discovery andw biological evaluation of novel 6,7-disubstituted-4-(2-fluorophenoxy)quinoline derivatives possessing 1,2,3-triazole-4-carboxamide moiety as c-Met kinase inhibitors.EBI Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University)
25409491 83 A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles.EBI Zhejiang University
25313996 91 Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase.EBI Merck Research Laboratories
25282552 30 Discovery of substituted 6-pheny-3H-pyridazin-3-one derivatives as novel c-Met kinase inhibitors.EBI Sungkyunkwan University
25200979 31 Design, synthesis and pharmacological evaluation of 2-(thiazol-2-amino)-4-arylaminopyrimidines as potent anaplastic lymphoma kinase (ALK) inhibitors.EBI Shanghai Institute of Materia Medica (SIMM)
25148209 58 Discovery of (S)-1-(1-(Imidazo[1,2-a]pyridin-6-yl)ethyl)-6-(1-methyl-1H-pyrazol-4-yl)-1H-[1,2,3]triazolo[4,5-b]pyrazine (volitinib) as a highly potent and selective mesenchymal-epithelial transition factor (c-Met) inhibitor in clinical development for treatment of cancer.EBI Hutchison MediPharma Limited
24139169 175 Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.EBI Nerviano Medical Sciences
24996144 20 Design, synthesis and structure-activity relationships of novel 4-phenoxyquinoline derivatives containing pyridazinone moiety as potential antitumor agents.EBI Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University)
24944742 63 Discovery of Anilinopyrimidines as Dual Inhibitors of c-Met and VEGFR-2: Synthesis, SAR, and Cellular Activity.EBI Shanghai Institute of Materia Medica
24792774 24 Discovery of novel type II c-Met inhibitors based on BMS-777607.EBI Fudan University
24773549 20 Discovery of 4-aryl-N-arylcarbonyl-2-aminothiazoles as Hec1/Nek2 inhibitors. Part I: optimization of in vitro potencies and pharmacokinetic properties.EBI Development Center for Biotechnology
24569110 11 Discovery of dual ZAP70 and Syk kinases inhibitors by docking into a rare C-helix-out conformation of Syk.EBI University of Zurich
23906342 14 Discovery of a selective kinase inhibitor (TAK-632) targeting pan-RAF inhibition: design, synthesis, and biological evaluation of C-7-substituted 1,3-benzothiazole derivatives.EBI Takeda Pharmaceutical Company Limited
24485123 43 Discovery of novel 6,7-disubstituted-4-phenoxyquinoline derivatives bearing 5-(aminomethylene)pyrimidine-2,4,6-trione moiety as c-Met kinase inhibitors.EBI Shenyang Pharmaceutical University
24479418 39 Cytotoxic and protein kinase inhibiting nakijiquinones and nakijiquinols from the sponge Dactylospongia metachromia.EBI Heinrich-Heine-Universit£t
24328302 94 Protein kinase and HDAC inhibitors from the endophytic fungus Epicoccum nigrum.EBI Heinrich-Heine-Universit£t D£sseldorf
24216091 24 Structure-based design, synthesis, and evaluation of imidazo[1,2-b]pyridazine and imidazo[1,2-a]pyridine derivatives as novel dual c-Met and VEGFR2 kinase inhibitors.EBI Takeda Pharmaceutical Company Limited
24210504 106 Design and synthesis of novel 3-(benzo[d]oxazol-2-yl)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine derivatives as selective G-protein-coupled receptor kinase-2 and -5 inhibitors.EBI Korea Research Institute of Chemical Technology
24157370 22 The sulfamide moiety affords higher inhibitory activity and oral bioavailability to a series of coumarin dual selective RAF/MEK inhibitors.EBI Chugai Pharmaceutical Co., Ltd
24100158 148 Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90).EBI Nerviano Medical Sciences S.r.l.
23993328 41 Synthesis and biological evaluation of 2-amino-5-aryl-3-benzylthiopyridine scaffold based potent c-Met inhibitors.EBI Chinese Academy of Sciences
24044867 86 Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.EBI Califia Bio Inc.
24012712 10 Design, synthesis, and structure-activity relationships of novel 6,7-disubstituted-4-phenoxyquinoline derivatives as potential antitumor agents.EBI Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University)
23944843 60 Lessons from (S)-6-(1-(6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)ethyl)quinoline (PF-04254644), an inhibitor of receptor tyrosine kinase c-Met with high protein kinase selectivity but broad phosphodiesterase family inhibition leading to myocardial degeneration in rats.EBI Pfizer Inc.
23838381 38 Discovery and optimization of novel 4-phenoxy-6,7-disubstituted quinolines possessing semicarbazones as c-Met kinase inhibitors.EBI Shenyang Pharmaceutical University
23937569 22 Selectivity data: assessment, predictions, concordance, and implications.EBI Lilly Research Laboratories
23920481 25 Synthesis and evaluation of heteroaryl substituted diazaspirocycles as scaffolds to probe the ATP-binding site of protein kinases.EBI The Institute of Cancer Research
23773865 49 Novel 6-aminofuro[3,2-c]pyridines as potent, orally efficacious inhibitors of cMET and RON kinases.EBI OSI Pharmaceuticals, LLC
23742252 81 Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase EBI Genomics Institute of the Novartis Research Foundation
23702473 10 Indazoles as potential c-Met inhibitors: design, synthesis and molecular docking studies.EBI Guangdong Pharmaceutical University
23644189 12 Design, synthesis and antitumour activity of bisquinoline derivatives connected by 4-oxy-3-fluoroaniline moiety.EBI Shenyang Pharmaceutical University
23628470 40 Discovery of novel 4-(2-fluorophenoxy)quinoline derivatives bearing 4-oxo-1,4-dihydrocinnoline-3-carboxamide moiety as c-Met kinase inhibitors.EBI Shenyang Pharmaceutical University
23602398 43 Conformation constraint of anilides enabling the discovery of tricyclic lactams as potent MK2 non-ATP competitive inhibitors.EBI Merck Research Laboratories
23587425 37 Potency switch between CHK1 and MK2: discovery of imidazo[1,2-a]pyrazine- and imidazo[1,2-c]pyrimidine-based kinase inhibitors.EBI Merck Research Laboratories
23535330 83 Structure-based design and optimization of 2-aminothiazole-4-carboxamide as a new class of CHK1 inhibitors.EBI Merck Research Laboratories
23474386 26 Novel 5-(benzyloxy)pyridin-2(1H)-one derivatives as potent c-Met inhibitors.EBI Chinese Academy of Sciences
23490150 48 Design and synthesis of novel pyrimido[4,5-b]azepine derivatives as HER2/EGFR dual inhibitors.EBI Takeda Pharmaceutical Co., Ltd
23434140 35 Substituted indolin-2-ones as p90 ribosomal S6 protein kinase 2 (RSK2) inhibitors: Molecular docking simulation and structure-activity relationship analysis.EBI East China University of Science and Technology
23403296 2 Olive secoiridoids and semisynthetic bioisostere analogues for the control of metastatic breast cancer.EBI University of Louisiana at Monroe
22749189 24 Inhibitors of the TAM subfamily of tyrosine kinases: synthesis and biological evaluation.EBI Centre Universitaire
23394126 170 Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).EBI Exelixis
23249297 75 Trimeric hemibastadin congener from the marine sponge Ianthella basta.EBI Heinrich-Heine University
23379595 55 Discovery of 1-[3-(1-methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl]-N-(pyridin-2-ylmethyl)methanesulfonamide (MK-8033): A Specific c-Met/Ron dual kinase inhibitor with preferential affinity for the activated state of c-Met.EBI Merck& Co., Inc.
23312472 129 Highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.EBI Pfizer Inc.
21835616 41 The discovery of benzanilides as c-Met receptor tyrosine kinase inhibitors by a directed screening approach.EBI AstraZeneca
23123015 22 Design, synthesis, and evaluation of imidazo[1,2-b]pyridazine derivatives having a benzamide unit as novel VEGFR2 kinase inhibitors.EBI Takeda Pharmaceutical Company Limited
23103095 125 Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.EBI Abbott Laboratories
22883026 34 Design and synthesis of novel DFG-out RAF/vascular endothelial growth factor receptor 2 (VEGFR2) inhibitors: 3. Evaluation of 5-amino-linked thiazolo[5,4-d]pyrimidine and thiazolo[5,4-b]pyridine derivatives.EBI Takeda Pharmaceutical Company Limited
22726925 216 Discovery of 5-(2-amino-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-N-(tert-butyl)pyridine-3-sulfonamide (CZC24758), as a potent, orally bioavailable and selective inhibitor of PI3K for the treatment of inflammatory disease.EBI Cellzome Ltd
23116168 42 Structural optimization and structure-activity relationships of N2-(4-(4-Methylpiperazin-1-yl)phenyl)-N8-phenyl-9H-purine-2,8-diamine derivatives, a new class of reversible kinase inhibitors targeting both EGFR-activating and resistance mutations.EBI Sichuan University
23098265 46 Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors.EBI University of Genoa
22934600 1 Potent HGF/c-Met axis inhibitors from Eucalyptus globulus: the coupling of phloroglucinol and sesquiterpenoid is essential for the activity.EBI Chinese Academy of Sciences
22924734 87 Discovery of a novel class of exquisitely selective mesenchymal-epithelial transition factor (c-MET) protein kinase inhibitors and identification of the clinical candidate 2-(4-(1-(quinolin-6-ylmethyl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-6-yl)-1H-pyrazol-1-yl)ethanol (PF-04217903) for the treatment ofEBI Pfizer Inc.
22734674 81 The discovery and optimization of a novel class of potent, selective, and orally bioavailable anaplastic lymphoma kinase (ALK) inhibitors with potential utility for the treatment of cancer.EBI Amgen Inc.
22548342 210 Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase¿ inhibitors.EBI Exelixis
22985853 22 Multisubstituted quinoxalines and pyrido[2,3-d]pyrimidines: synthesis and SAR study as tyrosine kinase c-Met inhibitors.EBI China Pharmaceutical University
22980219 55 Design and synthesis of pyrrolo[3,2-d]pyrimidine HER2/EGFR dual inhibitors: improvement of the physicochemical and pharmacokinetic profiles for potent in vivo anti-tumor efficacy.EBI Takeda Pharmaceutical Co. Ltd
22863529 31 Discovery of novel 2-aminopyridine-3-carboxamides as c-Met kinase inhibitors.EBI Chinese Academy of Sciences
22727637 85 Exploration of diverse hinge-binding scaffolds for selective Aurora kinase inhibitors.EBI Abbott Laboratories
22738630 76 Structure-based optimization of aminopyridines as PKC¿ inhibitors.EBI Department of Chemistry at Vertex Pharmaceuticals (Europe) Ltd
22452518 22 Discovery of the novel potent and selective FLT3 inhibitor 1-{5-[7-(3- morpholinopropoxy)quinazolin-4-ylthio]-[1,3,4]thiadiazol-2-yl}-3-p-tolylurea and its anti-acute myeloid leukemia (AML) activities in vitro and in vivo.EBI Sichuan University
22439974 79 Design and synthesis of pyrrolo[3,2-d]pyrimidine human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors: exploration of novel back-pocket binders.EBI Takeda Pharmaceutical Company Limited
22404346 52 Design of potent and selective hybrid inhibitors of the mitotic kinase Nek2: structure-activity relationship, structural biology, and cellular activity.EBI The Institute of Cancer Research
22372864 25 Synthesis and biological evaluation of pyrimidine-based dual inhibitors of human epidermal growth factor receptor 1 (HER-1) and HER-2 tyrosine kinases.EBI Hanmi Research Center
22595176 31 Discovery and optimization of a potent and selective triazolopyridinone series of c-Met inhibitors.EBI Amgen Inc.
22579487 53 Synthesis and structure-activity relationship of aminopyridines with substituted benzoxazoles as c-Met kinase inhibitors.EBI Korea Research Institute of Chemical Technology
22320343 21 Structure-based design of novel class II c-Met inhibitors: 1. Identification of pyrazolone-based derivatives.EBI Amgen Inc.
22320327 250 Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series.EBI Amgen Inc.
22168626 32 Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF) V600E.EBI Ambit Biosciences
21608528 166 Discovery of a 5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one (MK-2461) inhibitor of c-Met kinase for the treatment of cancer.EBI Merck Research Laboratories
21429632 43 Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.EBI University of the Pacific
21353571 26 Structure based design and syntheses of amino-1H-pyrazole amide derivatives as selective Raf kinase inhibitors in melanoma cells.EBI Hanyang University
21128646 88 Aurora kinase inhibitors based on the imidazo[1,2-a]pyrazine core: fluorine and deuterium incorporation improve oral absorption and exposure.EBI Merck Research Laboratories
21123062 48 Fused bicyclic derivatives of 2,4-diaminopyrimidine as c-Met inhibitors.EBI Cephalon, Inc
18469809 41 A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity.EBI Nerviano Medical Sciences Oncology
20570525 56 Discovery of novel purine derivatives with potent and selective inhibitory activity against c-Src tyrosine kinase.EBI Chinese Academy of Sciences
20570511 22 Discovery of aminopyridines substituted with benzoxazole as orally active c-Met kinase inhibitors.EBI Korea Research Institute of Chemical Technology
20420387 118 Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase.EBI GlaxoSmithKline
20153646 28 Indirubin derivatives as potent FLT3 inhibitors with anti-proliferative activity of acute myeloid leukemic cells.EBI Institute of Science and Technology
20138514 93 3-Aryl-4-(arylhydrazono)-1H-pyrazol-5-ones: Highly ligand efficient and potent inhibitors of GSK3beta.EBI Vertex Pharmaceuticals Inc
20153204 109 Optimization of 6,6-dimethyl pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing.EBI Nerviano Medical Sciences Srl
19716697 110 The discovery of thienopyridine analogues as potent IkappaB kinase beta inhibitors. Part II.EBI Boehringer Ingelheim Pharmaceuticals
19854051 56 N-(4-(6,7-Disubstituted-quinolin-4-yloxy)-3-fluorophenyl)-2-oxo-3-phenylimidazolidine-1-carboxamides: a novel series of dual c-Met/VEGFR2 receptor tyrosine kinase inhibitors.EBI MethylGene Inc
18183025 12060 A quantitative analysis of kinase inhibitor selectivity.EBI Ambit Biosciences
19397322 58 Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.EBI National Cancer Institute
18077425 197 Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.EBI Harvard Medical School
18324759 133 Evaluation of a series of naphthamides as potent, orally active vascular endothelial growth factor receptor-2 tyrosine kinase inhibitors.EBI Amgen Inc.
18311900 89 Novel 2,3-dihydro-1,4-benzoxazines as potent and orally bioavailable inhibitors of tumor-driven angiogenesis.EBI Amgen Inc.
18077363 314 A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.EBI University of Oxford
18278858 93 Structure-based design of novel 2-amino-6-phenyl-pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-ones as potent and orally active inhibitors of lymphocyte specific kinase (Lck): synthesis, SAR, and in vivo anti-inflammatory activity.EBI Amgen Inc.
15177483 33 SAR of benzoylpyridines and benzophenones as p38alpha MAP kinase inhibitors with oral activity.EBI Novartis Institutes for BioMedical Research
22377675 44 Indeno[1,2-b]indole derivatives as a novel class of potent human protein kinase CK2 inhibitors.EBI Westf£lische Wilhelms-Universit£t M£nster
22221201 32 VX-322: a novel dual receptor tyrosine kinase inhibitor for the treatment of acute myelogenous leukemia.EBI University of Kentucky
16476733 18 Inhibition of S/G2 phase CDK4 reduces mitotic fidelity.EBI University of Queensland
22381355 16 Design, synthesis and molecular docking studies of some novel spiro[indoline-3, 4'-piperidine]-2-ones as potential c-Met inhibitors.EBI Southern Medical University
22269278 50 Angiogenesis inhibitors identified by cell-based high-throughput screening: synthesis, structure-activity relationships and biological evaluation of 3-[(E)-styryl]benzamides that specifically inhibit endothelial cell proliferation.EBI Chugai Pharmaceutical Co., Ltd.
22136433 67 7,8-dichloro-1-oxo-ß-carbolines as a versatile scaffold for the development of potent and selective kinase inhibitors with unusual binding modes.EBI Ludwig-Maximilians University of Munich
22225917 44 Design and synthesis of a highly selective, orally active and potent anaplastic lymphoma kinase inhibitor (CH5424802).EBI Chugai Pharmaceutical Co., Ltd
21967808 52 Improvement in oral bioavailability of 2,4-diaminopyrimidine c-Met inhibitors by incorporation of a 3-amidobenzazepin-2-one group.EBI Cephalon, Inc.
22154349 123 5-(2-amino-pyrimidin-4-yl)-1H-pyrrole and 2-(2-amino-pyrimidin-4-yl)-1,5,6,7-tetrahydro-pyrrolo[3,2-c]pyridin-4-one derivatives as new classes of selective and orally available Polo-like kinase 1 inhibitors.EBI Nerviano Medical Sciences srl
22119469 107 Novel and selective spiroindoline-based inhibitors of Sky kinase.EBI Pfizer Inc.
22138308 18 Identification of new aminoacid amides containing the imidazo[2,1-b]benzothiazol-2-ylphenyl moiety as inhibitors of tumorigenesis by oncogenic Met signaling.EBI CNRS UMR 6216
22014550 337 Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).EBI Ansaris
22003817 71 Design and synthesis of novel human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors bearing a pyrrolo[3,2-d]pyrimidine scaffold.EBI Takeda Pharmaceutical Company Limited
22001029 28 Design and synthesis of triazolopyridazines substituted with methylisoquinolinone as selective c-Met kinase inhibitors.EBI Korea Research Institute of Chemical Technology
21982797 128 9,10-secosteroids, protein kinase inhibitors from the Chinese gorgonian Astrogorgia sp.EBI Peking University
22014755 36 Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells.EBI Hanyang University
21794960 194 Imidazo[2,1-b]thiazole guanylhydrazones as RSK2 inhibitors.EBI Universit£ di Bologna
22037378 31824 Comprehensive analysis of kinase inhibitor selectivity.EBI Ambit Biosciences
21936542 143 Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase.EBI Novartis Institute for BioMedical Research
21823617 58 9-substituted 6,6-dimethyl-11-oxo-6,11-dihydro-5H-benzo[b]carbazoles as highly selective and potent anaplastic lymphoma kinase inhibitors.EBI Chugai Pharmaceutical Co., Ltd.
21812414 106 Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK).EBI Pfizer Inc.
21641696 450 Combined SVM-based and docking-based virtual screening for retrieving novel inhibitors of c-Met.EBI Sichuan University
21741249 32 Arthrinins A-D: novel diterpenoids and further constituents from the sponge derived fungus Arthrinium sp.EBI Heinrich-Heine-Universit£t
21665484 37 Discovery of novel c-Met kinase inhibitors bearing a thieno[2,3-d]pyrimidine or furo[2,3-d]pyrimidine scaffold.EBI Chinese Academy of Sciences
21708465 141 Synthesis of an aryloxy oxo pyrimidinone library that displays ALK-selective inhibition.EBI St. Jude Children's Research Hospital
21705217 60 Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38a MAP kinase inhibitors.EBI Bristol-Myers Squibb
20674350 63 Discovery of imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.EBI Merck Research Laboratories
21524503 73 Dual IGF-1R/SRC inhibitors based on a N'-aroyl-2-(1H-indol-3-yl)-2-oxoacetohydrazide structure.EBI Technische Universit£t Braunschweig
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21517068 45 Acenaphtho[1,2-b]pyrrole-based selective fibroblast growth factor receptors 1 (FGFR1) inhibitors: design, synthesis, and biological activity.EBI East China University of Science and Technology
21561771 39 Discovery of novel tetracyclic compounds as anaplastic lymphoma kinase inhibitors.EBI Chugai Pharmaceutical Co. Ltd.
21561768 12 Identification and synthesis of N'-(2-oxoindolin-3-ylidene)hydrazide derivatives against c-Met kinase.EBI Chinese Academy of Sciences
21470862 110 NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor.EBI Nerviano Medical Sciences srl
21405128 47 Synthesis and c-Met kinase inhibition of 3,5-disubstituted and 3,5,7-trisubstituted quinolines: identification of 3-(4-acetylpiperazin-1-yl)-5-(3-nitrobenzylamino)-7- (trifluoromethyl)quinoline as a novel anticancer agent.EBI Chinese Academy of Sciences
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21038853 133 4-(Pyrazol-4-yl)-pyrimidines as selective inhibitors of cyclin-dependent kinase 4/6.EBI Novartis Institutes for Biomedical Research
20873740 111 Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding.EBI Nerviano Medical Sciences Srl
20855207 26 Discovery of orally bioavailable imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.EBI Merck Research Laboratories
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19654408 2521 AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).EBI Ambit Biosciences
20483608 139 New pyrazolo[1,5a]pyrimidines as orally active inhibitors of Lck.EBI Novartis Institute of Biomedical Research
20397705 208 Identification of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as a new class of orally and selective Polo-like kinase 1 inhibitors.EBI Nerviano Medical Sciences Srl
20382527 26 Design, synthesis and structure-activity relationships of novel biarylamine-based Met kinase inhibitors.EBI Bristol-Myers Squibb Research and Development
20363625 69 Identification of a novel series of potent RON receptor tyrosine kinase inhibitors.EBI MethylGene Inc.
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20141146 234 Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors.EBI Nerviano Medical Sciences Srl
20093027 92 Discovery of 6-benzyloxyquinolines as c-Met selective kinase inhibitors.EBI Chugai Pharmaceutical Co, Ltd
20071170 36 Identification of potent and selective VEGFR receptor tyrosine kinase inhibitors having new amide isostere headgroups.EBI MethylGene Inc
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19888761 52 Discovery of a novel Her-1/Her-2 dual tyrosine kinase inhibitor for the treatment of Her-1 selective inhibitor-resistant non-small cell lung cancer.EBI Hanmi Research Center
19839593 4 Tea catechins inhibit hepatocyte growth factor receptor (MET kinase) activity in human colon cancer cells: kinetic and molecular docking studies.EBI Oregon State University
19791746 14 Kinase inhibitor data modeling and de novo inhibitor design with fragment approaches.EBI Eli Lilly and Company Lilly Research Laboratories
19775160 79 2-{3-[4-(Alkylsulfinyl)phenyl]-1-benzofuran-5-yl}-5-methyl-1,3,4-oxadiazole derivatives as novel inhibitors of glycogen synthase kinase-3beta with good brain permeability.EBI Takeda Pharmaceutical Company, Ltd.
19369077 70 Discovery of 4-azaindoles as novel inhibitors of c-Met kinase.EBI UCB Celltech
19362847 51 Design and synthesis of a novel tyrosine kinase inhibitor template.EBI St Jude Children's Research Hospital
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19414255 58 Structure-based design of 3-aryl-6-amino-triazolo[4,3-b]pyridazine inhibitors of Pim-1 kinase.EBI Vertex Pharmaceuticals Inc
19269177 21 Syntheses of novel 2,3-diaryl-substituted 5-cyano-4-azaindoles exhibiting c-Met inhibition activity.EBI Technical University of Darmstadt
19211249 95 N-(3-fluoro-4-(2-arylthieno[3,2-b]pyridin-7-yloxy)phenyl)-2-oxo-3-phenylimidazolidine-1-carboxamides: a novel series of dual c-Met/VEGFR2 receptor tyrosine kinase inhibitors.EBI MethylGene Inc.
19059779 32 Discovery of a novel series of quinoxalines as inhibitors of c-Met kinase.EBI UCB Celltech
19053831 39 Search for inhibitors of bacterial and human protein kinases among derivatives of diazepines[1,4] annelated with maleimide and indole cycles.EBI Institute of General Genetics
18682324 33 Evaluation of indazole-based compounds as a new class of potent KDR/VEGFR-2 inhibitors.EBI Amgen, Inc.
18610999 24 Naturally occurring homoisoflavonoids function as potent protein tyrosine kinase inhibitors by c-Src-based high-throughput screening.EBI Institute of Materia Medica
18606543 68 2-Alkenylthieno[2,3-b]pyridine-5-carbonitriles: Potent and selective inhibitors of PKCtheta.EBI Wyeth Research
18529047 156 Design, synthesis, and biological evaluation of novel 3-aryl-4-(1H-indole-3yl)-1,5-dihydro-2H-pyrrole-2-ones as vascular endothelial growth factor receptor (VEGF-R) inhibitors.EBI Eberhard-Karls University
18479916 24 Discovery of orally active pyrrolopyridine- and aminopyridine-based Met kinase inhibitors.EBI Bristol-Myers Squibb Research and Development
18313174 26 Synthesis and biological evaluation of diversely substituted indolin-2-ones.EBI Université Blaise Pascal
17964000 16 Structure activity relationships of quinoline-containing c-Met inhibitors.EBI Pfizer Global Research and Development
17185414 30 Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK.EBI Genomics Institute of the Novartis Research Foundation
18289854 44 Identification of pyrrolo[2,1-f][1,2,4]triazine-based inhibitors of Met kinase.EBI Bristol-Myers Squibb Research and Development
18248988 16 Entry into a new class of protein kinase inhibitors by pseudo ring design.EBI Novartis Institutes for BioMedical Research
18055203 51 Identification of 2-amino-5-(thioaryl)thiazoles as inhibitors of nerve growth factor receptor TrkA.EBI Bristol-Myers Squibb Research and Development
17826092 37 Optimization of triarylimidazoles for Tie2: influence of conformation on potency.EBI GlaxoSmithKline
17606372 66 5-((4-Aminopiperidin-1-yl)methyl)pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
17499505 78 Hit-to-lead studies on benzimidazole inhibitors of ITK: discovery of a novel class of kinase inhibitors.EBI Boehringer Ingelheim Pharmaceuticals Inc.
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17270437 68 New C-5 substituted pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
17239587 43 1,2,3-Thiadiazole substituted pyrazolones as potent KDR/VEGFR-2 kinase inhibitors.EBI Cephalon Inc.
16765046 63 Discovery of 2-pyrimidyl-5-amidothiophenes as potent inhibitors for AKT: synthesis and SAR studies.EBI Chiron Corporation
16750628 47 Hit-to-lead optimization of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of KDR kinase inhibitors.EBI Abbott Laboratories
16249085 26 Pyrazoloheteroaryls: novel p38alpha MAP kinase inhibiting scaffolds with oral activity.EBI Novartis Institutes for BioMedical Research
16134929 22 Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity.EBI Bristol-Myers Squibb Co
16111887 104 New dual inhibitors of EGFR and HER2 protein tyrosine kinases.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
15743179 79 Novel potent orally active selective VEGFR-2 tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of N-phenyl-N'-{4-(4-quinolyloxy)phenyl}ureas.EBI Kirin Brewery Co. Ltd.
15177482 86 Novel p38 inhibitors with potent oral efficacy in several models of rheumatoid arthritis.EBI Novartis Institutes for BioMedical Research
15012985 31 Orally active anti-proliferation agents: novel diphenylamine derivatives as FGF-R2 autophosphorylation inhibitors.EBI Kirin Brewery Co., Ltd.
12941313 18 Identification of a new chemical class of potent angiogenesis inhibitors based on conformational considerations and database searching.EBI Novartis Pharma AG
12672234 64 Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase.EBI Boehringer Ingelheim Pharmaceuticals
12039590 50 Pyrrolo[2,3-d]pyrimidines containing diverse N-7 substituents as potent inhibitors of Lck.EBI Abbott Bioresearch Center
28411406 16 Discovery of novel 2-substituted-4-(2-fluorophenoxy) pyridine derivatives possessing pyrazolone and triazole moieties as dual c-Met/VEGFR-2 receptor tyrosine kinase inhibitorsBDB China Pharmaceutical University
25173590 20 Design, synthesis and pharmacological evaluation of 6,7-disubstituted-4-phenoxyquinoline derivatives as potential antitumor agents.BDB Shenyang Pharmaceutical University, Ministry of Education
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16492761 51 An efficient rapid system for profiling the cellular activities of molecular libraries.BDB Genomics Institute of the Novartis Research Foundation
20338520 24 A structure-guided approach to creating covalent FGFR inhibitors.BDB Harvard Medical School
19260711 12 Discovery of N-(4-(2-Amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607), a Selective and Orally Efficacious Inhibitor of the Met Kinase Superfamily.BDB Bristol-Myers Squibb Company
17098432 10 Anti-breast cancer activity of LFM-A13, a potent inhibitor of Polo-like kinase (PLK).BDB Paradigm Pharmaceuticals
18763753 29 Design, synthesis, and biological evaluation of potent c-Met inhibitors.BDB Amgen
18434145 56 Discovery of a novel and potent series of thieno[3,2-b]pyridine-based inhibitors of c-Met and VEGFR2 tyrosine kinases.BDB MethylGene Inc.
18426196 18 Discovery and optimization of triazolopyridazines as potent and selective inhibitors of the c-Met kinase.BDB Amgen
18553959 21 Discovery of a potent, selective, and orally bioavailable c-Met inhibitor: 1-(2-hydroxy-2-methylpropyl)-N-(5-(7-methoxyquinolin-4-yloxy)pyridin-2-yl)-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide (AMG 458).BDB Amgen
18690676 19 Discovery of pyrrolopyridine-pyridone based inhibitors of Met kinase: synthesis, X-ray crystallographic analysis, and biological activities.BDB Bristol-Myers Squibb Company
16884310 97 Novel 2-aminopyrimidine carbamates as potent and orally active inhibitors of Lck: synthesis, SAR, and in vivo antiinflammatory activity.BDB Amgen