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623 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
27688180 50 Design and discovery of 4-anilinoquinazoline-urea derivatives as dual TK inhibitors of EGFR and VEGFR-2.EBI China Pharmaceutical University
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
27884697 65 3-Cyano-6-(5-methyl-3-pyrazoloamino) pyridines (Part 2): A dual inhibitor of Aurora kinase and tubulin polymerization.EBI CXS Corporation
27573544 43 Discovery of novel inhibitors of Aurora kinases with indazole scaffold: In silico fragment-based and knowledge-based drug design.EBI Taiwan National Health Research Institutes
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)
27484508 58 Identification of new potent phthalazine derivatives with VEGFR-2 and EGFR kinase inhibitory activity.EBI Cairo University
27839918 28 Discovery of TAK-659 an orally available investigational inhibitor of Spleen Tyrosine Kinase (SYK).EBI Takeda California, Inc.
28340913 4 Synthesis, activity and docking studies of phenylpyrimidine-carboxamide Sorafenib derivatives.EBI Jiangxi Science& Technology Normal University
27769623 21 Metabolism-based structure optimization: Discovery of a potent and orally available tyrosine kinase ALK inhibitor bearing the tetracyclic benzo[b]carbazolone core.EBI Ocean University of China
27777009 11 Design, synthesis and activity of novel sorafenib analogues bearing chalcone unit.EBI Jiangxi Science& Technology Normal University
27933954 122 Discovery of [5-Amino-1-(2-methyl-3H-benzimidazol-5-yl)pyrazol-4-yl]-(1H-indol-2-yl)methanone (CH5183284/Debio 1347), An Orally Available and Selective Fibroblast Growth Factor Receptor (FGFR) Inhibitor.EBI Chugai Pharmaceutical Co., Ltd.
27739691 7 Fragment-to-Lead Medicinal Chemistry Publications in 2015.EBI Astex Pharmaceuticals
27299736 37 The"Cyclopropyl Fragment" is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules.EBI St. John's University
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
27176944 26 Design, synthesis and evaluation of 6-aryl-indenoisoquinolone derivatives dual targeting ERa and VEGFR-2 as anti-breast cancer agents.EBI China Pharmaceutical University
27131066 36 An orally available tyrosine kinase ALK and RET dual inhibitor bearing the tetracyclic benzo[b]carbazolone core.EBI Chinese Academy of Sciences
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)
27109867 48 The Identification and Pharmacological Characterization of 6-(tert-Butylsulfonyl)-N-(5-fluoro-1H-indazol-3-yl)quinolin-4-amine (GSK583), a Highly Potent and Selective Inhibitor of RIP2 Kinase.EBI GlaxoSmithKline
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
26881908 13 De Novo Design at the Edge of Chaos.EBI Swiss Federal Institute of Technology (ETH)
27096042 21 Evolution of a New Class of VEGFR-2 Inhibitors from Scaffold Morphing and Redesign.EBI Novartis Institutes for Biomedical Research
27096041 27 Core Replacements in a Potent Series of VEGFR-2 Inhibitors and Their Impact on Potency, Solubility, and hERG.EBI Novartis Institutes for Biomedical Research
26555154 36 AXL Inhibitors in Cancer: A Medicinal Chemistry Perspective.EBI University of Edinburgh
27011159 97 Structure-Activity Relationship Studies of Mitogen Activated Protein Kinase Interacting Kinase (MNK) 1 and 2 and BCR-ABL1 Inhibitors Targeting Chronic Myeloid Leukemic Cells.EBI Experimental Therapeutics Centre
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
27117427 77 Design, synthesis and biological evaluation of pyrazolylaminoquinazoline derivatives as highly potent pan-fibroblast growth factor receptor inhibitors.EBI Chinese Academy of Sciences (CAS)
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
27086121 120 Anilinoquinazoline inhibitors of the RET kinase domain-Elaboration of the 7-position.EBI University of Manchester
26951750 59 Identification of a 5-[3-phenyl-(2-cyclic-ether)-methylether]-4-aminopyrrolo[2,3-d]pyrimidine series of IGF-1R inhibitors.EBI Novartis Institutes for Biomedical Research
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
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
26874741 156 The discovery of 2-substituted phenol quinazolines as potent RET kinase inhibitors with improved KDR selectivity.EBI University of Manchester
27020685 4 Synthetic approaches to the 2014 new drugs.EBI Pfizer Inc.
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
26922228 21 Increasing the binding affinity of VEGFR-2 inhibitors by extending their hydrophobic interaction with the active site: Design, synthesis and biological evaluation of 1-substituted-4-(4-methoxybenzyl)phthalazine derivatives.EBI Egyptian Russian University
26906472 6 Design, synthesis, and docking studies of afatinib analogs bearing cinnamamide moiety as potent EGFR inhibitors.EBI Jiangxi Science& 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
26826581 40 Design and discovery of 4-anilinoquinazoline-acylamino derivatives as EGFR and VEGFR-2 dual TK inhibitors.EBI China Pharmaceutical University
26698536 56 Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase.EBI Chinese Academy of Sciences
26741358 56 Design, synthesis and biological evaluation of N-phenylquinazolin-4-amine hybrids as dual inhibitors of VEGFR-2 and HDAC.EBI China Pharmaceutical University
26753815 81 Expanding the structural diversity of diarylureas as multi-target tyrosine kinase inhibitors.EBI The First Affiliated Hospital of Xi'an Jiaotong University
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
26652860 68 A Pyrazolo[3,4-d]pyrimidin-4-amine Derivative Containing an Isoxazole Moiety Is a Selective and Potent Inhibitor of RET Gatekeeper Mutants.EBI Korea Institute of Science and Technology (KIST)
26475519 40 Hybrids from 4-anilinoquinazoline and hydroxamic acid as dual inhibitors of vascular endothelial growth factor receptor-2 and histone deacetylase.EBI China Pharmaceutical University
26344911 10 Ynamide Click chemistry in development of triazole VEGFR2 TK modulators.EBI Universit£ de Strasbourg
26342134 39 Discovery of novel VEGFR-2 inhibitors. Part 5: Exploration of diverse hinge-binding fragments via core-refining approach.EBI The First Affiliated Hospital of Xi'an Jiaotong University
26526740 111 Synthesis and biological evaluation of di-aryl urea derivatives as c-Kit inhibitors.EBI Univ. Lille
26318056 25 Investigation of new 2-aryl substituted Benzothiopyrano[4,3-d]pyrimidines as kinase inhibitors targeting vascular endothelial growth factor receptor 2.EBI Universit£ di Pisa
26384287 65 Highly potent and selective pyrazolylpyrimidines as Syk kinase inhibitors.EBI Kangwon National University
26342867 52 Discovery of 6-phenylimidazo[2,1-b]thiazole derivatives as a new type of FLT3 inhibitors.EBI Sichuan University
26313252 22 Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor.EBI AstraZeneca
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
26344591 18 Synthesis, antiangiogenesis evaluation and molecular docking studies of 1-aryl-3-[(thieno[3,2-b]pyridin-7-ylthio)phenyl]ureas: Discovery of a new substitution pattern for type II VEGFR-2 Tyr kinase inhibitors.EBI Universidade do Minho
26204510 6 4-Fluoro-3',4',5'-trimethoxychalcone as a new anti-invasive agent. From discovery to initial validation in an in vivo metastasis model.EBI Ghent University
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
26115571 38 Cyclin dependent kinase (CDK) inhibitors as anticancer drugs.EBI Eli Lilly and Company
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
25982075 18 Discovery of biphenyl-aryl ureas as novel VEGFR-2 inhibitors. Part 4: exploration of diverse hinge-binding fragments.EBI Xi'an Jiaotong University
25965804 80 Discovery of 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumor cells.EBI Eli Lilly and Company
26081023 55 Identification of a potent 5-phenyl-thiazol-2-ylamine-based inhibitor of FLT3 with activity against drug resistance-conferring point mutations.EBI National Health Research Institutes
26071861 14 Indoline ureas as potential anti-hepatocellular carcinoma agents targeting VEGFR-2: Synthesis, inávitro biological evaluation and molecular docking.EBI Egyptian Russian University
25980912 41 Design of selective PI3Ka inhibitors starting from a promiscuous pan kinase scaffold.EBI AstraZeneca
26121481 37 Discovery of Highly Isoform Selective Thiazolopiperidine Inhibitors of Phosphoinositide 3-Kinase┐.EBI Vertex Pharmaceuticals Inc.
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
22983304 4 Metabolic chiral inversion of brivanib and its relevance to safety and pharmacology.EBI Bristol-Myers Squibb
21289073 8 Metabolism and disposition of [14C]brivanib alaninate after oral administration to rats, monkeys, and humans.EBI Bristol-Myers Squibb
25908516 10 Design, synthesis and biological evaluation of deuterated Tivozanib for improving pharmacokinetic properties.EBI Sichuan University
25763473 108 The Discovery of Orally Bioavailable Tyrosine Threonine Kinase (TTK) Inhibitors: 3-(4-(heterocyclyl)phenyl)-1H-indazole-5-carboxamides as Anticancer Agents.EBI EntreMed Inc.
25743214 12 LEADOPT: an automatic tool for structure-based lead optimization, and its application in structural optimizations of VEGFR2 and SYK inhibitors.EBI Sichuan University
25474320 10 Nintedanib: from discovery to the clinic.EBI Boehringer Ingelheim Pharma GmbH & Co. KG
25882519 45 The design, synthesis and biological evaluation of conformationally restricted 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multi-targeted receptor tyrosine kinase and microtubule inhibitors as potential antitumor agents.EBI Duquesne University
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.
25637123 29 Discovery of biphenyl-based VEGFR-2 inhibitors. Part 3: design, synthesis and 3D-QSAR studies.EBI Xi'an Jiaotong University
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
25461318 8 Design, synthesis and evaluation of novel 2-(1H-imidazol-2-yl) pyridine Sorafenib derivatives as potential BRAF inhibitors and anti-tumor agents.EBI China Pharmaceutical University
25086238 13 Design, synthesis and biological evaluation of novel thieno[3,2-d]pyrimidine derivatives containing diaryl urea moiety as potent antitumor agents.EBI Shenyang Pharmaceutical University
25064347 22 Discovery of N-(2-phenyl-1H-benzo[d]imidazol-5-yl)quinolin-4-amine derivatives as novel VEGFR-2 kinase inhibitors.EBI China Pharmaceutical University
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
25022204 78 Discovery of (7-aryl-1,5-naphthyridin-2-yl)ureas as dual inhibitors of ERK2 and Aurora B kinases with antiproliferative activity against cancer cells.EBI Universit£ de Nantes
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
24867403 156 The discovery of Polo-like kinase 4 inhibitors: design and optimization of spiro[cyclopropane-1,3'[3H]indol]-2'(1'H).ones as orally bioavailable antitumor agents.EBI EntreMed Inc.
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
24583357 4 Recent advances in the structural library of functionalized quinazoline and quinazolinone scaffolds: synthetic approaches and multifarious applications.EBI Quaid-i-Azam University
25589937 3 Distinct binding mode of multikinase inhibitor lenvatinib revealed by biochemical characterization.EBI Eisai Co., Ltd
25467150 5 Novel benzothiazinones (BTOs) as allosteric modulator or substrate competitive inhibitor of glycogen synthase kinase 3▀ (GSK-3▀) with cellular activity of promoting glucose uptake.EBI Fudan University
25462265 2 Design, synthesis and in vitro antitumor activity of novel N-substituted-4-phenyl/benzylphthalazin-1-ones.EBI Egyptian Russian University
25462247 20 In vitro and in vivo characterization of a benzofuran derivative, a potential anticancer agent, as a novel Aurora B kinase inhibitor.EBI Fudan University
25440879 13 Design, synthesis and biological evaluation of novel thieno[3,2-d]pyrimidine derivatives possessing diaryl semicarbazone scaffolds as potent antitumor agents.EBI Shenyang Pharmaceutical 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)
25383627 85 Discovery of selective and noncovalent diaminopyrimidine-based inhibitors of epidermal growth factor receptor containing the T790M resistance mutation.EBI Genentech Inc.
25305330 75 Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.EBI Southeast University
24890652 44 The design and discovery of water soluble 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multitargeted receptor tyrosine kinase inhibitors and microtubule targeting antitumor agents.EBI Duquesne University
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
24904961 27 Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents.EBI Qilu Pharmaceutical Co, Ltd
24900886 66 Discovery of a New Series of Naphthamides as Potent VEGFR-2 Kinase Inhibitors.EBI Chinese Academy of Sciences
24900865 7 Discovery of antitubulin agents with antiangiogenic activity as single entities with multitarget chemotherapy potential.EBI Duquesne University
24786585 200 Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-▀ type I receptor kinase as cancer immunotherapeutic/antifibrotic agent.EBI Ewha Womans University
24779514 128 Discovery of GS-9973, a selective and orally efficacious inhibitor of spleen tyrosine kinase.EBI Gilead Sciences, Inc.
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
24601669 5 Potential anti-angiogenesis effects of p-terphenyl compounds from Polyozellus multiplex.EBI Meiji Pharmaceutical University
24565969 69 Design, synthesis and biological evaluation of novel 6-alkenylamides substituted of 4-anilinothieno[2,3-d]pyrimidines as irreversible epidermal growth factor receptor inhibitors.EBI Chinese Academy of Sciences
24424304 10 Recent progress in the identification of BRAF inhibitors as anti-cancer agents.EBI Cairo University
24368209 7 A development of chimeric VEGFR2 TK inhibitor based on two ligand conformers from PDB: 1Y6A complex--medicinal chemistry consequences of a TKs analysis.EBI Comenius University
24359159 60 Discovery of 1-methyl-1H-imidazole derivatives as potent Jak2 inhibitors.EBI AstraZeneca
23498918 41 Discovery of N-[5-({2-[(cyclopropylcarbonyl)amino]imidazo[1,2-b]pyridazin-6-yl}oxy)-2-methylphenyl]-1,3-dimethyl-1H-pyrazole-5-carboxamide (TAK-593), a highly potent VEGFR2 kinase inhibitor.EBI Takeda Pharmaceutical Company Limited
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
23550937 72 Monocarbonyl curcumin analogues: heterocyclic pleiotropic kinase inhibitors that mediate anticancer properties.EBI Emory University
23434139 47 Synthesis and biological activity of 5-chloro-N4-substituted phenyl-9H-pyrimido[4,5-b]indole-2,4-diamines as vascular endothelial growth factor receptor-2 inhibitors and antiangiogenic agents.EBI Duquesne University
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
23375090 54 N2-Trimethylacetyl substituted and unsubstituted-N4-phenylsubstituted-6-(2-pyridin-2-ylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines: design, cellular receptor tyrosine kinase inhibitory activities and in vivo evaluation as antiangiogenic, antimetastatic and antitumor agents.EBI Duquesne University
23362959 72 Structure-activity relationship studies of pyrazolo[3,4-d]pyrimidine derivatives leading to the discovery of a novel multikinase inhibitor that potently inhibits FLT3 and VEGFR2 and evaluation of its activity against acute myeloid leukemia in vitro and in vivo.EBI Sichuan University
23249297 75 Trimeric hemibastadin congener from the marine sponge Ianthella basta.EBI Heinrich-Heine University
23391364 78 Design, modification and 3D QSAR studies of novel naphthalin-containing pyrazoline derivatives with/without thiourea skeleton as anticancer agents.EBI Nanjing University
23265875 78 Design and synthesis of tricyclic cores for kinase inhibition.EBI Abbott Bioresearch Center
23312472 129 Highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.EBI Pfizer Inc.
22929232 89 Synthesis and optimization of substituted furo[2,3-d]-pyrimidin-4-amines and 7H-pyrrolo[2,3-d]pyrimidin-4-amines as ACK1 inhibitors.EBI Amgen Inc.
22765894 223 The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors.EBI Exelixis
22612866 123 Protein-ligand crystal structures can guide the design of selective inhibitors of the FGFR tyrosine kinase.EBI AstraZeneca
19081278 81 Molecular modeling studies of vascular endothelial growth factor receptor tyrosine kinase inhibitors using QSAR and docking.EBI Lanzhou University
17293140 160 3D QSAR studies on a series of potent and high selective inhibitors for three kinases of RTK family.EBI Dalian University
17194588 92 N-(3-Cyano-4,5,6,7-tetrahydro-1-benzothien-2-yl)amides as potent, selective, inhibitors of JNK2 and JNK3.EBI GlaxoSmithKline R&D
23124213 4 Novel 1,4-benzoxazine and 1,4-benzodioxine inhibitors of angiogenesis.EBI University of Ljubljana
23127890 96 SAR and in vivo evaluation of 4-aryl-2-aminoalkylpyrimidines as potent and selective Janus kinase 2 (JAK2) inhibitors.EBI Exelixis
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
23117174 74 5-(1,3-Benzothiazol-6-yl)-4-(4-methyl-1,3-thiazol-2-yl)-1H-imidazole derivatives as potent and selective transforming growth factor-ß type I receptor inhibitors.EBI Taisho Pharmaceutical Co., Ltd
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
21381769 56 Macrocycles are great cycles: applications, opportunities, and challenges of synthetic macrocycles in drug discovery.EBI Universite£ de Sherbrooke
23151054 15 Rational design of highly selective spleen tyrosine kinase inhibitors.EBI Hoffmann-La Roche Inc.
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
23088521 12 Novel 3-Azaindolyl-4-arylmaleimides exhibiting potent antiangiogenic efficacy, protein kinase inhibition, and antiproliferative activity.EBI Johannes Gutenberg University of Mainz
23039927 44 Multitargeted drug development: Discovery and profiling of dihydroxy substituted 1-aza-9-oxafluorenes as lead compounds targeting Alzheimer disease relevant kinases.EBI Martin-Luther University Halle-Wittenberg
22780961 3 Predicting new indications for approved drugs using a proteochemometric method.EBI Georgetown University Medical Center
22694093 16 Life beyond kinases: structure-based discovery of sorafenib as nanomolar antagonist of 5-HT receptors.EBI National Institute of Biological Sciences
23025996 4 Identification of novel 3,5-diarylpyrazoline derivatives containing salicylamide moiety as potential anti-melanoma agents.EBI Nanjing University
22548342 210 Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase¿ inhibitors.EBI Exelixis
23131541 2 Synthesis, in silico, in vitro, and in vivo investigation of 5-[¹¹C]methoxy-substituted sunitinib, a tyrosine kinase inhibitor of VEGFR-2.EBI Universidad de Talca
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
22901387 18 Discovery of 6-substituted 4-anilinoquinazolines with dioxygenated rings as novel EGFR tyrosine kinase inhibitors.EBI Nanjing University
22863529 31 Discovery of novel 2-aminopyridine-3-carboxamides as c-Met kinase inhibitors.EBI Chinese Academy of Sciences
22853993 18 A combined targeted/phenotypic approach for the identification of new antiangiogenics agents active on a zebrafish model: from in silico screening to cyclodextrin formulation.EBI University of Siena
22695126 98 Pyrazole diaminopyrimidines as dual inhibitors of KDR and Aurora B kinases.EBI Abbott Laboratories
22727637 85 Exploration of diverse hinge-binding scaffolds for selective Aurora kinase inhibitors.EBI Abbott Laboratories
22726931 113 3-Phenyl-1H-5-pyrazolylamine-based derivatives as potent and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3).EBI National Health Research Institutes
22444679 2 Radioiodinated sunitinib as a potential radiotracer for imaging angiogenesis-radiosynthesis and first radiopharmacological evaluation of 5-[125I]Iodo-sunitinib.EBI Helmholtz-Zentrum Dresden-Rossendorf eV
22749281 1 Synthesis and in vitro evaluation of [18F](R)-FEPAQ: a potential PET ligand for VEGFR2.EBI Columbia University College of Physicians and Surgeons
22739090 86 Novel tricyclic indeno[2,1-d]pyrimidines with dual antiangiogenic and cytotoxic activities as potent antitumor agents.EBI Duquesne University
22738639 6 Contribution of indazolinone tautomers to kinase activity.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
22560627 70 2-Anilino-4-(benzimidazol-2-yl)pyrimidines--a multikinase inhibitor scaffold with antiproliferative activity toward cancer cell lines.EBI Technische Universit£t Braunschweig
22542012 155 The design, synthesis, and biological evaluation of PIM kinase inhibitors.EBI Exelixis
22236250 16 Exploring activity cliffs in medicinal chemistry.EBI Rheinische Friedrich-Wilhelms-Universit£t
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.
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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
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19321350 12 Structure-based virtual screening of Src kinase inhibitors.EBI Konkuk University
19317452 155 Discovery of 4-(benzylaminomethylene)isoquinoline-1,3-(2H,4H)-diones and 4-[(pyridylmethyl)aminomethylene]isoquinoline-1,3-(2H,4H)-diones as potent and selective inhibitors of the cyclin-dependent kinase 4.EBI Wyeth Research
19301902 104 Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases.EBI University of Regensburg
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.
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19110422 12 5-Substituted pyrido[2,3-d]pyrimidine, an inhibitor against three receptor tyrosine kinases.EBI Mahidol University
19109024 5 Synthesis of novel 1,4-benzoxazin-3-one derivatives as inhibitors against tyrosine kinases.EBI Santen Pharmaceutical Co. Ltd
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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
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18815050 34 4-Anilino-7-alkenylquinoline-3-carbonitriles as potent MEK1 kinase inhibitors.EBI Wyeth Research
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18678484 57 A novel 5-[1,3,4-oxadiazol-2-yl]-N-aryl-4,6-pyrimidine diamine having dual EGFR/HER2 kinase activity: design, synthesis, and biological activity.EBI Johnson & Johnson Pharmaceutical Research and Development
18676144 93 Discovery of imidazole vinyl pyrimidines as a novel class of kinase inhibitors which inhibit Tie-2 and are orally bioavailable.EBI AstraZeneca
18640036 71 Synthesis and evaluation of heteroaryl-ketone derivatives as a novel class of VEGFR-2 inhibitors.EBI ImClone Systems Inc
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18606543 68 2-Alkenylthieno[2,3-b]pyridine-5-carbonitriles: Potent and selective inhibitors of PKCtheta.EBI Wyeth Research
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18557606 64 7-Aminopyrazolo[1,5-a]pyrimidines as potent multitargeted receptor tyrosine kinase inhibitors.EBI Abbott Laboratories
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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
18524423 16 Design, synthesis and characterization of N9/N7-substituted 6-aminopurines as VEGF-R and EGF-R inhibitors.EBI Eberhard-Karls-University
18501615 2 A peptoid antagonist of VEGF receptor 2 recognizes a 'hotspot' in the extracellular domain distinct from the hormone-binding site.EBI University of Texas Southwestern Medical Center
18467105 71 Design, synthesis and biological evaluation of substituted pyrrolo[2,3-d]pyrimidines as multiple receptor tyrosine kinase inhibitors and antiangiogenic agents.EBI Duquesne University
18447379 96 Discovery of aryl aminoquinazoline pyridones as potent, selective, and orally efficacious inhibitors of receptor tyrosine kinase c-Kit.EBI Amgen Inc
18313174 26 Synthesis and biological evaluation of diversely substituted indolin-2-ones.EBI Université Blaise Pascal
17197699 3 Structure and regulation of the human Nek2 centrosomal kinase.EBI University of Oxford
17185414 30 Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK.EBI Genomics Institute of the Novartis Research Foundation
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18289854 44 Identification of pyrrolo[2,1-f][1,2,4]triazine-based inhibitors of Met kinase.EBI Bristol-Myers Squibb Research and Development
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17983745 4 Discovery of indenopyrazoles as EGFR and VEGFR-2 tyrosine kinase inhibitors by in silico high-throughput screening.EBI Gakushuin University
17869515 30 Discovery of N-phenyl nicotinamides as potent inhibitors of Kdr.EBI Amgen
17869514 20 Neutral 5-substituted 4-anilinoquinazolines as potent, orally active inhibitors of erbB2 receptor tyrosine kinase.EBI AstraZeneca
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17826092 37 Optimization of triarylimidazoles for Tie2: influence of conformation on potency.EBI GlaxoSmithKline
17658776 109 Design, synthesis, and biological activity of 5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-one-based potent and selective Chk-1 inhibitors.EBI Abbott Laboratories
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
17574417 98 SAR of a novel 'Anthranilamide Like' series of VEGFR-2, multi protein kinase inhibitors for the treatment of cancer.EBI Bayer Research Center
17574416 39 Design, synthesis, and evaluation of 3,4-disubstituted pyrazole analogues as anti-tumor CDK inhibitors.EBI Johnson & Johnson Pharmaceutical Research & Development L.L.C.
17532631 105 Synthesis and evaluation of pyrazolo[3,4-b]pyridine CDK1 inhibitors as anti-tumor agents.EBI Johnson & Johnson Pharmaceutical Research & Development L.L.C.
17481894 64 4-Aryl-5-cyano-2-aminopyrimidines as VEGF-R2 inhibitors: synthesis and biological evaluation.EBI Johnson & Johnson Pharmaceutical Research and Development
17481893 146 Novel inhibitors of VEGF receptors-1 and -2 based on azole-5-carboxamide templates.EBI Chemical Diversity, Inc.
17425296 161 1,4-Dihydroindeno[1,2-c]pyrazoles with acetylenic side chains as novel and potent multitargeted receptor tyrosine kinase inhibitors with low affinity for the hERG ion channel.EBI Abbott Laboratories
17391959 100 Synthesis and biological evaluation of 5-substituted 1,4-dihydroindeno[1,2-c]pyrazoles as multitargeted receptor tyrosine kinase inhibitors.EBI Abbott Laboratories
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17343372 143 Discovery of N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea (ABT-869), a 3-aminoindazole-based orally active multitargeted receptor tyrosine kinase inhibitor.EBI Abbott Laboratories
17317182 36 Synthesis and biological study of 2-amino-4-aryl-5-chloropyrimidine analogues as inhibitors of VEGFR-2 and cyclin dependent kinase 1 (CDK1).EBI Johnson & Johnson Pharmaceutical Research & Development
17289388 8 Evaluation of the anti-hepatitis C virus effect of novel potent, selective, and orally bioavailable JNK and VEGFR kinase inhibitors.EBI Tibotec BVBA
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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
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17234412 1 Synthesis of 3-(1H-benzimidazol-2-yl)-5-isoquinolin-4-ylpyrazolo[1,2-b]pyridine, a potent cyclin dependent kinase 1 (CDK1) inhibitor.EBI Johnson & Johnson Pharmaceutical Research & Development L. L. C.
17234410 82 Discovery of thienopyridines as Src-family selective Lck inhibitors.EBI Abbott Bioresearch Center
17188873 225 ortho-Substituted azoles as selective and dual inhibitors of VEGF receptors 1 and 2.EBI Chemical Diversity, Inc.
17188869 53 Thienopyridine urea inhibitors of KDR kinase.EBI Abbott Laboratories
17188862 27 Inhibition of Src kinase activity by 7-ethynyl-4-phenylamino-3-quinolinecarbonitriles: identification of SKS-927.EBI Wyeth Research
17149885 20 Profile and molecular modeling of 3-(indole-3-yl)-4-(3,4,5-trimethoxyphenyl)-1 H-pyrrole-2,5-dione (1) as a highly selective VEGF-R2/3 inhibitor.EBI Eberhard Karls University
17027260 41 Design and effective synthesis of novel templates, 3,7-diphenyl-4-amino-thieno and furo-[3,2-c]pyridines as protein kinase inhibitors and in vitro evaluation targeting angiogenetic kinases.EBI GlaxoSmithKline K.K.
16970394 147 Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity.EBI Amgen, Inc.
16931012 61 Discovery and preliminary structure-activity relationship studies of novel benzotriazine based compounds as Src inhibitors.EBI TargeGen, Inc.
16893647 1 Synthesis and biological evaluation of benzamides and benzamidines as selective inhibitors of VEGFR tyrosine kinases.EBI Gakushuin University
16890434 64 Novel C-3 N-urea, amide, and carbamate dihydroindazolo[5,4-a]pyrrolo[3,4-c]carbazole analogs as potent TIE-2 and VEGF-R2 dual inhibitors.EBI Cephalon, Inc.
16887347 88 Novel tricyclic azepine derivatives: Biological evaluation of pyrimido[4,5-b]-1,4-benzoxazepines, thiazepines, and diazepines as inhibitors of the epidermal growth factor receptor tyrosine kinase.EBI ImClone Systems Inc
16789733 41 Discovery and evaluation of N-cyclopropyl- 2,4-difluoro-5-((2-(pyridin-2-ylamino)thiazol-5- ylmethyl)amino)benzamide (BMS-605541), a selective and orally efficacious inhibitor of vascular endothelial growth factor receptor-2.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
16759855 130 1,4-Dihydroindeno[1,2-c]pyrazoles as novel multitargeted receptor tyrosine kinase inhibitors.EBI Abbott Laboratories
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
16735117 50 Isothiazolopyrimidines and isoxazolopyrimidines as novel multi-targeted inhibitors of receptor tyrosine kinases.EBI Abbott Laboratories
16570908 39 Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an in vivo active potent VEGFR-2 inhibitor.EBI Pharmaceutical Research Institute
16516473 444 Novel 4-anilinoquinazolines with C-6 carbon-linked side chains: synthesis and structure-activity relationship of a series of potent, orally active, EGF receptor tyrosine kinase inhibitors.EBI Centre de Recherches
16480264 7 Design, synthesis, and biological evaluation of 3,4-diarylmaleimides as angiogenesis inhibitors.EBI Johannes Gutenberg-University
16460933 19 Structure-guided identification of novel VEGFR-2 kinase inhibitors via solution phase parallel synthesis.EBI Cephalon, Inc.
16386418 15 Arylphthalazines. Part 2: 1-(Isoquinolin-5-yl)-4-arylamino phthalazines as potent inhibitors of VEGF receptors I and II.EBI ImClone Systems
16368234 26 Potent 2-[(pyrimidin-4-yl)amine}-1,3-thiazole-5-carbonitrile-based inhibitors of VEGFR-2 (KDR) kinase.EBI Merck Research Laboratories
16364640 79 2-((1H-Azol-1-yl)methyl)-N-arylbenzamides: novel dual inhibitors of VEGFR-1/2 kinases.EBI Chemical Diversity Inc.
16321531 86 Hetaryl imidazoles: a novel dual inhibitors of VEGF receptors I and II.EBI Chemical Diversity, Inc.
16321529 30 Naphthofuroquinone derivatives: inhibition of receptor tyrosine kinases.EBI Korea Research Institute of Chemical Technology
16302797 232 2-(Quinazolin-4-ylamino)-[1,4]benzoquinones as covalent-binding, irreversible inhibitors of the kinase domain of vascular endothelial growth factor receptor-2.EBI Wyeth Research
16216503 5 Synthesis of a novel biotin-tagged photoaffinity probe for VEGF receptor tyrosine kinases.EBI Korea Research Institute of Chemical Technology
16216502 119 Scaffold oriented synthesis. Part 1: Design, preparation, and biological evaluation of thienopyrazoles as kinase inhibitors.EBI Abbott Laboratories
16216497 67 Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection.EBI Abbott Bioresearch Center
16203139 46 New heterocyclic analogues of 4-(2-chloro-5-methoxyanilino)quinazolines as potent and selective c-Src kinase inhibitors.EBI Centre de Recherches
16198560 19 Pyrimido-oxazepine as a versatile template for the development of inhibitors of specific kinases.EBI ImClone Systems Inc
16143524 46 Arylphthalazines: identification of a new phthalazine chemotype as inhibitors of VEGFR kinase.EBI ImClone Systems
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
16107139 12 Indolin-2-ones with high in vivo efficacy in a model for multiple sclerosis.EBI LEO Pharma A/S
15999992 25 Synthesis and identification of [1,3,5]triazine-pyridine biheteroaryl as a novel series of potent cyclin-dependent kinase inhibitors.EBI Johnson & Johnson Pharmaceutical Research and Development
15943473 136 Design, synthesis, and evaluation of orally active 4-(2,4-difluoro-5-(methoxycarbamoyl)phenylamino)pyrrolo[2,1-f][1,2,4]triazines as dual vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 inhibitors.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
15916429 11 Synthesis, modeling, and in vitro activity of (3'S)-epi-K-252a analogues. Elucidating the stereochemical requirements of the 3'-sugar alcohol on trkA tyrosine kinase activity.EBI Cephalon, Inc.
15771417 48 2-Hydroxy-4,6-diamino-[1,3,5]triazines: a novel class of VEGF-R2 (KDR) tyrosine kinase inhibitors.EBI Johnson & Johnson Pharmaceutical Research and Development
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.
15713401 21 Synthesis and SAR of 4-(3-hydroxyphenylamino)pyrrolo[2,1-f][1,2,4]triazine based VEGFR-2 kinase inhibitors.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
15711537 653 A small molecule-kinase interaction map for clinical kinase inhibitors.EBI Ambit Biosciences
15615512 21 Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
15566298 34 The discovery of orally active triaminotriazine aniline amides as inhibitors of p38 MAP kinase.EBI Bristol-Myers Squibb
15546730 9 Discovery of novel 2-(aminoheteroaryl)-thiazole-5-carboxamides as potent and orally active Src-family kinase p56(Lck) inhibitors.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
15482913 16 A 13C NMR approach to categorizing potential limitations of alpha,beta-unsaturated carbonyl systems in drug-like molecules.EBI Abbott Bioresearch Center
15267243 18 Discovery of the pyrrolo[2,1-f][1,2,4]triazine nucleus as a new kinase inhibitor template.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
15177482 86 Novel p38 inhibitors with potent oral efficacy in several models of rheumatoid arthritis.EBI Novartis Institutes for BioMedical Research
15109663 26 A-420983: a potent, orally active inhibitor of lck with efficacy in a model of transplant rejection.EBI Abbott Bioresearch Center
15012985 31 Orally active anti-proliferation agents: novel diphenylamine derivatives as FGF-R2 autophosphorylation inhibitors.EBI Kirin Brewery Co., Ltd.
14684325 154 Design and synthesis of aminopropyl tetrahydroindole-based indolin-2-ones as selective and potent inhibitors of Src and Yes tyrosine kinase.EBI SUGEN, Inc.
14640546 46 A new class of potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: structure-activity relationships for a series of 9-alkoxymethyl-12-(3-hydroxypropyl)indeno[2,1-a]pyrrolo[3,4-c]carbazole-5-ones and the identification of CEP-5214 and its dimethylglycine ester prodrug clinEBI Cephalon, Inc
14592495 58 Discovery and initial SAR of 2-amino-5-carboxamidothiazoles as inhibitors of the Src-family kinase p56(Lck).EBI Bristol-Myers Squibb Pharmaceutical Research Institute
12941331 90 Macrocyclic bisindolylmaleimides as inhibitors of protein kinase C and glycogen synthase kinase-3.EBI Johnson & Johnson Pharmaceutical Research & Development
12941313 18 Identification of a new chemical class of potent angiogenesis inhibitors based on conformational considerations and database searching.EBI Novartis Pharma AG
12825933 17 Development of natural product-derived receptor tyrosine kinase inhibitors based on conservation of protein domain fold.EBI Institut für molekulare Physiologie
12270156 6 Synthesis and kinase inhibitory activity of 3'-(S)-epi-K-252a.EBI Cephalon, Inc.
12086491 116 Potent and selective inhibitors of platelet-derived growth factor receptor phosphorylation. 1. Synthesis, structure-activity relationship, and biological effects of a new class of quinazoline derivatives.EBI Pharmaceutical Research Institute
12039590 50 Pyrrolo[2,3-d]pyrimidines containing diverse N-7 substituents as potent inhibitors of Lck.EBI Abbott Bioresearch Center
11934592 20 Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor.EBI Merck Research Laboratories
11012022 92 Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck II.EBI BASF Bioresearch Corporation
11012021 59 Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck I.EBI BASF Bioresearch Corporation
10853665 104 Substituted 5,7-diphenyl-pyrrolo[2,3d]pyrimidines: potent inhibitors of the tyrosine kinase c-Src.EBI Novartis Pharma AG
20222760 61 Quinazoline-urea, new protein kinase inhibitors in treatment of prostate cancer.BDB UniversitÚ Lille Nord de France
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
27388635 2 5-Benzylidene-2,4-thiazolidenedione derivatives: Design, synthesis and evaluation as inhibitors of angiogenesis targeting VEGR-2.BDB Bharati Vidyapeeth's College of Pharmacy
26669707 22 Discovery of 1,3-Diaryl-pyridones as Potent VEGFR-2 Inhibitors: Design, Synthesis, and Biological Evaluation.BDB East China University of Science & Technology
26032487 92 Discovery of new 4-alkoxyquinazoline-based derivatives as potent VEGFR2 inhibitors.BDB Nanjing University
25899678 1 Discovery of novel tricyclic pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-amine derivatives as VEGFR-2 inhibitors.BDB Suez Canal 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
24922538 5 Design, synthesis and biological evaluation of type-II VEGFR-2 inhibitors based on quinoxaline scaffold.BDB Ain Shams University, Abassia, Cairo 11566, Egypt.
24119291 26 Design, synthesis and biological evaluation of pazopanib derivatives as antitumor agents.BDB Shandong Institute of Pharmaceutical Industry, Ji'nan, Shandong, 250101, China.
23534475 27 De novo design of protein kinase inhibitors by in silico identification of hinge region-binding fragments.BDB University of Dundee
17539825 74 1H-1,2,4-triazol-3-yl-anilines: novel potent inhibitors of vascular endothelial growth factor receptors 1 and 2.BDB ChemDiv Inc.
19199284 24 Development and biological evaluation of a novel aurora A kinase inhibitor.BDB Parc de Recerca Biomedica de Barcelona
15742375 56 From the insoluble dye indirubin towards highly active, soluble CDK2-inhibitors.BDB Schering AG
15696596 33 Inhibition of angiogenesis-relevant receptor tyrosine kinases by sulindac analogues.BDB Max-Planck-Institut für Molekulare Physiologie
17441906 10 The discovery of novel vascular endothelial growth factor receptor tyrosine kinases inhibitors: pharmacophore modeling, virtual screening and docking studies.BDB Shanghai Jiaotong University
20338520 24 A structure-guided approach to creating covalent FGFR inhibitors.BDB Harvard Medical School
20020776 56 In vivo structure-activity relationship study of dorsomorphin analogues identifies selective VEGF and BMP inhibitors.BDB Vanderbilt University
19764794 60 Selective inhibitors of the mutant B-Raf pathway: discovery of a potent and orally bioavailable aminoisoquinoline.BDB Amgen
19748785 115 Design, synthesis, and X-ray crystal structures of 2,4-diaminofuro[2,3-d]pyrimidines as multireceptor tyrosine kinase and dihydrofolate reductase inhibitors.BDB Duquesne University
18620382 41 Discovery of 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methyl-benzenesulfonamide (Pazopanib), a novel and potent vascular endothelial growth factor receptor inhibitor.BDB GSK
18321037 129 Structure-guided design of aminopyrimidine amides as potent, selective inhibitors of lymphocyte specific kinase: synthesis, structure-activity relationships, and inhibition of in vivo T cell activation.BDB Amgen
18287029 12 Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity.BDB Plexxikon
18714982 44 Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-lineage kinase 1 crystallography, and oral in vivo activity in 1-methyl-4-phenyltetrahydropyridine models.BDB Cephalon
16951187 11 AMG 706, an oral, multikinase inhibitor that selectively targets vascular endothelial growth factor, platelet-derived growth factor, and kit receptors, potently inhibits angiogenesis and induces regression in tumor xenografts.BDB Amgen
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.
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
18260617 131 3-Amino-benzo[d]isoxazoles as Novel Multitargeted Inhibitors of Receptor Tyrosine Kinases.BDB Abbott Laboratories
17676829 78 Discovery of Novel Benzimidazoles as Potent Inhibitors of TIE-2 and VEGFR-2 Tyrosine Kinase Receptors.BDB GSK
16884310 97 Novel 2-aminopyrimidine carbamates as potent and orally active inhibitors of Lck: synthesis, SAR, and in vivo antiinflammatory activity.BDB Amgen
17276681 42 Discovery of novel 2,3-diarylfuro[2,3-b]pyridin-4-amines as potent and selective inhibitors of Lck: synthesis, SAR, and pharmacokinetic properties.BDB Amgen
17696416 45 Design, Synthesis, and Evaluation of Orally Active Benzimidazoles and Benzoxazoles as Vascular Endothelial Growth Factor-2 Receptor Tyrosine Kinase Inhibitors.BDB Amgen
15466206 10 BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis.BDB Bayer Pharmaceuticals Corporation
17276055 17 Orally active 4-amino-5-diarylurea-furo[2,3-d]pyrimidine derivatives as anti-angiogenic agent inhibiting VEGFR2 and Tie-2.BDB GlaxoSmithKline
17253678 70 Evolution of a highly selective and potent 2-(pyridin-2-yl)-1,3,5-triazine Tie-2 kinase inhibitor.BDB Amgen
17253679 69 Alkynylpyrimidine amide derivatives as potent, selective, and orally active inhibitors of Tie-2 kinase.BDB Amgen
17064066 70 N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5-(tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor.BDB AstraZeneca
16460936 82 Inhibitors of VEGF receptors-1 and -2 based on the 2-((pyridin-4-yl)ethyl)pyridine template.BDB Chemical Diversity, Inc
16275072 70 N-(Aryl)-4-(azolylethyl)thiazole-5-carboxamides: novel potent inhibitors of VEGF receptors I and II.BDB Chemical Diversity, Inc
16162008 146 Thienopyrimidine ureas as novel and potent multitargeted receptor tyrosine kinase inhibitors.BDB Abbott Laboratories
12039591 63 Pyrazolo[3,4-d]pyrimidines containing an extended 3-substituent as potent inhibitors of Lck - a selectivity insight.BDB Abbott Bioresearch Center
15225695 64 4-Acylamino-6-arylfuro[2,3-d]pyrimidines: potent and selective glycogen synthase kinase-3 inhibitors.BDB Tsukuba Research Laboratories
12749903 69 Novel pyrrolyllactone and pyrrolyllactam indolinones as potent cyclin-dependent kinase 2 inhibitors.BDB SUGEN, Inc.
14761189 54 Discovery of a new class of anilinoquinazoline inhibitors with high affinity and specificity for the tyrosine kinase domain of c-Src.BDB AstraZeneca
16000000 188 Synthesis and structure-activity relationships of soluble 7-substituted 3-(3,5-dimethoxyphenyl)-1,6-naphthyridin-2-amines and related ureas as dual inhibitors of the fibroblast growth factor receptor-1 and vascular endothelial growth factor receptor-2 tyrosine kinases.BDB University of Auckland
15357981 39 Isoindolinone ureas: a novel class of KDR kinase inhibitors.BDB Abbott Laboratories
15743202 37 Discovery and evaluation of 2-anilino-5-aryloxazoles as a novel class of VEGFR2 kinase inhibitors.BDB GlaxoSmithKline
15990302 20 Discovery of a novel and potent series of dianilinopyrimidineurea and urea isostere inhibitors of VEGFR2 tyrosine kinase.BDB GlaxoSmithKline
15837294 36 Novel 4-amino-furo[2,3-d]pyrimidines as Tie-2 and VEGFR2 dual inhibitors.BDB GlaxoSmithKline
12217372 23 Synthesis and initial SAR studies of 3,6-disubstituted pyrazolo[1,5-a]pyrimidines: a new class of KDR kinase inhibitors.BDB Merck Research Laboratories
12729639 20 2,4-disubstituted pyrimidines: a novel class of KDR kinase inhibitors.BDB Merck Research Laboratories
12443771 19 Optimization of a pyrazolo[1,5-a]pyrimidine class of KDR kinase inhibitors: improvements in physical properties enhance cellular activity and pharmacokinetics.BDB Merck Research Laboratories
12852948 10 Design and synthesis of 1,5-diarylbenzimidazoles as inhibitors of the VEGF-receptor KDR.BDB Merck Research Laboratories
15125964 18 The discovery of N-(1,3-thiazol-2-yl)pyridin-2-amines as potent inhibitors of KDR kinase.BDB Merck Research Laboratories
14698157 19 Optimization of the indolyl quinolinone class of KDR (VEGFR-2) kinase inhibitors: effects of 5-amido- and 5-sulphonamido-indolyl groups on pharmacokinetics and hERG binding.BDB Merck Research Laboratories
12941314 17 Discovery and evaluation of 3-(5-thien-3-ylpyridin-3-yl)-1H-indoles as a novel class of KDR kinase inhibitors.BDB Merck Research Laboratories
15012992 18 Design and synthesis of 3,7-diarylimidazopyridines as inhibitors of the VEGF-receptor KDR.BDB Merck Research Laboratories
15566305 14 Potent N-(1,3-thiazol-2-yl)pyridin-2-amine vascular endothelial growth factor receptor tyrosine kinase inhibitors with excellent pharmacokinetics and low affinity for the hERG ion channel.BDB Merck Research Laboratories
12127526 75 Rational design of 4,5-disubstituted-5,7-dihydro-pyrrolo[2,3-d]pyrimidin-6-ones as a novel class of inhibitors of epidermal growth factor receptor (EGF-R) and Her2(p185(erbB)) tyrosine kinases.BDB SUGEN, Inc.
10893303 100 Identification of substituted 3-[(4,5,6, 7-tetrahydro-1H-indol-2-yl)methylene]-1,3-dihydroindol-2-ones as growth factor receptor inhibitors for VEGF-R2 (Flk-1/KDR), FGF-R1, and PDGF-Rbeta tyrosine kinases.BDB SUGEN, Inc.
10602697 92 Design, synthesis, and evaluations of substituted 3-[(3- or 4-carboxyethylpyrrol-2-yl)methylidenyl]indolin-2-ones as inhibitors of VEGF, FGF, and PDGF receptor tyrosine kinases.BDB SUGEN, Inc.
10882357 87 New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven angiogenesis.BDB Novartis Pharmaceuticals
12646019 48 Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosine kinase.BDB SUGEN, Inc.
11881999 123 Novel 4-anilinoquinazolines with C-7 basic side chains: design and structure activity relationship of a series of potent, orally active, VEGF receptor tyrosine kinase inhibitors.BDB AstraZeneca
10639280 101 Design and structure-activity relationship of a new class of potent VEGF receptor tyrosine kinase inhibitors.BDB AstraZeneca