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309 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
27789138 355 Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors.EBI AbbVie Bioresearch Center
28109791 44 Identification of a selective inhibitor of transforming growth factor▀-activated kinase 1 by biosensor-based screening of focused libraries.EBI Chugai Pharmaceutical Co., Ltd.
27966954 19 Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding.EBI High Magnetic Field Laboratory
27816515 143 Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.EBI Merck& Co.
27994749 47 Optimization of Highly Kinase Selective Bis-anilino Pyrimidine PAK1 Inhibitors.EBI AstraZeneca
27583770 82 Discovery of 6-Fluoro-5-(R)-(3-(S)-(8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)-2-methylphenyl)-2-(S)-(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro-1H-carbazole-8-carboxamide (BMS-986142): A Reversible Inhibitor of Bruton's Tyrosine Kinase (BTK) Conformationally Constrained by Two LockeEBI Bristol-Myers Squibb Research and Development
27299736 37 The"Cyclopropyl Fragment" is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules.EBI St. John's University
27491023 286 Tyrosine Kinase Inhibitors. 20. Optimization of Substituted Quinazoline and Pyrido[3,4-d]pyrimidine Derivatives as Orally Active, Irreversible Inhibitors of the Epidermal Growth Factor Receptor Family.EBI University of Auckland
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
27010810 24 Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors.EBI OriBase Pharma
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
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
26713112 36 Design of Selective PAK1 Inhibitor G-5555: Improving Properties by Employing an Unorthodox Low-pK a Polar Moiety.EBI Genentech
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
26475520 43 Targeting EGFR/HER2 tyrosine kinases with a new potent series of 6-substituted 4-anilinoquinazoline hybrids: Design, synthesis, kinase assay, cell-based assay, and molecular docking.EBI Korea University of Science and Technology (UST)
26396681 58 Discovery of RAF265: A Potent mut-B-RAF Inhibitor for the Treatment of Metastatic Melanoma.EBI Novartis Institutes for Biomedical Research
26342867 52 Discovery of 6-phenylimidazo[2,1-b]thiazole derivatives as a new type of FLT3 inhibitors.EBI Sichuan University
26320619 88 Design and synthesis of carbazole carboxamides as promising inhibitors of Bruton's tyrosine kinase (BTK) and Janus kinase 2 (JAK2).EBI Bristol-Myers Squibb Pharmaceutical Research Institute
26288682 64 Structure-Based Design of Selective Janus Kinase 2 Imidazo[4,5-d]pyrrolo[2,3-b]pyridine Inhibitors.EBI Bristol-Myers Squibb Research& Development
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
26087137 30 Fragment-Based Discovery of a Small Molecule Inhibitor of Bruton's Tyrosine Kinase.EBI Takeda California, 10410 Science Center Drive, San Diego, California 92121, United States.
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
25844760 52 Tetrahydroindazoles as Interleukin-2 Inducible T-Cell Kinase Inhibitors. Part II. Second-Generation Analogues with Enhanced Potency, Selectivity, and Pharmacodynamic Modulation in Vivo.EBI Genentech Inc.
25699576 42 Development of novel ACK1/TNK2 inhibitors using a fragment-based approach.EBI University of South Florida
25089810 79 Novel acylureidoindolin-2-one derivatives as dual Aurora B/FLT3 inhibitors for the treatment of acute myeloid leukemia.EBI National Taiwan University
24980703 296 Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors.EBI Nerviano Medical Sciences
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
25589930 62 Discovery of a Type III Inhibitor of LIM Kinase 2 That Binds in a DFG-Out Conformation.EBI Lexicon Pharmaceuticals
25369270 93 Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634.EBI Galapagos NV
25313996 91 Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase.EBI Merck Research Laboratories
25221654 39 Design and Synthesis of Orally Bioavailable Benzimidazole Reverse Amides as Pan RAF Kinase Inhibitors.EBI Novartis Institutes for Biomedical Research
24139169 175 Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.EBI Nerviano Medical Sciences
24915291 73 Discovery of a series of 2,5-diaminopyrimidine covalent irreversible inhibitors of Bruton's tyrosine kinase with in vivo antitumor activity.EBI Peking University
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
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
23301767 154 Substituted 4-(thiazol-5-yl)-2-(phenylamino)pyrimidines are highly active CDK9 inhibitors: synthesis, X-ray crystal structures, structure-activity relationship, and anticancer activities.EBI University of Nottingham
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
23253074 38 Optimization of inhibitors of the tyrosine kinase EphB4. 2. Cellular potency improvement and binding mode validation by X-ray crystallography.EBI University of Zurich
23398373 88 Design and optimization of selective protein kinase C¿ (PKC¿) inhibitors for the treatment of autoimmune diseases.EBI Vertex Pharmaceuticals (Europe) Ltd.
23312943 166 Optimization of highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.EBI Pfizer Inc.
23312472 129 Highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.EBI Pfizer Inc.
23273517 53 Synthesis and biological evaluation of analogues of the kinase inhibitor nilotinib as Abl and Kit inhibitors.EBI National Center for Advancing Translational Sciences
10741557 26 Naphthyl ketones: a new class of Janus kinase 3 inhibitors.EBI AstraZeneca
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.
21903390 79 Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor.EBI GlaxoSmithKline R&D
19303774 87 1-Aryl-3,4-dihydroisoquinoline inhibitors of JNK3.EBI GlaxoSmithKline R&D
19427202 8 Natural product inhibitors of protein-protein interactions mediated by Src-family SH2 domains.EBI Max Planck Institute of Biochemistry
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
23098265 46 Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors.EBI University of Genoa
22827572 67 Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK).EBI GlaxoSmithKline Research and Development
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.
22257213 98 Discovery and development of spleen tyrosine kinase (SYK) inhibitors.EBI Rigel, Inc.
22746295 91 Mitogen-activated protein kinase-activated protein kinase 2 (MAPKAP-K2) as an antiinflammatory target: discovery and in vivo activity of selective pyrazolo[1,5-a]pyrimidine inhibitors using a focused library and structure-based optimization approach.EBI Teijin Pharma Ltd.
22039836 188 Optimization of a potent class of arylamide colony-stimulating factor-1 receptor inhibitors leading to anti-inflammatory clinical candidate 4-cyano-N-[2-(1-cyclohexen-1-yl)-4-[1-[(dimethylamino)acetyl]-4-piperidinyl]phenyl]-1H-imidazole-2-carboxamide (JNJ-28312141).EBI Johnson& Johnson Pharmaceutical Research& Development
24900387 11 Discovery of a novel chemotype of tyrosine kinase inhibitors by fragment-based docking and molecular dynamics.EBI TBA
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
22695126 98 Pyrazole diaminopyrimidines as dual inhibitors of KDR and Aurora B kinases.EBI Abbott Laboratories
22320388 116 Development of Toxoplasma gondii calcium-dependent protein kinase 1 (TgCDPK1) inhibitors with potent anti-toxoplasma activity.EBI University of Washington
22727637 85 Exploration of diverse hinge-binding scaffolds for selective Aurora kinase inhibitors.EBI Abbott Laboratories
24900482 32 Targeted kinase selectivity from kinase profiling data.EBI TBA
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
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
22503250 128 Synthesis and SAR studies of imidazo-[1,2-a]-pyrazine Aurora kinase inhibitors with improved off-target kinase selectivity.EBI AMRI
22465635 95 Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families.EBI Abbott Laboratories
22464456 27 X-ray crystallographic structure-based design of selective thienopyrazole inhibitors for interleukin-2-inducible tyrosine kinase.EBI Sanofi US
24900358 69 Discovery and Hit-to-Lead Optimization of Non-ATP Competitive MK2 (MAPKAPK2) Inhibitors.EBI TBA
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
15975507 13 Features of selective kinase inhibitors.EBI University of California-San Francisco
18469809 41 A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity.EBI Nerviano Medical Sciences Oncology
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
20038108 19 Novel synthesis and structural characterization of a high-affinity paramagnetic kinase probe for the identification of non-ATP site binders by nuclear magnetic resonance.EBI Wyeth Research
19703774 56 C-5 substituted heteroaryl-3-pyridinecarbonitriles as PKCtheta inhibitors: part II.EBI Wyeth Research
18183025 12060 A quantitative analysis of kinase inhibitor selectivity.EBI Ambit Biosciences
17850214 99 The selectivity of protein kinase inhibitors: a further update.EBI University of Dundee
19610618 41 Inhibition of the insulin-like growth factor-1 receptor (IGF1R) tyrosine kinase as a novel cancer therapy approach.EBI University of South Florida
19397322 58 Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.EBI National Cancer Institute
19522465 102 Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120).EBI Boehringer Ingelheim Pharma GmbH&Co KG
19320489 125 Discovery and development of aurora kinase inhibitors as anticancer agents.EBI Vertex Pharmaceuticals (Europe) Ltd.
14593182 34 Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor.EBI Pfizer Global Researchand Development
18789685 172 Kinase array design, back to front: biaryl amides.EBI GlaxoSmithKline R&D
18077425 197 Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.EBI Harvard Medical School
18434148 43 Synthesis and PKCtheta inhibitory activity of a series of 4-(indol-5-ylamino)thieno[2,3-b]pyridine-5-carbonitriles.EBI Wyeth Research
18395443 37 Discovery and preclinical studies of 5-isopropyl-6-(5-methyl-1,3,4-oxadiazol-2-yl)-N-(2-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine (BMS-645737), an in vivo active potent VEGFR-2 inhibitor.EBI Bristol-Myers Squibb
17371799 12 Metabolism and pharmacokinetics of a novel Src kinase inhibitor TG100435 ([7-(2,6-dichloro-phenyl)-5-methyl-benzo[1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-amine) and its active N-oxide metabolite TG100855 ([7-(2,6-dichloro-phenyl)-5-methylbenzo[1,2,4]triazin-3-yl]-{4-[2-(1-oxy-pyrrEBI TargeGen, Inc.
17360485 10 Antitumor activity of MLN8054, an orally active small-molecule inhibitor of Aurora A kinase.EBI Millennium Pharmaceuticals Inc.
18359226 50 Pyrazolo-pyrimidines: a novel heterocyclic scaffold for potent and selective p38 alpha inhibitors.EBI Bristol-Myers Squibb Research and Development
18324761 65 Naphthamides as novel and potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: design, synthesis, and evaluation.EBI Amgen Inc.
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
17997320 29 Novel pyrazolo[1,5-a]pyrimidines as c-Src kinase inhibitors that reduce IKr channel blockade.EBI Kissei Pharmaceutical Company Ltd
17983756 55 Novel 2-phenylquinolin-7-yl-derived imidazo[1,5-a]pyrazines as potent insulin-like growth factor-I receptor (IGF-IR) inhibitors.EBI OSI Pharmaceuticals, Inc.
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.
18271520 423 Discovery of kinase inhibitors by high-throughput docking and scoring based on a transferable linear interaction energy model.EBI University of Zurich
18083554 54 N-(3-(phenylcarbamoyl)arylpyrimidine)-5-carboxamides as potent and selective inhibitors of Lck: structure, synthesis and SAR.EBI Amgen Inc.
17935989 146 Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.EBI Abbott Laboratories
17887663 34 Structure-based design and synthesis of (5-arylamino-2H-pyrazol-3-yl)-biphenyl-2',4'-diols as novel and potent human CHK1 inhibitors.EBI Pfizer Global Research and Development
17113292 73 Discovery of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine--a potent, orally active Src kinase inhibitor with anti-tumor activity in preclinical assays.EBI TargeGen, Inc.
17095233 45 Synthesis and c-Src inhibitory activity of imidazo[1,5-a]pyrazine derivatives as an agent for treatment of acute ischemic stroke.EBI Kissei Pharmaceutical Company Ltd
15115396 112 General model for estimation of the inhibition of protein kinases using Monte Carlo simulations.EBI Yale University
11931608 17 Inhibition of protein-protein association by small molecules: approaches and progress.EBI Pfizer Global Research and Development
11448224 9 Nonpeptidic, monocharged, cell permeable ligands for the p56lck SH2 domain.EBI Boehringer Ingelheim (Canada) Ltd.
10737750 7 SH2-directed ligands of the Lck tyrosine kinase.EBI The Albert Einstein College of Medicine
10346928 19 Ligands for the tyrosine kinase p56lck SH2 domain: discovery of potent dipeptide derivatives with monocharged, nonhydrolyzable phosphate replacements.EBI Boehringer Ingelheim Pharmaceuticals Inc.
11992778 26 Structure-based design of peptidomimetic antagonists of p56(lck) SH2 domain.EBI Roche Products Limited
 48 The preparation and sar of 4-(anilino), 4-(phenoxy), and 4-(thiophenoxy)-quinazolines: Inhibitors of p56lck and EGF-R tyrosine kinase activityEBI TBA
22310227 89 5-Aryl-4-carboxamide-1,3-oxazoles: potent and selective GSK-3 inhibitors.EBI GlaxoSmithKline
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
16249345 25 Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580.EBI GlaxoSmithKline
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
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.
22101132 41 Discovery of novel 5-alkynyl-4-anilinopyrimidines as potent, orally active dual inhibitors of EGFR and Her-2 tyrosine kinases.EBI Shionogi& Co., Ltd
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
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
21999461 90 1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase.EBI Rhône-Poulenc Rorer
21958547 108 Imidazo[1,5-a]quinoxalines as irreversible BTK inhibitors for the treatment of rheumatoid arthritis.EBI Pfizer Inc.
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
21855335 185 Discovery of novel imidazo[1,2-a]pyrazin-8-amines as Brk/PTK6 inhibitors.EBI Merck Research Laboratories
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.
21536449 16 Design and evaluation of 3-aminopyrazolopyridinone kinase inhibitors inspired by the natural product indirubin.EBI Institute of Cancer Research
21733693 7 Development of potent B-RafV600E inhibitors containing an arylsulfonamide headgroup.EBI GlaxoSmithKline Oncology CEDD
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
21493067 22 In vitro and in vivo evaluation of 6-aminopyrazolyl-pyridine-3-carbonitriles as JAK2 kinase inhibitors.EBI AstraZeneca R&D Boston
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
21391610 139 Discovery and structure-activity relationship of 3-aminopyrid-2-ones as potent and selective interleukin-2 inducible T-cell kinase (Itk) inhibitors.EBI Vertex Pharmaceuticals (Europe) Ltd.
21375264 77 Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally bioavailable and highly selective inhibitorsEBI Roche Palo Alto LLC
21341678 49 Design and optimization of potent and orally bioavailable tetrahydronaphthalene Raf inhibitors.EBI Millennium Pharmaceuticals, Inc.
24900250 81 Kinase Inhibition by Deoxy Analogues of the Resorcylic Lactone L-783277EBI TBA
21084189 29 Click chemistry inspired one-pot synthesis of 1,4-disubstituted 1,2,3-triazoles and their Src kinase inhibitory activity.EBI Institute of Technology and Science
21177105 38 Novel pyrrolo[2,1-f][1,2,4]triazin-4-amines: Dual inhibitors of EGFR and HER2 protein tyrosine kinases.EBI Bristol-Myers Squibb Research and Development
21035336 42 5-amino-pyrazoles as potent and selective p38a inhibitors.EBI Bristol-Myers Squibb Research and Development
20961062 42 Indazolylpyrazolopyrimidine as highly potent B-Raf inhibitors with in vivo activity.EBI Pfizer Inc.
20932747 61 The rational design of a novel potent analogue of the 5'-AMP-activated protein kinase inhibitor compound C with improved selectivity and cellular activity.EBI Ansaris
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
20817473 57 Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity.EBI Nerviano Medical Sciences-Oncology
20684549 76 Discovery of a potent, selective, and orally bioavailable pyridinyl-pyrimidine phthalazine aurora kinase inhibitor.EBI Amgen Inc.
19654408 2521 AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).EBI Ambit Biosciences
19039322 50 Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells.EBI Center for Molecular Medicine of the Austrian Academy of Sciences
18559524 21 BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy.EBI Boehringer Ingelheim Austria GmbH
16783341 34 Rational design of inhibitors that bind to inactive kinase conformations.EBI Novartis Research Foundation
20483608 139 New pyrazolo[1,5a]pyrimidines as orally active inhibitors of Lck.EBI Novartis Institute of Biomedical Research
20462263 127 Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors.EBI Cyclacel Ltd.
20459125 60 Analysis of kinase inhibitor selectivity using a thermodynamics-based partition index.EBI Amgen Inc.
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
20346655 117 Imidazo[2,1-b]thiazoles: multitargeted inhibitors of both the insulin-like growth factor receptor and members of the epidermal growth factor family of receptor tyrosine kinases.EBI Abbott Laboratories
20307980 22 B-Raf kinase inhibitors: hit enrichment through scaffold hopping.EBI Wyeth Research
20218619 44 Discovery and evaluation of 7-alkyl-1,5-bis-aryl-pyrazolopyridinones as highly potent, selective, and orally efficacious inhibitors of p38alpha mitogen-activated protein kinase.EBI Amgen Inc.
19884006 47 Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors.EBI Wyeth Research
20166671 85 Selectively nonselective kinase inhibition: striking the right balance.EBI Schering-Plough
20153643 68 Optimization of 5-vinylaryl-3-pyridinecarbonitriles as PKCtheta inhibitors.EBI Wyeth Research
19879134 94 Imidazo[1,2-a]pyrazine diaryl ureas: inhibitors of the receptor tyrosine kinase EphB4.EBI CGI Pharmaceuticals, Inc.
19854052 420 Discovery of pyrimidine benzimidazoles as Src-family selective Lck inhibitors. Part II.EBI Genomics Institute of the Novartis Research Foundation (GNF)
20148563 42 BRAF inhibitors based on an imidazo[4,5]pyridin-2-one scaffold and a meta substituted middle ring.EBI Institute of Cancer Research
20143778 70 Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.EBI Curis Inc
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
19945867 39 Ring-fused pyrazole derivatives as potent inhibitors of lymphocyte-specific kinase (Lck): Structure, synthesis, and SAR.EBI Taisho Pharmaceutical Co., Ltd
19926477 100 2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.EBI Abbott Laboratories
19762237 58 First generation 5-vinyl-3-pyridinecarbonitrile PKCtheta inhibitors.EBI Wyeth Research
19682896 49 C-5 Substituted heteroaryl 3-pyridinecarbonitriles as PKCtheta inhibitors: Part I.EBI Wyeth Research
19674899 54 Disubstituted pyrimidines as Lck inhibitors.EBI Merck Research Laboratories
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
19857964 3 Structural basis for the inhibitor recognition of human Lyn kinase domain.EBI Osaka Prefecture University
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.
19361991 80 Structure-based design and parallel synthesis of N-benzyl isatin oximes as JNK3 MAP kinase inhibitors.EBI Vertex Pharmaceuticals Inc
19427203 28 Synthetic staurosporines via a ring closing metathesis strategy as potent JAK3 inhibitors and modulators of allergic responses.EBI Johnson& Johnson Pharmaceutical Research& Development L.L.C. 920 Route 202
19362830 47 Identification of pyrazolo[1,5-a]pyrimidine-3-carboxylates as B-Raf kinase inhibitors.EBI Wyeth Research
19572547 51 9-(Arenethenyl)purines as dual Src/Abl kinase inhibitors targeting the inactive conformation: design, synthesis, and biological evaluation.EBI ARIAD Pharmaceuticals, Inc.
1479375 215 Protein-Tyrosine Kinase Inhibition: Mechanism-Based Discovery of Antitumor AgentsEBI TBA
 2 Pyrazolo[3,4-c]pyridazines as Novel and Selective Inhibitors of Cyclin-Dependent KinasesEBI TBA
 46 The synthesis and SAR of new 4-(N-alkyl-N-phenyl)amino-6,7-dimethoxyquinazolines and 4-(N-alkyl-N-phenyl)aminopyrazolo[3,4- TBA
 8 Synthesis of a series of brominated 1-phenyl-2-pyridylethenes as inhibitors of the protein-tyrosine kinase p56lckEBI TBA
 15 Arylamides of hydroxylated isoquinolines as protein-tyrosine kinase inhibitorsEBI TBA
 34 Synthesis and evaluation of new protein-tyrosine kinase inhibitors. Part 2. Phenylhydrazones.EBI TBA
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 6 Structural influences of styryl-based inhibitors on epidermal growth factor receptor and p56lck tyrosine-specific protein kinases.EBI TBA
19447612 59 Optimization of 5-phenyl-3-pyridinecarbonitriles as PKCtheta inhibitors.EBI Wyeth Research
19394221 2 Application of combinatorial biocatalysis for a unique ring expansion of dihydroxymethylzearalenone.EBI AMRI
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
19111463 46 Second generation 4-(4-methyl-1H-indol-5-ylamino)-2-phenylthieno[2,3-b]pyridine-5-carbonitrile PKCtheta inhibitors.EBI Wyeth Research
19101143 70 Discovery and optimization of imidazo[1,2-a]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R).EBI GlaxoSmithKline
19053756 27 Examining the chirality, conformation and selective kinase inhibition of 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile (CP-690,550).EBI National Human Genome Research Institute
19019675 52 Beyond the MEK-pocket: can current MEK kinase inhibitors be utilized to synthesize novel type III NCKIs? Does the MEK-pocket exist in kinases other than MEK?EBI Pfizer Global Research and Development
18993068 75 Identification and optimization of N3,N6-diaryl-1H-pyrazolo[3,4-d]pyrimidine-3,6-diamines as a novel class of ACK1 inhibitors.EBI Amgen Inc.
18977146 2 The importance of CH/pi hydrogen bonds in rational drug design: An ab initio fragment molecular orbital study to leukocyte-specific protein tyrosine (LCK) kinase.EBI Kissei Pharmaceutical Company Ltd.
18817365 73 Discovery of highly selective and potent p38 inhibitors based on a phthalazine scaffold.EBI Amgen, Inc.
18799314 8 Binding is not enough: flexibility is needed for photocrosslinking of Lck kinase by benzophenone photoligands.EBI Hunter College of CUNY
18793846 33 Discovery of pyrimidine benzimidazoles as Lck inhibitors: part I.EBI Genomics Institute of the Novartis Research Foundation (GNF)
18723346 26 Discovery of amido-benzisoxazoles as potent c-Kit inhibitors.EBI Amgen Inc.
18606543 68 2-Alkenylthieno[2,3-b]pyridine-5-carbonitriles: Potent and selective inhibitors of PKCtheta.EBI Wyeth Research
18602262 56 Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes.EBI GlaxoSmithKline R&D
18585046 32 A novel Syk family kinase inhibitor: design, synthesis, and structure-activity relationship of 1,2,4-triazolo[4,3-c]pyrimidine and 1,2,4-triazolo[1,5-c]pyrimidine derivatives.EBI Kissei Pharmaceutical Company Ltd
18554909 50 Discovery of a potent and selective c-Kit inhibitor for the treatment of inflammatory diseases.EBI Amgen Inc.
18447379 96 Discovery of aryl aminoquinazoline pyridones as potent, selective, and orally efficacious inhibitors of receptor tyrosine kinase c-Kit.EBI Amgen Inc
17897956 3 Lateral compartmentalization of T cell receptor versus CD45 by galectin-N-glycan binding and microfilaments coordinate basal and activation signaling.EBI University of California
16441060 12 A common protein fold topology shared by flavonoid biosynthetic enzymes and therapeutic targets.EBI Griffith University
18313298 40 The discovery of (R)-2-(sec-butylamino)-N-(2-methyl-5-(methylcarbamoyl)phenyl) thiazole-5-carboxamide (BMS-640994)-A potent and efficacious p38alpha MAP kinase inhibitor.EBI Bristol-Myers Squibb
18289854 44 Identification of pyrrolo[2,1-f][1,2,4]triazine-based inhibitors of Met kinase.EBI Bristol-Myers Squibb Research and Development
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
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
17350837 59 Synthesis, structural analysis, and SAR studies of triazine derivatives as potent, selective Tie-2 inhibitors.EBI Amgen Inc.
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
17280833 52 Discovery of 4-amino-5,6-biaryl-furo[2,3-d]pyrimidines as inhibitors of Lck: development of an expedient and divergent synthetic route and preliminary SAR.EBI Amgen Inc.
17270437 68 New C-5 substituted pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
17234410 82 Discovery of thienopyridines as Src-family selective Lck inhibitors.EBI Abbott Bioresearch Center
16997556 32 The development of 2-benzimidazole substituted pyrimidine based inhibitors of lymphocyte specific kinase (Lck).EBI Procter and Gamble Pharmaceuticals
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.
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
16757169 26 The development of novel 1,2-dihydro-pyrimido[4,5-c]pyridazine based inhibitors of lymphocyte specific kinase (Lck).EBI Procter and Gamble Pharmaceuticals
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
16682201 37 Development of N-4,6-pyrimidine-N-alkyl-N'-phenyl ureas as orally active inhibitors of lymphocyte specific tyrosine kinase.EBI Procter & Gamble Pharmaceuticals
16682193 62 Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
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
16366598 51 (6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad antiproliferative activity against tumor cells.EBI Johnson & Johnson Pharmaceutical Research and Development
16216497 67 Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection.EBI Abbott Bioresearch Center
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
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
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
15317461 53 Identification of 1,5-naphthyridine derivatives as a novel series of potent and selective TGF-beta type I receptor inhibitors.EBI GlaxoSmithKline
15214778 8 Identification of non-phosphate-containing small molecular weight inhibitors of the tyrosine kinase p56 Lck SH2 domain via in silico screening against the pY + 3 binding site.EBI University of Maryland
15109663 26 A-420983: a potent, orally active inhibitor of lck with efficacy in a model of transplant rejection.EBI Abbott Bioresearch Center
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.
14592495 60 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
14505648 8 Design and synthesis of small chemical inhibitors containing different scaffolds for lck SH2 domain.EBI Mogam Biotechnology Research Institute
12941342 21 Potent quinoxaline-based inhibitors of PDGF receptor tyrosine kinase activity. Part 2: the synthesis and biological activities of RPR127963 an orally bioavailable inhibitor.EBI Aventis Pharmaceuticals
12852972 79 Discovery of 2-amino-heteroaryl-benzothiazole-6-anilides as potent p56(lck) inhibitors.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
12798323 72 Molecular design, synthesis, and structure-Activity relationships leading to the potent and selective p56(lck) inhibitor BMS-243117.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
12672234 64 Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase.EBI Boehringer Ingelheim Pharmaceuticals
12482439 51 Design and synthesis of potent, orally bioavailable dihydroquinazolinone inhibitors of p38 MAP kinase.EBI Merck Research Laboratories
12372522 51 Synthesis and SAR of novel imidazoquinoxaline-based Lck inhibitors: improvement of cell potency.EBI Bristol Myers Squibb Pharmaceutical Research Institute
12217360 27 Design and characterization of non-phosphopeptide inhibitors for Src family SH2 domains.EBI Mogam Biotechnology Research Institute
12139450 29 Discovery of 2-phenylamino-imidazo[4,5-h]isoquinolin-9-ones: a new class of inhibitors of lck kinase.EBI Boehringer Ingelheim Pharmaceuticals Inc.
12086485 10 Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate.EBI Boehringer Ingelheim Pharmaceuticals
12039590 51 Pyrrolo[2,3-d]pyrimidines containing diverse N-7 substituents as potent inhibitors of Lck.EBI Abbott Bioresearch Center
11992777 46 Discovery and initial SAR of imidazoquinoxalines as inhibitors of the Src-family kinase p56(Lck).EBI Bristol Myers Squibb Pharmaceutical Research Institute
11934592 24 Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor.EBI Merck Research Laboratories
11909733 30 Beta-carbolines as specific inhibitors of cyclin-dependent kinases.EBI Institute of Molecular and Cell Biology
11714603 7 Synthesis of antitumor dendritic imides.EBI University San Pablo-CEU
11597418 47 Pyrimidinylimidazole inhibitors of p38: cyclic N-1 imidazole substituents enhance p38 kinase inhibition and oral activity.EBI GlaxoSmithKline Pharmaceuticals
11277536 130 7-Pyrrolidinyl- and 7-piperidinyl-5-aryl-pyrrolo[2,3-d]pyrimidines--potent inhibitors of the tyrosine kinase c-Src.EBI Novartis Pharma Research
11012022 102 Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck II.EBI BASF Bioresearch Corporation
11012021 69 Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck I.EBI BASF Bioresearch Corporation
10612598 29 4-Pyridin-5-yl-2-(3,4,5-trimethoxyphenylamino)pyrimidines: potent and selective inhibitors of ZAP 70.EBI Celltech Therapeutics Limited
10476877 15 NMR-based discovery of phosphotyrosine mimetics that bind to the Lck SH2 domain.EBI Abbott Laboratories
10377223 57 Design and synthesis of potent, selective, and orally bioavailable tetrasubstituted imidazole inhibitors of p38 mitogen-activated protein kinase.EBI Merck Research Laboratories
10052978 22 Phosphotyrosine-containing dipeptides as high-affinity ligands for the p56lck SH2 domain.EBI Boehringer Ingelheim Pharmaceuticals Inc.
9873567 28 The development of novel and selective p56lck tyrosine kinase inhibitors.EBI R. W. Johnson Pharmaceutical Research Institute
9871562 2 1-Methoxy-agroclavine from Penicillium sp. WC75209, a novel inhibitor of the Lck tyrosine kinase.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
9719597 12 Structure-based design and synthesis of high affinity tripeptide ligands of the Grb2-SH2 domain.EBI Novartis Pharma Inc.
9632358 45 Discovery of a novel series of potent and selective substrate-based inhibitors of p60c-src protein tyrosine kinase: conformational and topographical constraints in peptide design.EBI University of Arizona
9599224 10 Potent antagonists of the SH2 domain of Grb2: optimization of the X+1 position of 3-amino-Z-Tyr(PO3H2)-X+1-Asn-NH2.EBI Novartis Pharma Inc.
8474097 19 Bicyclic compounds as ring-constrained inhibitors of protein-tyrosine kinase p56lck.EBI National Cancer Institute
8411019 6 Hydroxylated 2-(5'-salicyl)naphthalenes as protein-tyrosine kinase inhibitors.EBI National Institutes of Health
8411012 19 Synthesis and protein-tyrosine kinase inhibitory activity of polyhydroxylated stilbene analogues of piceatannol.EBI Purdue University
8105084 6 Non-amine based analogues of lavendustin A as protein-tyrosine kinase inhibitors.EBI National Institutes of Health
8064792 25 5,7-Dimethoxy-3-(4-pyridinyl)quinoline is a potent and selective inhibitor of human vascular beta-type platelet-derived growth factor receptor tyrosine kinase.EBI Sterling Winthrop Pharmaceuticals Research Division
7932563 60 Synthesis and biochemical evaluation of a series of aminoflavones as potential inhibitors of protein-tyrosine kinases p56lck, EGFr, and p60v-src.EBI Purdue University
7902440 104 Tyrphostins. 3. Structure-activity relationship studies of alpha-substituted benzylidenemalononitrile 5-S-aryltyrphostins.EBI Hebrew University of Jerusalem
1995903 49 Synthesis and protein-tyrosine kinase inhibitory activities of flavonoid analogues.EBI Purdue University
23305300 12 A Hexylchloride-Based Catch-and-Release System for Chemical Proteomic Applications.BDB University of Washington
16492761 51 An efficient rapid system for profiling the cellular activities of molecular libraries.BDB Genomics Institute of the Novartis Research Foundation
12534346 22 The specificities of protein kinase inhibitors: an update.BDB University of Dundee
20189109 42 Affinity reagents that target a specific inactive form of protein kinases.BDB University of Washington
10467133 4 Structural basis for selective inhibition of Src family kinases by PP1.BDB Princeton University
19764794 60 Selective inhibitors of the mutant B-Raf pathway: discovery of a potent and orally bioavailable aminoisoquinoline.BDB Amgen
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
17600705 43 N-4-Pyrimidinyl-1H-indazol-4-amine inhibitors of Lck: indazoles as phenol isosteres with improved pharmacokinetics.BDB GSK
18006306 12 Biphenyl amide p38 kinase inhibitors 1: Discovery and binding mode.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
17253679 69 Alkynylpyrimidine amide derivatives as potent, selective, and orally active inhibitors of Tie-2 kinase.BDB Amgen
14981513 6 VX-680, a potent and selective small-molecule inhibitor of the Aurora kinases, suppresses tumor growth in vivo.BDB Vertex Pharmaceuticals (Europe) Limited
17154512 78 2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatinib, BMS-354825) as a potent pan-Src kinase iBDB Bristol-Myers Squibb Company
12039591 63 Pyrazolo[3,4-d]pyrimidines containing an extended 3-substituent as potent inhibitors of Lck - a selectivity insight.BDB Abbott Bioresearch Center
11741480 41 A novel approach for the development of selective Cdk4 inhibitors: library design based on locations of Cdk4 specific amino acid residues.BDB Banyu Tsukuba Research Institute
10974196 31 Biochemical and cellular effects of c-Src kinase-selective pyrido[2,3-d]pyrimidine tyrosine kinase inhibitors.BDB Parke-Davis Pharmaceutical Research