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76 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
27816515 143 Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.EBI Merck& Co.
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
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
26396685 19 Oxopyrido[2,3-d]pyrimidines as Covalent L858R/T790M Mutant Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors.EBI Amgen Inc.
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
26258521 104 Development of Selective Covalent Janus Kinase 3 Inhibitors.EBI Harvard Medical School
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.
26071372 89 Synthesis and evaluation of novel 1H-pyrrolo[2,3-b]pyridine-5-carboxamide derivatives as potent and orally efficacious immunomodulators targeting JAK3.EBI Astellas Pharma Inc.
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.
25630223 5 Target engagement in lead generation.EBI Eli Lilly and Company
25455497 20 Design, synthesis and structure-activity relationships of a novel class of sulfonylpyridine inhibitors of Interleukin-2 inducible T-cell kinase (ITK).EBI Evotec UK Ltd
24918870 74 Property- and structure-guided discovery of a tetrahydroindazole series of interleukin-2 inducible T-cell kinase inhibitors.EBI Genentech Inc.
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
24900859 4 Treatment of Immunological or Inflammatory Disorders with ITK Kinase Inhibitors.EBI Therachem Research Medilab (India) Pvt. Ltd.
24767842 29 Discovery and optimization of indazoles as potent and selective interleukin-2 inducible T cell kinase (ITK) inhibitors.EBI Genentech Inc.
24685542 67 Purine derivatives as potent Bruton's tyrosine kinase (BTK) inhibitors for autoimmune diseases.EBI Bristol-Myers Squibb Research and Development
24138940 34 Structure-based design and synthesis of potent benzothiazole inhibitors of interleukin-2 inducible T cell kinase (ITK).EBI Evotec (UK) Ltd
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
23398373 88 Design and optimization of selective protein kinase C¿ (PKC¿) inhibitors for the treatment of autoimmune diseases.EBI Vertex Pharmaceuticals (Europe) Ltd.
23103095 125 Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.EBI Abbott Laboratories
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
23098091 91 Covalent inhibitors of interleukin-2 inducible T cell kinase (itk) with nanomolar potency in a whole-blood assay.EBI Pfizer Inc.
22738630 76 Structure-based optimization of aminopyridines as PKC¿ inhibitors.EBI Department of Chemistry at Vertex Pharmaceuticals (Europe) Ltd
22464456 27 X-ray crystallographic structure-based design of selective thienopyrazole inhibitors for interleukin-2-inducible tyrosine kinase.EBI Sanofi US
15975507 13 Features of selective kinase inhibitors.EBI University of California-San Francisco
20000469 179 Hit to lead account of the discovery of bisbenzamide and related ureidobenzamide inhibitors of Rho kinase.EBI Boehringer Ingelheim Pharmaceuticals
19716697 110 The discovery of thienopyridine analogues as potent IkappaB kinase beta inhibitors. Part II.EBI Boehringer Ingelheim Pharmaceuticals
18183025 12060 A quantitative analysis of kinase inhibitor selectivity.EBI Ambit Biosciences
18359226 50 Pyrazolo-pyrimidines: a novel heterocyclic scaffold for potent and selective p38 alpha inhibitors.EBI Bristol-Myers Squibb Research and Development
18077363 314 A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.EBI University of Oxford
18278858 93 Structure-based design of novel 2-amino-6-phenyl-pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-ones as potent and orally active inhibitors of lymphocyte specific kinase (Lck): synthesis, SAR, and in vivo anti-inflammatory activity.EBI Amgen Inc.
17935989 146 Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.EBI Abbott Laboratories
22310227 89 5-Aryl-4-carboxamide-1,3-oxazoles: potent and selective GSK-3 inhibitors.EBI GlaxoSmithKline
16249345 25 Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580.EBI GlaxoSmithKline
22037378 31824 Comprehensive analysis of kinase inhibitor selectivity.EBI Ambit Biosciences
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
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.
21316219 81 Optimisation of ITK inhibitors through successive iterative design cycles.EBI Nycomed GmbH
21035336 42 5-amino-pyrazoles as potent and selective p38a inhibitors.EBI Bristol-Myers Squibb Research and Development
20965724 57 Identification of potent ITK inhibitors through focused compound library design including structural information.EBI Nycomed GmbH
19654408 2521 AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).EBI Ambit Biosciences
20472447 45 Synthesis and biological evaluation of novel (4 or 5-aryl)pyrazolyl-indoles as inhibitors of interleukin-2 inducible T-cell kinase (ITK).EBI Nycomed Pharma Pvt. Ltd
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
19926477 100 2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.EBI Abbott Laboratories
19414255 58 Structure-based design of 3-aryl-6-amino-triazolo[4,3-b]pyridazine inhibitors of Pim-1 kinase.EBI Vertex Pharmaceuticals Inc
19246196 104 5-Aminomethylbenzimidazoles as potent ITK antagonists.EBI Boehringer Ingelheim Pharmaceuticals Inc.
18823779 27 5-Aminomethyl-1H-benzimidazoles as orally active inhibitors of inducible T-cell kinase (Itk).EBI Johnson & Johnson Pharmaceutical Research and Development
18819799 72 Discovery, SAR and X-ray structure of 1H-benzimidazole-5-carboxylic acid cyclohexyl-methyl-amides as inhibitors of inducible T-cell kinase (Itk).EBI Johnson & Johnson
18819794 53 Itk kinase inhibitors: initial efforts to improve the metabolical stability and the cell activity of the benzimidazole lead.EBI Johnson & Johnson
18667312 24 Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase.EBI The Scripps Research Institute
18606543 68 2-Alkenylthieno[2,3-b]pyridine-5-carbonitriles: Potent and selective inhibitors of PKCtheta.EBI Wyeth Research
17499505 78 Hit-to-lead studies on benzimidazole inhibitors of ITK: discovery of a novel class of kinase inhibitors.EBI Boehringer Ingelheim Pharmaceuticals Inc.
16970394 147 Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity.EBI Amgen, 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
16682193 62 Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
16481166 53 Discovery and SAR of 2-amino-5-[(thiomethyl)aryl]thiazoles as potent and selective Itk inhibitors.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
16216497 67 Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection.EBI Abbott Bioresearch Center
15317461 53 Identification of 1,5-naphthyridine derivatives as a novel series of potent and selective TGF-beta type I receptor inhibitors.EBI GlaxoSmithKline
12672234 64 Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase.EBI Boehringer Ingelheim Pharmaceuticals
27791347 41 Discovery of a JAK3-Selective Inhibitor: Functional Differentiation of JAK3-Selective Inhibition over pan-JAK or JAK1-Selective Inhibition.BDB Pfizer Worldwide R&D
23594111 7 Discovery of a Selective Irreversible BMX Inhibitor for Prostate Cancer.BDB Chinese Academy of Sciences
14766749 2 Crystal structures of interleukin-2 tyrosine kinase and their implications for the design of selective inhibitors.BDB Vertex
18930400 60 2-Aminobenzimidazoles as potent ITK antagonists: trans-stilbene-like moieties targeting the kinase specificity pocket.BDB Boehringer Ingelheim Pharmaceuticals Inc.
19111460 94 Discovery of potent inhibitors of interleukin-2 inducible T-cell kinase (ITK) through structure-based drug design.BDB Boehringer Ingelheim Pharmaceuticals Inc.