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87 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
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
27261178 32 Novel JAK1-selective benzimidazole inhibitors with enhanced membrane permeability.EBI Konkuk University
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
26927423 58 Structure-based design and development of (benz)imidazole pyridones as JAK1-selective kinase inhibitors.EBI Merck& Co.
26701356 100 Structure-Based Design and Synthesis of 3-Amino-1,5-dihydro-4H-pyrazolopyridin-4-one Derivatives as Tyrosine Kinase 2 Inhibitors.EBI Takeda Pharmaceutical Company Limited
26632965 80 Optimization of a Novel Series of Ataxia-Telangiectasia Mutated Kinase Inhibitors as Potential Radiosensitizing Agents.EBI Duke University School of Medicine
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
26614408 106 Identification of azabenzimidazoles as potent JAK1 selective inhibitors.EBI AstraZeneca
26351728 96 Benzimidazole Derivatives as Potent JAK1-Selective Inhibitors.EBI Konkuk 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
26288683 43 Discovery of a Highly Selective JAK2 Inhibitor, BMS-911543, for the Treatment of Myeloproliferative Neoplasms.EBI Bristol-Myers Squibb R&D
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
26086931 38 Strategies for the Discovery of Target-Specific or Isoform-Selective Modulators.EBI Shandong University
26231159 1 Discovery of Tyk2 inhibitors via the virtual site-directed fragment-based drug design.EBI Chungnam National 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
26258521 104 Development of Selective Covalent Janus Kinase 3 Inhibitors.EBI Harvard Medical School
25987372 104 9H-Carbazole-1-carboxamides as potent and selective JAK2 inhibitors.EBI Bristol-Myers Squibb Co.
25699576 42 Development of novel ACK1/TNK2 inhibitors using a fragment-based approach.EBI University of South Florida
25415535 118 Inhibitors of c-Jun N-terminal kinases: an update.EBI Eberhard Karls Universit£t T£bingen
24980703 296 Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors.EBI Nerviano Medical Sciences
25453808 101 Discovery of pyrrolo[1,2-b]pyridazine-3-carboxamides as Janus kinase (JAK) inhibitors.EBI Bristol-Myers Squibb Company
25383627 85 Discovery of selective and noncovalent diaminopyrimidine-based inhibitors of epidermal growth factor receptor containing the T790M resistance mutation.EBI Genentech Inc.
25369270 93 Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634.EBI Galapagos NV
24417533 63 Discovery and development of Janus kinase (JAK) inhibitors for inflammatory diseases.EBI Pfizer Inc.
24139169 175 Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.EBI Nerviano Medical Sciences
24042009 89 Design and evaluation of novel 8-oxo-pyridopyrimidine Jak1/2 inhibitors.EBI Genentech Inc.
23265875 78 Design and synthesis of tricyclic cores for kinase inhibition.EBI Abbott Bioresearch Center
23214979 74 3-Amido pyrrolopyrazine JAK kinase inhibitors: development of a JAK3 vs JAK1 selective inhibitor and evaluation in cellular and in vivo models.EBI Hoffmann-La Roche
23127890 96 SAR and in vivo evaluation of 4-aryl-2-aminoalkylpyrimidines as potent and selective Janus kinase 2 (JAK2) inhibitors.EBI Exelixis
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
21604762 152 Discovery of the macrocycle 11-(2-pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26-triaza-tetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene (SB1518), a potent Janus kinase 2/fms-like tyrosine kinase-3 (JAK2/FLT3) inhibitor for the treatment of myelofibrosis and lymphEBI S*BIO Pte. Ltd.
23116168 42 Structural optimization and structure-activity relationships of N2-(4-(4-Methylpiperazin-1-yl)phenyl)-N8-phenyl-9H-purine-2,8-diamine derivatives, a new class of reversible kinase inhibitors targeting both EGFR-activating and resistance mutations.EBI Sichuan University
23061660 92 Discovery of potent and selective pyrazolopyrimidine janus kinase 2 inhibitors.EBI Genentech
22698084 99 Discovery and optimization of C-2 methyl imidazopyrrolopyridines as potent and orally bioavailable JAK1 inhibitors with selectivity over JAK2.EBI Genentech
21413800 56 A one-pot synthesis and biological activity of ageladine A and analogues.EBI Macquarie University
22591402 127 Identification of imidazo-pyrrolopyridines as novel and potent JAK1 inhibitors.EBI Argenta Discovery Ltd.
22339472 148 Discovery of the macrocycle (9E)-15-(2-(pyrrolidin-1-yl)ethoxy)-7,12,25-trioxa-19,21,24-triaza-tetracyclo[18.3.1.1(2,5).1(14,18)]hexacosa-1(24),2,4,9,14(26),15,17,20,22-nonaene (SB1578), a potent inhibitor of janus kinase 2/fms-like tyrosine kinase-3 (JAK2/FLT3) for the treatment of rheumatoid arthEBI S BIO Pte. Ltd.
21155605 39 Identification of a potent Janus kinase 3 inhibitor with high selectivity within the Janus kinase family.EBI Novartis Institutes for BioMedical Research
21106455 60 Diamino-1,2,4-triazole derivatives are selective inhibitors of TYK2 and JAK1 over JAK2 and JAK3.EBI SRI International
19648005 41 Identification of small molecule inhibitors of proline-rich tyrosine kinase 2 (Pyk2) with osteogenic activity in osteoblast cells.EBI Amgen Inc.
18183025 12060 A quantitative analysis of kinase inhibitor selectivity.EBI Ambit Biosciences
18077425 197 Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.EBI Harvard Medical School
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
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
22087750 145 Discovery of potent and highly selective thienopyridine Janus kinase 2 inhibitors.EBI Amgen, Inc.
22037378 31824 Comprehensive analysis of kinase inhibitor selectivity.EBI Ambit Biosciences
21942426 113 Discovery of 1-amino-5H-pyrido[4,3-b]indol-4-carboxamide inhibitors of Janus kinase 2 (JAK2) for the treatment of myeloproliferative disorders.EBI Merck& Co.
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
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
21105711 79 Discovery of CP-690,550: a potent and selective Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases and organ transplant rejection.EBI Pfizer Inc.
21035336 42 5-amino-pyrazoles as potent and selective p38a inhibitors.EBI Bristol-Myers Squibb Research and Development
19654408 2521 AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).EBI Ambit Biosciences
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
20231096 81 Discovery and SAR of potent, orally available 2,8-diaryl-quinoxalines as a new class of JAK2 inhibitors.EBI Novartis Institutes for Biomedical Research
20138510 60 2-Amino-aryl-7-aryl-benzoxazoles as potent, selective and orally available JAK2 inhibitors.EBI Novartis Institutes for BioMedical Research
19926477 100 2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.EBI Abbott Laboratories
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
19035792 85 Assessment of chemical coverage of kinome space and its implications for kinase drug discovery.EBI GlaxoSmithKline
17185414 30 Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK.EBI Genomics Institute of the Novartis Research Foundation
16970394 147 Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity.EBI Amgen, Inc.
16216497 67 Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection.EBI Abbott Bioresearch Center
12482439 51 Design and synthesis of potent, orally bioavailable dihydroquinazolinone inhibitors of p38 MAP kinase.EBI Merck Research Laboratories
11934592 20 Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor.EBI Merck Research Laboratories
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
27840070 28 Selective JAK3 Inhibitors with a Covalent Reversible Binding Mode Targeting a New Induced Fit Binding Pocket.BDB Eberhard-Karls-University Tuebingen
16492761 51 An efficient rapid system for profiling the cellular activities of molecular libraries.BDB Genomics Institute of the Novartis Research Foundation
21439476 12 Jak1 has a dominant role over Jak3 in signal transduction through γc-containing cytokine receptors.BDB University of Luxembourg