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224 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
28291695 36 Structure-based drug design of novel ASK1 inhibitors using an integrated lead optimization strategy.EBI Takeda California Inc.
27789138 355 Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors.EBI AbbVie Bioresearch Center
28005359 66 Cyclin-Dependent Kinase (CDK) Inhibitors: Structure-Activity Relationships and Insights into the CDK-2 Selectivity of 6-Substituted 2-Arylaminopurines.EBI Newcastle University
28131714 119 Indolyl-naphthyl-maleimides as potent and selective inhibitors of protein kinase C-a/▀.EBI Novartis Institutes for BioMedical Research
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.
28039836 41 Structure-based design and synthesis of imidazo[1,2-a]pyridine derivatives as novel and potent Nek2 inhibitors with inávitro and inávivo antitumor activities.EBI East China Normal University
28280261 84 Non-kinase targets of protein kinase inhibitors.EBI The University of Sydney
27816515 143 Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.EBI Merck& Co.
27391135 28 3-Hydrazinoindolin-2-one derivatives: Chemical classification and investigation of their targets as anticancer agents.EBI Egyptian Russian University
27171036 164 Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.EBI University of Nebraska Medical Center
27078757 121 Discovery of a Potent, Selective, Orally Bioavailable, and Efficacious Novel 2-(Pyrazol-4-ylamino)-pyrimidine Inhibitor of the Insulin-like Growth Factor-1 Receptor (IGF-1R).EBI AstraZeneca
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
26900761 4 Feeling Nature's PAINS: Natural Products, Natural Product Drugs, and Pan Assay Interference Compounds (PAINS).EBI Monash University (Parkville Campus)
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
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
26316466 8 Discovery of novel nonpeptide allosteric inhibitors interrupting the interaction of CDK2/cyclin A3 by virtual screening and bioassays.EBI Dalian Medical University
26115571 38 Cyclin dependent kinase (CDK) inhibitors as anticancer drugs.EBI Eli Lilly and Company
25262942 189 Rational design of inhibitors of the bacterial cell wall synthetic enzyme GlmU using virtual screening and lead-hopping.EBI AstraZeneca
25730262 195 10-iodo-11H-indolo[3,2-c]quinoline-6-carboxylic acids are selective inhibitors of DYRK1A.EBI Technische Universit£t Braunschweig
25835317 63 Design, Synthesis, and Structure-Activity Relationship Studies of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as a New Class of Src Inhibitors with Potent Activities in Models of Triple Negative Breast Cancer.EBI Sichuan University
25738750 84 Discovery and optimization of a novel series of Dyrk1B kinase inhibitors to explore a MEK resistance hypothesis.EBI AstraZeneca
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.
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
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
25313996 91 Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase.EBI Merck Research Laboratories
24813737 107 Discovery of 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine inhibitors of Erk2.EBI Array BioPharma 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
24462666 105 Discovery of 6-aryl-azabenzimidaoles that inhibit the TBK1/IKK-e kinases.EBI AstraZeneca
24417566 43 Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5).EBI Icahn School of Medicine at Mount Sinai
24295046 1 Design, synthesis, and biological evaluation of 1-phenylpyrazolo[3,4-e]pyrrolo[3,4-g]indolizine-4,6(1H,5H)-diones as new glycogen synthase kinase-3▀ inhibitors.EBI Universit£ di Napoli Federico II
24332088 79 Modulating the interaction between CDK2 and cyclin A with a quinoline-based inhibitor.EBI Merck Research Laboratories
24157370 22 The sulfamide moiety affords higher inhibitory activity and oral bioavailability to a series of coumarin dual selective RAF/MEK inhibitors.EBI Chugai Pharmaceutical Co., Ltd
23481650 78 N-substituted azaindoles as potent inhibitors of Cdc7 kinase.EBI Amgen Inc.
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
24900658 10 Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.EBI Hoffmann-La Roche Inc.
23252711 46 Comparative structural and functional studies of 4-(thiazol-5-yl)-2-(phenylamino)pyrimidine-5-carbonitrile CDK9 inhibitors suggest the basis for isotype selectivity.EBI University of Oxford
22910137 1 Synthesis and identification of novel indolo[2,3-a]pyrimido[5,4-c]carbazoles as a new class of anti-cancer agents.EBI TBA
21764580 51 Identification of 2-(4-pyridyl)thienopyridinones as GSK-3ß inhibitors.EBI GlaxoSmithKline
19303774 87 1-Aryl-3,4-dihydroisoquinoline inhibitors of JNK3.EBI GlaxoSmithKline R&D
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
23099093 84 Synthesis and structure-activity relationships of a novel series of pyrimidines as potent inhibitors of TBK1/IKKe kinases.EBI MRC Technology
22883026 34 Design and synthesis of novel DFG-out RAF/vascular endothelial growth factor receptor 2 (VEGFR2) inhibitors: 3. Evaluation of 5-amino-linked thiazolo[5,4-d]pyrimidine and thiazolo[5,4-b]pyridine derivatives.EBI Takeda Pharmaceutical Company Limited
22726925 216 Discovery of 5-(2-amino-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-N-(tert-butyl)pyridine-3-sulfonamide (CZC24758), as a potent, orally bioavailable and selective inhibitor of PI3K for the treatment of inflammatory disease.EBI Cellzome Ltd
21381769 56 Macrocycles are great cycles: applications, opportunities, and challenges of synthetic macrocycles in drug discovery.EBI Universite£ de Sherbrooke
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
23063403 21 Recent results in protein kinase inhibition for tropical diseases.EBI Montclair State University
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.
23021994 108 Identification of pyrimidine derivatives as hSMG-1 inhibitors.EBI Pfizer Inc.
22554206 33 Discovery of pyrroloaminopyrazoles as novel PAK inhibitors.EBI Pfizer Inc.
24900464 66 Potent and Selective Inhibitors of CK2 Kinase Identified through Structure-Guided Hybridization.EBI TBA
22738630 76 Structure-based optimization of aminopyridines as PKC¿ inhibitors.EBI Department of Chemistry at Vertex Pharmaceuticals (Europe) Ltd
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
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.
22437109 31 2-anilino-4-aryl-8H-purine derivatives as inhibitors of PDK1.EBI S*BIO Pte. Ltd
24900264 106 The Discovery of VX-745: A Novel and Selective p38a Kinase Inhibitor.EBI TBA
22305584 145 Discovery of azabenzimidazole derivatives as potent, selective inhibitors of TBK1/IKKe kinases.EBI AstraZeneca R&D Boston
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
16584130 95 Selectivity and potency of cyclin-dependent kinase inhibitors.EBI Georgetown University
15559249 55 Pharmacological inhibitors of glycogen synthase kinase 3.EBI The Rockefeller University
18469809 41 A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity.EBI Nerviano Medical Sciences Oncology
20621725 9 Structure-based optimization of potent PDK1 inhibitors.EBI Nerviano Medical Sciences Srl
20000735 12 Through the"gatekeeper door": exploiting the active kinase conformation.EBI Nerviano Medical Sciences
20138514 93 3-Aryl-4-(arylhydrazono)-1H-pyrazol-5-ones: Highly ligand efficient and potent inhibitors of GSK3beta.EBI Vertex Pharmaceuticals Inc
20138512 82 Discovery of potent and bioavailable GSK-3beta inhibitors.EBI Roche Palo Alto
20097066 53 Semi-synthetic aristolactams--inhibitors of CDK2 enzyme.EBI Schering Plough Research Institute
18183025 12060 A quantitative analysis of kinase inhibitor selectivity.EBI Ambit Biosciences
19397322 58 Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.EBI National Cancer Institute
9677190 49 Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors.EBI University of California
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
18321716 7 ATP competitive inhibitors of D-alanine-D-alanine ligase based on protein kinase inhibitor scaffolds.EBI Institute of Molecular Physiology
18680271 8 NMR screening for lead compounds using tryptophan-mutated proteins.EBI Institute for Biochemistry
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
18271520 423 Discovery of kinase inhibitors by high-throughput docking and scoring based on a transferable linear interaction energy model.EBI University of Zurich
17935989 146 Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.EBI Abbott Laboratories
16876403 85 Structure-based drug design of a highly potent CDK1,2,4,6 inhibitor with novel macrocyclic quinoxalin-2-one structure.EBI Banyu Tsukuba Research Institute in collaboration with Merck Research Laboratories
16451062 46 Discovery of novel and potent thiazoloquinazolines as selective Aurora A and B kinase inhibitors.EBI Centre de Recherches
15857136 4 Conformation mining: an algorithm for finding biologically relevant conformations.EBI Rational Discovery LLC
15267232 65 Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3.EBI Lilly Research Laboratories
15214773 76 Fragment-based drug discovery.EBI Sunesis Pharmaceuticals Inc.
15115396 112 General model for estimation of the inhibition of protein kinases using Monte Carlo simulations.EBI Yale University
12672248 50 Kinase inhibitors: not just for kinases anymore.EBI Northwestern University
12954055 47 Synthesis and discovery of macrocyclic polyoxygenated bis-7-azaindolylmaleimides as a novel series of potent and highly selective glycogen synthase kinase-3beta inhibitors.EBI Johnson and Johnson Pharmaceutical Research and Development
10743948 22 5-Arylamino-2-methyl-4,7-dioxobenzothiazoles as inhibitors of cyclin-dependent kinase 4 and cytotoxic agents.EBI Ewha Womans University
22310227 89 5-Aryl-4-carboxamide-1,3-oxazoles: potent and selective GSK-3 inhibitors.EBI GlaxoSmithKline
17018693 30 Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities.EBI GlaxoSmithKline Pharmaceuticals Inc.
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.
22004849 9 Selection of cyclic-peptide inhibitors targeting Aurora kinase A: problems and solutions.EBI University of Arizona
22148278 132 Discovery of kinase spectrum selective macrocycle (16E)-14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene (SB1317/TG02), a potent inhibitor of cyclin dependent kinases (CDKs), Janus kinase 2 (JAK2), and fms-like tyrosine kinaseEBI S BIO Pte. 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
22119469 107 Novel and selective spiroindoline-based inhibitors of Sky kinase.EBI Pfizer Inc.
22119465 18 Structure-based design of PDK1 inhibitors.EBI S BIO Pte Ltd
21986585 2 A modular approach to trim cellular targets in anticancer drug discovery.EBI Instituto Universitario de Bio-Org£nica Antonio Gonz£lez (IUBO-AG)
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
21824779 67 Design and synthesis of novel amide AKT1 inhibitors with selectivity over CDK2.EBI Amgen Inc.
21699136 16 Selectivity of kinase inhibitor fragments.EBI GlaxoSmithKline R&D
21775140 69 Discovery of novel imidazo[1,2-a]pyridines as inhibitors of the insulin-like growth factor-1 receptor tyrosine kinase.EBI AstraZeneca
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
21684737 48 Discovery of a novel class of 2-aminopyrimidines as CDK1 and CDK2 inhibitors.EBI Keimyung University
21627121 22 Irreversible Nek2 kinase inhibitors with cellular activity.EBI University of California
21620699 51 Substituted N-aryl-6-pyrimidinones: a new class of potent, selective, and orally active p38 MAP kinase inhibitors.EBI Pfizer Inc.
20630752 40 Discovery and optimization of N-acyl and N-aroylpyrazolines as B-Raf kinase inhibitors.EBI Millennium Pharmaceuticals Inc.
21353545 39 Structure-activity relationship study of 2,4-diaminothiazoles as Cdk5/p25 kinase inhibitors.EBI Harvard Medical School
21414779 64 Discovery of 2,4-bis-arylamino-1,3-pyrimidines as insulin-like growth factor-1 receptor (IGF-1R) inhibitors.EBI Amgen Inc.
24900229 41 Aminoindazole PDK1 Inhibitors: A Case Study in Fragment-Based Drug Discovery.EBI TBA
24900250 81 Kinase Inhibition by Deoxy Analogues of the Resorcylic Lactone L-783277EBI TBA
21080629 153 Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity.EBI University of Regensburg
20965724 57 Identification of potent ITK inhibitors through focused compound library design including structural information.EBI Nycomed GmbH
20855207 26 Discovery of orally bioavailable imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.EBI Merck Research Laboratories
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
18559524 21 BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy.EBI Boehringer Ingelheim Austria GmbH
16408016 6 Assignment of protein function in the postgenomic era.EBI The Scripps Research Institute
20675134 88 Discovery of imidazo[1,2-b]pyridazine derivatives as IKKbeta inhibitors. Part 1: Hit-to-lead study and structure-activity relationship.EBI Daiichi Sankyo Co., Ltd
20462263 127 Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors.EBI Cyclacel Ltd.
19894727 164 Discovery of 4-morpholino-6-aryl-1H-pyrazolo[3,4-d]pyrimidines as highly potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): optimization of the 6-aryl substituent.EBI Wyeth Research
20188552 75 Discovery and optimization of 2-(4-substituted-pyrrolo[2,3-b]pyridin-3-yl)methylene-4-hydroxybenzofuran-3(2H)-ones as potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR).EBI Wyeth Research
19884006 47 Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors.EBI Wyeth Research
20167481 66 Rational design of potent GSK3beta inhibitors with selectivity for Cdk1 and Cdk2.EBI Sanofi-aventis
20137943 60 Azole-based inhibitors of AKT/PKB for the treatment of cancer.EBI Amgen Inc.
20137932 47 2-Aminothiadiazole inhibitors of AKT1 as potential cancer therapeutics.EBI Amgen Inc.
19864136 45 Non-hinge-binding pyrazolo[1,5-a]pyrimidines as potent B-Raf kinase inhibitors.EBI Wyeth Research
19854649 49 Discovery of highly potent and selective type I B-Raf kinase inhibitors.EBI Wyeth Research
20060294 21 Novel 3-aminopyrazole inhibitors of MK-2 discovered by scaffold hopping strategy.EBI Novartis Institutes for BioMedical Research
20097074 5 New potential antitumor compounds from the plant Aristolochia manshuriensis as inhibitors of the CDK2 enzyme.EBI Schering Plough Research Institute
20093027 92 Discovery of 6-benzyloxyquinolines as c-Met selective kinase inhibitors.EBI Chugai Pharmaceutical Co, Ltd
19926477 100 2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.EBI Abbott Laboratories
19857966 62 Discovery of pyrazol-3-ylamino pyrazines as novel JAK2 inhibitors.EBI AstraZeneca R&D Boston
19954867 2 Radiosynthesis and radiopharmacological evaluation of cyclin-dependent kinase 4 (Cdk4) inhibitors.EBI Institute of Radiopharmacy
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
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
19632122 54 Fascaplysin-inspired diindolyls as selective inhibitors of CDK4/cyclin D1.EBI University of Leicester
19203813 48 Synthesis and biological evaluation of 3,6-disubstituted [1,2,4]triazolo[3,4-b][1,3,4]thiadiazole derivatives as a novel class of potential anti-tumor agents.EBI National Organization for Drug Control and Research
18842409 28 A diaminocyclohexyl analog of SNS-032 with improved permeability and bioavailability properties.EBI Sunesis Pharmaceuticals
18835709 91 Synthesis and evaluation of pyrazolo[1,5-b]pyridazines as selective cyclin dependent kinase inhibitors.EBI GlaxoSmithKline
19414255 58 Structure-based design of 3-aryl-6-amino-triazolo[4,3-b]pyridazine inhibitors of Pim-1 kinase.EBI Vertex Pharmaceuticals Inc
19358610 2 Halogen bonding--a novel interaction for rational drug design?EBI Chinese Academy of Sciences
19338355 104 From a natural product lead to the identification of potent and selective benzofuran-3-yl-(indol-3-yl)maleimides as glycogen synthase kinase 3beta inhibitors that suppress proliferation and survival of pancreatic cancer cells.EBI University of Illinois at Chicago
19327989 40 Synthesis and SAR of 4-substituted-2-aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors.EBI Pfizer Global R&D
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
19211246 320 N-substituted 2'-(aminoaryl)benzothiazoles as kinase inhibitors: hit identification and scaffold hopping.EBI 4SC AG
19097792 24 Identification of amidoheteroaryls as potent inhibitors of mutant (V600E) B-Raf kinase with in vivo activity.EBI AstraZeneca R&D Boston
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
18996007 30 The discovery of AZD5597, a potent imidazole pyrimidine amide CDK inhibitor suitable for intravenous dosing.EBI AstraZeneca Pharmaceuticals
18986805 39 Imidazole pyrimidine amides as potent, orally bioavailable cyclin-dependent kinase inhibitors.EBI AstraZeneca Pharmaceuticals
18938080 102 Discovery and SAR of novel 4-thiazolyl-2-phenylaminopyrimidines as potent inhibitors of spleen tyrosine kinase (SYK).EBI Vertex Pharmaceuticals, Inc.
18929484 26 Imidazo[5,1-f][1,2,4]triazin-2-amines as novel inhibitors of polo-like kinase 1.EBI GlaxoSmithKline
18926699 30 Modifications of the isonipecotic acid fragment of SNS-032: analogs with improved permeability and lower efflux ratio.EBI Sunesis Pharmaceuticals
18818075 25 The identification of pyrazolo[1,5-a]pyridines as potent p38 kinase inhibitors.EBI GlaxoSmithKline
18815031 41 Imidazoles: SAR and development of a potent class of cyclin-dependent kinase inhibitors.EBI AstraZeneca
18691885 60 Novel N9-arenethenyl purines as potent dual Src/Abl tyrosine kinase inhibitors.EBI ARIAD Pharmaceuticals, Inc.
18650093 88 Design, synthesis and biological evaluation of new tryptamine and tetrahydro-beta-carboline-based selective inhibitors of CDK4.EBI University of Leicester
18625560 3 Synthesis and evaluation of pyrazolo[3,4-b]pyridines and its structural analogues as TNF-alpha and IL-6 inhibitors.EBI Piramal Life Sciences Limited
18617397 21 Imidazole piperazines: SAR and development of a potent class of cyclin-dependent kinase inhibitors with a novel binding mode.EBI AstraZeneca Pharmaceuticals
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
18494457 160 4-(Phenylaminomethylene)isoquinoline-1,3(2H,4H)-diones as potent and selective inhibitors of the cyclin-dependent kinase 4 (CDK4).EBI Wyeth Research
18457385 41 Recent developments in fragment-based drug discovery.EBI Astex Therapeutics Ltd.
18393402 2 Natural products as leads to potential drugs: an old process or the new hope for drug discovery?EBI National Cancer Institute-Frederick
18313174 26 Synthesis and biological evaluation of diversely substituted indolin-2-ones.EBI Université Blaise Pascal
18037537 53 An efficient tool for identifying inhibitors based on 3D-QSAR and docking using feature-shape pharmacophore of biologically active conformation--a case study with CDK2/cyclinA.EBI Institute of Chemical Biology (CSIR)
17707953 23 Selectivity criterion for pyrazolo[3,4-b]pyrid[az]ine derivatives as GSK-3 inhibitors: CoMFA and molecular docking studies.EBI National Institute of Pharmaceutical Education and Research
18353638 71 Synthesis and biological evaluation of 3,5-diaminoindazoles as cyclin-dependent kinase inhibitors.EBI Keimyung University
18289854 44 Identification of pyrrolo[2,1-f][1,2,4]triazine-based inhibitors of Met kinase.EBI Bristol-Myers Squibb Research and Development
18248988 16 Entry into a new class of protein kinase inhibitors by pseudo ring design.EBI Novartis Institutes for BioMedical Research
18055203 51 Identification of 2-amino-5-(thioaryl)thiazoles as inhibitors of nerve growth factor receptor TrkA.EBI Bristol-Myers Squibb Research and Development
17826092 37 Optimization of triarylimidazoles for Tie2: influence of conformation on potency.EBI GlaxoSmithKline
17459703 111 Synthesis and SAR of aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors.EBI UCB
17303421 56 Synthesis and activity of quinolinyl-methylene-thiazolinones as potent and selective cyclin-dependent kinase 1 inhibitors.EBI Roche Research Center
17178224 28 3-Hydroxychromones as cyclin-dependent kinase inhibitors: synthesis and biological evaluation.EBI Keimyung 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.
16913703 2 Novel structural features of CDK inhibition revealed by an ab initio computational method combined with dynamic simulations.EBI University of Cambridge
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
16682186 16 Synthesis and evaluation of N-acyl sulfonamides as potential prodrugs of cyclin-dependent kinase inhibitor JNJ-7706621.EBI Johnson & Johnson Pharmaceutical Research & Development LLC
16682184 25 Identification of potent 5-pyrimidinyl-2-aminothiazole CDK4, 6 inhibitors with significant selectivity over CDK1, 2, 5, 7, and 9.EBI Banyu Tsukuba Research Institute
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
16213715 4 Structural basis for the GSK-3beta binding affinity and selectivity against CDK-2 of 1-(4-aminofurazan-3yl)-5-dialkylaminomethyl-1H-[1,2,3] triazole-4-carboxylic acid derivatives.EBI Universidade do Porto
15955699 33 (1H-imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: further optimisation as highly potent and selective MSK-1-inhibitors.EBI GlaxoSmithKline Pharmaceuticals
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
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
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
12941335 8 Bone-targeted 2,6,9-trisubstituted purines: novel inhibitors of Src tyrosine kinase for the treatment of bone diseases.EBI ARIAD Pharmaceuticals, Inc.
12852762 10 A computational model of binding thermodynamics: the design of cyclin-dependent kinase 2 inhibitors.EBI University of California
12672234 64 Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase.EBI Boehringer Ingelheim Pharmaceuticals
11934592 24 Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor.EBI Merck Research Laboratories
11378364 34 Indazolylamino quinazolines and pyridopyrimidines as inhibitors of the EGFr and C-erbB-2.EBI Research Biomet. Glaxo Wellcome Medicines Research Centre
10633045 1 Binding mode of the 4-anilinoquinazoline class of protein kinase inhibitor: X-ray crystallographic studies of 4-anilinoquinazolines bound to cyclin-dependent kinase 2 and p38 kinase.EBI Glaxo Wellcome Inc.
26158339 24 Type II Inhibitors Targeting CDK2.BDB University of Oxford
25619419 5 Tampering with cell division by using small-molecule inhibitors of CDK-CKS protein interactions.BDB UniversitÚ Pierre et Marie Curie
24803299 10 Arylazopyrazole AAP1742 inhibits CDKs and induces apoptosis in multiple myeloma cells via Mcl-1 downregulation.BDB Institute of Experimental Botany ASCR and Palacky University
23534475 27 De novo design of protein kinase inhibitors by in silico identification of hinge region-binding fragments.BDB University of Dundee
19359241 26 Discovery and exploitation of inhibitor-resistant aurora and polo kinase mutants for the analysis of mitotic networks.BDB University of Manchester
22893598 12 A Novel Approach to the Discovery of Small-Molecule Ligands of CDK2.BDB Moffitt Cancer Center and Research Institute
12534346 22 The specificities of protein kinase inhibitors: an update.BDB University of Dundee
15742375 56 From the insoluble dye indirubin towards highly active, soluble CDK2-inhibitors.BDB Schering AG
16492148 12 Structural basis of Src tyrosine kinase inhibition with a new class of potent and selective trisubstituted purine-based compounds.BDB ARIAD Pharmaceuticals
21035734 70 Discovery and characterization of 2-anilino-4- (thiazol-5-yl)pyrimidine transcriptional CDK inhibitors as anticancer agents.BDB Cyclacel Limited
16873019 6 MASPIT: three-hybrid trap for quantitative proteome fingerprinting of small molecule-protein interactions in mammalian cells.BDB GPC Biotech Incorporated
16492568 12 Differential binding of inhibitors to active and inactive CDK2 provides insights for drug design.BDB Cyclacel Ltd
15123247 29 Structural determinants of CDK4 inhibition and design of selective ATP competitive inhibitors.BDB Cyclacel Limited