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415 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
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/ß.EBI Novartis Institutes For Biomedical Research
28109791 44 Identification of a selective inhibitor of transforming growth factorß-activated kinase 1 by biosensor-based screening of focused libraries.EBI Chugai Pharmaceutical
28039836 41 Structure-based design and synthesis of imidazo[1,2-a]pyridine derivatives as novel and potent Nek2 inhibitors with in vitro and in vivo antitumor activities.EBI East China Normal University
28039837 21 Explicit treatment of active-site waters enhances quantum mechanical/implicit solvent scoring: Inhibition of CDK2 by new pyrazolo[1,5-a]pyrimidines.EBI Masaryk 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
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
27363938 2 A chromatography-free isolation of rohitukine from leaves of Dysoxylum binectariferum: Evaluation for in vitro cytotoxicity, Cdk inhibition and physicochemical properties.EBI India Academy of Scientific & Innovative Research (Acsir)
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
27297568 50 Benzamide capped peptidomimetics as non-ATP competitive inhibitors of CDK2 using the REPLACE strategy.EBI University of South Carolina
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)
27189674 84 RETRACTED: Design, synthesis, structure-activity relationship and kinase inhibitory activity of substituted 3-methyl-1-phenyl-1H-pyrazolo[3,4-d]pyrimidin-4-ones.EBI Beni-Suef University
27055065 92 Rapid Discovery of Pyrido[3,4-d]pyrimidine Inhibitors of Monopolar Spindle Kinase 1 (MPS1) Using a Structure-Based Hybridization Approach.EBI The Institute of Cancer Research
27089211 38 Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors.EBI Zhejiang University
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
27117263 51 Discovery and optimization of 1,7-disubstituted-2,2-dimethyl-2,3-dihydroquinazolin-4(1H)-ones as potent and selective PKC¿ inhibitors.EBI Takeda Pharmaceutical
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
26851505 65 5-Substituted 3-isopropyl-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidines with anti-proliferative activity as potent and selective inhibitors of cyclin-dependent kinases.EBI Palack£
26706349 12 Synthesis and pharmacological evaluation of dehydroabietic acid thiourea derivatives containing bisphosphonate moiety as an inducer of apoptosis.EBI Southeast University
26706352 2 Bis-isatin hydrazones with novel linkers: Synthesis and biological evaluation as cytotoxic agents.EBI Egyptian Russian University
26741853 95 Synthesis, biological evaluation and molecular modeling of a novel series of 7-azaindole based tri-heterocyclic compounds as potent CDK2/Cyclin E inhibitors.EBI University of Tours
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
25914804 20 Discovery of novel 5-fluoro-N(2),N(4)-diphenylpyrimidine-2,4-diamines as potent inhibitors against CDK2 and CDK9.EBI Chinese Academy of Medical Sciences and Peking Union Medical College
26408454 51 An integrated approach for discovery of highly potent and selective Mnk inhibitors: Screening, synthesis and SAR analysis.EBI University of South Australia
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
26318067 34 Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors.EBI Hanyang University
26316466 8 Discovery of novel nonpeptide allosteric inhibitors interrupting the interaction of CDK2/cyclin A3 by virtual screening and bioassays.EBI Dalian Medical 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
26115571 38 Cyclin dependent kinase (CDK) inhibitors as anticancer drugs.EBI Eli Lilly
25262942 189 Rational design of inhibitors of the bacterial cell wall synthetic enzyme GlmU using virtual screening and lead-hopping.EBI Astrazeneca
25007344 73 Optimization of potent DFG-in inhibitors of platelet derived growth factor receptorß (PDGF-Rß) guided by water thermodynamics.EBI Christian-Albrechts-University of Kiel
25730262 195 10-iodo-11H-indolo[3,2-c]quinoline-6-carboxylic acids are selective inhibitors of DYRK1A.EBI Technische Universit£T Braunschweig
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
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
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
25369270 93 Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634.EBI Galapagos
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
24139169 175 Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.EBI Nerviano Medical Sciences
24798019 30 Acridone alkaloids from Glycosmis chlorosperma as DYRK1A inhibitors.EBI Institut De Chimie Des Substances Naturelles
25010935 1 Design and synthesis of pyrimidine molecules endowed with thiazolidin-4-one as new anticancer agents.EBI Jamia Hamdard (Hamdard University)
24973661 10 9- and 11-substituted 4-azapaullones are potent and selective inhibitors of African trypanosoma.EBI Technische Universit£T Braunschweig
24793884 151 Synthesis and structure-activity relationship of trisubstituted thiazoles as Cdc7 kinase inhibitors.EBI Amgen
24681986 42 Synthesis and kinase inhibitory activity of new sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazines.EBI Siedlce University of Natural Sciences and Humanities
24462666 105 Discovery of 6-aryl-azabenzimidaoles that inhibit the TBK1/IKK-e kinases.EBI Astrazeneca
23906342 14 Discovery of a selective kinase inhibitor (TAK-632) targeting pan-RAF inhibition: design, synthesis, and biological evaluation of C-7-substituted 1,3-benzothiazole derivatives.EBI Takeda Pharmaceutical
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-3ß inhibitors.EBI Universit£
24256217 177 Structure-based design of orally bioavailable 1H-pyrrolo[3,2-c]pyridine inhibitors of mitotic kinase monopolar spindle 1 (MPS1).EBI The Institute of Cancer Research
24332088 79 Modulating the interaction between CDK2 and cyclin A with a quinoline-based inhibitor.EBI Merck Research Laboratories
24286762 34 Fragment based discovery of arginine isosteres through REPLACE: towards non-ATP competitive CDK inhibitors.EBI University of South Carolina
24120542 90 The optimization of aminooxadiazoles as orally active inhibitors of Cdc7.EBI Amgen
23454515 66 Chemical synthesis and biological validation of immobilized protein kinase inhibitory Leucettines.EBI Universit£
24185375 76 Synthesis, structure-activity relationship and biological evaluation of 2,4,5-trisubstituted pyrimidine CDK inhibitors as potential anti-tumour agents.EBI University of Nottingham
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
23481650 78 N-substituted azaindoles as potent inhibitors of Cdc7 kinase.EBI Amgen
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
23249297 75 Trimeric hemibastadin congener from the marine sponge Ianthella basta.EBI Heinrich-Heine University
24900658 10 Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.EBI Hoffmann-La Roche
23312943 166 Optimization of highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.EBI Pfizer
23312472 129 Highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.EBI Pfizer
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
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
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
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
21381769 56 Macrocycles are great cycles: applications, opportunities, and challenges of synthetic macrocycles in drug discovery.EBI Universite£
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
23039927 44 Multitargeted drug development: Discovery and profiling of dihydroxy substituted 1-aza-9-oxafluorenes as lead compounds targeting Alzheimer disease relevant kinases.EBI Martin-Luther-University Halle-Wittenberg
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
23021994 108 Identification of pyrimidine derivatives as hSMG-1 inhibitors.EBI Pfizer
22554206 33 Discovery of pyrroloaminopyrazoles as novel PAK inhibitors.EBI Pfizer
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 Vertex Pharmaceuticals
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
24900442 51 Discovery of a Novel Series of CHK1 Kinase Inhibitors with a Distinctive Hinge Binding Mode.EBI TBA
22437109 31 2-anilino-4-aryl-8H-purine derivatives as inhibitors of PDK1.EBI S*Bio
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
24900361 27 Exploring aigialomycin d and its analogues as protein kinase inhibitors for cancer targets.EBI TBA
21353571 26 Structure based design and syntheses of amino-1H-pyrazole amide derivatives as selective Raf kinase inhibitors in melanoma cells.EBI Hanyang University
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
20932759 100 4,5-Dihydro-1H-pyrazolo[4,3-h]quinazolines as potent and selective Polo-like kinase 1 (PLK1) inhibitors.EBI Nerviano Medical Sciences
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
20627564 51 Activity of substituted thiophene sulfonamides against malarial and mammalian cyclin dependent protein kinases.EBI Walter Reed Army Institute of Research
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
20138512 82 Discovery of potent and bioavailable GSK-3beta inhibitors.EBI Roche Palo Alto
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
20097066 53 Semi-synthetic aristolactams--inhibitors of CDK2 enzyme.EBI Schering-Plough Research Institute
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
20030405 7 Benzo[e]isoindole-1,3-diones as potential inhibitors of glycogen synthase kinase-3 (GSK-3). Synthesis, kinase inhibitory activity, zebrafish phenotype, and modeling of binding mode.EBI Peking University
19854650 70 Heterobiaryl purine derivatives as potent antiproliferative agents: inhibitors of cyclin dependent kinases. Part II.EBI Amri
19846305 86 Biaryl purine derivatives as potent antiproliferative agents: inhibitors of cyclin dependent kinases. Part I.EBI Amri
19778024 31 Discovery of a 2,4-disubstituted pyrrolo[1,2-f][1,2,4]triazine inhibitor (BMS-754807) of insulin-like growth factor receptor (IGF-1R) kinase in clinical development.EBI Bristol-Myers Squibb
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
19397322 58 Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.EBI National Cancer Institute-Bethesda
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
18789685 172 Kinase array design, back to front: biaryl amides.EBI Glaxosmithkline
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
18232649 60 Meriolins (3-(pyrimidin-4-yl)-7-azaindoles): synthesis, kinase inhibitory activity, cellular effects, and structure of a CDK2/cyclin A/meriolin complex.EBI University of Oxford
17935989 146 Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.EBI Abbott Laboratories
17339109 33 Synthesis and biological evaluation of pyrido[3',2':4,5]furo[3,2-d]pyrimidine derivatives as novel PI3 kinase p110alpha inhibitors.EBI Astellas Pharma
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 Astrazeneca
15857136 4 Conformation mining: an algorithm for finding biologically relevant conformations.EBI Rational Discovery
15999997 85 Design and synthesis of the first generation of novel potent, selective, and in vivo active (benzothiazol-2-yl)acetonitrile inhibitors of the c-Jun N-terminal kinase.EBI Serono Pharmaceutical Research Institute
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 Eli Lilly
15214773 76 Fragment-based drug discovery.EBI Sunesis Pharmaceuticals
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
12852764 20 Synthesis and in vitro characterization of 1-(4-aminofurazan-3-yl)-5-dialkylaminomethyl-1H-[1,2,3]triazole-4-carboxylic acid derivatives. A new class of selective GSK-3 inhibitors.EBI Novo Nordisk
15013000 31 Discovery and in vitro evaluation of potent TrkA kinase inhibitors: oxindole and aza-oxindoles.EBI Glaxosmithkline
10743948 22 5-Arylamino-2-methyl-4,7-dioxobenzothiazoles as inhibitors of cyclin-dependent kinase 4 and cytotoxic agents.EBI Ewha Womans University
 76 Synthesis and activity of 2,6,9-trisubstituted purinesEBI TBA
22377675 44 Indeno[1,2-b]indole derivatives as a novel class of potent human protein kinase CK2 inhibitors.EBI Westf£Lische Wilhelms-Universit£T M£Nster
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
16476733 18 Inhibition of S/G2 phase CDK4 reduces mitotic fidelity.EBI University of Queensland
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
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
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
22119469 107 Novel and selective spiroindoline-based inhibitors of Sky kinase.EBI Pfizer
22119465 18 Structure-based design of PDK1 inhibitors.EBI S Bio
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
22036212 8 Synthesis of 6-(het) ary Xylocydine analogues and evaluating their inhibitory activities of CDK1 and CDK2 in vitro.EBI Jilin University
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
22000924 25 Design, synthesis and biological study of novel pyrido[2,3-d]pyrimidine as anti-proliferative CDK2 inhibitors.EBI National Organization For Drug Control & Research
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
21907583 48 CNS and antimalarial activity of synthetic meridianin and psammopemmin analogs.EBI University of South Florida
21824779 67 Design and synthesis of novel amide AKT1 inhibitors with selectivity over CDK2.EBI Amgen
21699136 16 Selectivity of kinase inhibitor fragments.EBI Glaxosmithkline
21775140 69 Discovery of novel imidazo[1,2-a]pyridines as inhibitors of the insulin-like growth factor-1 receptor tyrosine kinase.EBI Astrazeneca
21723120 100 Synthesis and SAR of new pyrazolo[4,3-h]quinazoline-3-carboxamide derivatives as potent and selective MPS1 kinase inhibitors.EBI Nerviano Medical Sciences
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
21080703 20 A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration.EBI Imperial College
21620699 51 Substituted N-aryl-6-pyrimidinones: a new class of potent, selective, and orally active p38 MAP kinase inhibitors.EBI Pfizer
20630752 40 Discovery and optimization of N-acyl and N-aroylpyrazolines as B-Raf kinase inhibitors.EBI Millennium Pharmaceuticals
20621478 37 Concise synthesis and CDK/GSK inhibitory activity of the missing 9-azapaullones.EBI Trinity College
21561767 48 Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant.EBI Ariad Pharmaceuticals
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
21417417 8 Pyrazolo[4,3-d]pyrimidine bioisostere of roscovitine: evaluation of a novel selective inhibitor of cyclin-dependent kinases with antiproliferative activity.EBI Palacky£? University and Institute of Experimental Botany Ascr
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
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
21094608 74 Discovery of pyrazolo[1,5-a]pyrimidine-based CHK1 inhibitors: a template-based approach--part 1.EBI Merck Research Laboratories
21094607 66 Discovery of pyrazolo[1,5-a]pyrimidine-based CHK1 inhibitors: a template-based approach--part 2.EBI Merck Research Laboratories
21144757 15 Design, synthesis, and testing of an 6-O-linked series of benzimidazole based inhibitors of CDK5/p25.EBI Duquesne University
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
21038853 133 4-(Pyrazol-4-yl)-pyrimidines as selective inhibitors of cyclin-dependent kinase 4/6.EBI Novartis Institutes For Biomedical Research
20873740 111 Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding.EBI Nerviano Medical Sciences
20855207 26 Discovery of orally bioavailable imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.EBI Merck Research Laboratories
20832307 43 Pyrazolobenzodiazepines: part I. Synthesis and SAR of a potent class of kinase inhibitors.EBI Hoffmann-La Roche
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
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
16408016 6 Assignment of protein function in the postgenomic era.EBI The Scripps Research Institute
15958589 2 Seliciclib (CYC202, R-Roscovitine) induces cell death in multiple myeloma cells by inhibition of RNA polymerase II-dependent transcription and down-regulation of Mcl-1.EBI Cyclacel
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
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
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
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
20361800 22 5,5'-substituted indirubin-3'-oxime derivatives as potent cyclin-dependent kinase inhibitors with anticancer activity.EBI Institute of Science and Technology
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
20223663 100 2-Arylureidophenyl-4-(3-oxa-8-azabicyclo[3.2.1]octan-8-yl)triazines as highly potent and selective ATP competitive mTOR inhibitors: optimization of human microsomal stability.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
20137932 47 2-Aminothiadiazole inhibitors of AKT1 as potential cancer therapeutics.EBI Amgen
20045222 40 Design, synthesis, and biological evaluation of novel pyrimidine derivatives as CDK2 inhibitors.EBI National Organization For Drug Control & Research
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
19854645 87 Synthesis and PKCtheta inhibitory activity of a series of 5-vinyl phenyl sulfonamide-3-pyridinecarbonitriles.EBI Wyeth Research
20060294 21 Novel 3-aminopyrazole inhibitors of MK-2 discovered by scaffold hopping strategy.EBI Novartis Institutes For Biomedical Research
20141146 234 Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors.EBI Nerviano Medical Sciences
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
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
19361991 80 Structure-based design and parallel synthesis of N-benzyl isatin oximes as JNK3 MAP kinase inhibitors.EBI Vertex Pharmaceuticals
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
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
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
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
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
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
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
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
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 Pharma
17303421 56 Synthesis and activity of quinolinyl-methylene-thiazolinones as potent and selective cyclin-dependent kinase 1 inhibitors.EBI Roche Research Center
17291769 133 Clubbed thiazoles by MAOS: a novel approach to cyclin-dependent kinase 5/p25 inhibitors as a potential treatment for Alzheimer's disease.EBI Dr. Reddys Laboratories
17178224 28 3-Hydroxychromones as cyclin-dependent kinase inhibitors: synthesis and biological evaluation.EBI Keimyung University
17149885 20 Profile and molecular modeling of 3-(indole-3-yl)-4-(3,4,5-trimethoxyphenyl)-1 H-pyrrole-2,5-dione (1) as a highly selective VEGF-R2/3 inhibitor.EBI Eberhard-Karls University
17123821 21 Design, synthesis, and antiproliferative and CDK2-cyclin a inhibitory activity of novel flavopiridol analogues.EBI University of Kansas
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
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
16750360 36 CA224, a non-planar analogue of fascaplysin, inhibits Cdk4 but not Cdk2 and arrests cells at G0/G1 inhibiting pRB phosphorylation.EBI De Montfort University
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
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
16384702 35 CDK2/cyclinA inhibitors: targeting the cyclinA recruitment site with small molecules derived from peptide leads.EBI Genentech
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
16216502 119 Scaffold oriented synthesis. Part 1: Design, preparation, and biological evaluation of thienopyrazoles as kinase inhibitors.EBI Abbott Laboratories
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
15999992 25 Synthesis and identification of [1,3,5]triazine-pyridine biheteroaryl as a novel series of potent cyclin-dependent kinase inhibitors.EBI Johnson & Johnson Pharmaceutical Research and Development
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
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
15566294 5 Optimization of protein kinase CK2 inhibitors derived from 4,5,6,7-tetrabromobenzimidazole.EBI Università
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
15482916 64 Discovery and SAR of 2-aminothiazole inhibitors of cyclin-dependent kinase 5/p25 as a potential treatment for Alzheimer's disease.EBI Pfizer
15149684 59 3-(7-Azaindolyl)-4-arylmaleimides as potent, selective inhibitors of glycogen synthase kinase-3.EBI Johnson & Johnson Pharmaceutical Research & Development
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
14552791 35 Aryl[a]pyrrolo[3,4-c]carbazoles as selective cyclin D1-CDK4 inhibitors.EBI Eli Lilly
14505655 61 A catch-and-release strategy for the combinatorial synthesis of 4-acylamino-1,3-thiazoles as potential CDK5 inhibitors.EBI Pharmacia
12941335 8 Bone-targeted 2,6,9-trisubstituted purines: novel inhibitors of Src tyrosine kinase for the treatment of bone diseases.EBI Ariad Pharmaceuticals
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
12182847 12 Peptide inhibitors of CDK2-cyclin A that target the cyclin recruitment-site: structural variants of the C-terminal Phe.EBI University of Nottingham
12036347 116 Structural classification of protein kinases using 3D molecular interaction field analysis of their ligand binding sites: target family landscapes.EBI Aventis Pharma Deutschland
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
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
28487075 36 N-(1H-Pyrazol-3-yl)quinazolin-4-amines as a novel class of casein kinase 1?/? inhibitors: Synthesis, biological evaluation and molecular modeling studies.EBI Rajiv Gandhi Proudyogiki Vishwavidyalaya
28557430 45 Identification of a Water-Soluble Indirubin Derivative as Potent Inhibitor of Insulin-like Growth Factor 1 Receptor through Structural Modification of the Parent Natural Molecule.EBI University of Kaiserslautern
22957720 5 Synthesis, biological evaluation and docking studies of new pyrrolo[2,3-d] pyrimidine derivatives as Src family-selective tyrosine kinase inhibitors.BDB Ankara University
21985426 27 Chromone containing sulfonamides as potent carbonic anhydrase inhibitors.BDB Ondokuz Mayis University
28262558 62 Potent and Selective KDM5 Inhibitor Stops Cellular Demethylation of H3K4me3 at Transcription Start Sites and Proliferation of MM1S Myeloma Cells.BDB University of Oxford
24327656 9 The molecular chaperone Hsp70 activates protein phosphatase 5 (PP5) by binding the tetratricopeptide repeat (TPR) domain.BDB University of Michigan
27359042 29 IDD388 Polyhalogenated Derivatives as Probes for an Improved Structure-Based Selectivity of AKR1B10 InhibitorsBDB Institut De Ge??Ne??Tique Et De Biologie Mole??Culaire Et Cellulaire
22366955 11 Blind prediction of host-guest binding affinities: a new SAMPL3 challenge.BDB University of California San Diego
25346162 16 Synthesis, Biological Evaluation, and Molecular Simulation of Chalcones and Aurones as Selective MAO-B Inhibitors.BDB Pontificia Universidad Catolica De Chile
24403173 12 Long residence times revealed by Aurora A kinase-targeting fluorescent probes derived from inhibitors MLN8237 and VX-689.BDB University of Tartu
 113 CDK2-CyclinA in CSAR_FULL_RELEASE_3JULY2012BDB Csar
17616524 6 Live cell monitoring of mu-opioid receptor-mediated G-protein activation reveals strong biological activity of close morphine biosynthetic precursors.BDB University of WÜRzburg
16492568 12 Differential binding of inhibitors to active and inactive CDK2 provides insights for drug design.BDB Cyclacel
16242653 33 A proteome-wide CDK/CRK-specific kinase inhibitor promotes tumor cell death in the absence of cell cycle progression.BDB Gpc Biotech
19827834 93 Structure-guided design of potent and selective pyrimidylpyrrole inhibitors of extracellular signal-regulated kinase (ERK) using conformational control.BDB Vertex Pharmaceuticals
19097791 44 2-(6-Phenyl-1H-indazol-3-yl)-1H-benzo[d]imidazoles: design and synthesis of a potent and isoform selective PKC-zeta inhibitor.BDB Pfizer
19200745 35 Design, synthesis and structure-activity relationships of 1,3,4-oxadiazole derivatives as novel inhibitors of glycogen synthase kinase-3beta.BDB Takeda Pharmaceutical
19603809 59 Identification of N,1,4,4-Tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a Potent, Orally Available Cyclin Dependent Kinase Inhibitor.BDB Nerviano Medical Sciences
19128055 24 Pyrazolo[1,5-a]-1,3,5-triazine as a purine bioisostere: access to potent cyclin-dependent kinase inhibitor (R)-roscovitine analogue.BDB Universite De Lyon
19143567 49 Fragment-based discovery of the pyrazol-4-yl urea (AT9283), a multitargeted kinase inhibitor with potent aurora kinase activity.BDB Astex
17098432 10 Anti-breast cancer activity of LFM-A13, a potent inhibitor of Polo-like kinase (PLK).BDB Paradigm Pharmaceuticals
18656911 39 Identification of N-(4-piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxamide (AT7519), a novel cyclin dependent kinase inhibitor using fragment-based X-ray crystallography and structure based drug design.BDB Astex
17697781 29 Structure-activity relationships of 3,4-dihydro-1H-quinazolin-2-one derivatives as potential CDK5 inhibitors.BDB Amgen
17570665 19 Discovery of a potent CDK2 inhibitor with a novel binding mode, using virtual screening and initial, structure-guided lead scoping.BDB Vernalis (R&D)
12244092 12 Structural basis for Chk1 inhibition by UCN-01.BDB Glaxosmithkline
16289938 24 Identification of a buried pocket for potent and selective inhibition of Chk1: prediction and verification.BDB Vernalis (R&D)
17064073 78 Discovery of [4-Amino-2-(1-methanesulfonylpiperidin-4-ylamino)pyrimidin-5-yl](2,3-difluoro-6-methoxyphenyl)methanone (R547), a potent and selective cyclin-dependent kinase inhibitor with significant in vivo antitumor activity.BDB Hoffmann-La Roche
16616492 3 A practical synthesis of the major 3-hydroxy-2-pyrrolidinone metabolite of a potent CDK2/cyclin A inhibitor.BDB Nerviano Medical Sciences
16290148 44 3-Amino-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: a new class of CDK2 inhibitors.BDB Nerviano Medical Sciences
16942020 12 Dissecting the determinants of cyclin-dependent kinase 2 and cyclin-dependent kinase 4 inhibitor selectivity.BDB University of Oxford
17064068 36 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.BDB Palacky University
11170642 12 Crystal structure of human cyclin-dependent kinase 2 in complex with the adenine-derived inhibitor H717.BDB Lawrence Berkeley National Laboratory
16325401 25 Triazolo[1,5-a]pyrimidines as novel CDK2 inhibitors: protein structure-guided design and SAR.BDB Vernalis (R&D)
15686876 17 Structure-guided design of pyrazolo[1,5-a]pyrimidines as inhibitors of human cyclin-dependent kinase 2.BDB Vernalis (R&D)
15985434 18 Crystal structure of pyridoxal kinase in complex with roscovitine and derivatives.BDB Chinese Academy of Sciences
10891109 19 Docking-based development of purine-like inhibitors of cyclin-dependent kinase-2.BDB Palacky University
12852944 26 3,5,6-Trisubstituted naphthostyrils as CDK2 inhibitors.BDB Hoffmann-La Roche
15012993 22 A new series of potent oxindole inhibitors of CDK2.BDB Hoffmann-La Roche
12659774 20 Synthesis of potent oxindole CDK2 inhibitors.BDB Hoffmann-La Roche
15225695 64 4-Acylamino-6-arylfuro[2,3-d]pyrimidines: potent and selective glycogen synthase kinase-3 inhibitors.BDB Tsukuba Research Laboratories
12941317 25 Anilinopyrazole as selective CDK2 inhibitors: design, synthesis, biological evaluation, and X-ray crystallographic analysis.BDB Glaxosmithkline
12941333 61 6-heteroaryl-pyrazolo[3,4-b]pyridines: potent and selective inhibitors of glycogen synthase kinase-3 (GSK-3).BDB Glaxosmithkline
12699760 19 5-aryl-pyrazolo[3,4-b]pyridazines: potent inhibitors of glycogen synthase kinase-3 (GSK-3).BDB Glaxosmithkline
15341487 213 N-Phenyl-4-pyrazolo[1,5-b]pyridazin-3-ylpyrimidin-2-amines as potent and selective inhibitors of glycogen synthase kinase 3 with good cellular efficacy.BDB Glaxosmithkline
15261277 30 Synthesis and biological activity of 2-anilino-4-(1H-pyrrol-3-yl) pyrimidine CDK inhibitors.BDB Cyclacel
15027857 66 2-Anilino-4-(thiazol-5-yl)pyrimidine CDK inhibitors: synthesis, SAR analysis, X-ray crystallography, and biological activity.BDB Cyclacel
11728181 188 Oxindole-based inhibitors of cyclin-dependent kinase 2 (CDK2): design, synthesis, enzymatic activities, and X-ray crystallographic analysis.BDB Glaxosmithkline
15081018 14 Imidazo[1,2-b]pyridazines: a potent and selective class of cyclin-dependent kinase inhibitors.BDB Astrazeneca
15081017 17 Imidazo[1,2-a]pyridines. Part 2: SAR and optimisation of a potent and selective class of cyclin-dependent kinase inhibitors.BDB Astrazeneca
12941325 18 Imidazo[1,2-a]pyridines: a potent and selective class of cyclin-dependent kinase inhibitors identified through structure-based hybridisation.BDB Astrazeneca
12941312 58 Cyclin-dependent kinase 4 inhibitors as a treatment for cancer. Part 2: identification and optimisation of substituted 2,4-bis anilino pyrimidines.BDB Astrazeneca
12941311 34 Cyclin-dependent kinase 4 inhibitors as a treatment for cancer. Part 1: identification and optimisation of substituted 4,6-bis anilino pyrimidines.BDB Astrazeneca
11960485 18 Structure-based design and synthesis of 2-benzylidene-benzofuran-3-ones as flavopiridol mimics.BDB Novartis Pharmaceuticals
15664865 37 Novel CDK inhibition profiles of structurally varied 1-aza-9-oxafluorenes.BDB Martin-Luther-University Halle-Wittenberg
12749903 69 Novel pyrrolyllactone and pyrrolyllactam indolinones as potent cyclin-dependent kinase 2 inhibitors.BDB Sugen
15713378 72 Benzodipyrazoles: a new class of potent CDK2 inhibitors.BDB Nerviano Medical Sciences
15189033 48 3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 1. Lead finding.BDB Pharmacia Italia
15828833 29 3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 2. Lead optimization.BDB Nerviano Medical Sciences
11311054 14 Indenopyrazoles as novel cyclin dependent kinase (CDK) inhibitors.BDB Dupont Pharmaceuticals
11354366 81 Quinazolines as cyclin dependent kinase inhibitors.BDB Dupont Pharmaceuticals
15482910 53 Parallel synthesis of acylsemicarbazide libraries: preparation of potent cyclin dependent kinase (cdk) inhibitors.BDB Dupont Pharmaceuticals
15974571 62 1-Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities.BDB Johnson & Johnson Pharmaceutical
12747775 56 Synthesis, structure-activity relationship, and biological studies of indolocarbazoles as potent cyclin D1-CDK4 inhibitors.BDB Eli Lilly
12824014 284 Novel, potent and selective cyclin D1/CDK4 inhibitors: indolo[6,7-a]pyrrolo[3,4-c]carbazoles.BDB Eli Lilly
14552792 53 Studies on cyclin-dependent kinase inhibitors: indolo-[2,3-a]pyrrolo[3,4-c]carbazoles versus bis-indolylmaleimides.BDB Eli Lilly
15149644 37 Synthesis of 1,7-annulated indoles and their applications in the studies of cyclin dependent kinase inhibitors.BDB Eli Lilly
15149678 32 1,7-annulated indolocarbazoles as cyclin-dependent kinase inhibitors.BDB Eli Lilly
15225699 27 Preparation of novel aza-1,7-annulated indoles and their conversion to potent indolocarbazole kinase inhibitors.BDB Eli Lilly
15546737 59 Aminoimidazo[1,2-a]pyridines as a new structural class of cyclin-dependent kinase inhibitors. Part 1: Design, synthesis, and biological evaluation.BDB Avenida De La Industria
15780638 45 Structure-based design of a new class of highly selective aminoimidazo[1,2-a]pyridine-based inhibitors of cyclin dependent kinases.BDB Eli Lilly
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
15801830 127 Pyrido[2,3-d]pyrimidin-7-ones as specific inhibitors of cyclin-dependent kinase 4.BDB Pfizer
15993068 101 2-Aminoquinazoline inhibitors of cyclin-dependent kinases.BDB Naeja Pharmaceutical
15801831 94 Discovery of a potent and selective inhibitor of cyclin-dependent kinase 4/6.BDB Pfizer
11101352 88 Pyrido[2,3-d]pyrimidin-7-one inhibitors of cyclin-dependent kinases.BDB Parke-Davis Pharmaceutical Research
14698155 68 Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. Part 4: Heterocycles at C3.BDB Bristol-Myers Squibb
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