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219 articles for thisTarget

The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
26318056 25 Investigation of new 2-aryl substituted Benzothiopyrano[4,3-d]pyrimidines as kinase inhibitors targeting vascular endothelial growth factor receptor 2.EBI Universit£ di Pisa
26318067 34 Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors.EBI Hanyang University
26233434 115 Design, synthesis and biological characterization of selective LIMK inhibitors.EBI Amakem Therapeutics N.V.
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
25662701 23 Synthesis and biological evaluation of 3-([1,2,4]triazolo[4,3-a]pyridin-3-yl)-4-(indol-3-yl)-maleimides as potent, selective GSK-3▀ inhibitors and neuroprotective agents.EBI Zhejiang University
26071372 89 Synthesis and evaluation of novel 1H-pyrrolo[2,3-b]pyridine-5-carboxamide derivatives as potent and orally efficacious immunomodulators targeting JAK3.EBI Astellas Pharma Inc.
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
25689347 29 Exploitation of the ability of┐-tocopherol to facilitate membrane co-localization of Akt and PHLPP1 to develop PHLPP1-targeted Akt inhibitors.EBI The Ohio State University
24980703 296 Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors.EBI Nerviano Medical Sciences
24913714 53 Discovery of a novel series of potent MK2 non-ATP competitive inhibitors using 1,2-substituted azoles as cis-amide isosteres.EBI Merck Research Laboratories
24811300 20 Biased and unbiased strategies to identify biologically active small molecules.EBI Institut de Chimie des Substances Naturelles
25462247 20 In vitro and in vivo characterization of a benzofuran derivative, a potential anticancer agent, as a novel Aurora B kinase inhibitor.EBI Fudan University
25409491 83 A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles.EBI Zhejiang University
25313996 91 Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase.EBI Merck Research Laboratories
25180768 11 2013 Philip S. Portoghese Medicinal Chemistry Lectureship: drug discovery targeting allosteric sites.EBI Vanderbilt University Medical Center
24900862 14 Phenylalanine-Based Inactivator of AKT Kinase: Design, Synthesis, and Biological Evaluation.EBI Virginia Commonwealth University
24139169 175 Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.EBI Nerviano Medical Sciences
24650640 43 Discovery of 4-anilinoa-carbolines as novel Brk inhibitors.EBI Martin-Luther University Halle-Wittenberg
24508830 13 Integrating docking scores, interaction profiles and molecular descriptors to improve the accuracy of molecular docking: toward the discovery of novel Akt1 inhibitors.EBI Zhejiang University
24440479 4 Discovery of N-(3-((7H-purin-6-yl)thio)-4-hydroxynaphthalen-1-yl)-sulfonamide derivatives as novel protein kinase and angiogenesis inhibitors for the treatment of cancer: Synthesis and biological evaluation. Part III.EBI Shandong University
24389511 25 Structure-based design, synthesis and biological evaluation of diphenylmethylamine derivatives as novel Akt1 inhibitors.EBI Zhejiang University
24479418 39 Cytotoxic and protein kinase inhibiting nakijiquinones and nakijiquinols from the sponge Dactylospongia metachromia.EBI Heinrich-Heine-Universit£t
24328302 94 Protein kinase and HDAC inhibitors from the endophytic fungus Epicoccum nigrum.EBI Heinrich-Heine-Universit£t D£sseldorf
24321345 11 Preparation and evaluation of deconstruction analogues of 7-deoxykalafungin as AKT kinase inhibitors.EBI Virginia Commonwealth University
24100158 148 Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90).EBI Nerviano Medical Sciences S.r.l.
24036042 2 Discovery of 4-amino-2-(thio)phenol derivatives as novel protein kinase and angiogenesis inhibitors for the treatment of cancer: synthesis and biological evaluation. Part II.EBI Shandong University
23920481 25 Synthesis and evaluation of heteroaryl substituted diazaspirocycles as scaffolds to probe the ATP-binding site of protein kinases.EBI The Institute of Cancer Research
23602398 43 Conformation constraint of anilides enabling the discovery of tricyclic lactams as potent MK2 non-ATP competitive inhibitors.EBI Merck Research Laboratories
23587425 37 Potency switch between CHK1 and MK2: discovery of imidazo[1,2-a]pyrazine- and imidazo[1,2-c]pyrimidine-based kinase inhibitors.EBI Merck Research Laboratories
23535330 83 Structure-based design and optimization of 2-aminothiazole-4-carboxamide as a new class of CHK1 inhibitors.EBI Merck Research Laboratories
23506825 71 Structure-based design, SAR analysis and antitumor activity of PI3K/mTOR dual inhibitors from 4-methylpyridopyrimidinone series.EBI Pfizer Inc.
23434140 35 Substituted indolin-2-ones as p90 ribosomal S6 protein kinase 2 (RSK2) inhibitors: Molecular docking simulation and structure-activity relationship analysis.EBI East China University of Science and Technology
23415083 13 Synthesis, characterization and Akt phosphorylation inhibitory activity of cyclopentanecarboxylate-substituted alkylphosphocholines.EBI Kyung Hee University
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
23550937 72 Monocarbonyl curcumin analogues: heterocyclic pleiotropic kinase inhibitors that mediate anticancer properties.EBI Emory University
23414845 44 Structure-based discovery of cellular-active allosteric inhibitors of FAK.EBI Takeda Pharmaceutical Company Ltd
23394126 170 Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).EBI Exelixis
23249297 75 Trimeric hemibastadin congener from the marine sponge Ianthella basta.EBI Heinrich-Heine University
23394218 159 Discovery of 4-amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide (AZD5363), an orally bioavailable, potent inhibitor of Akt kinases.EBI AstraZeneca
23312943 166 Optimization of highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.EBI Pfizer Inc.
23312472 129 Highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.EBI Pfizer Inc.
22621397 39 Irreversible protein kinase inhibitors: balancing the benefits and risks.EBI Covalution Pharma BV
23103095 125 Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.EBI Abbott Laboratories
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
22934575 124 Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.EBI Array BioPharma Inc.
22533986 181 Discovery and optimization of a series of 3-(3-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amines: orally bioavailable, selective, and potent ATP-independent Akt inhibitors.EBI ArQule Inc.
22548342 210 Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase¿ inhibitors.EBI Exelixis
22889562 3 Synthesis, cytotoxicity of new 4-arylidene curcumin analogues and their multi-functions in inhibition of both NF-¿B and Akt signalling.EBI Sun Yat-sen University
22795331 51 Pyrimidinopyrimidine inhibitors of ketohexokinase: exploring the ring C2 group that interacts with Asp-27B in the ligand binding pocket.EBI Janssen Pharmaceutical Companies of Johnson& Johnson
22560627 70 2-Anilino-4-(benzimidazol-2-yl)pyrimidines--a multikinase inhibitor scaffold with antiproliferative activity toward cancer cell lines.EBI Technische Universit£t Braunschweig
22248236 24 Diverse heterocyclic scaffolds as allosteric inhibitors of AKT.EBI AstraZeneca
22320327 250 Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series.EBI Amgen Inc.
22450127 64 Pyrazolopyrimidines as dual Akt/p70S6K inhibitors.EBI Exelixis
22342124 9 Design and evaluation of a series of pyrazolopyrimidines as p70S6K inhibitors.EBI Exelixis
20591679 1 Development of chemical probes: toward the mode of action of a methylene-linked di(aryl acetate) E1.EBI University College London
15975507 13 Features of selective kinase inhibitors.EBI University of California-San Francisco
18469809 41 A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity.EBI Nerviano Medical Sciences Oncology
20000735 12 Through the"gatekeeper door": exploiting the active kinase conformation.EBI Nerviano Medical Sciences
20153204 109 Optimization of 6,6-dimethyl pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing.EBI Nerviano Medical Sciences Srl
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
19081716 57 Optimization of a series of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine inhibitors of IGF-1R: elimination of an acid-mediated decomposition pathway.EBI GlaxoSmithKline
14593182 34 Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor.EBI Pfizer Global Researchand Development
18434148 43 Synthesis and PKCtheta inhibitory activity of a series of 4-(indol-5-ylamino)thieno[2,3-b]pyridine-5-carbonitriles.EBI Wyeth Research
18362070 79 Scaffold oriented synthesis. Part 2: Design, synthesis and biological evaluation of pyrimido-diazepines as receptor tyrosine kinase inhibitors.EBI Abbott Laboratories
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
17983756 55 Novel 2-phenylquinolin-7-yl-derived imidazo[1,5-a]pyrazines as potent insulin-like growth factor-I receptor (IGF-IR) inhibitors.EBI OSI Pharmaceuticals, Inc.
18054229 35 Development of potent, allosteric dual Akt1 and Akt2 inhibitors with improved physical properties and cell activity.EBI Merck& Co.
18479914 52 Allosteric inhibitors of Akt1 and Akt2: a naphthyridinone with efficacy in an A2780 tumor xenograft model.EBI Merck Research Laboratories
18296048 50 Rapid assembly of diverse and potent allosteric Akt inhibitors.EBI Merck Research Laboratories
18248814 24 Imidazo[4,5-c]quinolines as inhibitors of the PI3K/PKB-pathway.EBI Novartis Institute for BioMedical Research
17935989 146 Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.EBI Abbott Laboratories
17887663 34 Structure-based design and synthesis of (5-arylamino-2H-pyrazol-3-yl)-biphenyl-2',4'-diols as novel and potent human CHK1 inhibitors.EBI Pfizer Global Research and Development
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
16789737 1 Synthesis, molecular characterization, and biological activity of novel synthetic derivatives of chromen-4-one in human cancer cells.EBI University of Pune
16460940 13 Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis.EBI Hoffmann-La Roche Inc.
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 Lilly Research Laboratories
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 Pharmaceuticals Inc.
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
22204902 9 Synthesis and biological activity of novel organoselenium derivatives targeting multiple kinases and capable of inhibiting cancer progression to metastases.EBI Institute of the Sir Mortimer Jewish General Hospital
22040023 63 Discovery of novel, potent, and selective inhibitors of 3-phosphoinositide-dependent kinase (PDK1).EBI Pfizer Inc.
22154349 123 5-(2-amino-pyrimidin-4-yl)-1H-pyrrole and 2-(2-amino-pyrimidin-4-yl)-1,5,6,7-tetrahydro-pyrrolo[3,2-c]pyridin-4-one derivatives as new classes of selective and orally available Polo-like kinase 1 inhibitors.EBI Nerviano Medical Sciences srl
22119469 107 Novel and selective spiroindoline-based inhibitors of Sky kinase.EBI Pfizer Inc.
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
22001093 4 Synthesis of GSK3ß mimetic inhibitors of Akt featuring a novel extended dipeptide surrogate.EBI H. Lee Moffitt Cancer Center and Research Institute
21982797 128 9,10-secosteroids, protein kinase inhibitors from the Chinese gorgonian Astrogorgia sp.EBI Peking University
22027102 7 Pharmacophore identification, virtual screening and biological evaluation of prenylated flavonoids derivatives as PKB/Akt1 inhibitors.EBI Zhejiang 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
21999461 90 1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase.EBI Rhône-Poulenc Rorer
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.
21823617 58 9-substituted 6,6-dimethyl-11-oxo-6,11-dihydro-5H-benzo[b]carbazoles as highly selective and potent anaplastic lymphoma kinase inhibitors.EBI Chugai Pharmaceutical Co., Ltd.
21714526 54 Structure-activity relationships of phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors: investigations of various 6,5-heterocycles to improve metabolic stability.EBI Amgen Inc.
21699136 16 Selectivity of kinase inhibitor fragments.EBI GlaxoSmithKline R&D
21741249 32 Arthrinins A-D: novel diterpenoids and further constituents from the sponge derived fungus Arthrinium sp.EBI Heinrich-Heine-Universit£t
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
21650457 25 Backbone cyclic peptide inhibitors of protein kinase B (PKB/Akt).EBI The Hebrew University of Jerusalem
21561771 39 Discovery of novel tetracyclic compounds as anaplastic lymphoma kinase inhibitors.EBI Chugai Pharmaceutical Co. Ltd.
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
21332118 157 Discovery and optimization of a series of benzothiazole phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors.EBI Amgen Inc.
21391610 139 Discovery and structure-activity relationship of 3-aminopyrid-2-ones as potent and selective interleukin-2 inducible T-cell kinase (Itk) inhibitors.EBI Vertex Pharmaceuticals (Europe) Ltd.
21341675 266 Structure-based design of potent and selective 3-phosphoinositide-dependent kinase-1 (PDK1) inhibitors.EBI GlaxoSmithKline
21420856 37 Discovery of spirocyclic sulfonamides as potent Akt inhibitors with exquisite selectivity against PKA.EBI Array BioPharma Inc.
21392984 50 Discovery and SAR of spirochromane Akt inhibitors.EBI Array BioPharma, Inc.
20971641 53 Discovery of dihydrothieno- and dihydrofuropyrimidines as potent pan Akt inhibitors.EBI Array BioPharma Inc.
21038853 133 4-(Pyrazol-4-yl)-pyrimidines as selective inhibitors of cyclin-dependent kinase 4/6.EBI Novartis Institutes for Biomedical Research
20875738 9 5,6,7,8-Tetrahydropyrido[4,3-d]pyrimidines as novel class of potent and highly selective CaMKII inhibitors.EBI Dainippon Sumitomo Pharma Co., Ltd
20873740 111 Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding.EBI Nerviano Medical Sciences Srl
20855207 26 Discovery of orally bioavailable imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.EBI Merck Research Laboratories
20817473 57 Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity.EBI Nerviano Medical Sciences-Oncology
20817449 19 4-methylpteridinones as orally active and selective PI3K/mTOR dual inhibitors.EBI Pfizer Inc.
20810279 86 Discovery of pyrrolopyrimidine inhibitors of Akt.EBI Array BioPharma Inc
19465931 12 Inhibitor hijacking of Akt activation.EBI University of California
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
10998351 24 Specificity and mechanism of action of some commonly used protein kinase inhibitors.EBI University of Dundee
20481595 48 Design of selective, ATP-competitive inhibitors of Akt.EBI Pfizer Global Research and Development
20483608 139 New pyrazolo[1,5a]pyrimidines as orally active inhibitors of Lck.EBI Novartis Institute of Biomedical Research
20462263 127 Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors.EBI Cyclacel Ltd.
20397705 208 Identification of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as a new class of orally and selective Polo-like kinase 1 inhibitors.EBI Nerviano Medical Sciences Srl
20363128 42 Optimization of 7-alkene-3-quinolinecarbonitriles as Src kinase inhibitors.EBI Wyeth Research
20074837 58 The identification of 8,9-dimethoxy-5-(2-aminoalkoxy-pyridin-3-yl)-benzo[c][2,7]naphthyridin-4-ylamines as potent inhibitors of 3-phosphoinositide-dependent kinase-1 (PDK-1).EBI Wyeth Research
19179070 89 Aminofurazans as potent inhibitors of AKT kinase.EBI GlaxoSmithKline
20347317 6 Synthesis and structure-activity relationship studies of peptidomimetic PKB/Akt inhibitors: the significance of backbone interactions.EBI The Hebrew University of Jerusalem
20307980 22 B-Raf kinase inhibitors: hit enrichment through scaffold hopping.EBI Wyeth Research
19884006 47 Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors.EBI Wyeth Research
20166671 85 Selectively nonselective kinase inhibition: striking the right balance.EBI Schering-Plough
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.
19969400 4 5-Substituted [1]pyrindine derivatives with antiproliferative activity.EBI INSERM
19879134 94 Imidazo[1,2-a]pyrazine diaryl ureas: inhibitors of the receptor tyrosine kinase EphB4.EBI CGI Pharmaceuticals, Inc.
20045647 35 Synthesis and optimization of thiadiazole derivatives as a novel class of substrate competitive c-Jun N-terminal kinase inhibitors.EBI Institute for Medical Research
20151677 67 Discovery of 4-amino-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamides as selective, orally active inhibitors of protein kinase B (Akt).EBI Institute of Cancer Research
20141146 234 Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors.EBI Nerviano Medical Sciences Srl
20093027 92 Discovery of 6-benzyloxyquinolines as c-Met selective kinase inhibitors.EBI Chugai Pharmaceutical Co, Ltd
20006500 60 Tetrasubstituted pyridines as potent and selective AKT inhibitors: Reduced CYP450 and hERG inhibition of aminopyridines.EBI GlaxoSmithKline
20006497 49 2,3,5-Trisubstituted pyridines as selective AKT inhibitors-Part I: Substitution at 2-position of the core pyridine for ROCK1 selectivity.EBI GlaxoSmithKline
20005102 34 2,3,5-Trisubstituted pyridines as selective AKT inhibitors. Part II: Improved drug-like properties and kinase selectivity from azaindazoles.EBI GlaxoSmithKline
19945869 7 Pyrrole derivatives as potent inhibitors of lymphocyte-specific kinase: Structure, synthesis, and SAR.EBI Taisho Pharmaceutical Co., Ltd
19945867 39 Ring-fused pyrazole derivatives as potent inhibitors of lymphocyte-specific kinase (Lck): Structure, synthesis, and SAR.EBI Taisho Pharmaceutical Co., Ltd
19926477 100 2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.EBI Abbott Laboratories
19734051 17 Computational modeling of novel inhibitors targeting the Akt pleckstrin homology domain.EBI The University of Texas
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
19497644 147 QSAR study of Akt/protein kinase B (PKB) inhibitors using support vector machine.EBI Zhejiang University
19604696 6 Discovery of a novel protein kinase B inhibitor by structure-based virtual screening.EBI Torrey Pines Institute for Molecular Studies
19362830 47 Identification of pyrazolo[1,5-a]pyrimidine-3-carboxylates as B-Raf kinase inhibitors.EBI Wyeth Research
19356929 17 Discovery and characterization of the N-phenyl-N'-naphthylurea class of p38 kinase inhibitors.EBI Boehringer Ingelheim Pharmaceutical
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
19285393 90 Discovery of 5-pyrrolopyridinyl-2-thiophenecarboxamides as potent AKT kinase inhibitors.EBI GlaxoSmithKline
19097777 55 Allosteric inhibitors of Akt1 and Akt2: discovery of [1,2,4]triazolo[3,4-f][1,6]naphthyridines with potent and balanced activity.EBI Merck Research Laboratories
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
18996009 36 Benzimidazole- and benzoxazole-based inhibitors of Rho kinase.EBI The Scripps Research Institute Florida
18990570 72 Chroman-3-amides as potent Rho kinase inhibitors.EBI The Scripps Research Institute
18815050 34 4-Anilino-7-alkenylquinoline-3-carbonitriles as potent MEK1 kinase inhibitors.EBI Wyeth Research
18550373 97 The design and synthesis of potent and cell-active allosteric dual Akt 1 and 2 inhibitors devoid of hERG activity.EBI Merck Research Laboratories
18539456 106 Discovery of potent and cell-active allosteric dual Akt 1 and 2 inhibitors.EBI Merck Research Laboratories
18457385 41 Recent developments in fragment-based drug discovery.EBI Astex Therapeutics Ltd.
15620258 2 A phthalide with in vitro growth inhibitory activity from an oidiodendron strain.EBI Cetek Corporation
18248988 16 Entry into a new class of protein kinase inhibitors by pseudo ring design.EBI Novartis Institutes for BioMedical Research
17826092 37 Optimization of triarylimidazoles for Tie2: influence of conformation on potency.EBI GlaxoSmithKline
17658776 109 Design, synthesis, and biological activity of 5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-one-based potent and selective Chk-1 inhibitors.EBI Abbott Laboratories
17574417 98 SAR of a novel 'Anthranilamide Like' series of VEGFR-2, multi protein kinase inhibitors for the treatment of cancer.EBI Bayer Research Center
17343372 143 Discovery of N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea (ABT-869), a 3-aminoindazole-based orally active multitargeted receptor tyrosine kinase inhibitor.EBI Abbott Laboratories
17276059 32 Modifications of the GSK3beta substrate sequence to produce substrate-mimetic inhibitors of Akt as potential anti-cancer therapeutics.EBI Yale University
17188862 27 Inhibition of Src kinase activity by 7-ethynyl-4-phenylamino-3-quinolinecarbonitriles: identification of SKS-927.EBI Wyeth Research
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
16990001 12 Synthesis and biological evaluation of 5-arylamino-6-chloro-1H-indazole-4,7-diones as inhibitors of protein kinase B/Akt.EBI ILDONG Pharmaceutical Co. Ltd.
16970394 147 Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity.EBI Amgen, Inc.
16765046 63 Discovery of 2-pyrimidyl-5-amidothiophenes as potent inhibitors for AKT: synthesis and SAR studies.EBI Chiron Corporation
16682193 62 Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
16216502 119 Scaffold oriented synthesis. Part 1: Design, preparation, and biological evaluation of thienopyrazoles as kinase inhibitors.EBI Abbott Laboratories
12672234 64 Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase.EBI Boehringer Ingelheim Pharmaceuticals
25453512 3 Design, synthesis, biological evaluation, and molecular docking of novel benzopyran and phenylpyrazole derivatives as Akt inhibitors.BDB Zhejiang University
18829454 12 Potent and selective disruption of protein kinase D functionality by a benzoxoloazepinolone.BDB University of Pittsburgh
20385558 8 Discovery of PDK1 kinase inhibitors with a novel mechanism of action by ultrahigh throughput screening.BDB Merck Research Laboratories
19179081 32 Non-peptidic substrate-mimetic inhibitors of Akt as potential anti-cancer agents.BDB Yale University
19309081 18 Pyranonaphthoquinone lactones: a new class of AKT selective kinase inhibitors alkylate a regulatory loop cysteine.BDB Wyeth Research
18834107 22 Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors.BDB The Scripps Research Institute
18800763 93 Identification of 4-(2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{[(3S)-3-piperidinylmethyl]oxy}-1H-imidazo[4,5-c]pyridin-4-yl)-2-methyl-3-butyn-2-ol (GSK690693), a novel inhibitor of AKT kinase.BDB GlaxoSmithKline
18294842 29 Optimization of 2,3,5-trisubstituted pyridine derivatives as potent allosteric Akt1 and Akt2 inhibitors.BDB Merck Research Laboratories
18249537 56 Development of pyridopyrimidines as potent Akt1/2 inhibitors.BDB Merck Research Laboratories
18456494 19 Synthesis and structure based optimization of novel Akt inhibitors.BDB Pfizer
16289938 24 Identification of a buried pocket for potent and selective inhibition of Chk1: prediction and verification.BDB Vernalis (R&D) Ltd
15801821 5 Virtual docking approaches to protein kinase B inhibition.BDB The Burnham Institute
15686884 48 Discovery of 2,3,5-trisubstituted pyridine derivatives as potent Akt1 and Akt2 dual inhibitors.BDB Merck Research Laboratories
15664853 66 Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors.BDB Merck Research Laboratories
14998327 12 Structure-based optimization of novel azepane derivatives as PKB inhibitors.BDB Roche Diagnostics GmbH
15634010 10 Design and crystal structures of protein kinase B-selective inhibitors in complex with protein kinase A and mutants.BDB Max-Planck-Institut fuer Biochemie