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132 articles for thisTarget


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PMIDDataArticle TitleOrganization
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.
1597853 2 A nonpromoting phorbol from the samoan medicinal plant Homalanthus nutans inhibits cell killing by HIV-1.EBI National Cancer Institute (NCI)
1992155 30 Design of potent protein kinase inhibitors using the bisubstrate approach.EBI URA CNRS 1309
2342075 11 Synthesis of quaternary amine ether lipids and evaluation of neoplastic cell growth inhibitory properties.EBI University of North Carolina
11454465 4 Synthesis of N-alkyl substituted indolocarbazoles as potent inhibitors of human cytomegalovirus replication.EBI GlaxoSmithKline Medicines Research Centre
27362616 41 G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitors: Current Trends and Future Perspectives.EBI Universit£ degli Studi di Messina
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 Srl
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 Company, Ltd
26896709 113 Systematic diversification of benzylidene heterocycles yields novel inhibitor scaffolds selective for Dyrk1A, Clk1 and CK2.EBI Saarland University
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
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
25000588 72 Discovery of selective and orally bioavailable protein kinase C┐ (PKC┐) inhibitors from a fragment hit.EBI AbbVie Bioresearch Center
24980703 296 Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors.EBI Nerviano Medical Sciences
24139169 175 Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.EBI Nerviano Medical Sciences
23394126 170 Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).EBI Exelixis
23398373 88 Design and optimization of selective protein kinase C¿ (PKC¿) inhibitors for the treatment of autoimmune diseases.EBI Vertex Pharmaceuticals (Europe) Ltd.
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
21797275 139 Structure-activity relationship and pharmacokinetic studies of sotrastaurin (AEB071), a promising novel medicine for prevention of graft rejection and treatment of psoriasis.EBI Novartis Institutes for BioMedical Research
22078216 146 2,6-Naphthyridines as potent and selective inhibitors of the novel protein kinase C isozymes.EBI Novartis Institutes for BioMedical Research
22625994 28 Structure-activity studies on the spiroketal moiety of a simplified analogue of debromoaplysiatoxin with antiproliferative activity.EBI Kyoto University
22738630 76 Structure-based optimization of aminopyridines as PKC¿ inhibitors.EBI Department of Chemistry at Vertex Pharmaceuticals (Europe) Ltd
18469809 41 A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity.EBI Nerviano Medical Sciences Oncology
19703774 56 C-5 substituted heteroaryl-3-pyridinecarbonitriles as PKCtheta inhibitors: part II.EBI Wyeth Research
9677190 49 Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors.EBI University of California
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
18077363 314 A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.EBI University of Oxford
17997320 29 Novel pyrazolo[1,5-a]pyrimidines as c-Src kinase inhibitors that reduce IKr channel blockade.EBI Kissei Pharmaceutical Company Ltd
17977729 40 Design and physicochemical properties of new fluorescent ligands of protein kinase C isozymes focused on CH/pi interaction.EBI Kyoto University
17350261 16 Novel bis(indolyl)maleimide pyridinophanes that are potent, selective inhibitors of glycogen synthase kinase-3.EBI Johnson& Johnson Pharmaceutical Research& Development
17095233 45 Synthesis and c-Src inhibitory activity of imidazo[1,5-a]pyrazine derivatives as an agent for treatment of acute ischemic stroke.EBI Kissei Pharmaceutical Company Ltd
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
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
15380221 58 Synthesis of anilino-monoindolylmaleimides as potent and selective PKCbeta inhibitors.EBI Central Pharmaceutical Research Institute
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
12166950 208 Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family.EBI Millennium Pharmaceuticals, Inc.
10999477 40 Synthesis and PKC isozyme surrogate binding of indothiolactam-V, a new thioamide analogue of tumor promoting indolactam-V.EBI Kyoto University
10843211 38 Structure-activity relationship studies of flavopiridol analogues.EBI Mitotix Inc.
10360754 26 Adenosine-5'-carboxylic acid peptidyl derivatives as inhibitors of protein kinases.EBI Tartu University
 80 Synthesis and PKC inhibitory activities of balanol analogs with a cyclopentane substructureEBI TBA
16249345 25 Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580.EBI GlaxoSmithKline
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
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
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.
21696964 12 Generation of 'Unnatural Natural Product' library and identification of a small molecule inhibitor of XIAP.EBI Keio University
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
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.
21035336 42 5-amino-pyrazoles as potent and selective p38a inhibitors.EBI Bristol-Myers Squibb Research and Development
20965724 57 Identification of potent ITK inhibitors through focused compound library design including structural information.EBI Nycomed GmbH
20873740 111 Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding.EBI Nerviano Medical Sciences Srl
20817520 40 Role of the phenolic hydroxyl group in the biological activities of simplified analogue of aplysiatoxin with antiproliferative activity.EBI Kyoto University
20817473 57 Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity.EBI Nerviano Medical Sciences-Oncology
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
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
19884006 47 Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors.EBI Wyeth Research
20153643 68 Optimization of 5-vinylaryl-3-pyridinecarbonitriles as PKCtheta inhibitors.EBI Wyeth Research
19879134 94 Imidazo[1,2-a]pyrazine diaryl ureas: inhibitors of the receptor tyrosine kinase EphB4.EBI CGI Pharmaceuticals, Inc.
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
19762237 58 First generation 5-vinyl-3-pyridinecarbonitrile PKCtheta inhibitors.EBI Wyeth Research
19682896 49 C-5 Substituted heteroaryl 3-pyridinecarbonitriles as PKCtheta inhibitors: Part I.EBI Wyeth Research
8176401 21 Anti-AIDS Agents, 11. Betulinic Acid and Platanic Acid as Anti-HIV Principles from Syzigium claviflorum, and the Anti-HIV Activity of Structurally Related TriterpenoidsEBI TBA
 4 Benzo[c]quinoliziniums: A new family of inhibitors for protein kinase CK IIEBI TBA
 42 A novel series of 4-phenoxyquinolines: potent and highly selective inhibitors of PDGF receptor autophosphorylationEBI TBA
 99 Discovery and structure-activity studies of a novel series of pyrido[2,3-d]pyrimidine tyrosine kinase inhibitorsEBI TBA
 77 Synthesis and protein kinase C inhibitory activities of indane analogs of balanolEBI TBA
 70 Potent and selective PKC inhibitory 5-membered ring analogs of balanol with replacement of the carboxamide moietyEBI TBA
 107 Synthesis and biological evaluation of conformationally constrained bicyclic and tricyclic balanol analogues as inhibitors of protein kinase CEBI TBA
 40 Ring size effect in the PKC inhibitory activities of perhydroazepine analogs of balanolEBI TBA
 40 Heteroatom effect in the PKC inhibitory activities of perhydroazepine analogs of balanolEBI TBA
 75 Increasing the cellular PKC inhibitory activity of balanol: A study of ester analogsEBI TBA
 4 Synthesis of bisindolylmaleimide macrocyclesEBI TBA
 88 Novel PKC inhibitory analogs of balanol with replacement of the ester functionalityEBI TBA
 40 Protein kinase C inhibitory activities of balanol analogs bearing carboxylic acid replacementsEBI TBA
 2 2-aryl-indolyl maleimides - novel and potent inhibitors of protein kinase CEBI TBA
 7 Conformationally constrained analogues of diacylglycerol (DAG). 4. Interaction of α-alkylidene-γ-lactones with protein kinase C (PK-C)EBI TBA
19447612 59 Optimization of 5-phenyl-3-pyridinecarbonitriles as PKCtheta inhibitors.EBI Wyeth Research
19379015 40 Conformationally constrained analogues of diacylglycerol (DAG). 31. Modulation of the biological properties of diacylgycerol lactones (DAG-lactones) containing rigid-rod acyl groups separated from the core lactone by spacer units of different lengths.EBI National Cancer Institute-Frederick
19111463 46 Second generation 4-(4-methyl-1H-indol-5-ylamino)-2-phenylthieno[2,3-b]pyridine-5-carbonitrile PKCtheta inhibitors.EBI Wyeth Research
19109017 4 (-)-Cercosporamide derivatives as novel antihyperglycemic agents.EBI Daiichi Sankyo Co., Ltd
19019675 52 Beyond the MEK-pocket: can current MEK kinase inhibitors be utilized to synthesize novel type III NCKIs? Does the MEK-pocket exist in kinases other than MEK?EBI Pfizer Global Research and Development
18606543 68 2-Alkenylthieno[2,3-b]pyridine-5-carbonitriles: Potent and selective inhibitors of PKCtheta.EBI Wyeth Research
18585046 32 A novel Syk family kinase inhibitor: design, synthesis, and structure-activity relationship of 1,2,4-triazolo[4,3-c]pyrimidine and 1,2,4-triazolo[1,5-c]pyrimidine derivatives.EBI Kissei Pharmaceutical Company Ltd
17395590 2 Minocycline down-regulates MHC II expression in microglia and macrophages through inhibition of IRF-1 and protein kinase C (PKC)alpha/betaII.EBI University of Wisconsin
18072722 42 Synthesis, conformational analysis, and biological evaluation of 1-hexylindolactam-V10 as a selective activator for novel protein kinase C isozymes.EBI Kyoto University
17826092 37 Optimization of triarylimidazoles for Tie2: influence of conformation on potency.EBI GlaxoSmithKline
16682193 62 Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
16640328 13 Design and synthesis of 8-octyl-benzolactam-V9, a selective activator for protein kinase C epsilon and eta.EBI Kyoto University
16216497 67 Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection.EBI Abbott Bioresearch Center
15771419 134 Novel indolylindazolylmaleimides as inhibitors of protein kinase C-beta: synthesis, biological activity, and cardiovascular safety.EBI Johnson & Johnson Pharmaceutical Research & Development
15317463 16 Imidazoquinoxaline Src-family kinase p56Lck inhibitors: SAR, QSAR, and the discovery of (S)-N-(2-chloro-6-methylphenyl)-2-(3-methyl-1-piperazinyl)imidazo- [1,5-a]pyrido[3,2-e]pyrazin-6-amine (BMS-279700) as a potent and orally active inhibitor with excellent in vivo antiinflammatory activity.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
15261294 17 Potent inhibition of checkpoint kinase activity by a hymenialdisine-derived indoloazepine.EBI Michigan State University
15149684 59 3-(7-Azaindolyl)-4-arylmaleimides as potent, selective inhibitors of glycogen synthase kinase-3.EBI Johnson & Johnson Pharmaceutical Research & Development
14552791 35 Aryl[a]pyrrolo[3,4-c]carbazoles as selective cyclin D1-CDK4 inhibitors.EBI Lilly Spain S.A.
12954072 46 New bivalent PKC ligands linked by a carbon spacer: enhancement in binding affinity.EBI Georgetown University Medical Center
12941331 96 Macrocyclic bisindolylmaleimides as inhibitors of protein kinase C and glycogen synthase kinase-3.EBI Johnson & Johnson Pharmaceutical Research & Development
12941324 66 Synthesis and binding selectivity of 7- and 15-decylbenzolactone-V8 for the C1 domains of protein kinase C isozymes.EBI Kyoto University
12824047 99 Novel IKK inhibitors: beta-carbolines.EBI Millennium Pharmaceuticals Inc.
12749884 126 Acyclic N-(azacycloalkyl)bisindolylmaleimides: isozyme selective inhibitors of PKCbeta.EBI Lilly Research Laboratories
12672234 64 Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase.EBI Boehringer Ingelheim Pharmaceuticals
12270156 8 Synthesis and kinase inhibitory activity of 3'-(S)-epi-K-252a.EBI Cephalon, Inc.
12039590 51 Pyrrolo[2,3-d]pyrimidines containing diverse N-7 substituents as potent inhibitors of Lck.EBI Abbott Bioresearch Center
11909733 30 Beta-carbolines as specific inhibitors of cyclin-dependent kinases.EBI Institute of Molecular and Cell Biology
11597418 47 Pyrimidinylimidazole inhibitors of p38: cyclic N-1 imidazole substituents enhance p38 kinase inhibition and oral activity.EBI GlaxoSmithKline Pharmaceuticals
11327599 25 Rational design, synthesis, and biological evaluation of rigid pyrrolidone analogues as potential inhibitors of prostate cancer cell growth.EBI Georgetotwn University
11266178 39 The amide hydrogen of (-)-indolactam-V and benzolactam-V8's plays a critical role in protein kinase C binding and tumor-promoting activities.EBI Kyoto University
11266177 26 The C4 hydroxyl group of phorbol esters is not necessary for protein kinase C binding.EBI Kyoto University
11012021 69 Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck I.EBI BASF Bioresearch Corporation
10743939 63 Synthesis and biological activities of NB-506 analogues modified at the glucose group.EBI Banyu Tsukuba Research Institute
10612598 29 4-Pyridin-5-yl-2-(3,4,5-trimethoxyphenylamino)pyrimidines: potent and selective inhibitors of ZAP 70.EBI Celltech Therapeutics Limited
10612590 56 Synthesis and biological activities of NB-506 analogues: Effects of the positions of two hydroxyl groups at the indole rings.EBI Banyu Tsukuba Research Institute in collaboration with Merck Research Laboratories
10397502 36 Selective binding of bryostatin analogues to the cysteine rich domains of protein kinase C isozymes.EBI Stanford University
9135029 29 Modeling, chemistry, and biology of the benzolactam analogues of indolactam V (ILV). 2. Identification of the binding site of the benzolactams in the CRD2 activator-binding domain of PKCdelta and discovery of an ILV analogue of improved isozyme selectivity.EBI Georgetown University Medical Center
9003521 249 Synthesis and protein kinase C inhibitory activities of balanol analogs with replacement of the perhydroazepine moiety.EBI A Division of Eli Lilly & Company
8709095 87 (S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16, 21-dimetheno-1H, 13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H)-d ione (LY333531) and related analogues: isozyme selective inhibitors of protein kinase C beta.EBI Lilly Research Laboratories
27943581 8 Reverse Biosynthesis: Generating Combinatorial Pools of Drug Leads from Enzyme-Mediated Fragmentation of Natural Products.BDB The University of Sydney
26469307 7 Phosphorylation of Capsaicinoid Derivatives Provides Highly Potent and Selective Inhibitors of the Transcription Factor STAT5b.BDB University of Leipzig
11121615 32 Synthesis and in vitro opioid activity profiles of DALDA analogues.BDB Clinical Research Institute of Montreal
16236500 26 Discovery, SAR, and X-ray structure of novel biaryl-based dipeptidyl peptidase IV inhibitors.BDB Johnson & Johnson Pharmaceutical
16279769 28 Synthesis, molecular modeling studies, and selective inhibitory activity against monoamine oxidase of 1-thiocarbamoyl-3,5-diaryl-4,5-dihydro-(1H)- pyrazole derivatives.BDB Universita degli Studi di Roma La Sapienza
15689148 19 Bis-huperzine B: highly potent and selective acetylcholinesterase inhibitors.BDB Shanghai Institute of Materia Medica
15664516 21 Specificity and affinity of natural product cyclopentapeptide inhibitors against A. fumigatus, human, and bacterial chitinases.BDB University of Dundee
15026054 55 Meridianins, a new family of protein kinase inhibitors isolated from the ascidian Aplidium meridianum.BDB CNRS