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273 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
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
1597853 2 A nonpromoting phorbol from the samoan medicinal plant Homalanthus nutans inhibits cell killing by HIV-1.EBI National Cancer Institute-Frederick
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
27362616 41 G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitors: Current Trends and Future Perspectives.EBI Universit£
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
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
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
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
25808573 3 Neristatin 1 provides critical insight into bryostatin 1 structure-function relationships.EBI National Cancer Institute-Bethesda
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
25633741 67 Discovery and profiling of a selective and efficacious Syk inhibitor.EBI Novartis Institutes For Biomedical Research
25766633 9 Dual inhibition of allosteric mitogen-activated protein kinase (MEK) and phosphatidylinositol 3-kinase (PI3K) oncogenic targets with a bifunctional inhibitor.EBI The University of Michigan Medical School
25437619 88 Design and synthesis of protein kinase C epsilon selective diacylglycerol lactones (DAG-lactones).EBI Seoul National University
25000588 72 Discovery of selective and orally bioavailable protein kinase C¿ (PKC¿) inhibitors from a fragment hit.EBI Abbvie Bioresearch Center
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
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
25313996 91 Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase.EBI Merck Research Laboratories
25254961 32 Optimized protein kinase C¿ (PKC¿) inhibitors reveal only modest anti-inflammatory efficacy in a rodent model of arthritis.EBI Abbvie Bioresearch Center
24794745 20 Synthesis, biological, and biophysical studies of DAG-indololactones designed as selective activators of RasGRP.EBI National Institute of Industrial Technology
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
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
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
23265875 78 Design and synthesis of tricyclic cores for kinase inhibition.EBI Abbott Bioresearch Center
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
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
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
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
22533818 84 Identification of glycogen synthase kinase-3 inhibitors with a selective sting for glycogen synthase kinase-3a.EBI Technische Universit£T Darmstadt
22738630 76 Structure-based optimization of aminopyridines as PKC¿ inhibitors.EBI Vertex Pharmaceuticals
22537682 6 Inverse Virtual Screening allows the discovery of the biological activity of natural compounds.EBI Universit£
21435888 7 The synthesis and evaluation of indolylureas as PKCa inhibitors.EBI Procter & Gamble Pharmaceuticals
21141896 2 Discovery of (7R)-14-cyclohexyl-7-{[2-(dimethylamino)ethyl](methyl) amino}-7,8-dihydro-6H-indolo[1,2-e][1,5]benzoxazocine-11-carboxylic acid (MK-3281), a potent and orally bioavailable finger-loop inhibitor of the hepatitis C virus NS5B polymerase.EBI P. Angeletti S.P.A. (Merck Research Laboratories)
21155605 39 Identification of a potent Janus kinase 3 inhibitor with high selectivity within the Janus kinase family.EBI Novartis Institutes For Biomedical Research
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
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
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
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
9834166 8 Phenylethanoid glycosides from Digitalis purpurea and Penstemon linarioides with PKCalpha-inhibitory activity.EBI Virginia Polytechnic Institute and State University
18395443 37 Discovery and preclinical studies of 5-isopropyl-6-(5-methyl-1,3,4-oxadiazol-2-yl)-N-(2-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine (BMS-645737), an in vivo active potent VEGFR-2 inhibitor.EBI Bristol-Myers Squibb
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
17977729 40 Design and physicochemical properties of new fluorescent ligands of protein kinase C isozymes focused on CH/pi interaction.EBI Kyoto University
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
17284021 10 Conformationally constrained analogues of diacylglycerol (DAG). 27. Modulation of membrane translocation of protein kinase C (PKC) isozymes alpha and delta by diacylglycerol lactones (DAG-lactones) containing rigid-rod acyl groups.EBI National Cancer Institute-Frederick
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
16460940 13 Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis.EBI Hoffmann-La Roche
16220969 219 Designed multiple ligands. An emerging drug discovery paradigm.EBI Organon Laboratories
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
15380221 58 Synthesis of anilino-monoindolylmaleimides as potent and selective PKCbeta inhibitors.EBI Central Pharmaceutical Research Institute
14736244 8 Conformationally constrained analogues of diacylglycerol. 20. The search for an elusive binding site on protein kinase C through relocation of the carbonyl pharmacophore along the sn-1 side chain of 1,2-diacylglycerol lactones.EBI National Cancer Institute-Frederick
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
12801241 4 Conformationally constrained analogues of diacylglycerol. 19. Synthesis and protein kinase C binding affinity of diacylglycerol lactones bearing an N-hydroxylamide side chain.EBI National Cancer Institute-Frederick
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
8691452 1 Molecular modeling and site-directed mutagenesis studies of a phorbol ester-binding site in protein kinase C.EBI National Cancer Institute-Bethesda
8289196 7 New hexahydroxybiphenyl derivatives as inhibitors of protein kinase C.EBI University of North Carolina
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
9990463 69 2,6,9-trisubstituted purines: optimization towards highly potent and selective CDK1 inhibitors.EBI Novartis Pharmaceuticals
 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
15953730 13 RO4383596, an orally active KDR, FGFR, and PDGFR inhibitor: synthesis and biological evaluation.EBI Hoffmann-La Roche
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
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
21999461 90 1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase.EBI RhôNe-Poulenc Rorer
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
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
21807510 31 Synthesis and biological evaluation of glycogen synthase kinase 3 (GSK-3) inhibitors: an fast and atom efficient access to 1-aryl-3-benzylureas.EBI Technische Universit£T Darmstadt
21880495 5 Chemical modifications of resveratrol for improved protein kinase C alpha activity.EBI University of Houston
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
21696964 12 Generation of 'Unnatural Natural Product' library and identification of a small molecule inhibitor of XIAP.EBI Keio University
20674350 63 Discovery of imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.EBI Merck Research Laboratories
21548579 4 Hippolides A-H, acyclic manoalide derivatives from the marine sponge Hippospongia lachne.EBI Second Military Medical University
21596562 9 Design and synthesis of protein kinase Ca activators based on 'out of pocket' interactions.EBI Riken Advanced Science Institute
21561771 39 Discovery of novel tetracyclic compounds as anaplastic lymphoma kinase inhibitors.EBI Chugai Pharmaceutical
24900231 22 Identification of Niclosamide as a New Small-Molecule Inhibitor of the STAT3 Signaling Pathway.EBI TBA
21035336 42 5-amino-pyrazoles as potent and selective p38a inhibitors.EBI Bristol-Myers Squibb Research and Development
20855207 26 Discovery of orally bioavailable imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.EBI Merck Research Laboratories
20817520 40 Role of the phenolic hydroxyl group in the biological activities of simplified analogue of aplysiatoxin with antiproliferative activity.EBI Kyoto University
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
20684591 87 Identification of orally available naphthyridine protein kinase D inhibitors.EBI Novartis Institutes For Biomedical Research
20382527 26 Design, synthesis and structure-activity relationships of novel biarylamine-based Met kinase inhibitors.EBI Bristol-Myers Squibb Research and Development
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
19879134 94 Imidazo[1,2-a]pyrazine diaryl ureas: inhibitors of the receptor tyrosine kinase EphB4.EBI Cgi Pharmaceuticals
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
20045644 32 Polar 3-alkylidene-5-pivaloyloxymethyl-5'-hydroxymethyl-gamma-lactones as protein kinase C ligands and antitumor agents.EBI Seoul National University
20093027 92 Discovery of 6-benzyloxyquinolines as c-Met selective kinase inhibitors.EBI Chugai Pharmaceutical
19945867 39 Ring-fused pyrazole derivatives as potent inhibitors of lymphocyte-specific kinase (Lck): Structure, synthesis, and SAR.EBI Taisho Pharmaceutical
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
8882431 4 Antineoplastic agents. 340. Isolation and structural elucidation of bryostatins 16-18.EBI Arizona State University
 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
 230 Potent and selective inhibitors of the Abl-kinase: phenylamino-pyrimidine (PAP) derivativesEBI 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
 90 Phenylamino-pyrimidine (PAP) — derivatives: a new class of potent and highly selective PDGF-receptor autophosphorylation inhibitorsEBI TBA
 8 Protein kinase C-α inhibitors; structure-activity relationships in bis-indole seriesEBI TBA
 40 Heteroatom effect in the PKC inhibitory activities of perhydroazepine analogs of balanolEBI 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 Synthesis of the benzofuran analogue of ILV, a new protein kinase C (PKC) activatorEBI TBA
 7 Conformationally constrained analogues of diacylglycerol (DAG). 4. Interaction of α-alkylidene-γ-lactones with protein kinase C (PK-C)EBI TBA
 4 Synthesis of ingenol analogs wth affinity for protein kinase CEBI TBA
 3 Conformationally constrained analogues of diacylglycerol. 5. 2,5-Dideoxy-3-O-tetradecanoyl-D-galactono-1,4-lactone: A superior homologue of 3-O-tetradecanoyl-2-deoxy-L-ribonolactone with PK-C binding affinity.EBI TBA
19438240 8 Design, synthesis, and biological activity of isophthalic acid derivatives targeted to the C1 domain of protein kinase C.EBI University of Helsinki
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
19364658 113 Identification and SAR of squarate inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2).EBI Wyeth Research
19285393 90 Discovery of 5-pyrrolopyridinyl-2-thiophenecarboxamides as potent AKT kinase inhibitors.EBI Glaxosmithkline
19109017 4 (-)-Cercosporamide derivatives as novel antihyperglycemic agents.EBI Daiichi Sankyo
19081248 12 Identification of small molecules that inhibit GSK-3beta through virtual screening.EBI Korea Research Institute of Chemical Technology
18707088 72 Conformationally constrained analogues of diacylglycerol. 30. An investigation of diacylglycerol-lactones containing heteroaryl groups reveals compounds with high selectivity for Ras guanyl nucleotide-releasing proteins.EBI National Cancer Institute-Frederick
18606543 68 2-Alkenylthieno[2,3-b]pyridine-5-carbonitriles: Potent and selective inhibitors of PKCtheta.EBI Wyeth Research
17848581 13 Pharmacologic inhibition of tpl2 blocks inflammatory responses in primary human monocytes, synoviocytes, and blood.EBI Wyeth Research
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
17303421 56 Synthesis and activity of quinolinyl-methylene-thiazolinones as potent and selective cyclin-dependent kinase 1 inhibitors.EBI Roche Research Center
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
16765046 63 Discovery of 2-pyrimidyl-5-amidothiophenes as potent inhibitors for AKT: synthesis and SAR studies.EBI Chiron
16722637 39 Conformationally constrained analogues of diacylglycerol. 26. Exploring the chemical space surrounding the C1 domain of protein kinase C with DAG-lactones containing aryl groups at the sn-1 and sn-2 positions.EBI National Cancer Institute-Frederick
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
16570908 39 Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an in vivo active potent VEGFR-2 inhibitor.EBI Pharmaceutical Research Institute
16539391 21 Branched diacylglycerol-lactones as potent protein kinase C ligands and alpha-secretase activators.EBI Research Institute of Pharmaceutical Sciences
16216497 67 Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection.EBI Abbott Bioresearch Center
16134942 19 Conformationally constrained analogues of diacylglycerol (DAG). 25. Exploration of the sn-1 and sn-2 carbonyl functionality reveals the essential role of the sn-1 carbonyl at the lipid interface in the binding of DAG-lactones to protein kinase C.EBI National Cancer Institute-Frederick
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
15771419 134 Novel indolylindazolylmaleimides as inhibitors of protein kinase C-beta: synthesis, biological activity, and cardiovascular safety.EBI Johnson & Johnson Pharmaceutical Research & Development
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
15566298 34 The discovery of orally active triaminotriazine aniline amides as inhibitors of p38 MAP kinase.EBI Bristol-Myers Squibb
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
15163204 18 Conformationally constrained analogues of diacylglycerol. 21. A solid-phase method of synthesis of diacylglycerol lactones as a prelude to a combinatorial approach for the synthesis of protein kinase C isozyme-specific ligands.EBI National Cancer Institute At Frederick
15149684 59 3-(7-Azaindolyl)-4-arylmaleimides as potent, selective inhibitors of glycogen synthase kinase-3.EBI Johnson & Johnson Pharmaceutical Research & Development
15125969 8 Design, synthesis, and structure-activity relationship of new isobenzofuranone ligands of protein kinase C.EBI Tohoku University
14552791 35 Aryl[a]pyrrolo[3,4-c]carbazoles as selective cyclin D1-CDK4 inhibitors.EBI Eli Lilly
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
12749884 126 Acyclic N-(azacycloalkyl)bisindolylmaleimides: isozyme selective inhibitors of PKCbeta.EBI Eli Lilly
12699375 10 Differential binding modes of diacylglycerol (DAG) and DAG lactones to protein kinase C (PK-C).EBI National Cancer Institute-Frederick
12672234 64 Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase.EBI Boehringer Ingelheim Pharmaceuticals
12540236 11 New amide-bearing benzolactam-based protein kinase C modulators induce enhanced secretion of the amyloid precursor protein metabolite sAPPalpha.EBI Georgetown University Medical Center
12270156 8 Synthesis and kinase inhibitory activity of 3'-(S)-epi-K-252a.EBI Cephalon
12039590 51 Pyrrolo[2,3-d]pyrimidines containing diverse N-7 substituents as potent inhibitors of Lck.EBI Abbott Bioresearch Center
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
11728178 15 Conformationally constrained analogues of diacylglycerol. 18. The incorporation of a hydroxamate moiety into diacylglycerol-lactones reduces lipophilicity and helps discriminate between sn-1 and sn-2 binding modes to protein kinase C (PK-C). Implications for isozyme specificity.EBI Seoul National University
11689073 4 Iridals are a novel class of ligands for phorbol ester receptors with modest selectivity for the RasGRP receptor subfamily.EBI University of Michigan Cancer Center
11597418 47 Pyrimidinylimidazole inhibitors of p38: cyclic N-1 imidazole substituents enhance p38 kinase inhibition and oral activity.EBI Glaxosmithkline
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
11206480 6 Synthesis of 7,8-disubstituted benzolactam-V8 and its binding to protein kinase C.EBI Institute of Organic Chemistry
31757666 314 Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors.EBI Merck
11012021 69 Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck I.EBI Basf Bioresearch
10966739 28 Conformationally constrained analogues of diacylglycerol (DAG). 17. Contrast between sn-1 and sn-2 DAG lactones in binding to protein kinase C.EBI National Cancer Institute-Bethesda
30755337 95 Optimization of an azetidine series as inhibitors of colony stimulating factor-1 receptor (CSF-1R) Type II to lead to the clinical candidate JTE-952.EBI Japan Tobacco
10762046 7 Diacylglycerols with lipophilically equivalent branched acyl chains display high affinity for protein kinase C (PK-C). A direct measure of the effect of constraining the glycerol backbone in DAG lactones.EBI National Cancer Institute-Bethesda
10743939 63 Synthesis and biological activities of NB-506 analogues modified at the glucose group.EBI Banyu Tsukuba Research Institute
10715158 31 Conformationally constrained analogues of diacylglycerol (DAG). 16. How much structural complexity is necessary for recognition and high binding affinity to protein kinase C?EBI National Cancer Institute-Bethesda
30530196 32 Chemistry-oriented synthesis (ChOS) and target deconvolution on neuroprotective effect of a novel scaffold, oxaza spiroquinone.EBI Gachon University
10612598 29 4-Pyridin-5-yl-2-(3,4,5-trimethoxyphenylamino)pyrimidines: potent and selective inhibitors of ZAP 70.EBI Celltech Therapeutics
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
31298542 108 Discovery of 3,4,6-Trisubstituted Piperidine Derivatives as Orally Active, Low hERG Blocking Akt Inhibitors via Conformational Restriction and Structure-Based Design.EBI Chinese Academy of Sciences
10514283 8 Protein kinase C ligands based on tetrahydrofuran templates containing a new set of phorbol ester pharmacophores.EBI Seoul National University
31417666 55 Discovery of Selective, Orally Bioavailable Pyrazolopyridine Inhibitors of Protein Kinase C? (PKC?) That Ameliorate Symptoms of Experimental Autoimmune Encephalomyelitis.EBI Vertex Pharmaceuticals
10397502 36 Selective binding of bryostatin analogues to the cysteine rich domains of protein kinase C isozymes.EBI Stanford University
10360738 5 Synthesis and protein kinase C binding activity of benzolactam-V7.EBI Institute of Organic Chemistry
10340602 100 Synthesis and biological activities of topoisomerase I inhibitors, 6-N-amino analogues of NB-506.EBI Banyu Tsukuba Research Institute
10090785 63 Use of a pharmacophore model for the design of EGFR tyrosine kinase inhibitors: isoflavones and 3-phenyl-4(1H)-quinolones.EBI Novartis
10021922 10 Synthesis, computer modeling and biological evaluation of novel protein kinase C agonists based on a 7-membered lactam moiety.EBI University of Tokyo
31693351 473 Discovery of 4EBI TBA
31343875 34 Synthesis and Structure-Activity Relationship Correlations of Gnidimacrin Derivatives as Potent HIV-1 Inhibitors and HIV Latency Reversing Agents.EBI Toho University
9873742 5 Conformationally constrained analogues of diacylglycerol (DAG). 15. The indispensable role of the sn-1 and sn-2 carbonyls in the binding of DAG-lactones to protein kinase C (PK-C).EBI National Institutes of Health
30733087 53 A review on flavones targeting serine/threonine protein kinases for potential anticancer drugs.EBI China Pharmaceutical University
9873429 6 Conformationally constrained analogues of diacylglycerol (DAG). 14. Dissection of the roles of the sn-1 and sn-2 carbonyls in DAG mimetics by isopharmacophore replacement.EBI National Cancer Institute-Bethesda
9341921 7 Syntheses and biological activities (topoisomerase inhibition and antitumor and antimicrobial properties) of rebeccamycin analogues bearing modified sugar moieties and substituted on the imide nitrogen with a methyl group.EBI Université
30384048 365 ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.EBI University of Florida
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
31526603 379 Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application.EBI Takeda Pharmaceutical
9003521 249 Synthesis and protein kinase C inhibitory activities of balanol analogs with replacement of the perhydroazepine moiety.EBI Eli Lilly
8960550 5 Conformationally constrained analogues of diacylglycerol. 13. Protein kinase C ligands based on templates derived from 2,3-dideoxy-L-erythro(threo)-hexono-1,4-lactone and 2-deoxyapiolactone.EBI National Cancer Institute-Bethesda
8893841 23 Structure-activity relationships in a series of substituted indolocarbazoles: topoisomerase I and protein kinase C inhibition and antitumoral and antimicrobial properties.EBI Université
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 Eli Lilly
8691423 89 4-(Phenylamino)pyrrolopyrimidines: potent and selective, ATP site directed inhibitors of the EGF-receptor protein tyrosine kinase.EBI Ciba Pharmaceuticals
26505898 123 Identification of N-(4-((1R,3S,5S)-3-Amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide (PIM447), a Potent and Selective Proviral Insertion Site of Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase Inhibitor in Clinical Trials for Hematological Malignancies.EBI Novartis Institutes For Biomedical Research
8568825 13 Conformationally constrained analogues of diacylglycerol. 12. Ultrapotent protein kinase C ligands based on a chiral 4,4-disubstituted heptono-1,4-lactone template.EBI National Cancer Institute-Bethesda
8568819 6 Conformationally constrained analogues of diacylglycerol. 11. Ultrapotent protein kinase C ligands based on a chiral 5-disubstituted tetrahydro-2-furanone template.EBI National Cancer Institute-Bethesda
8568806 9 Conformationally constrained analogues of diacylglycerol. 10. Ultrapotent protein kinase C ligands based on a racemic 5-disubstituted tetrahydro-2-furanone template.EBI National Cancer Institute-Bethesda
8176711 18 Protein kinase C. Modeling of the binding site and prediction of binding constants.EBI National Cancer Institute-Bethesda
23803585 7 Effects of the methoxy group in the side chain of debromoaplysiatoxin on its tumor-promoting and anti-proliferative activities.EBI Kyoto University
7799398 5 The discovery of novel, structurally diverse protein kinase C agonists through computer 3D-database pharmacophore search. Molecular modeling studies.EBI National Cancer Institute-Bethesda
21388717 1 Glycoglycerolipid analogues inhibit PKC translocation to the plasma membrane and downstream signaling pathways in PMA-treated fibroblasts and human glioblastoma cells, U87MG.EBI University of Milan
7807122 4 New cytotoxic peroxylactones from the marine sponge, Plakinastrella onkodes.EBI Harbor Branch Oceanographic Institution
9834165 5 Isolation and structure elucidation of new PKCalpha inhibitors from Pinus flexilis.EBI Virginia Polytechnic and State University
17618015 13 Bioactive peroxides as potential therapeutic agents.EBI The Hebrew University of Jerusalem
11334563 5 Computational analysis of PKA-balanol interactions.EBI University of California At San Diego
10753478 11 Inhibition of protein kinase C(alpha) by dequalinium analogues: dependence on linker length and geometry.EBI The City University of New York
10052965 9 Syntheses and biological activities of rebeccamycin analogues. Introduction of a halogenoacetyl substituent.EBI Universit£
9572888 4 Syntheses and biological evaluation of indolocarbazoles, analogues of rebeccamycin, modified at the imide heterocycle.EBI Universit£
14505650 12 An aminopyridazine-based inhibitor of a pro-apoptotic protein kinase attenuates hypoxia-ischemia induced acute brain injury.EBI Northwestern University
27731641 5 Isolation of Phorbol Esters from Euphorbia grandicornis and Evaluation of Protein Kinase C- and Human Platelet-Activating Effects of Euphorbiaceae Diterpenes.EBI Kaohsiung Medical University
30274941 36 A novel 2,4-diaminopyrimidine derivative as selective inhibitor of protein kinase C theta prevents allograft rejection in a rat heart transplant model.EBI Astellas Pharma
29135244 5 Natural Products with Heteroatom-Rich Ring Systems.EBI University of Auckland
29558119 30 Bioactive Indolocarbazoles from the Marine-Derived Streptomyces sp. DT-A61.EBI Zhejiang University
30026041 139 Synthesis and anticancer activity of novel bisindolylhydroxymaleimide derivatives with potent GSK-3 kinase inhibition.EBI University College Cork
29945794 193 ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.EBI Vertex Pharmaceuticals
29545102 159 Discovery of a highly potent orally bioavailable imidazo-[1, 2-a]pyrazine Aurora inhibitor.EBI Merck
29870245 39 Discovery of Novel Small-Molecule Inhibitors of NF-?B Signaling with Antiinflammatory and Anticancer Properties.EBI University of Colorado
29688013 81 Fragment-Based Drug Discovery of Potent Protein Kinase C Iota Inhibitors.EBI Agency For Science, Technology and Research (A*Star)
29107425 90 Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders.EBI Korea Institute of Science & Technology (Kist)
29860841 140 ?-Arylidene Diacylglycerol-Lactones (DAG-Lactones) as Selective Ras Guanine-Releasing Protein 3 (RasGRP3) Ligands.EBI Seoul National University
29853332 50 Benzofuro[3,2-d]pyrimidines inspired from cercosporamide CaPkc1 inhibitor: Synthesis and evaluation of fluconazole susceptibility restoration.EBI Universit£
28259529 31 Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer.EBI The Ohio State University
28699740 294 Design, Synthesis, and Evaluation of the Highly Selective and Potent G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitor for the Potential Treatment of Heart Failure.EBI Takeda Pharmaceutical
28991459 71 Methyl 3-(3-(4-(2,4,4-Trimethylpentan-2-yl)phenoxy)-propanamido)benzoate as a Novel and Dual Malate Dehydrogenase (MDH) 1/2 Inhibitor Targeting Cancer Metabolism.EBI Dongguk University
28478927 46 Discovery of novel substituted benzo-anellated 4-benzylamino pyrrolopyrimidines as dual EGFR and VEGFR2 inhibitors.EBI Martin-Luther-University Halle-Wittenberg
28392275 24 Exploring the influence of indololactone structure on selectivity for binding to the C1 domains of PKC?, PKC?, and RasGRP.EBI National Institute of Industrial Technology
27943581 8 Reverse Biosynthesis: Generating Combinatorial Pools of Drug Leads from Enzyme-Mediated Fragmentation of Natural Products.BDB The University of Sydney
27128528 42 Inhibitors of Glycogen Synthase Kinase 3 with Exquisite Kinome-Wide Selectivity and Their Functional Effects.BDB Harvard Medical School
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
18804034 9 Identification of chemical inhibitors to human tissue transglutaminase by screening existing drug libraries.BDB Duke University Medical Center
17585751 48 Novel vanilloid receptor-1 antagonists: 3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacokinetic properties.BDB Amgen
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 Sapienza University of Rome
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
 127 DISCOVERY AND STRUCTURE-ACTIVITY STUDIES OF A NOVEL SERIES OF PYRIDO[2,3-d]PYRIMIDINE TYROSINE KINASE INHIBITORSBDB Parke-Davis Pharmaceutical Research