98 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
PMID
Data
Article Title
Organization
Indolyl-naphthyl-maleimides as potent and selective inhibitors of protein kinase C-a/ß.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Novartis Institutes For Biomedical Research
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Icahn School of Medicine At Mount Sinai
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-3ß inhibitors and neuroprotective agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Zhejiang University
Design and synthesis of protein kinase C epsilon selective diacylglycerol lactones (DAG-lactones).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Seoul National University
Discovery of selective and orally bioavailable protein kinase C¿ (PKC¿) inhibitors from a fragment hit.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Abbvie Bioresearch Center
Strategies for the modulation of phase II metabolism in a series of PKCe inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Vertex Pharmaceuticals
Synthesis, biological, and biophysical studies of DAG-indololactones designed as selective activators of RasGRP.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
National Institute of Industrial Technology
Thienoquinolines as novel disruptors of the PKCe/RACK2 protein-protein interaction.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Innsbruck Medical University
Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Exelixis
Design and optimization of selective protein kinase C¿ (PKC¿) inhibitors for the treatment of autoimmune diseases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Vertex Pharmaceuticals
Multitargeted drug development: Discovery and profiling of dihydroxy substituted 1-aza-9-oxafluorenes as lead compounds targeting Alzheimer disease relevant kinases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Martin-Luther-University Halle-Wittenberg
Structure-activity relationship and pharmacokinetic studies of sotrastaurin (AEB071), a promising novel medicine for prevention of graft rejection and treatment of psoriasis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Novartis Institutes For Biomedical Research
A one-pot synthesis and biological activity of ageladine A and analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Macquarie University
2,6-Naphthyridines as potent and selective inhibitors of the novel protein kinase C isozymes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Novartis Institutes For Biomedical Research
Structure-activity studies on the spiroketal moiety of a simplified analogue of debromoaplysiatoxin with antiproliferative activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Kyoto University
Pyrazole diaminopyrimidines as dual inhibitors of KDR and Aurora B kinases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Abbott Laboratories
Structure-based optimization of aminopyridines as PKC¿ inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Vertex Pharmaceuticals
Exploring aigialomycin d and its analogues as protein kinase inhibitors for cancer targets.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
TBA
Substituted 2H-isoquinolin-1-ones as potent Rho-kinase inhibitors: part 3, aryl substituted pyrrolidines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Boehringer Ingelheim Pharmaceuticals
Hit to lead account of the discovery of bisbenzamide and related ureidobenzamide inhibitors of Rho kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Boehringer Ingelheim Pharmaceuticals
Binding of curcumin and its long chain derivatives to the activator binding domain of novel protein kinase C.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Houston
C-5 substituted heteroaryl-3-pyridinecarbonitriles as PKCtheta inhibitors: part II.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Wyeth Research
Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of California
Synthesis and PKCtheta inhibitory activity of a series of 4-(indol-5-ylamino)thieno[2,3-b]pyridine-5-carbonitriles.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Wyeth Research
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Oxford
Design and physicochemical properties of new fluorescent ligands of protein kinase C isozymes focused on CH/pi interaction.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Kyoto University
Structure-based drug design of a highly potent CDK1,2,4,6 inhibitor with novel macrocyclic quinoxalin-2-one structure.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories
Synthesis of anilino-monoindolylmaleimides as potent and selective PKCbeta inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Central Pharmaceutical Research Institute
Synthesis and PKC isozyme surrogate binding of indothiolactam-V, a new thioamide analogue of tumor promoting indolactam-V.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Kyoto University
Binding of isoxazole and pyrazole derivatives of curcumin with the activator binding domain of novel protein kinase C.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Houston
Generation of 'Unnatural Natural Product' library and identification of a small molecule inhibitor of XIAP.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Keio University
Role of the phenolic hydroxyl group in the biological activities of simplified analogue of aplysiatoxin with antiproliferative activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Kyoto University
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Ambit Biosciences
Substituted 2H-isoquinolin-1-one as potent Rho-Kinase inhibitors. Part 1: Hit-to-lead account.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Boehringer Ingelheim Pharmaceuticals
Optimization of 5-vinylaryl-3-pyridinecarbonitriles as PKCtheta inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Wyeth Research
Synthesis and PKCtheta inhibitory activity of a series of 5-vinyl phenyl sulfonamide-3-pyridinecarbonitriles.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Wyeth Research
C-5 Substituted heteroaryl 3-pyridinecarbonitriles as PKCtheta inhibitors: Part I.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Wyeth Research
Synthesis and biological evaluation of novel 4-azaindolyl-indolyl-maleimides as glycogen synthase kinase-3beta (GSK-3beta) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Zhejiang University
Anti-AIDS Agents, 11. Betulinic Acid and Platanic Acid as Anti-HIV Principles from Syzigium claviflorum, and the Anti-HIV Activity of Structurally Related Triterpenoids![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
TBA
Potent and selective PKC inhibitory 5-membered ring analogs of balanol with replacement of the carboxamide moiety![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
TBA
Protein kinase C inhibitory activities of balanol analogs bearing carboxylic acid replacements![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
TBA
Bisindolylmaleimide inhibitors of protein kinase C. Further conformational restriction of a tertiary amine side chain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
TBA
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
National Cancer Institute-Frederick
Second generation 4-(4-methyl-1H-indol-5-ylamino)-2-phenylthieno[2,3-b]pyridine-5-carbonitrile PKCtheta inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Wyeth Research
2-Alkenylthieno[2,3-b]pyridine-5-carbonitriles: Potent and selective inhibitors of PKCtheta.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Wyeth Research
Protein kinase C epsilon regulates gamma-aminobutyrate type A receptor sensitivity to ethanol and benzodiazepines through phosphorylation of gamma2 subunits.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of California San Francisco
Anthraquinones and betaenone derivatives from the sponge-associated fungus Microsphaeropsis species: novel inhibitors of protein kinases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Heinrich-Heine-UniversitäT
Synthesis, conformational analysis, and biological evaluation of 1-hexylindolactam-V10 as a selective activator for novel protein kinase C isozymes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Kyoto University
Design and synthesis of 8-octyl-benzolactam-V9, a selective activator for protein kinase C epsilon and eta.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Kyoto University
New bivalent PKC ligands linked by a carbon spacer: enhancement in binding affinity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Georgetown University Medical Center
Macrocyclic bisindolylmaleimides as inhibitors of protein kinase C and glycogen synthase kinase-3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Johnson & Johnson Pharmaceutical Research & Development
Synthesis and binding selectivity of 7- and 15-decylbenzolactone-V8 for the C1 domains of protein kinase C isozymes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Kyoto University
Acyclic N-(azacycloalkyl)bisindolylmaleimides: isozyme selective inhibitors of PKCbeta.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eli Lilly
Rational design, synthesis, and biological evaluation of rigid pyrrolidone analogues as potential inhibitors of prostate cancer cell growth.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Georgetotwn University
The amide hydrogen of (-)-indolactam-V and benzolactam-V8's plays a critical role in protein kinase C binding and tumor-promoting activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Kyoto University
The C4 hydroxyl group of phorbol esters is not necessary for protein kinase C binding.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Kyoto University
Synthesis of 7,8-disubstituted benzolactam-V8 and its binding to protein kinase C.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Institute of Organic Chemistry
Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Merck
Discovery of (R)-5-((5-(1-methyl-1H-pyrazol-4-yl)-4-(methylamino)pyrimidin-2-yl)amino)-3-(piperidin-3-yloxy)picolinonitrile, a novel CHK1 inhibitor for hematologic malignancies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Zhejiang University
Selective binding of bryostatin analogues to the cysteine rich domains of protein kinase C isozymes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Stanford University
ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Florida
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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Georgetown University Medical Center
Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Takeda Pharmaceutical
Synthesis and protein kinase C inhibitory activities of balanol analogs with replacement of the perhydroazepine moiety.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eli Lilly
(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](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eli Lilly
Effects of the methoxy group in the side chain of debromoaplysiatoxin on its tumor-promoting and anti-proliferative activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Kyoto University
A novel 2,4-diaminopyrimidine derivative as selective inhibitor of protein kinase C theta prevents allograft rejection in a rat heart transplant model.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Astellas Pharma
ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Vertex Pharmaceuticals
Synthesis and anticancer activity of novel bisindolylhydroxymaleimide derivatives with potent GSK-3 kinase inhibition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University College Cork
ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Vertex Pharmaceuticals
Fragment-Based Drug Discovery of Potent Protein Kinase C Iota Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Agency For Science, Technology and Research (A*Star)
?-Arylidene Diacylglycerol-Lactones (DAG-Lactones) as Selective Ras Guanine-Releasing Protein 3 (RasGRP3) Ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Seoul National University
Exploring the influence of indololactone structure on selectivity for binding to the C1 domains of PKC?, PKC?, and RasGRP.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
National Institute of Industrial Technology
Biological profile of the less lipophilic and synthetically more accessible bryostatin 7 closely resembles that of bryostatin 1.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
National Cancer Institute-Bethesda
Discovery of 3-(1H-indol-3-yl)-4-[2-(4-methylpiperazin-1-yl)quinazolin-4-yl]pyrrole-2,5-dione (AEB071), a potent and selective inhibitor of protein kinase C isotypes.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Novartis
Increasing the cellular PKC inhibitory activity of balanol: a study of ester analogs.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Sphinx Pharmaceuticals
Synthesis and protein kinase inhibitory activity of balanol analogues with modified benzophenone subunits.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Sphinx Laboratories
Synthesis and protein kinase C inhibitory activities of acyclic balanol analogs that are highly selective for protein kinase C over protein kinase A.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Sphinx Laboratories
SYNTHESIS AND BIOLOGICAL EVALUATION OF CONFORMATIONALLY CONSTRAINED BICYCLIC AND TRICYCLIC BALANOL ANALOGUES AS INHIBITORS OF PROTEIN KINASE C.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Sphinx Laboratories
Ring Size effect in the PKC inhibitory activities of perhydroazepine analogs of balanol.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Sphinx Laboratories