PMID

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Article Title

Organization

Indolyl-naphthyl-maleimides as potent and selective inhibitors of protein kinase C-a/ß.

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).

Icahn School of Medicine At Mount Sinai

Novel ROCK inhibitors for the treatment of pulmonary arterial hypertension.

Novartis Horsham Research Centre

Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).

Exelixis

Design and optimization of selective protein kinase C¿ (PKC¿) inhibitors for the treatment of autoimmune diseases.

Vertex Pharmaceuticals

Structure-activity relationship and pharmacokinetic studies of sotrastaurin (AEB071), a promising novel medicine for prevention of graft rejection and treatment of psoriasis.

Novartis Institutes For Biomedical Research

2,6-Naphthyridines as potent and selective inhibitors of the novel protein kinase C isozymes.

Novartis Institutes For Biomedical Research

Structure-activity studies on the spiroketal moiety of a simplified analogue of debromoaplysiatoxin with antiproliferative activity.

Kyoto University

An Optimized Immunoaffinity Fluorescent Method for Natural Product Target Elucidation.

University of California

C-5 substituted heteroaryl-3-pyridinecarbonitriles as PKCtheta inhibitors: part II.

Wyeth Research

A quantitative analysis of kinase inhibitor selectivity.

Ambit Biosciences

Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors.

University of California

Synthesis and PKCtheta inhibitory activity of a series of 4-(indol-5-ylamino)thieno[2,3-b]pyridine-5-carbonitriles.

Wyeth Research

Pyrazolo-pyrimidines: a novel heterocyclic scaffold for potent and selective p38 alpha inhibitors.

Bristol-Myers Squibb Research and Development

Design and physicochemical properties of new fluorescent ligands of protein kinase C isozymes focused on CH/pi interaction.

Kyoto University

Structure-based drug design of a highly potent CDK1,2,4,6 inhibitor with novel macrocyclic quinoxalin-2-one structure.

Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories

Synthesis and PKC isozyme surrogate binding of indothiolactam-V, a new thioamide analogue of tumor promoting indolactam-V.

Kyoto University

 

Synthesis and PKC inhibitory activities of balanol analogs with a cyclopentane substructure

TBA

Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).

Ansaris

Comprehensive analysis of kinase inhibitor selectivity.

Ambit Biosciences

Generation of 'Unnatural Natural Product' library and identification of a small molecule inhibitor of XIAP.

Keio University

Role of the phenolic hydroxyl group in the biological activities of simplified analogue of aplysiatoxin with antiproliferative activity.

Kyoto University

AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).

Ambit Biosciences

Imidazo[2,1-b]thiazoles: multitargeted inhibitors of both the insulin-like growth factor receptor and members of the epidermal growth factor family of receptor tyrosine kinases.

Abbott Laboratories

Optimization of 5-vinylaryl-3-pyridinecarbonitriles as PKCtheta inhibitors.

Wyeth Research

Synthesis and PKCtheta inhibitory activity of a series of 5-vinyl phenyl sulfonamide-3-pyridinecarbonitriles.

Wyeth Research

2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.

Abbott Laboratories

First generation 5-vinyl-3-pyridinecarbonitrile PKCtheta inhibitors.

Wyeth Research

C-5 Substituted heteroaryl 3-pyridinecarbonitriles as PKCtheta inhibitors: Part I.

Wyeth Research

 

Synthesis and protein kinase C inhibitory activities of indane analogs of balanol

TBA

 

Potent and selective PKC inhibitory 5-membered ring analogs of balanol with replacement of the carboxamide moiety

TBA

 

Heteroatom effect in the PKC inhibitory activities of perhydroazepine analogs of balanol

TBA

 

Novel PKC inhibitory analogs of balanol with replacement of the ester functionality

TBA

Optimization of 5-phenyl-3-pyridinecarbonitriles as PKCtheta inhibitors.

Wyeth Research

Second generation 4-(4-methyl-1H-indol-5-ylamino)-2-phenylthieno[2,3-b]pyridine-5-carbonitrile PKCtheta inhibitors.

Wyeth Research

2-Alkenylthieno[2,3-b]pyridine-5-carbonitriles: Potent and selective inhibitors of PKCtheta.

Wyeth Research

Synthesis, conformational analysis, and biological evaluation of 1-hexylindolactam-V10 as a selective activator for novel protein kinase C isozymes.

Kyoto University

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.

Bristol-Myers Squibb Pharmaceutical Research Institute

Design and synthesis of 8-octyl-benzolactam-V9, a selective activator for protein kinase C epsilon and eta.

Kyoto University

Novel Aurora A and Protein Kinase C (?, ?1, ?2, and ?) Multitarget Inhibitors: Impact of Selenium Atoms on the Potency and Selectivity.

Mcgill University

Discovery of

Zhejiang University

Synthesis and binding selectivity of 7- and 15-decylbenzolactone-V8 for the C1 domains of protein kinase C isozymes.

Kyoto University

Acyclic N-(azacycloalkyl)bisindolylmaleimides: isozyme selective inhibitors of PKCbeta.

Eli Lilly

Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.

Beijing Normal University

The amide hydrogen of (-)-indolactam-V and benzolactam-V8's plays a critical role in protein kinase C binding and tumor-promoting activities.

Kyoto University

The C4 hydroxyl group of phorbol esters is not necessary for protein kinase C binding.

Kyoto University

Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors.

Merck

Selective binding of bryostatin analogues to the cysteine rich domains of protein kinase C isozymes.

Stanford University

ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.

University of Florida

Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application.

Takeda Pharmaceutical

Synthesis and protein kinase C inhibitory activities of balanol analogs with replacement of the perhydroazepine moiety.

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.

Eli Lilly

Effects of the methoxy group in the side chain of debromoaplysiatoxin on its tumor-promoting and anti-proliferative activities.

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.

Astellas Pharma

Mutations M184V and Y115F in HIV-1 reverse transcriptase discriminate against "nucleotide-competing reverse transcriptase inhibitors".

Mcgill University

Synthesis and in vitro opioid activity profiles of DALDA analogues.

Clinical Research Institute of Montreal

Discovery, SAR, and X-ray structure of novel biaryl-based dipeptidyl peptidase IV inhibitors.

Johnson & Johnson Pharmaceutical

Bis-huperzine B: highly potent and selective acetylcholinesterase inhibitors.

Shanghai Institute of Materia Medica

Specificity and affinity of natural product cyclopentapeptide inhibitors against A. fumigatus, human, and bacterial chitinases.

University of Dundee

Meridianins, a new family of protein kinase inhibitors isolated from the ascidian Aplidium meridianum.

Cnrs