PMID

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Article Title

Organization

Design of potent protein kinase inhibitors using the bisubstrate approach.

Ura Cnrs 1309

Design, synthesis, and characterization of an ATP-peptide conjugate inhibitor of protein kinase A.

Johns Hopkins University School of Medicine

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

Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors.

Hanyang University

Design, synthesis and biological characterization of selective LIMK inhibitors.

Amakem Therapeutics

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

Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis.

Hoffmann-La Roche

Discovery of novel and potent thiazoloquinazolines as selective Aurora A and B kinase inhibitors.

Astrazeneca

Kinase inhibitors: not just for kinases anymore.

Northwestern University

Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family.

Millennium Pharmaceuticals

Structure-activity relationship studies of flavopiridol analogues.

Mitotix

2,6,9-trisubstituted purines: optimization towards highly potent and selective CDK1 inhibitors.

Novartis Pharmaceuticals

 

A novel series of 4-phenoxyquinolines: potent and highly selective inhibitors of PDGF receptor autophosphorylation

TBA

 

Potent and selective inhibitors of the Abl-kinase: phenylamino-pyrimidine (PAP) derivatives

TBA

 

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

TBA

 

Phenylamino-pyrimidine (PAP) — derivatives: a new class of potent and highly selective PDGF-receptor autophosphorylation inhibitors

TBA

 

Selective inhibition of the tyrosine kinase pp60^src by analogs of 5,10-dihydropyrimido[4,5-b]quinolin-4(1H)-one

TBA

Design, synthesis, and biological activity of 5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-one-based potent and selective Chk-1 inhibitors.

Abbott Laboratories

Discovery of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of potent and selective checkpoint kinase 1 inhibitors.

Abbott Laboratories

Discovery of 2-pyrimidyl-5-amidothiophenes as potent inhibitors for AKT: synthesis and SAR studies.

Chiron

Evolution of the thienopyridine class of inhibitors of IkappaB kinase-beta: part I: hit-to-lead strategies.

Boehringer Ingelheim Pharmaceuticals

Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute

Identification of ellagic acid as potent inhibitor of protein kinase CK2: a successful example of a virtual screening application.

Università

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

Mcgill University

Novel 4-anilinoquinazolines with C-6 carbon-linked side chains: synthesis and structure-activity relationship of a series of potent, orally active, EGF receptor tyrosine kinase inhibitors.

Astrazeneca

(6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad antiproliferative activity against tumor cells.

Johnson & Johnson Pharmaceutical Research and Development

Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection.

Abbott Bioresearch Center

Identification of a Potent, Selective, and Brain-Penetrant Rho Kinase Inhibitor and its Activity in a Mouse Model of Huntington's Disease.

Charles River Laboratories

Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections.

Csir-Indian Institute of Integrative Medicine

Discovery of CH7057288 as an Orally Bioavailable, Selective, and Potent pan-TRK Inhibitor.

Chugai Pharmaceutical

Recent advances in development of hetero-bivalent kinase inhibitors.

Cha University

The discovery of orally active triaminotriazine aniline amides as inhibitors of p38 MAP kinase.

Bristol-Myers Squibb

Aryl[a]pyrrolo[3,4-c]carbazoles as selective cyclin D1-CDK4 inhibitors.

Eli Lilly

Macrocyclic bisindolylmaleimides as inhibitors of protein kinase C and glycogen synthase kinase-3.

Johnson & Johnson Pharmaceutical Research & Development

Identification of a new chemical class of potent angiogenesis inhibitors based on conformational considerations and database searching.

Novartis Pharma

Novel IKK inhibitors: beta-carbolines.

Millennium Pharmaceuticals

Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase.

Boehringer Ingelheim Pharmaceuticals

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

Beijing Normal University

Structural classification of protein kinases using 3D molecular interaction field analysis of their ligand binding sites: target family landscapes.

Aventis Pharma Deutschland

The development of novel and selective p56lck tyrosine kinase inhibitors.

R. W. Johnson Pharmaceutical Research Institute

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 of highly substituted dibenzo[b,f]azocines and their evaluation as protein kinase inhibitors.

St. Jude Children'S Research Hospital

An aminopyridazine-based inhibitor of a pro-apoptotic protein kinase attenuates hypoxia-ischemia induced acute brain injury.

Northwestern University

 

SYNTHESIS AND BIOLOGICAL EVALUATION OF CONFORMATIONALLY CONSTRAINED BICYCLIC AND TRICYCLIC BALANOL ANALOGUES AS INHIBITORS OF PROTEIN KINASE C.

Sphinx Laboratories