PMID

Data

Article Title

Organization

Identification of the First Selective Activin Receptor-Like Kinase 1 Inhibitor, a Reversible Version of L-783277.

Korea University

Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.

Merck

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

Fragment-based drug discovery of potent and selective MKK3/6 inhibitors.

Takeda California

Development of amino-pyrimidine inhibitors of c-Jun N-terminal kinase (JNK): kinase profiling guided optimization of a 1,2,3-benzotriazole lead.

Roche Palo Alto

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

Exelixis

A quantitative analysis of kinase inhibitor selectivity.

Ambit Biosciences

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

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.

Serono Pharmaceutical Research Institute

Potent and selective inhibitors of PDGF receptor phosphorylation. 2. Synthesis, structure activity relationship, improvement of aqueous solubility, and biological effects of 4-[4-(N-substituted (thio)carbamoyl)-1-piperazinyl]-6,7-dimethoxyquinazoline derivatives.

Kyowa Hakko Kogyo

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

Millennium Pharmaceuticals

Comprehensive analysis of kinase inhibitor selectivity.

Ambit Biosciences

Substituted N-aryl-6-pyrimidinones: a new class of potent, selective, and orally active p38 MAP kinase inhibitors.

Pfizer

Discovery and structure-activity relationship of 3-aminopyrid-2-ones as potent and selective interleukin-2 inducible T-cell kinase (Itk) inhibitors.

Vertex Pharmaceuticals

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

Ambit Biosciences

Non-hinge-binding pyrazolo[1,5-a]pyrimidines as potent B-Raf kinase inhibitors.

Wyeth Research

Synthesis and SAR of 4-substituted-2-aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors.

Pfizer

Pharmacologic inhibition of tpl2 blocks inflammatory responses in primary human monocytes, synoviocytes, and blood.

Wyeth Research

Scaffold modified Vemurafenib analogues as highly selective mitogen activated protein kinase kinase 4 (MKK4) inhibitors.

Eberhard Karls Universit£T T£Bingen

Non-'classical' MEKs: A review of MEK3-7 inhibitors.

Northwestern University

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

Beijing Normal University

Design, synthesis and biological evaluation of 7H-pyrrolo[2,3-d]pyrimidin-4-amine derivatives as selective Btk inhibitors with improved pharmacokinetic properties for the treatment of rheumatoid arthritis.

Sichuan University and Collaborative Innovation Center

Potent and selective inhibitors of platelet-derived growth factor receptor phosphorylation. 1. Synthesis, structure-activity relationship, and biological effects of a new class of quinazoline derivatives.

Pharmaceutical Research Institute

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

Merck

Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.

Merck And

SAR of 4-hydroxypiperidine and hydroxyalkyl substituted heterocycles as novel p38 map kinase inhibitors.

Novartis Pharma

Discovery of 4

TBA

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

ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors.

Vertex Pharmaceuticals

ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.

Vertex Pharmaceuticals

Boron-based inhibitors of acyl protein thioesterases 1 and 2.

Technical University of Dortmund