PMID

Data

Article Title

Organization

Structure-based drug design of novel ASK1 inhibitors using an integrated lead optimization strategy.

Takeda California Inc

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

Merck & Co.

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

Pyrrolo[3,2-b]quinoxaline derivatives as types I1/2 and II Eph tyrosine kinase inhibitors: structure-based design, synthesis, and in vivo validation.

University of Z£rich

Amino acid conjugates of lithocholic acid as antagonists of the EphA2 receptor.

Universit£ degli Studi di Parma

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.

Cellzome Ltd

Development of Toxoplasma gondii calcium-dependent protein kinase 1 (TgCDPK1) inhibitors with potent anti-toxoplasma activity.

University of Washington

The discovery of thienopyridine analogues as potent IkappaB kinase beta inhibitors. Part II.

Boehringer Ingelheim Pharmaceuticals Inc

A quantitative analysis of kinase inhibitor selectivity.

Ambit Biosciences

Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.

National Cancer Institute-Bethesda

Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.

Harvard Medical School

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

Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant.

ARIAD Pharmaceuticals Inc

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

Ambit Biosciences

Structure-based optimization of potent and selective inhibitors of the tyrosine kinase erythropoietin producing human hepatocellular carcinoma receptor B4 (EphB4).

University of Zurich

Discovery and characterization of the N-phenyl-N'-naphthylurea class of p38 kinase inhibitors.

Boehringer Ingelheim Pharmaceuticals Inc

Assessment of chemical coverage of kinome space and its implications for kinase drug discovery.

GlaxoSmithKline

A small molecule-kinase interaction map for clinical kinase inhibitors.

Ambit Biosciences

NMR-Guided Design of Potent and Selective EphA4 Agonistic Ligands.

University of California

Structural optimization and structure-activity relationship studies of N-phenyl-7,8-dihydro-6H-pyrimido[5,4-b][1,4]oxazin-4-amine derivatives as a new class of inhibitors of RET and its drug resistance mutants.

Sichuan University/Collaborative Innovation Center of Biotherapy

Structure-guided optimization of a novel class of ASK1 inhibitors with increased sp

Takeda Research in California

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

Beijing Normal University

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

Merck & Co.

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

Merck and Co.

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 Company Limited

A Selective and Brain Penetrant p38?MAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction.

Northwestern University

Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders.

Korea Institute of Science and Technology (KIST)

Design and synthesis of selective CDK8/19 dual inhibitors: Discovery of 4,5-dihydrothieno[3',4':3,4]benzo[1,2-d]isothiazole derivatives.

Takeda Pharmaceutical Co., Ltd

[125I]Tyr10-cortistatin14 labels all five somatostatin receptors.

Novartis Pharma AG