PMID

Data

Article Title

Organization

Discovery of 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumor cells.

Eli Lilly

Discovery of 1H-pyrazol-3(2H)-ones as potent and selective inhibitors of protein kinase R-like endoplasmic reticulum kinase (PERK).

Amgen

Triazolo[4,5-d]pyrimidine Derivatives as Inhibitors of GCN2.

Dart Neuroscience

Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development.

Glaxosmithkline

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

A quantitative analysis of kinase inhibitor selectivity.

Ambit Biosciences

Comprehensive analysis of kinase inhibitor selectivity.

Ambit Biosciences

Potent GCN2 Inhibitor Capable of Reversing MDSC-Driven T Cell Suppression Demonstrates In Vivo Efficacy as a Single Agent and in Combination with Anti-Angiogenesis Therapy.

Rapt Therapeutics

Discovery of 4

TBA

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

Vertex Pharmaceuticals