>1000x BD2-selective BET bromodomain inh.
orally available in dog
rational design from prior lead
Journal of Medicinal Chemistry
GlaxoSmithKline, Stevenage, UK
The GSK BET BD2 inhibitor, GSK852, is one of a series of BD2-targeting compounds published last month by GSK (see a fragment-based approach here, a DEL screening approach here, and a pincolinamide…