>1000x BD2-selective BET bromodomain inh.

orally available in dog

rational design from prior lead

Journal of Medicinal Chemistry

GlaxoSmithKline, Stevenage, UK

Chemical structure of GSK852 BET BD2 inhibitor

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…

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