Chemical structure of GSK852 BET BD2 inhibitor

>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…

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