molecules of the month


>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
1 min read

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 molecule here). Each of these campaigns is impressive and educational in different ways, and the collective GSK BD2 effort is a tour de force of lead finding and optimization strategies (for additional BET efforts recently published by GSK and others, see May 2020, Mar. 2020, Feb. 2020, and Jan. 2021). GSK852 was particularly interesting for its chemical structure, the use of a quaternary center to block metabolism and improve solubility. GSK has invested significant resources into drugging epigenetic modulators and the publication of their efforts will be helpful to the community in understanding the challenging biology…

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