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Sep. 18, 2021

GSK232: A Potent and Selective CECR2 Bromodomain Inhibitor

GSK232

potent, selective CECR2 bromodomain inh. cell permeable tool compound from HTS + SBDD on ATAD2, CECR2 model J. Med. Chem., May 28, 2020 GlaxoSmithKline, Stevenage, UK

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Drug Hunter Team

GSK232 is a highly selective cell-penetrant inhibitor of the non-BET CECR2 bromodomain with >500-fold selectivity over BET-family bromodomains identified during a campaign to find selective inhibitors of the bromodomain ATAD2. Since bromodomain-containing complexes are highly modular and have scaffolding functions, their roles in biology are [...]

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