Publications by Mark J Bird

Publications by authors named "Mark J Bird"

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GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain.

Paul Bamborough Heather A Barnett Isabelle Becher Mark J Bird Chun-Wa Chung

ACS Med Chem Lett

June 2016

The BRPF (Bromodomain and PHD Finger-containing) protein family are important scaffolding proteins for assembly of MYST histone acetyltransferase complexes. A selective benzimidazolone BRPF1 inhibitor showing micromolar activity in a cellular target engagement assay was recently described. Herein, we report the optimization of this series leading to the identification of a superior BRPF1 inhibitor suitable for in vivo studies.

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