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ACS Med Chem Lett. 2016 May 9;7(6):552-7. doi: 10.1021/acsmedchemlett.6b00092. eCollection 2016 Jun 9.

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

Author information

1
Epinova Discovery Performance Unit, Quantitative Pharmacology, Experimental Medicine Unit, Flexible Discovery Unit, and Platform Technology and Science, GlaxoSmithKline , Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K.
2
Cellzome GmbH, GlaxoSmithKline , Meyerhofstrasse 1, 69117 Heidelberg, Germany.
3
Epinova Discovery Performance Unit, Quantitative Pharmacology, Experimental Medicine Unit, Flexible Discovery Unit, and Platform Technology and Science, GlaxoSmithKline, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K.; WestCHEM, Department of Pure and Applied Chemistry, University of Strathclyde, Thomas Graham Building, 295 Cathedral Street, Glasgow G1 1XL, U.K.
4
WestCHEM, Department of Pure and Applied Chemistry, University of Strathclyde , Thomas Graham Building, 295 Cathedral Street, Glasgow G1 1XL, U.K.

Abstract

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.

KEYWORDS:

BET; BRD1; BRPF1; BRPF2; BRPF3; bromodomain; chemical probe; epigenetics; inhibitor

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