National Center for
5G4R: Bromodomain Of Human Brpf1 With N-1,3-dimethyl-6-2r-2- Methylpiperazin-1-yl-2-oxo-2,3-dihydro-1h-1,3-benzodiazol- 5-yl-2-methoxybenzamide
ACS Med Chem Lett (2016) 7 p.552-557
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.
* Click molecule labels to explore molecular sequence information.