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GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain.
- Source :
-
ACS medicinal chemistry letters [ACS Med Chem Lett] 2016 May 09; Vol. 7 (6), pp. 552-7. Date of Electronic Publication: 2016 May 09 (Print Publication: 2016). - Publication Year :
- 2016
-
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.
Details
- Language :
- English
- ISSN :
- 1948-5875
- Volume :
- 7
- Issue :
- 6
- Database :
- MEDLINE
- Journal :
- ACS medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 27326325
- Full Text :
- https://doi.org/10.1021/acsmedchemlett.6b00092