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

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.
PDB ID: 5G4RDownload
MMDB ID: 141007
PDB Deposition Date: 2016/5/16
Updated in MMDB: 2016/08
Experimental Method:
x-ray diffraction
Resolution: 1.96  Å
Source Organism:
Similar Structures:
Biological Unit for 5G4R: monomeric; determined by software (PISA)
Molecular Components in 5G4R
Label Count Molecule
Protein (1 molecule)
Peregrin(Gene symbol: BRPF1)
Molecule annotation
Chemical (1 molecule)
* Click molecule labels to explore molecular sequence information.

Citing MMDB