6FFE

Human BRD2 C-terminal bromodomain with 2-((4-acetyl-3-cyclopropyl-3,4-dihydroquinoxalin-1(2H)-yl)methyl)benzoic acid

Summary for 6FFE

• Entry DOI: 10.2210/pdb6ffe/pdb
• Related: 6FFD
• Descriptor: Bromodomain-containing protein 2, DI(HYDROXYETHYL)ETHER, 1,2-ETHANEDIOL, ... (5 entities in total)
• Functional Keywords: inhibitor, histone, epigenetic reader, bromodomain, brd4, bromodomain containing protein 4, antagonist, transcription
• Biological source: Homo sapiens (Human)
• Total number of polymer chains: 1
• Total formula weight: 14119.25

Authors

Chung, C. (deposition date: 2018-01-07, release date: 2019-01-30, Last modification date: 2020-02-12)

• Primary citation: Law, R.P.,Atkinson, S.J.,Bamborough, P.,Chung, C.W.,Demont, E.H.,Gordon, L.J.,Lindon, M.,Prinjha, R.K.,Watson, A.J.B.,Hirst, D.J.; Discovery of Tetrahydroquinoxalines as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the Second Bromodomain.; J.Med.Chem., 61:4317-4334, 2018; PubMed: 29656650; DOI: 10.1021/acs.jmedchem.7b01666

Experimental method

X-RAY DIFFRACTION (1.76 Å)