5A85

N-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH 8-(3R,4R)-3-(cyclohexylmethoxy)piperidin-4-ylamino-3-methyl-1,2-dihydro-1,7- naphthyridin-2-one

Summary for 5A85

Entry DOI	10.2210/pdb5a85/pdb
Related	5A81 5A82 5A83
Descriptor	BROMODOMAIN-CONTAINING PROTEIN 4, 1,2-ETHANEDIOL, (3R,4R)-3-(cyclohexylmethoxy)piperidin-4-yl]amino}-3-methyl-1,2-dihydro-1,7-naphthyridin-2-one, ... (4 entities in total)
Functional Keywords	hydrolase, inhibitor, histone, epigenetic reader, bromodomain, brd4, bromodomain containing protein 4, antagonist
Biological source	HOMO SAPIENS (HUMAN)
Cellular location	Nucleus: O60885
Total number of polymer chains	1
Total formula weight	15531.94
Authors	Chung, C.,Bamborough, P.,Demont, E. (deposition date: 2015-07-11, release date: 2015-08-12, Last modification date: 2015-08-26)
Primary citation	Bamborough, P.,Chung, C.,Furze, R.C.,Grandi, P.,Michon, A.,Sheppard, R.J.,Barnett, H.,Diallo, H.,Dixon, D.P.,Douault, C.,Jones, E.J.,Karamshi, B.,Mitchell, D.J.,Prinjha, R.K.,Rau, C.,Watson, R.J.,Werner, T.,Demont, E.H. Structure-Based Optimization of Naphthyridones Into Potent Atad2 Bromodomain Inhibitors. J.Med.Chem., 58:6151-, 2015 Cited by PubMed: 26230603 DOI: 10.1021/ACS.JMEDCHEM.5B00773 PDB entries with the same primary citation
Experimental method	X-RAY DIFFRACTION (1.72 Å)

Structure validation