5MKZ

N-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH 4-chloro-2-methyl-5-(((3-methylthiophen-2-yl)methyl)amino)pyridazin-3(2H)-one

Summary for 5MKZ

Entry DOI	10.2210/pdb5mkz/pdb
Descriptor	Bromodomain-containing protein 4, 4-chloranyl-2-methyl-5-[(3-methylthiophen-2-yl)methylamino]pyridazin-3-one, GLYCEROL, ... (4 entities in total)
Functional Keywords	inhibitor, histone, epigenetic reader, bromodomain, brd4, bromodomain containing protein 4, antagonist, transcription
Biological source	Homo sapiens (Human)
Cellular location	Nucleus: O60885
Total number of polymer chains	1
Total formula weight	15645.41
Authors	Chung, C.-W. (deposition date: 2016-12-05, release date: 2017-12-20, Last modification date: 2018-01-24)
Primary citation	Humphreys, P.G.,Bamborough, P.,Chung, C.W.,Craggs, P.D.,Gordon, L.,Grandi, P.,Hayhow, T.G.,Hussain, J.,Jones, K.L.,Lindon, M.,Michon, A.M.,Renaux, J.F.,Suckling, C.J.,Tough, D.F.,Prinjha, R.K. Discovery of a Potent, Cell Penetrant, and Selective p300/CBP-Associated Factor (PCAF)/General Control Nonderepressible 5 (GCN5) Bromodomain Chemical Probe. J. Med. Chem., 60:695-709, 2017 Cited by PubMed: 28002667 DOI: 10.1021/acs.jmedchem.6b01566 PDB entries with the same primary citation
Experimental method	X-RAY DIFFRACTION (1.62 Å)

Structure validation