5MLJ

Bromodomain of Human GCN5 with 4-bromo-2-methyl-5-(((3R,5R)-1-methyl-5-phenylpiperidin-3-yl)amino)pyridazin-3(2H)-one

Summary for 5MLJ

Entry DOI	10.2210/pdb5mlj/pdb
Descriptor	Histone acetyltransferase KAT2A, 1,2-ETHANEDIOL, 4-bromo-2-methyl-5-[[(3~{R},5~{R})-1-methyl-5-phenyl-piperidin-3-yl]amino]pyridazin-3-one, ... (4 entities in total)
Functional Keywords	inhibitor, histone, epigenetic reader, bromodomain, gcn5, kat2a, antagonist, transcription
Biological source	Homo sapiens (Human)
Cellular location	Nucleus : Q92830
Total number of polymer chains	2
Total formula weight	27453.32
Authors	Chung, C.-W. (deposition date: 2016-12-06, release date: 2017-12-20, Last modification date: 2024-05-08)
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 (1.8 Å)

Structure validation