5MKX

1.68A STRUCTURE PCAF BROMODOMAIN WITH 4-chloro-2-methyl-5-(methylamino)pyridazin-3(2H)-one

Summary for 5MKX

Entry DOI	10.2210/pdb5mkx/pdb
Descriptor	Histone acetyltransferase KAT2B, 4-chloranyl-2-methyl-5-(methylamino)pyridazin-3-one, SULFATE ION, ... (6 entities in total)
Functional Keywords	inhibitor, histone, epigenetic reader, bromodomain, pcaf, antagonist, transcription
Biological source	Homo sapiens (Human)
Cellular location	Nucleus : Q92831
Total number of polymer chains	2
Total formula weight	29116.43
Authors	Chung, C.-W. (deposition date: 2016-12-05, release date: 2017-12-20, Last modification date: 2022-07-13)
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 (1.68 Å)

Structure validation