5ML0

Bromodomain of Mouse PCAF with (R)-4-chloro-2-methyl-5-((1-methylpiperidin-3-yl)amino)pyridazin-3(2H)-one

Summary for 5ML0

Entry DOI	10.2210/pdb5ml0/pdb
Descriptor	Histone acetyltransferase KAT2B, 4-chlorol-2-methyl-5-[[(3~{R})-1-methylpiperidin-3-yl]amino]pyridazin-3-one, 1,2-ETHANEDIOL, ... (4 entities in total)
Functional Keywords	inhibitor, histone, epigenetic reader, bromodomain, pcaf, antagonist, transcription
Biological source	Mus musculus (Mouse)
Cellular location	Nucleus : Q9JHD1
Total number of polymer chains	1
Total formula weight	13572.09
Authors	Chung, C.-W. (deposition date: 2016-12-05, 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 (1.64 Å)

Structure validation