5A5S

NN-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH 5-5-methoxypyridin-3-yl-3- methyl-8-piperidin-4-ylamino-1,2-dihydro-1,7-naphthyridin-2-one

Summary for 5A5S

• Entry DOI: 10.2210/pdb5a5s/pdb
• Related: 5A5N 5A5O 5A5P 5A5Q 5A5R
• Descriptor: BROMODOMAIN-CONTAINING PROTEIN 4, 1,2-ETHANEDIOL, 5-(5-methoxypyridin-3-yl)-3-methyl-8-[(piperidin-4-yl)amino]-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: 15527.93

Authors

Chung, C.,Bamborough, P.,Demont, E. (deposition date: 2015-06-20, release date: 2015-07-22, Last modification date: 2024-05-08)

• Primary citation: Demont, E.H.,Chung, C.,Furze, R.C.,Grandi, P.,Michon, A.,Wellaway, C.,Barrett, N.,Bridges, A.M.,Craggs, P.D.,Diallo, H.,Dixon, D.P.,Douault, C.,Emmons, A.J.,Jones, E.J.,Karamshi, B.V.,Locke, K.,Mitchell, D.J.,Mouzon, B.H.,Prinjha, R.K.,Roberts, A.D.,Sheppard, R.J.,Watson, R.J.,Bamborough, P.; Fragment-Based Discovery of Low-Micromolar Atad2 Bromodomain Inhibitors.; J.Med.Chem., 58:5649-, 2015; PubMed: 26155854; DOI: 10.1021/ACS.JMEDCHEM.5B00772

Experimental method

X-RAY DIFFRACTION (1.36 Å)