5A85
N-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH 8-(3R,4R)-3-(cyclohexylmethoxy)piperidin-4-ylamino-3-methyl-1,2-dihydro-1,7- naphthyridin-2-one
Summary for 5A85
Entry DOI | 10.2210/pdb5a85/pdb |
Related | 5A81 5A82 5A83 |
Descriptor | BROMODOMAIN-CONTAINING PROTEIN 4, 1,2-ETHANEDIOL, (3R,4R)-3-(cyclohexylmethoxy)piperidin-4-yl]amino}-3-methyl-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 | 15531.94 |
Authors | Chung, C.,Bamborough, P.,Demont, E. (deposition date: 2015-07-11, release date: 2015-08-12, Last modification date: 2024-05-08) |
Primary citation | Bamborough, P.,Chung, C.,Furze, R.C.,Grandi, P.,Michon, A.,Sheppard, R.J.,Barnett, H.,Diallo, H.,Dixon, D.P.,Douault, C.,Jones, E.J.,Karamshi, B.,Mitchell, D.J.,Prinjha, R.K.,Rau, C.,Watson, R.J.,Werner, T.,Demont, E.H. Structure-Based Optimization of Naphthyridones Into Potent Atad2 Bromodomain Inhibitors. J.Med.Chem., 58:6151-, 2015 Cited by PubMed: 26230603DOI: 10.1021/ACS.JMEDCHEM.5B00773 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (1.72 Å) |
Structure validation
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