8PXN
N-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH (1R,1'R)-7,7'-(ethane-1,2-diylbis(oxy))bis(1,3-dimethyl-1,3-dihydro-2H-benzo[d]azepin-2-one)
Summary for 8PXN
Entry DOI | 10.2210/pdb8pxn/pdb |
Related | 8PXM |
Descriptor | Bromodomain-containing protein 4, 1,2-ETHANEDIOL, (1R)-7-[2-[[(1R)-1,3-dimethyl-2-oxidanylidene-1H-3-benzazepin-7-yl]oxy]ethoxy]-1,3-dimethyl-1H-3-benzazepin-2-one, ... (4 entities in total) |
Functional Keywords | inhibitor, histone, epigenetic reader, bromodomain, brd4, bromodomain containing protein 4, antagonist, transcription |
Biological source | Homo sapiens (human) |
Total number of polymer chains | 4 |
Total formula weight | 61386.68 |
Authors | |
Primary citation | Bamborough, P.,Chung, C.W.,Goodwin, N.C.,Mitchell, D.J.,Neipp, C.E.,Phillipou, A.,Preston, A.,Prinjha, R.K.,Soden, P.E.,Watson, R.J.,Demont, E.H. Design and Characterization of 1,3-Dihydro-2 H -benzo[ d ]azepin-2-ones as Rule-of-5 Compliant Bivalent BET Inhibitors. Acs Med.Chem.Lett., 14:1231-1236, 2023 Cited by PubMed: 37736196DOI: 10.1021/acsmedchemlett.3c00242 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (1.952 Å) |
Structure validation
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