5HM0
Crystal structure of the first bromodomain of human BRD4 bound to benzoisoxazoloazepine 3
Summary for 5HM0
Entry DOI | 10.2210/pdb5hm0/pdb |
Descriptor | Bromodomain-containing protein 4, 6-(4-chlorophenyl)-1-methyl-4H-[1,2]oxazolo[5,4-d][2]benzazepine (3 entities in total) |
Functional Keywords | bromodomain, transcription |
Biological source | Homo sapiens (Human) |
Cellular location | Nucleus: O60885 |
Total number of polymer chains | 1 |
Total formula weight | 15435.10 |
Authors | Jayaram, H.,Poy, F.,Setser, J.W.,Bellon, S.F. (deposition date: 2016-01-15, release date: 2016-02-10, Last modification date: 2023-09-27) |
Primary citation | Albrecht, B.K.,Gehling, V.S.,Hewitt, M.C.,Vaswani, R.G.,Cote, A.,Leblanc, Y.,Nasveschuk, C.G.,Bellon, S.,Bergeron, L.,Campbell, R.,Cantone, N.,Cooper, M.R.,Cummings, R.T.,Jayaram, H.,Joshi, S.,Mertz, J.A.,Neiss, A.,Normant, E.,O'Meara, M.,Pardo, E.,Poy, F.,Sandy, P.,Supko, J.,Sims, R.J.,Harmange, J.C.,Taylor, A.M.,Audia, J.E. Identification of a Benzoisoxazoloazepine Inhibitor (CPI-0610) of the Bromodomain and Extra-Terminal (BET) Family as a Candidate for Human Clinical Trials. J.Med.Chem., 59:1330-1339, 2016 Cited by PubMed: 26815195DOI: 10.1021/acs.jmedchem.5b01882 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (1.395 Å) |
Structure validation
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