4Z1Q
Crystal structure of the first bromodomain of human BRD4 bound to benzotriazolo-diazepine scaffold
Summary for 4Z1Q
Entry DOI | 10.2210/pdb4z1q/pdb |
Descriptor | Bromodomain-containing protein 4, 5-[(4R)-6-(4-chlorophenyl)-1,4-dimethyl-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1,5]benzodiazepin-8-yl]pyridin-2-amine (3 entities in total) |
Functional Keywords | bromodomain, transcription |
Biological source | Homo sapiens (Human) |
Cellular location | Nucleus: O60885 |
Total number of polymer chains | 2 |
Total formula weight | 30828.26 |
Authors | Setser, J.W.,Poy, F.,Tang, Y.,Bellon, S.F. (deposition date: 2015-03-27, release date: 2015-04-08, Last modification date: 2024-03-06) |
Primary citation | Taylor, A.M.,Vaswani, R.G.,Gehling, V.S.,Hewitt, M.C.,Leblanc, Y.,Audia, J.E.,Bellon, S.,Cummings, R.T.,Cote, A.,Harmange, J.C.,Jayaram, H.,Joshi, S.,Lora, J.M.,Mertz, J.A.,Neiss, A.,Pardo, E.,Nasveschuk, C.G.,Poy, F.,Sandy, P.,Setser, J.W.,Sims, R.J.,Tang, Y.,Albrecht, B.K. Discovery of Benzotriazolo[4,3-d][1,4]diazepines as Orally Active Inhibitors of BET Bromodomains. Acs Med.Chem.Lett., 7:145-150, 2016 Cited by PubMed: 26985289DOI: 10.1021/ml500411h PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (1.399 Å) |
Structure validation
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