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5CS8

Crystal Structure of the first bromodomain of human BRD4 in complex with benzo[cd]indol-2(1H)-one ligand

Summary for 5CS8
Entry DOI10.2210/pdb5cs8/pdb
Related5COI 5CP5 5CPE 5CQT 5CRM 5CRZ 5CTL
DescriptorBromodomain-containing protein 4, methyl 2-[(1-ethyl-2-oxo-1,2-dihydrobenzo[cd]indol-6-yl)sulfamoyl]benzoate, NITRATE ION, ... (6 entities in total)
Functional Keywordsbrd4, bromodomain, four alpha helices, bromodomain binding inhibitor, signaling protein-inhibitor complex, signaling protein/inhibitor
Biological sourceHomo sapiens (Human)
Cellular locationNucleus: O60885
Total number of polymer chains1
Total formula weight17764.26
Authors
Zhang, Y.,Song, M.,Liu, Z.,Xue, X.,Xu, Y. (deposition date: 2015-07-23, release date: 2016-01-13, Last modification date: 2023-11-08)
Primary citationXue, X.,Zhang, Y.,Liu, Z.,Song, M.,Xing, Y.,Xiang, Q.,Wang, Z.,Tu, Z.,Zhou, Y.,Ding, K.,Xu, Y.
Discovery of Benzo[cd]indol-2(1H)-ones as Potent and Specific BET Bromodomain Inhibitors: Structure-Based Virtual Screening, Optimization, and Biological Evaluation
J.Med.Chem., 59:1565-1579, 2016
Cited by
PubMed: 26731490
DOI: 10.1021/acs.jmedchem.5b01511
PDB entries with the same primary citation
Experimental method
X-RAY DIFFRACTION (1.62 Å)
Structure validation

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