Loading
PDBj
MenuPDBj@FacebookPDBj@TwitterPDBj@YouTubewwPDB FoundationwwPDB
RCSB PDBPDBeBMRBAdv. SearchSearch help

4C66

Discovery of Epigenetic Regulator I-BET762: Lead Optimization to Afford a Clinical Candidate Inhibitor of the BET Bromodomains

Summary for 4C66
Entry DOI10.2210/pdb4c66/pdb
Related4C67
DescriptorBROMODOMAIN-CONTAINING PROTEIN 4, 4-(2-chlorophenyl)-2-ethyl-9-methyl-6,8-dihydrothieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-10-ium (3 entities in total)
Functional Keywordscell cycle, transcription regulation, inhibitor, epigenetic reader, antagonist
Biological sourceHOMO SAPIENS (HUMAN)
Cellular locationNucleus: O60885
Total number of polymer chains1
Total formula weight15314.12
Authors
Chung, C.,Mirguet, O. (deposition date: 2013-09-17, release date: 2013-10-02, Last modification date: 2013-10-30)
Primary citationMirguet, O.,Gosmini, R.,Toum, J.,Clement, C.,Barnathan, M.,Brusq, J.,Mordaunt, J.E.,Grimes, R.,Crowe, M.,Pineau, O.,Ajakane, M.,Daugan, A.,Jeffrey, P.,Cutler, L.,Haynes, A.,Smithers, N.,Chung, C.,Bamborough, P.,Uings, I.J.,Lewis, T.,Witherington, J.,Parr, N.,Prinjha, R.,Nicodeme, E.
Discovery of Epigenetic Regulator I-Bet762: Lead Optimization to Afford a Clinical Candidate Inhibitor of the Bet Bromodomains.
J.Med.Chem., 56:7501-, 2013
Cited by
PubMed: 24015967
DOI: 10.1021/JM401088K
PDB entries with the same primary citation
Experimental method
X-RAY DIFFRACTION (1.87 Å)
Structure validation

217705

PDB entries from 2024-03-27

PDB statisticsPDBj update infoContact PDBjnumon