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Ligands
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9S3 1-[(2s,4r)-2-methyl-4-(phenylamino)-6-[4-(piperidin-1-ylmethyl)phenyl]-3,4-dihydroquinolin-1(2h)-yl]ethanone
Non-standard Residues
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Glycosylation
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Code : 4UYH   PDBj   RCSB PDB   PDBe
Header : TRANSCRIPTION
Title : N-TERMINAL BROMODOMAIN OF HUMAN BRD2 WITH 1-((2R,4S)-2-methyl-4-(phenylamino)-6-(4-(piperidin-1-ylmethyl)phenyl)-3,4-dihydroquinolin-1(2H)-yl)ethanone
Release Data : 2014-10-08
Compound :
mol_id molecule chains synonym
1 BROMODOMAIN-CONTAINING PROTEIN 2 A,B,C O27.1.1, REALLY INTERESTING NEW GENE 3 PROTEIN, HUMAN BRD2
fragment: N-TERMINAL BROMODOMAIN, RESIDUES 67-200
Source :
mol_id organism_scientific organism_common expression_system
1 HOMO SAPIENS  (taxid:9606) HUMAN ESCHERICHIA COLI  (taxid:562)
Authors : Chung, C., Bamborough, P., Gosmini, R.
Keywords : TRANSCRIPTION, HISTONE, EPIGENETIC READER, BET, BRD2, BROMODOMAIN
Exp. method : X-RAY DIFFRACTION ( 1.73 Å )
Citation :

The Discovery of I-Bet726 (Gsk1324726A), a Potent Tetrahydroquinoline Apoa1 Up-Regulator and Selective Bet Bromodomain Inhibitor.

Gosmini, R.,Nguyen, V.L.,Toum, J.  et al.
(2014)  J.Med.Chem.  57 : 8111

PubMed: 25249180
DOI: 10.1021/JM5010539

Chain : A, B, C
UniProt : P25440 (BRD2_HUMAN)
Reaction : -