4UYH
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
Summary for 4UYH
Entry DOI | 10.2210/pdb4uyh/pdb |
Related | 4UYD 4UYE 4UYF 4UYG |
Descriptor | BROMODOMAIN-CONTAINING PROTEIN 2, 1-[(2S,4R)-2-methyl-4-(phenylamino)-6-[4-(piperidin-1-ylmethyl)phenyl]-3,4-dihydroquinolin-1(2H)-yl]ethanone, SULFATE ION, ... (5 entities in total) |
Functional Keywords | transcription, histone, epigenetic reader, bet, brd2, bromodomain |
Biological source | HOMO SAPIENS (HUMAN) |
Total number of polymer chains | 3 |
Total formula weight | 54807.61 |
Authors | Chung, C.,Bamborough, P.,Gosmini, R. (deposition date: 2014-08-31, release date: 2014-10-08, Last modification date: 2024-05-08) |
Primary citation | Gosmini, R.,Nguyen, V.L.,Toum, J.,Simon, C.,Brusq, J.M.,Krysa, G.,Mirguet, O.,Riou-Eymard, A.M.,Boursier, E.V.,Trottet, L.,Bamborough, P.,Clark, H.,Chung, C.W.,Cutler, L.,Demont, E.H.,Kaur, R.,Lewis, A.J.,Schilling, M.B.,Soden, P.E.,Taylor, S.,Walker, A.L.,Walker, M.D.,Prinjha, R.K.,Nicodeme, E. The Discovery of I-Bet726 (Gsk1324726A), a Potent Tetrahydroquinoline Apoa1 Up-Regulator and Selective Bet Bromodomain Inhibitor. J.Med.Chem., 57:8111-, 2014 Cited by PubMed: 25249180DOI: 10.1021/JM5010539 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (1.73 Å) |
Structure validation
Download full validation report