4UIY
N-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH N-(1,1-dioxo-1-thian-4-yl)- 5-methyl-4-oxo-7-3-(trifluoromethyl)phenyl-4H,5H-thieno-3,2-c- pyridine-2-carboximidamide
Summary for 4UIY
Entry DOI | 10.2210/pdb4uiy/pdb |
Related | 4UIT 4UIU 4UIV 4UIW 4UIX 4UIZ |
Descriptor | BROMODOMAIN-CONTAINING PROTEIN 4, 1,2-ETHANEDIOL, N-[1,1-bis(oxidanylidene)thian-4-yl]-5-methyl-4-oxidanylidene-7-[3-(trifluoromethyl)phenyl]thieno[3,2-c]pyridine-2-carboximidamide, ... (4 entities in total) |
Functional Keywords | transcription, inhibitor, histone, epigenetic reader, bromodomain, brd4, bromodomain containing protein 4, antagonist |
Biological source | HOMO SAPIENS (HUMAN) |
Cellular location | Nucleus: O60885 |
Total number of polymer chains | 1 |
Total formula weight | 15769.11 |
Authors | Chung, C.,Theodoulou, N.T.,Bamborough, P.,Humphreys, P.G. (deposition date: 2015-04-03, release date: 2015-04-22, Last modification date: 2024-05-08) |
Primary citation | Theodoulou, N.H.,Bamborough, P.,Bannister, A.J.,Becher, I.,Bit, R.A.,Che, K.H.,Chung, C.,Dittmann, A.,Drewes, G.,Drewry, D.H.,Gordon, L.,Grandi, P.,Leveridge, M.,Lindon, M.,Michon, A.,Molnar, J.,Robson, S.C.,Tomkinson, N.C.O.,Kouzarides, T.,Prinjha, R.K.,Humphreys, P.G. The Discovery of I-Brd9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition. J.Med.Chem., 59:1425-, 2016 Cited by PubMed: 25856009DOI: 10.1021/ACS.JMEDCHEM.5B00256 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (1.3 Å) |
Structure validation
Download full validation report