6Z7L

N-TERMINAL BROMODOMAIN OF HUMAN BRD4 with GSK789

This is a non-PDB format compatible entry.

Summary for 6Z7L

• Entry DOI: 10.2210/pdb6z7l/pdb
• Descriptor: Bromodomain-containing protein 4, (3~{R},4~{R})-~{N}-cyclohexyl-4-[[5-(furan-2-yl)-3-methyl-2-oxidanylidene-1~{H}-1,7-naphthyridin-8-yl]amino]-1-methyl-piperidine-3-carboxamide (3 entities in total)
• Functional Keywords: inhibitor, histone, epigenetic reader, bromodomain, brd4, bromodomain containing protein 4, antagonist, transcription
• Biological source: Homo sapiens (Human)
• Total number of polymer chains: 1
• Total formula weight: 15562.95

Authors

Chung, C. (deposition date: 2020-05-31, release date: 2020-07-29, Last modification date: 2020-09-23)

• Primary citation: Watson, R.J.,Bamborough, P.,Barnett, H.,Chung, C.W.,Davis, R.,Gordon, L.,Grandi, P.,Petretich, M.,Phillipou, A.,Prinjha, R.K.,Rioja, I.,Soden, P.,Werner, T.,Demont, E.H.; GSK789: A Selective Inhibitor of the First Bromodomains (BD1) of the Bromo and Extra Terminal Domain (BET) Proteins.; J.Med.Chem., 63:9045-9069, 2020; PubMed: 32691589; DOI: 10.1021/acs.jmedchem.0c00614

Experimental method

X-RAY DIFFRACTION (1.624 Å)