PDB Information

PDB5KHM
MethodX-RAY DIFFRACTION
Host OrganismEscherichia coli
Gene SourceHomo sapiens
Primary Citation
Optimization of a Series of Bivalent Triazolopyridazine Based Bromodomain and Extraterminal Inhibitors: The Discovery of (3R)-4-[2-[4-[1-(3-Methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)-4-piperidyl]phenoxy]ethyl]-1,3-dimethyl-piperazin-2-one (AZD5153).
Bradbury, R.H., Callis, R., Carr, G.R., Chen, H., Clark, E., Feron, L., Glossop, S., Graham, M.A., Hattersley, M., Jones, C., Lamont, S.G., Ouvry, G., Patel, A., Patel, J., Rabow, A.A., Roberts, C.A., Stokes, S., Stratton, N., Walker, G.E., Ward, L., Whalley, D., Whittaker, D., Wrigley, G., Waring, M.J.
J.Med.Chem.
HeaderTranscription Factor
Released2016-06-15
Resolution1.480
CATH Insert Date16 Oct, 2016

PDB Images (5)

PDB Prints

PDB Chains (2)

Chain ID Date inserted into CATH CATH Status
A 17 Oct, 2016 Chopped
B 17 Oct, 2016 Chopped

CATH Domains (2)

Domain ID Date inserted into CATH Superfamily CATH Status
5khmA01 21 Oct, 2016 1.20.920.10 Assigned
5khmB01 22 Oct, 2016 1.20.920.10 Assigned

UniProtKB Entries (2)

Accession Gene ID Taxon Description
O60885 BRD4_HUMAN Homo sapiens Bromodomain-containing protein 4
O60885 BRD4_HUMAN Homo sapiens Bromodomain-containing protein 4