Structure of PDB 5z1r Chain A

Receptor sequence
>5z1rA (length=134) Species: 9606 (Homo sapiens) [Search protein sequence]
HHHHHLVPRGSNPPPPETSNPNKPKRQTNQLQYLLRVVLKTLWKHQFAWP
FQQPVDAVKLNLPDYYKIIKTPMDMGTIKKRLENNYYWNAQECIQDFNTM
FTNCYIYNKPGDDIVLMAEALEKLFLQKINELPT
3D structure
PDB5z1r Y08060: A Selective BET Inhibitor for Treatment of Prostate Cancer.
ChainA
Resolution1.62 Å
3D
structure
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Enzymatic activity
Enzyme Commision number ?
Interaction with ligand
Site
#
Ligand Ligand
chain
Binding residues on receptor
(original residue number in PDB)
Binding residues on receptor
(residue number reindexed from 1)
Binding affinity
BS01 EFL A W81 V87 L94 N140 I146 W49 V55 L62 N108 I114 PDBbind-CN: -logKd/Ki=5.70,IC50=1.99uM
BindingDB: IC50=1990nM
External links
PDB RCSB:5z1r, PDBe:5z1r, PDBj:5z1r
PDBsum5z1r
PubMed29541371
UniProtO60885|BRD4_HUMAN Bromodomain-containing protein 4 (Gene Name=BRD4)

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