Structure of PDB 5z1t Chain A

Receptor sequence
>5z1tA (length=135) Species: 9606 (Homo sapiens) [Search protein sequence]
HHHHHLVPRGSNPPPPETSNPNKPKRQTNQLQYLLRVVLKTLWKHQFAWP
FQQPVDAVKLNLPDYYKIIKTPMDMGTIKKRLENNYYWNAQECIQDFNTM
FTNCYIYNKPGDDIVLMAEALEKLFLQKINELPTE
3D structure
PDB5z1t Y08060: A Selective BET Inhibitor for Treatment of Prostate Cancer.
ChainA
Resolution1.42 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 EFN A W81 V87 L94 N140 I146 W49 V55 L62 N108 I114 PDBbind-CN: -logKd/Ki=6.20,IC50=0.63uM
BindingDB: Kd=498nM,IC50=630nM
External links
PDB RCSB:5z1t, PDBe:5z1t, PDBj:5z1t
PDBsum5z1t
PubMed29541371
UniProtO60885|BRD4_HUMAN Bromodomain-containing protein 4 (Gene Name=BRD4)

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