Structure of PDB 5xxh Chain A

Receptor sequence
>5xxhA (length=117) Species: 9606 (Homo sapiens) [Search protein sequence]
RKKIFKPEELRQALMPTLEALYRQDPESLPFRQPVDPQLLGIPDYFDIVK
NPMDLSTIKRKLDTGQYQEPWQYVDDVWLMFNNAWLYNRKTSRVYKFCSK
LAEVFEQEIDPVMQSLG
3D structure
PDB5xxh Discovery and optimization of 1-(1H-indol-1-yl)ethanone derivatives as CBP/EP300 bromodomain inhibitors for the treatment of castration-resistant prostate cancer.
ChainA
Resolution1.62 Å
3D
structure
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Enzymatic activity
Enzyme Commision number 2.3.1.-
2.3.1.48: histone acetyltransferase.
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 E0D A L1109 P1110 V1115 N1168 R1173 V1174 L29 P30 V35 N88 R93 V94 MOAD: ic50=6.8uM
BindingDB: IC50=6800nM
Gene Ontology
Molecular Function
GO:0004402 histone acetyltransferase activity
Biological Process
GO:0006355 regulation of DNA-templated transcription

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Molecular Function
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Biological Process
External links
PDB RCSB:5xxh, PDBe:5xxh, PDBj:5xxh
PDBsum5xxh
PubMed29448139
UniProtQ92793|CBP_HUMAN CREB-binding protein (Gene Name=CREBBP)

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