Structure of PDB 5w0l Chain A

Receptor sequence
>5w0lA (length=114) Species: 9606 (Homo sapiens) [Search protein sequence]
KIFKPEELRQALMPTLEALYRQDPESLPFRQPVDPQLLGIPDYFDIVKNP
MDLSTIKRKLDTGQYQEPWQYVDDVWLMFNNAWLYNRKTSRVYKFCSKLA
EVFEQEIDPVMQSL
3D structure
PDB5w0l GNE-781, A Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP).
ChainA
Resolution1.549 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 9UD A L1109 P1110 V1115 I1122 N1168 R1173 V1174 L27 P28 V33 I40 N86 R91 V92 MOAD: ic50=1.1nM
PDBbind-CN: -logKd/Ki=4.74,IC50=18uM
BindingDB: EC50=14nM,IC50=12nM
Gene Ontology
Molecular Function
GO:0004402 histone acetyltransferase activity
Biological Process
GO:0006355 regulation of DNA-templated transcription

View graph for
Molecular Function
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Biological Process
External links
PDB RCSB:5w0l, PDBe:5w0l, PDBj:5w0l
PDBsum5w0l
PubMed28892380
UniProtQ92793|CBP_HUMAN CREB-binding protein (Gene Name=CREBBP)

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