Structure of PDB 5kj2 Chain A

Receptor sequence
>5kj2A (length=323) Species: 9606 (Homo sapiens) [Search protein sequence]
KFSAKRLPSTRLGTFLENRVNDFLRRQNHPESGEVTVRVVHASDKTVEVK
PGMKARFVDSGEMAESFPYRTKALFAFEEIDGVDLCFFGMHVQEYGSDCP
PPNQRRVYISYLDSVHFFRPKCLRTAVYHEILIGYLEYVKKLGYTTGHIW
ACPPSEGDDYIFHCHPPDQKIPKPKRLQEWYKKMLDKAVSERIVHDYKDI
FKQATEDRLTSAKELPYFEGDFWPNVLEESIKELEQKTSKDLSQKLYATM
EKHKEVFFVIRLIAGPAANSLPPIVDPDPLIPCDLMDGRDAFLTLARDRH
LEFSSLRRAQWSTGCMLVELHTQ
3D structure
PDB5kj2 Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours.
ChainA
Resolution1.95 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 6TF A F1374 L1398 D1399 S1400 Y1414 P1440 H1451 Q1455 I1457 P1458 R1462 L1463 W1466 F88 L112 D113 S114 Y128 P154 H165 Q169 I171 P172 R176 L177 W180 BindingDB: IC50=60nM
Gene Ontology
Molecular Function
GO:0004402 histone acetyltransferase activity
Biological Process
GO:0006355 regulation of DNA-templated transcription

View graph for
Molecular Function

View graph for
Biological Process
External links
PDB RCSB:5kj2, PDBe:5kj2, PDBj:5kj2
PDBsum5kj2
PubMed28953875
UniProtQ09472|EP300_HUMAN Histone acetyltransferase p300 (Gene Name=EP300)

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