Structure of PDB 5i8g Chain A

Receptor sequence
>5i8gA (length=226) Species: 9606 (Homo sapiens) [Search protein sequence]
GSRKKIFKPEELRQALMPTLEALYRQDPESLPFRQPVDPQLLGIPDYFDI
VKNPMDLSTIKRKLDTGQYQEPWQYVDDVWLMFNNAWLYNRKTSRVYKFC
SKLAEVFEQEIDPVMQSLGYCCGRKYEFSPQTLCCYGKQLCTIPRDAAYY
SYQNRYHFCEKCFTLGDDPSQPQTTISKDQFEKKKNDTLDPEPFVDCKEC
GRKMHQICVLHYDIIWPSGFVCDNCL
3D structure
PDB5i8g Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637).
ChainA
Resolution1.41 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 ZN A C1199 C1200 H1291 C1294 C121 C122 H205 C208
BS02 ZN A C1283 C1286 C1308 C1311 C197 C200 C222 C225
BS03 ZN A C1213 C1219 C1237 C135 C141 C159
BS04 69E A L1109 P1110 Q1113 V1115 L1120 N1168 V1174 L31 P32 Q35 V37 L42 N90 V96 MOAD: Kd=0.03uM
PDBbind-CN: -logKd/Ki=7.52,Kd=0.03uM
BindingDB: IC50=30nM,Kd=30nM,EC50=300nM
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:5i8g, PDBe:5i8g, PDBj:5i8g
PDBsum5i8g
PubMed27190605
UniProtQ92793|CBP_HUMAN CREB-binding protein (Gene Name=CREBBP)

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