Structure of PDB 5idp Chain A

Receptor sequence
>5idpA (length=342) Species: 9606 (Homo sapiens) [Search protein sequence]
KMDYDFKVKLSSERERVEDLFEYEGCKVGRGTYGHVYKAKRKDGKDDKDY
ALKQIEGTGISMSACREIALLRELKHPNVISLQKVFLSHADRKVWLLFDY
AEHDLWHIIKFHRASKVQLPRGMVKSLLYQILDGIHYLHANWVLHRDLKP
ANILVMGEGPERGRVKIADMGFARLFNSPLKTFWYRAPELLLGARHYTKA
IDIWAIGCIFAELLTSEPIFHCRQETSNPYHHDQLDRIFNVMGFPADKDW
EDIKKMPEHSTLMKDFRRNTYTNCSLIKYMEKHKVKPDSKAFHLLQKLLT
MDPIKRITSEQAMQDPYFLEDPLPTSDVFAGCQIPYPKREFL
3D structure
PDB5idp Structure-Based Optimization of Potent, Selective, and Orally Bioavailable CDK8 Inhibitors Discovered by High-Throughput Screening.
ChainA
Resolution2.65 Å
3D
structure
Catalytic site residues are labeled in the structure
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Enzymatic activity
Catalytic site (original residue number in PDB) D151 K153 N156 D173 N181 T196
Catalytic site (residue number reindexed from 1) D147 K149 N152 D169 N177 T182
Enzyme Commision number 2.7.11.22: cyclin-dependent kinase.
2.7.11.23: [RNA-polymerase]-subunit kinase.
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 6A6 A V27 Y32 V35 A50 F97 D98 A100 A155 L158 D173 R356 V28 Y33 V36 A51 F98 D99 A101 A151 L154 D169 R339 PDBbind-CN: -logKd/Ki=7.35,IC50=45nM
BindingDB: IC50=800nM
Gene Ontology
Molecular Function
GO:0004672 protein kinase activity
GO:0005524 ATP binding
Biological Process
GO:0006468 protein phosphorylation

View graph for
Molecular Function

View graph for
Biological Process
External links
PDB RCSB:5idp, PDBe:5idp, PDBj:5idp
PDBsum5idp
PubMed27490956
UniProtP49336|CDK8_HUMAN Cyclin-dependent kinase 8 (Gene Name=CDK8)

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