Structure of PDB 3kb7 Chain A

Receptor sequence
>3kb7A (length=290) Species: 9606 (Homo sapiens) [Search protein sequence]
EIPEVLVDPRSRRRYVRGRFLGKGGFAKCFEISDADTKEVFAGKIVPKSL
LLKPHQREKMSMEISIHRSLAHQHVVGFHGFFEDNDFVFVVLELCRRRSL
LELHKRRKALTEPEARYYLRQIVLGCQYLHRNRVIHRDLKLGNLFLNEDL
EVKIGDFGLATKVEYDGERKKTLCGTPNYIAPEVLSKKGHSFEVDVWSIG
CIMYTLLVGKPPFETSCLKETYLRIKKNEYSIPKHINPVAASLIQKMLQT
DPTARPTINELLNDEFFTSGYIPARLPITCLTIPPRFSIA
3D structure
PDB3kb7 Identification of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as a new class of orally and selective Polo-like kinase 1 inhibitors
ChainA
Resolution2.5 Å
3D
structure
Catalytic site residues are labeled in the structure
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Enzymatic activity
Catalytic site (original residue number in PDB) D176 K178 G180 N181 D194 T214
Catalytic site (residue number reindexed from 1) D138 K140 G142 N143 D156 T176
Enzyme Commision number 2.7.11.21: polo 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 071 A L59 C67 A80 K82 C133 R136 S137 E140 F183 D194 L21 C29 A42 K44 C95 R98 S99 E102 F145 D156 MOAD: ic50=0.007uM
PDBbind-CN: -logKd/Ki=8.15,IC50=7nM
BindingDB: IC50=7nM
BS02 ZN A H93 C212 H55 C174
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:3kb7, PDBe:3kb7, PDBj:3kb7
PDBsum3kb7
PubMed20397705
UniProtP53350|PLK1_HUMAN Serine/threonine-protein kinase PLK1 (Gene Name=PLK1)

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