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PDZ binding kinase

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Target not currently curated in GtoImmuPdb

Target id: 2140

Nomenclature: PDZ binding kinase

Abbreviated Name: PBK

Family: TOPK family

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 322 8p21.1 PBK PDZ binding kinase
Mouse - 330 14 34.36 cM Pbk PDZ binding kinase
Rat - 337 15p12 Pbk PDZ binding kinase
Previous and Unofficial Names Click here for help
Spermatogenesis-related protein kinase | T-LAK cell-originated protein kinase | SPK | TOPK | cancer/testis antigen 84 ( CT84 ) | T-lymphokine-activated killer cell-originated protein kinase
Database Links Click here for help
Alphafold
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction Click here for help
EC Number: 2.7.12.2

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
OTS964 Small molecule or natural product Primary target of this compound Hs Inhibition 7.6 pIC50 2
pIC50 7.6 (IC50 2.8x10-8 M) [2]
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen Click here for help
A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service.

A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase HotspotSM platform.

http://www.millipore.com/techpublications/tech1/pf3036
http://www.reactionbiology.com/webapps/main/pages/kinase.aspx


Reference: ...1

Key to terms and symbols Click column headers to sort
Target used in screen: nd/PBK(TOPK)
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
K-252a Small molecule or natural product Hs Inhibitor Inhibition 2.7
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 27.8
JAK inhibitor I Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 39.1
SB 218078 Small molecule or natural product Hs Inhibitor Inhibition 39.9
Y27632 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 56.7
GSK-3beta inhibitor II Small molecule or natural product Hs Inhibitor Inhibition 62.7
PDK1/Akt/Flt dual pathway inhibitor Small molecule or natural product Hs Inhibitor Inhibition 64.5
VEGF receptor tyrosine kinase inhibitor III Small molecule or natural product Hs Inhibitor Inhibition 66.2
Syk inhibitor II Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 66.4
PKR inhibitor Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 67.4
Displaying the top 10 most potent ligands  View all ligands in screen »
Immuno Process Associations
Immuno Process:  Inflammation
GO Annotations:  Associated to 1 GO processes, IEA only
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GO:0050728 negative regulation of inflammatory response IEA
Immuno Process:  Immune regulation
GO Annotations:  Associated to 1 GO processes, IEA only
click arrow to show/hide IEA associations
GO:0050728 negative regulation of inflammatory response IEA

References

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1. Anastassiadis T, Deacon SW, Devarajan K, Ma H, Peterson JR. (2011) Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. Nat Biotechnol, 29 (11): 1039-45. [PMID:22037377]

2. Matsuo Y, Park JH, Miyamoto T, Yamamoto S, Hisada S, Alachkar H, Nakamura Y. (2014) TOPK inhibitor induces complete tumor regression in xenograft models of human cancer through inhibition of cytokinesis. Sci Transl Med, 6 (259): 259ra145. [PMID:25338756]

How to cite this page

TOPK family: PDZ binding kinase. Last modified on 03/06/2015. Accessed on 23/09/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2140.