testis specific serine kinase 2 | Testis specific kinase (TSSK) family | IUPHAR/BPS Guide to PHARMACOLOGY

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testis specific serine kinase 2

Target not currently curated in GtoImmuPdb

Target id: 2258

Nomenclature: testis specific serine kinase 2

Abbreviated Name: TSSK2

Family: Testis specific kinase (TSSK) family

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 358 22q11.21 TSSK2 testis specific serine kinase 2
Mouse - 358 16 A3 Tssk2 testis-specific serine kinase 2
Rat - 358 11 q23 Tssk2 testis-specific serine kinase 2
Previous and Unofficial Names
serine/threonine kinase 22B (spermiogenesis associated) | SPOGA2 | STK22B | Tsk2
Database Links
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 2.7.11.1

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
compound 2c [PMID: 24900538] Hs Inhibition 7.5 pIC50 3
pIC50 7.5 (IC50 3.06x10-8 M) [3]
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen
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: 1-2

Key to terms and symbols Click column headers to sort
Target used in screen: TSSK2/TSSK2
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Hs Inhibitor Inhibition 1.2 -0.5 0.5
K-252a Hs Inhibitor Inhibition 16.6 8.0 0.0
SU11652 Hs Inhibitor Inhibition 66.9 62.0 26.0
sunitinib Hs Inhibitor Inhibition 72.9
nilotinib Hs Inhibitor Inhibition 73.5
Gö 6976 Hs Inhibitor Inhibition 74.3 64.0 40.0
PDK1/Akt/Flt dual pathway inhibitor Hs Inhibitor Inhibition 75.0 97.0 100.0
PDGF receptor tyrosine kinase inhibitor IV Hs Inhibitor Inhibition 75.1 85.0 97.0
PDGF receptor tyrosine kinase inhibitor II Hs Inhibitor Inhibition 78.0 96.0 96.0
p38 MAP kinase inhibitor III Hs Inhibitor Inhibition 78.2 98.0 101.0
Displaying the top 10 most potent ligands  View all ligands in screen »

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. Gao Y, Davies SP, Augustin M, Woodward A, Patel UA, Kovelman R, Harvey KJ. (2013) A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. Biochem. J., 451 (2): 313-28. [PMID:23398362]

3. Wang T, Lamb ML, Block MH, Davies AM, Han Y, Hoffmann E, Ioannidis S, Josey JA, Liu ZY, Lyne PD et al.. (2012) Discovery of Disubstituted Imidazo[4,5-b]pyridines and Purines as Potent TrkA Inhibitors. ACS Med Chem Lett, 3 (9): 705-9. [PMID:24900538]

How to cite this page

Testis specific kinase (TSSK) family: testis specific serine kinase 2. Last modified on 29/01/2016. Accessed on 30/09/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2258.