testis specific serine kinase 1B | Testis specific kinase (TSSK) family | IUPHAR/BPS Guide to PHARMACOLOGY

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testis specific serine kinase 1B

Target not currently curated in GtoImmuPdb

Target id: 2257

Nomenclature: testis specific serine kinase 1B

Abbreviated Name: TSSK1

Family: Testis specific kinase (TSSK) family

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 367 5q22.2 TSSK1B testis specific serine kinase 1B
Mouse - 365 16 A3 Tssk1 testis-specific serine kinase 1
Rat - 365 11q23 Tssk1b testis-specific serine kinase 1B
Previous and Unofficial Names
Tsk1 | serine/threonine kinase 22A (spermiogenesis associated) | serine/threonine kinase 22D (spermiogenesis associated) | SPOGA4 | STK22D, TSSK1 | testis-specific serine kinase 1B
Database Links
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
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
ceritinib Hs Inhibition 7.6 pIC50 4
pIC50 7.6 (IC50 2.3x10-8 M) [4]
compound 20 [PMID: 30998356] Hs Inhibition 6.7 pIC50 5
pIC50 6.7 (IC50 2.17x10-7 M) [5]
Description: Measuring in vitro enzyme inhibitory activity.
DiscoveRx KINOMEscan® screen
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
http://www.discoverx.com/services/drug-discovery-development-services/kinase-profiling/kinomescan
Reference: 2,6

Key to terms and symbols Click column headers to sort
Target used in screen: TSSK1B
Ligand Sp. Type Action Value Parameter
staurosporine Hs Inhibitor Inhibition 7.6 pKd
NVP-TAE684 Hs Inhibitor Inhibition 7.6 pKd
lestaurtinib Hs Inhibitor Inhibition 7.0 pKd
GSK-1838705A Hs Inhibitor Inhibition 6.3 pKd
tamatinib Hs Inhibitor Inhibition 6.0 pKd
fedratinib Hs Inhibitor Inhibition 5.9 pKd
PHA-665752 Hs Inhibitor Inhibition 5.7 pKd
KW-2449 Hs Inhibitor Inhibition 5.6 pKd
SB203580 Hs Inhibitor Inhibition <5.5 pKd
ruboxistaurin Hs Inhibitor Inhibition <5.5 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
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: 1,3

Key to terms and symbols Click column headers to sort
Target used in screen: TSSK1/STK22D(TSSK1)
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
K-252a Hs Inhibitor Inhibition 0.8 -1.0 0.0
staurosporine Hs Inhibitor Inhibition 1.0 0.0 -1.0
midostaurin Hs Inhibitor Inhibition 8.2 15.0 6.0
SU11652 Hs Inhibitor Inhibition 8.4 8.0 0.0
Gö 6976 Hs Inhibitor Inhibition 10.1 12.0 10.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 13.7 16.0 12.0
Cdk2 inhibitor IV Hs Inhibitor Inhibition 15.3 14.0 2.0
Syk inhibitor Hs Inhibitor Inhibition 17.0 19.0 14.0
SB 218078 Hs Inhibitor Inhibition 17.7 92.0 70.0
sunitinib Hs Inhibitor Inhibition 20.7
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. Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK, Zarrinkar PP. (2011) Comprehensive analysis of kinase inhibitor selectivity. Nat. Biotechnol., 29 (11): 1046-51. [PMID:22037378]

3. 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]

4. Marsilje TH, Pei W, Chen B, Lu W, Uno T, Jin Y, Jiang T, Kim S, Li N, Warmuth M et al.. (2013) Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2 clinical trials. J. Med. Chem., 56 (14): 5675-90. [PMID:23742252]

5. Riggs JR, Elsner J, Cashion D, Robinson D, Tehrani L, Nagy M, Fultz KE, Krishna Narla R, Peng X, Tran T et al.. (2019) Design and Optimization Leading to an Orally Active TTK Protein Kinase Inhibitor with Robust Single Agent Efficacy. J. Med. Chem., 62 (9): 4401-4410. [PMID:30998356]

6. Wodicka LM, Ciceri P, Davis MI, Hunt JP, Floyd M, Salerno S, Hua XH, Ford JM, Armstrong RC, Zarrinkar PP et al.. (2010) Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. Chem. Biol., 17 (11): 1241-9. [PMID:21095574]

How to cite this page

Testis specific kinase (TSSK) family: testis specific serine kinase 1B. Last modified on 02/05/2019. Accessed on 12/12/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2257.