testis associated actin remodelling kinase 1 | TESK subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

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testis associated actin remodelling kinase 1

Target not currently curated in GtoImmuPdb

Target id: 2239

Nomenclature: testis associated actin remodelling kinase 1

Abbreviated Name: TESK1

Family: TESK subfamily

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 626 9p13 TESK1 testis associated actin remodelling kinase 1
Mouse - 627 4 A5-C1 Tesk1 testis specific protein kinase 1
Rat - 628 5 q22 Tesk1 testis associated actin remodelling kinase 1
Previous and Unofficial Names
dual specificity testis-specific protein kinase 1 | testicular protein kinase 1
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: 2.7.12.1

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 31 [PMID: 22902653] Hs Inhibition 6.3 pIC50 2
pIC50 6.3 (IC50 4.55x10-7 M) [2]
compound 30 [PMID: 22902653] Hs Inhibition 5.9 pIC50 2
pIC50 5.9 (IC50 1.133x10-6 M) [2]
compound 35 [PMID: 22902653] Hs Inhibition <4.5 pIC50 2
pIC50 <4.5 (IC50 >3x10-5 M) [2]
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: 1,3

Key to terms and symbols Click column headers to sort
Target used in screen: TESK1
Ligand Sp. Type Action Value Parameter
dasatinib Hs Inhibitor Inhibition 7.5 pKd
PD-173955 Hs Inhibitor Inhibition 7.1 pKd
foretinib Hs Inhibitor Inhibition 6.6 pKd
lestaurtinib Hs Inhibitor Inhibition 6.5 pKd
PP-242 Hs Inhibitor Inhibition 6.5 pKd
staurosporine Hs Inhibitor Inhibition 6.5 pKd
tamatinib Hs Inhibitor Inhibition 6.4 pKd
crizotinib Hs Inhibitor Inhibition 6.4 pKd
Ki-20227 Hs Inhibitor Inhibition 6.0 pKd
PLX-4720 Hs Inhibitor Inhibition 5.8 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »

References

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1. 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]

2. He L, Seitz SP, Trainor GL, Tortolani D, Vaccaro W, Poss M, Tarby CM, Tokarski JS, Penhallow B, Hung CY et al.. (2012) Modulation of cofilin phosphorylation by inhibition of the Lim family kinases. Bioorg. Med. Chem. Lett., 22 (18): 5995-8. [PMID:22902653]

3. 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

TESK subfamily: testis associated actin remodelling kinase 1. Last modified on 09/05/2018. Accessed on 26/09/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2239.