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testis associated actin remodelling kinase 1

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Target id: 2239

Nomenclature: testis associated actin remodelling kinase 1

Abbreviated Name: TESK1

Family: TESK subfamily

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 626 9p13.3 TESK1 testis associated actin remodelling kinase 1
Mouse - 627 4 A5 Tesk1 testis specific protein kinase 1
Rat - 628 5q22 Tesk1 testis associated actin remodelling kinase 1
Previous and Unofficial Names Click here for help
dual specificity testis-specific protein kinase 1 | testicular protein kinase 1
Database Links Click here for help
Alphafold Q15569 (Hs), O70146 (Mm), Q63572 (Rn)
BRENDA 2.7.12.1
ChEMBL Target CHEMBL5604 (Hs)
Ensembl Gene ENSG00000107140 (Hs), ENSMUSG00000028458 (Mm), ENSRNOG00000053729 (Rn)
Entrez Gene 7016 (Hs), 21754 (Mm), 29460 (Rn)
Human Protein Atlas ENSG00000107140 (Hs)
KEGG Enzyme 2.7.12.1
KEGG Gene hsa:7016 (Hs), mmu:21754 (Mm), rno:29460 (Rn)
OMIM 601782 (Hs)
Pharos Q15569 (Hs)
RefSeq Nucleotide NM_006285 (Hs), NM_011571 (Mm), NM_031578 (Rn)
RefSeq Protein NP_006276 (Hs), NP_035701 (Mm), NP_113766 (Rn)
UniProtKB Q15569 (Hs), O70146 (Mm), Q63572 (Rn)
Wikipedia TESK1 (Hs)
Enzyme Reaction Click here for help
EC Number: 2.7.12.1

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
compound 31 [PMID: 22902653] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.3 pIC50 2
⤷ pIC50 6.3 (IC50 4.55x10-7 M) [2]
compound 30 [PMID: 22902653] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 5.9 pIC50 2
⤷ pIC50 5.9 (IC50 1.133x10-6 M) [2]
compound 35 [PMID: 22902653] Small molecule or natural product Click here for species-specific activity table Hs Inhibition <4.5 pIC50 2
⤷ pIC50 <4.5 (IC50 >3x10-5 M) [2]
DiscoveRx KINOMEscan® screen Click here for help
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 Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.5 pKd
PD-173955 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.1 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.6 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.5 pKd
PP-242 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.5 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.5 pKd
tamatinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.4 pKd
crizotinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.4 pKd
Ki-20227 Small molecule or natural product Hs Inhibitor Inhibition 6.0 pKd
PLX-4720 Small molecule or natural product Ligand has a PDB structure 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 18/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2239.