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tousled like kinase 1

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Target id: 2242

Nomenclature: tousled like kinase 1

Abbreviated Name: TLK1

Family: Tousled-like kinase (TLK) family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 766 2q31.1 TLK1 tousled like kinase 1
Mouse - 766 2 C2 Tlk1 tousled-like kinase 1
Rat - 516 3 q21 Tlk1 tousled-like kinase 1
Previous and Unofficial Names Click here for help
PKU-BETA
Database Links Click here for help
Alphafold Q9UKI8 (Hs), Q8C0V0 (Mm)
BRENDA 2.7.11.1
ChEMBL Target CHEMBL5388 (Hs)
Ensembl Gene ENSG00000198586 (Hs), ENSMUSG00000041997 (Mm), ENSRNOG00000009300 (Rn)
Entrez Gene 9874 (Hs), 228012 (Mm), 311118 (Rn)
Human Protein Atlas ENSG00000198586 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:9874 (Hs), mmu:228012 (Mm), rno:311118 (Rn)
OMIM 608438 (Hs)
Pharos Q9UKI8 (Hs)
RefSeq Nucleotide NM_012290 (Hs), NM_172664 (Mm), NM_001107734 (Rn)
RefSeq Protein NP_036422 (Hs), NP_766252 (Mm), NP_001101204 (Rn)
UniProtKB Q9UKI8 (Hs), Q8C0V0 (Mm)
Wikipedia TLK1 (Hs)
Enzyme Reaction Click here for help
EC Number: 2.7.11.1
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: 1-2
Key to terms and symbols Click column headers to sort
Target used in screen: TLK1
Ligand Sp. Type Action Value Parameter
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.6 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.0 pKd
tamatinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.3 pKd
enzastaurin Small molecule or natural product Hs Inhibitor Inhibition 6.3 pKd
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.2 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 6.2 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.1 pKd
fedratinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 5.9 pKd
ruboxistaurin Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.7 pKd
AT-7519 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.6 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. 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

Tousled-like kinase (TLK) family: tousled like kinase 1. Last modified on 29/01/2016. Accessed on 16/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2242.