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tousled like kinase 2

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Target id: 2243

Nomenclature: tousled like kinase 2

Abbreviated Name: TLK2

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 - 772 17q23.2 TLK2 tousled like kinase 2
Mouse - 718 11 E1 Tlk2 tousled-like kinase 2 (Arabidopsis)
Rat - 750 10 q32.1 Tlk2 tousled-like kinase 2
Previous and Unofficial Names Click here for help
PKU-ALPHA | protein kinase U-alpha
Database Links Click here for help
Alphafold Q86UE8 (Hs), O55047 (Mm)
BRENDA 2.7.11.1
ChEMBL Target CHEMBL5404 (Hs)
Ensembl Gene ENSG00000146872 (Hs), ENSMUSG00000020694 (Mm), ENSRNOG00000006285 (Rn)
Entrez Gene 11011 (Hs), 24086 (Mm), 303592 (Rn)
Human Protein Atlas ENSG00000146872 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:11011 (Hs), mmu:24086 (Mm), rno:303592 (Rn)
OMIM 608439 (Hs)
Pharos Q86UE8 (Hs)
RefSeq Nucleotide NM_006852 (Hs), NM_001112705 (Mm), NM_001191652 (Rn)
RefSeq Protein NP_006843 (Hs), NP_001106176 (Mm), NP_001178581 (Rn)
UniProtKB Q86UE8 (Hs), O55047 (Mm)
Wikipedia TLK2 (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: 2,4
Key to terms and symbols Click column headers to sort
Target used in screen: TLK2
Ligand Sp. Type Action Value Parameter
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.8 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.2 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 6.6 pKd
sunitinib Small molecule or natural product Approved drug 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
enzastaurin Small molecule or natural product Hs Inhibitor Inhibition 5.8 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 5.7 pKd
fedratinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 5.7 pKd
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 5.7 pKd
dovitinib Small molecule or natural product Hs Inhibitor Inhibition 5.6 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen Click here for help
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: TLK2/TLK2
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 2.8 0.5 0.5
K-252a Small molecule or natural product Hs Inhibitor Inhibition 3.1 1.0 0.0
SB 218078 Small molecule or natural product Hs Inhibitor Inhibition 14.1 62.0 68.0
PKR inhibitor Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 16.4 19.0 3.0
SU9516 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 42.8 63.0 11.0
JAK3 inhibitor VI Small molecule or natural product Hs Inhibitor Inhibition 50.8 38.0 5.0
Syk inhibitor Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 63.2 87.0 43.0
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 63.3
PKCbeta inhibitor Small molecule or natural product Hs Inhibitor Inhibition 74.1 44.0 7.0
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 75.0 95.0 72.0
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. 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. 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 2. Last modified on 29/01/2016. Accessed on 16/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2243.