tousled like kinase 2 | Tousled-like kinase (TLK) family | IUPHAR/BPS Guide to PHARMACOLOGY

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tousled like kinase 2

Target not currently curated in GtoImmuPdb

Target id: 2243

Nomenclature: tousled like kinase 2

Abbreviated Name: TLK2

Family: Tousled-like kinase (TLK) family

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 750 17q23 TLK2 tousled like kinase 2
Mouse - 750 11 E1 Tlk2 tousled-like kinase 2 (Arabidopsis)
Rat - 750 10 q32.1 Tlk2 tousled-like kinase 2
Previous and Unofficial Names
PKU-ALPHA | protein kinase U-alpha
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: 2.7.11.1
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: 2,4

Key to terms and symbols Click column headers to sort
Target used in screen: TLK2
Ligand Sp. Type Action Value Parameter
staurosporine Hs Inhibitor Inhibition 7.8 pKd
lestaurtinib Hs Inhibitor Inhibition 7.2 pKd
SU-14813 Hs Inhibitor Inhibition 6.6 pKd
sunitinib Hs Inhibitor Inhibition 6.5 pKd
tamatinib Hs Inhibitor Inhibition 6.4 pKd
enzastaurin Hs Inhibitor Inhibition 5.8 pKd
KW-2449 Hs Inhibitor Inhibition 5.7 pKd
fedratinib Hs Inhibitor Inhibition 5.7 pKd
bosutinib Hs Inhibitor Inhibition 5.7 pKd
dovitinib 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
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 Hs Inhibitor Inhibition 2.8 0.5 0.5
K-252a Hs Inhibitor Inhibition 3.1 1.0 0.0
SB 218078 Hs Inhibitor Inhibition 14.1 62.0 68.0
PKR inhibitor Hs Inhibitor Inhibition 16.4 19.0 3.0
SU9516 Hs Inhibitor Inhibition 42.8 63.0 11.0
JAK3 inhibitor VI Hs Inhibitor Inhibition 50.8 38.0 5.0
Syk inhibitor Hs Inhibitor Inhibition 63.2 87.0 43.0
sunitinib Hs Inhibitor Inhibition 63.3
PKCbeta inhibitor Hs Inhibitor Inhibition 74.1 44.0 7.0
midostaurin Hs Inhibitor Inhibition 75.0 95.0 72.0
Displaying the top 10 most potent ligands  View all ligands in screen »

References

Show »

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 20/09/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2243.