serine/threonine kinase 10 | SLK subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

serine/threonine kinase 10

Target id: 2211

Nomenclature: serine/threonine kinase 10

Abbreviated Name: LOK

Family: SLK subfamily

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for serine/threonine kinase 10 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 968 5q35.1 STK10 serine/threonine kinase 10
Mouse - 966 11 A4 Stk10 serine/threonine kinase 10
Rat - 980 10 q12.3 Stk10 serine/threonine kinase 10
Previous and Unofficial Names
Gek1
Database Links
BRENDA
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Human STK10 (LOK) with SB-633825. Note the enzyme is in the inactive conformation in this structure. 4USE has the kinase in its active conformation.
PDB Id:  4USD
Ligand:  SB-633825
Resolution:  3.05Å
Species:  Human
References:  5
Enzyme Reaction
EC Number: 2.7.11.1

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 Affinity Units Reference
bosutinib Hs - 7.3 pIC50 4
pIC50 7.3 (IC50 5.2x10-8 M) [4]
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: 2,6

Key to terms and symbols Click column headers to sort
Target used in screen: LOK
Ligand Sp. Type Action Affinity Units
staurosporine Hs Inhibitor Inhibition 10.4 pKd
foretinib Hs Inhibitor Inhibition 9.3 pKd
AST-487 Hs Inhibitor Inhibition 9.0 pKd
lestaurtinib Hs Inhibitor Inhibition 8.2 pKd
bosutinib Hs Inhibitor Inhibition 8.1 pKd
doramapimod Hs Inhibitor Inhibition 7.9 pKd
KW-2449 Hs Inhibitor Inhibition 7.9 pKd
neratinib Hs Inhibitor Inhibition 7.9 pKd
sunitinib Hs Inhibitor Inhibition 7.7 pKd
erlotinib Hs Inhibitor Inhibition 7.7 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: LOK/LOK(STK10)
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Hs Inhibitor Inhibition 0.3 1.0 1.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 4.0 0.0 0.0
K-252a Hs Inhibitor Inhibition 5.1 3.0 1.0
SU11652 Hs Inhibitor Inhibition 7.1 15.0 5.0
SU11274 Hs Inhibitor Inhibition 9.1 13.0 10.0
SB 218078 Hs Inhibitor Inhibition 9.3 116.0 100.0
SU6656 Hs Inhibitor Inhibition 9.5 63.0 78.0
PKCbeta inhibitor Hs Inhibitor Inhibition 11.5 21.0 6.0
PDGF RTK inhibitor Hs Inhibitor Inhibition 11.9 6.0 7.0
bosutinib Hs Inhibitor Inhibition 12.6
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. Remsing Rix LL, Rix U, Colinge J, Hantschel O, Bennett KL, Stranzl T, Müller A, Baumgartner C, Valent P, Augustin M et al.. (2009) Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells. Leukemia, 23 (3): 477-85. [PMID:19039322]

5. The Structural Genomics Consortium. Human serine/threonine kinase 10. Accessed on 24/07/2015. Modified on 24/07/2015. thesgc.org, http://www.thesgc.org/structures/4usd

6. 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

SLK subfamily: serine/threonine kinase 10. Last modified on 13/02/2017. Accessed on 26/09/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2211.