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serine/threonine kinase 10

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Target id: 2211

Nomenclature: serine/threonine kinase 10

Abbreviated Name: LOK

Family: SLK subfamily

Contents:

Gene and Protein Information Click here for help
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 - 967 10q12 Stk10 serine/threonine kinase 10
Previous and Unofficial Names Click here for help
Gek1
Database Links Click here for help
Alphafold O94804 (Hs), O55098 (Mm), E9PTG8 (Rn)
BRENDA 2.7.11.1
ChEMBL Target CHEMBL3981 (Hs)
Ensembl Gene ENSG00000072786 (Hs), ENSMUSG00000020272 (Mm), ENSRNOG00000004217 (Rn)
Entrez Gene 6793 (Hs), 20868 (Mm), 29398 (Rn)
Human Protein Atlas ENSG00000072786 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:6793 (Hs), mmu:20868 (Mm), rno:29398 (Rn)
OMIM 603919 (Hs)
Pharos O94804 (Hs)
RefSeq Nucleotide NM_005990 (Hs), NM_009288 (Mm), NM_019206 (Rn)
RefSeq Protein NP_005981 (Hs), NP_033314 (Mm), NP_062079 (Rn)
SynPHARM 81443 (in complex with bosutinib)
UniProtKB O94804 (Hs), O55098 (Mm), E9PTG8 (Rn)
Wikipedia STK10 (Hs)
Selected 3D Structures Click here for help
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 Click here for help
EC Number: 2.7.11.1

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
DDR1/2 inhibitor 5n Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 8.0 pKd 6
⤷ pKd 8.0 (Kd 1x10-8 M) [6]
bosutinib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs - 7.3 pIC50 4
⤷ pIC50 7.3 (IC50 5.2x10-8 M) [4]
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: 2,7
Key to terms and symbols Click column headers to sort
Target used in screen: LOK
Ligand Sp. Type Action Value Parameter
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 10.4 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.3 pKd
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 9.0 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.2 pKd
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.1 pKd
doramapimod Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.9 pKd
neratinib Small molecule or natural product Approved drug Hs Inhibitor Inhibition 7.9 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 7.9 pKd
erlotinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.7 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure 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 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: LOK/LOK(STK10)
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 0.3 1.0 1.0
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 4.0 0.0 0.0
K-252a Small molecule or natural product Hs Inhibitor Inhibition 5.1 3.0 1.0
SU11652 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.1 15.0 5.0
SU11274 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.1 13.0 10.0
SB 218078 Small molecule or natural product Hs Inhibitor Inhibition 9.3 116.0 100.0
SU6656 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.5 63.0 78.0
PKCbeta inhibitor Small molecule or natural product Hs Inhibitor Inhibition 11.5 21.0 6.0
PDGF RTK inhibitor Small molecule or natural product Hs Inhibitor Inhibition 11.9 6.0 7.0
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 12.6
Displaying the top 10 most potent ligands  View all ligands in screen »
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process:  Immune regulation
Immuno Process:  Chemotaxis & migration
Immuno Process:  Cellular signalling

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. 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. Wang Z, Zhang Y, Pinkas DM, Fox AE, Luo J, Huang H, Cui S, Xiang Q, Xu T, Xun Q et al.. (2018) Design, Synthesis, and Biological Evaluation of 3-(Imidazo[1,2- a]pyrazin-3-ylethynyl)-4-isopropyl- N-(3-((4-methylpiperazin-1-yl)methyl)-5-(trifluoromethyl)phenyl)benzamide as a Dual Inhibitor of Discoidin Domain Receptors 1 and 2. J Med Chem, 61 (17): 7977-7990. [PMID:30075624]

7. 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 16/10/2018. Accessed on 19/09/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2211.