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serine/threonine kinase 39

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Target not currently curated in GtoImmuPdb

Target id: 2224

Nomenclature: serine/threonine kinase 39

Abbreviated Name: STLK3

Family: FRAY subfamily

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 545 2q24.3 STK39 serine/threonine kinase 39
Mouse - 556 2 C1.3 Stk39 serine/threonine kinase 39
Rat - 553 3q21 Stk39 serine threonine kinase 39
Previous and Unofficial Names Click here for help
DCHT | pancreatic serine/threonine-protein kinase | PSTK1 | SPAK | serine threonine kinase 39
Database Links Click here for help
Alphafold Q9UEW8 (Hs), Q9Z1W9 (Mm), O88506 (Rn)
BRENDA 2.7.11.1
ChEMBL Target CHEMBL1163108 (Hs), CHEMBL4105808 (Rn)
Ensembl Gene ENSG00000198648 (Hs), ENSMUSG00000027030 (Mm), ENSRNOG00000024808 (Rn)
Entrez Gene 27347 (Hs), 53416 (Mm), 54348 (Rn)
Human Protein Atlas ENSG00000198648 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:27347 (Hs), mmu:53416 (Mm), rno:54348 (Rn)
OMIM 607648 (Hs)
Pharos Q9UEW8 (Hs)
RefSeq Nucleotide NM_013233 (Hs), NM_016866 (Mm), NM_019362 (Rn)
RefSeq Protein NP_037365 (Hs), NP_058562 (Mm), NP_062235 (Rn)
UniProtKB Q9UEW8 (Hs), Q9Z1W9 (Mm), O88506 (Rn)
Wikipedia STK39 (Hs)
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
aplithianine A Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.5 pIC50 3
⤷ pIC50 7.5 (IC50 3.5x10-8 M) [3]
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: STK39
Ligand Sp. Type Action Value Parameter
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.9 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.8 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.8 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 6.4 pKd
dovitinib Small molecule or natural product Hs Inhibitor Inhibition 6.3 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 6.1 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.0 pKd
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 5.8 pKd
fedratinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 5.8 pKd
ruxolitinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 5.7 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
Key to terms and symbols Click column headers to sort
Target used in screen: nd/STK39(STLK3)
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 8.0
Flt-3 inhibitor III Small molecule or natural product Hs Inhibitor Inhibition 75.4
aloisine A Small molecule or natural product Hs Inhibitor Inhibition 76.1
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 76.5
dorsomorphin Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 76.8
ATM/ATR kinase inhibitor Small molecule or natural product Hs Inhibitor Inhibition 77.0
alsterpaullone Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 77.5
aloisine Small molecule or natural product Hs Inhibitor Inhibition 77.8
LY 294002 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 78.4
Tpl2 kinase inhibitor Small molecule or natural product Hs Inhibitor Inhibition 78.6
Displaying the top 10 most potent ligands  View all ligands in screen »
Immuno Process Associations
Immuno Process:  Chemotaxis & migration
Immuno Process:  Cytokine production & signalling
Immuno Process:  Inflammation
Immuno Process:  Immune regulation

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. Du L, Wilson BAP, Li N, Shah R, Dalilian M, Wang D, Smith EA, Wamiru A, Goncharova EI, Zhang P et al.. (2023) Discovery and Synthesis of a Naturally Derived Protein Kinase Inhibitor that Selectively Inhibits Distinct Classes of Serine/Threonine Kinases. J Nat Prod, 86 (10): 2283-2293. [PMID:37843072]

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

FRAY subfamily: serine/threonine kinase 39. Last modified on 11/01/2024. Accessed on 19/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=2224.