serine/threonine kinase 39 | FRAY subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

serine/threonine kinase 39

Target id: 2224

Nomenclature: serine/threonine kinase 39

Abbreviated Name: STLK3

Family: FRAY 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 39 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 545 2q24.3 STK39 serine/threonine kinase 39
Mouse - 556 2 C3 Stk39 serine/threonine kinase 39
Rat - 553 3 q21 Stk39 serine threonine kinase 39
Previous and Unofficial Names
DCHT | pancreatic serine/threonine-protein kinase | PSTK1 | SPAK | serine threonine kinase 39
Database Links
BRENDA
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
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: 2-3

Key to terms and symbols Click column headers to sort
Target used in screen: STK39
Ligand Sp. Type Action Affinity Units
staurosporine Hs Inhibitor Inhibition 6.9 pKd
sunitinib Hs Inhibitor Inhibition 6.8 pKd
NVP-TAE684 Hs Inhibitor Inhibition 6.8 pKd
SU-14813 Hs Inhibitor Inhibition 6.4 pKd
dovitinib Hs Inhibitor Inhibition 6.3 pKd
KW-2449 Hs Inhibitor Inhibition 6.1 pKd
lestaurtinib Hs Inhibitor Inhibition 6.0 pKd
AST-487 Hs Inhibitor Inhibition 5.8 pKd
fedratinib Hs Inhibitor Inhibition 5.8 pKd
ruxolitinib 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
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 Hs Inhibitor Inhibition 8.0
Flt-3 inhibitor III Hs Inhibitor Inhibition 75.4
aloisine A Hs Inhibitor Inhibition 76.1
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 76.5
dorsomorphin Hs Inhibitor Inhibition 76.8
ATM/ATR kinase inhibitor Hs Inhibitor Inhibition 77.0
alsterpaullone Hs Inhibitor Inhibition 77.5
aloisine Hs Inhibitor Inhibition 77.8
LY 294002 Hs Inhibitor Inhibition 78.4
Tpl2 kinase inhibitor Hs Inhibitor Inhibition 78.6
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. 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 29/01/2016. Accessed on 17/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2224.