serine/threonine kinase 24 | YSK subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

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serine/threonine kinase 24

Target id: 2217

Nomenclature: serine/threonine kinase 24

Abbreviated Name: MST3

Family: YSK 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 24 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 431 13q31.2-q32.3 STK24 serine/threonine kinase 24
Mouse - 431 14 E5 Stk24 serine/threonine kinase 24
Rat - 431 15 q25 Stk24 serine/threonine kinase 24
Previous and Unofficial Names
mammalian STE20-like protein kinase 3 | MST3B | STK3
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 MST3 kinase.
PDB Id:  3A7F
Resolution:  1.55Å
Species:  Human
References:  4
Image of receptor 3D structure from RCSB PDB
Description:  Human MST3 kinase in complex with adenine.
PDB Id:  3A7I
Ligand:  adenine
Resolution:  1.45Å
Species:  Human
References:  4
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 Inhibition 8.4 pIC50 5
pIC50 8.4 (IC50 3.9x10-9 M) [5]
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: MST3
Ligand Sp. Type Action Affinity Units
neratinib Hs Inhibitor Inhibition 8.2 pKd
sunitinib Hs Inhibitor Inhibition 7.2 pKd
SU-14813 Hs Inhibitor Inhibition 7.0 pKd
staurosporine Hs Inhibitor Inhibition 6.9 pKd
bosutinib Hs Inhibitor Inhibition 6.4 pKd
dovitinib Hs Inhibitor Inhibition 6.4 pKd
lestaurtinib Hs Inhibitor Inhibition 6.1 pKd
KW-2449 Hs Inhibitor Inhibition 6.0 pKd
AST-487 Hs Inhibitor Inhibition 5.9 pKd
JNJ-28312141 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: 1,3

Key to terms and symbols Click column headers to sort
Target used in screen: MST3/MST3(STK24)
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Hs Inhibitor Inhibition 1.6 0.5 1.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 2.9 0.0 1.0
bosutinib Hs Inhibitor Inhibition 11.0
PKR inhibitor Hs Inhibitor Inhibition 11.6 3.0 0.0
SB 218078 Hs Inhibitor Inhibition 14.3 80.0 65.0
SU11652 Hs Inhibitor Inhibition 22.2 8.0 1.0
JAK3 inhibitor VI Hs Inhibitor Inhibition 23.5 12.0 1.0
K-252a Hs Inhibitor Inhibition 25.8 14.0 0.0
Gö 6983 Hs Inhibitor Inhibition 36.6 21.0 5.0
midostaurin Hs Inhibitor Inhibition 39.1 17.0 7.0
Displaying the top 10 most potent ligands  View all ligands in screen »

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. Ko TP, Jeng WY, Liu CI, Lai MD, Wu CL, Chang WJ, Shr HL, Lu TJ, Wang AH. (2010) Structures of human MST3 kinase in complex with adenine, ADP and Mn2+. Acta Crystallogr. D Biol. Crystallogr., 66 (Pt 2): 145-54. [PMID:20124694]

5. 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]

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

YSK subfamily: serine/threonine kinase 24. Last modified on 13/02/2017. Accessed on 21/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2217.