Top ▲

serine/threonine kinase 24

Click here for help

Target id: 2217

Nomenclature: serine/threonine kinase 24

Abbreviated Name: MST3

Family: YSK subfamily

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 443 13q32.2 STK24 serine/threonine kinase 24
Mouse - 431 14 64.95 cM Stk24 serine/threonine kinase 24
Rat - 431 15q24 Stk24 serine/threonine kinase 24
Previous and Unofficial Names Click here for help
mammalian STE20-like protein kinase 3 | MST3B | STK3
Database Links Click here for help
Alphafold Q9Y6E0 (Hs), Q99KH8 (Mm), B0LT89 (Rn)
BRENDA 2.7.11.1
ChEMBL Target CHEMBL5082 (Hs)
Ensembl Gene ENSG00000102572 (Hs), ENSMUSG00000063410 (Mm), ENSRNOG00000011511 (Rn)
Entrez Gene 8428 (Hs), 223255 (Mm), 361092 (Rn)
Human Protein Atlas ENSG00000102572 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:8428 (Hs), mmu:223255 (Mm), rno:361092 (Rn)
OMIM 604984 (Hs)
Pharos Q9Y6E0 (Hs)
RefSeq Nucleotide NM_001032296 (Hs), NM_145465 (Mm), NM_001127494 (Rn)
RefSeq Protein NP_001027467 (Hs), NP_663440 (Mm), NP_001120966 (Rn)
SynPHARM 81653 (in complex with bosutinib)
UniProtKB Q9Y6E0 (Hs), Q99KH8 (Mm), B0LT89 (Rn)
Wikipedia STK24 (Hs)
Selected 3D Structures Click here for help
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
Image of receptor 3D structure from RCSB PDB
Description:  Human MST3 kinase.
PDB Id:  3A7F
Resolution:  1.55Å
Species:  Human
References:  4
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
bosutinib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 8.4 pIC50 5
⤷ pIC50 8.4 (IC50 3.9x10-9 M) [5]
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: 2,6
Key to terms and symbols Click column headers to sort
Target used in screen: MST3
Ligand Sp. Type Action Value Parameter
neratinib Small molecule or natural product Approved drug Hs Inhibitor Inhibition 8.2 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.2 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 7.0 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.9 pKd
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.4 pKd
dovitinib Small molecule or natural product Hs Inhibitor Inhibition 6.4 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.1 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 6.0 pKd
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 5.9 pKd
JNJ-28312141 Small molecule or natural product 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: 1,3
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 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 1.6 0.5 1.0
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 2.9 0.0 1.0
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 11.0
PKR inhibitor Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 11.6 3.0 0.0
SB 218078 Small molecule or natural product Hs Inhibitor Inhibition 14.3 80.0 65.0
SU11652 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 22.2 8.0 1.0
JAK3 inhibitor VI Small molecule or natural product Hs Inhibitor Inhibition 23.5 12.0 1.0
K-252a Small molecule or natural product Hs Inhibitor Inhibition 25.8 14.0 0.0
Gö 6983 Small molecule or natural product Hs Inhibitor Inhibition 36.6 21.0 5.0
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 39.1 17.0 7.0
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. 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 18/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2217.