ribosomal protein S6 kinase A4 | MSK subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

Top ▲

ribosomal protein S6 kinase A4

Target not currently curated in GtoImmuPdb

Target id: 1524

Nomenclature: ribosomal protein S6 kinase A4

Abbreviated Name: MSK2

Family: MSK subfamily

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 766 11q11-q13 RPS6KA4 ribosomal protein S6 kinase A4
Mouse - 773 19 Rps6ka4 ribosomal protein S6 kinase
Rat - 773 1q43 Rps6ka4 ribosomal protein S6 kinase A4
Previous and Unofficial Names
nuclear mitogen- and stress-activated protein kinase 2 | Ribosomal protein S6 kinase α4 | Ccdc88b | coiled-coil domain containing 88B | ribosomal protein S6 kinase alpha-4 | ribosomal protein S6 kinase, polypeptide 4 | ribosomal protein kinase B | RSK-B | ribosomal protein S6 kinase, 90kDa, polypeptide 4 | ribosomal protein S6 kinase
Database Links
BRENDA
ChEMBL Target
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

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 Parameter Reference
compound 8 [PMID: 17480064] Hs Inhibition 5.5 pIC50 2
pIC50 5.5 (IC50 3.01x10-6 M) [2]
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: 3,5

Key to terms and symbols Click column headers to sort
Target used in screen: RPS6KA4(Kin.Dom.1-N-terminal)
Ligand Sp. Type Action Affinity Parameter
lestaurtinib Hs Inhibitor Inhibition 7.2 pKd
sunitinib Hs Inhibitor Inhibition 7.0 pKd
staurosporine Hs Inhibitor Inhibition 6.9 pKd
SU-14813 Hs Inhibitor Inhibition 6.7 pKd
midostaurin Hs Inhibitor Inhibition 6.6 pKd
dovitinib Hs Inhibitor Inhibition 6.2 pKd
alvocidib Hs Inhibitor Inhibition 5.9 pKd
AST-487 Hs Inhibitor Inhibition 5.7 pKd
KW-2449 Hs Inhibitor Inhibition 5.7 pKd
NVP-TAE684 Hs Inhibitor Inhibition 5.6 pKd
Target used in screen: RPS6KA4(Kin.Dom.2-C-terminal)
Ligand Sp. Type Action Affinity Parameter
BI-2536 Hs Inhibitor Inhibition 7.9 pKd
tamatinib Hs Inhibitor Inhibition 7.4 pKd
GSK690693 Hs Inhibitor Inhibition 7.3 pKd
PP-242 Hs Inhibitor Inhibition 7.2 pKd
fedratinib Hs Inhibitor Inhibition 6.8 pKd
ruxolitinib Hs Inhibitor Inhibition 6.5 pKd
GSK-461364A Hs Inhibitor Inhibition 6.1 pKd
KW-2449 Hs Inhibitor Inhibition 6.0 pKd
gefitinib Hs Inhibitor Inhibition 5.9 pKd
lestaurtinib Hs Inhibitor Inhibition 5.9 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: 1,4

Key to terms and symbols Click column headers to sort
Target used in screen: MSK2/MSK2(RPS6KA4)
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
K-252a Hs Inhibitor Inhibition 2.5 -1.0 0.0
staurosporine Hs Inhibitor Inhibition 6.7 0.5 -0.5
SB 218078 Hs Inhibitor Inhibition 12.4 56.0 64.0
midostaurin Hs Inhibitor Inhibition 16.8 12.0 8.0
indirubin derivative E804 Hs Inhibitor Inhibition 21.7 15.0 2.0
PKR inhibitor Hs Inhibitor Inhibition 28.0 20.0 6.0
Gö 6976 Hs Inhibitor Inhibition 29.9 2.0 5.0
Ro-32-0432 Hs Inhibitor Inhibition 33.3
GF109203X Hs Inhibitor Inhibition 34.9 18.0 3.0
H-89 Hs Inhibitor Inhibition 38.8 9.0 2.0
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. Anderson DR, Meyers MJ, Vernier WF, Mahoney MW, Kurumbail RG, Caspers N, Poda GI, Schindler JF, Reitz DB, Mourey RJ. (2007) Pyrrolopyridine inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2). J. Med. Chem., 50 (11): 2647-54. [PMID:17480064]

3. 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]

4. 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]

5. 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

MSK subfamily: ribosomal protein S6 kinase A4. Last modified on 30/03/2016. Accessed on 23/04/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1524.