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	2.7.11.1
ChEMBL Target	CHEMBL3125 (Hs)
Ensembl Gene	ENSG00000162302 (Hs), ENSMUSG00000024952 (Mm), ENSRNOG00000021117 (Rn)
Entrez Gene	8986 (Hs), 56613 (Mm), 361715 (Rn)
Human Protein Atlas	ENSG00000162302 (Hs)
KEGG Enzyme	2.7.11.1
KEGG Gene	hsa:8986 (Hs), mmu:56613 (Mm), rno:361715 (Rn)
OMIM	603606 (Hs)
Pharos	O75676 (Hs)
RefSeq Nucleotide	NM_001006944 (Hs), NM_019924 (Mm), NM_001108517 (Rn)
RefSeq Protein	NP_001006945 (Hs), NP_064308 (Mm), NP_001101987 (Rn)
UniProtKB	O75676 (Hs), Q9Z2B9 (Mm)
Wikipedia	RPS6KA4 (Hs)

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 Value 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 Value 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 Value 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 »

Immuno Process Associations

Immuno Process:  Cytokine production & signalling GO Annotations:  Associated to 2 GO processes GO:0001818 negative regulation of cytokine production TAS GO:0070498 interleukin-1-mediated signaling pathway IMP

Immuno Process:  Inflammation GO Annotations:  Associated to 1 GO processes, IEA only click arrow to show/hide IEA associations GO:0006954 inflammatory response IEA