serum/glucocorticoid regulated kinase family member 3 | SGK family | IUPHAR/BPS Guide to PHARMACOLOGY

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serum/glucocorticoid regulated kinase family member 3

Target not currently curated in GtoImmuPdb

Target id: 1536

Nomenclature: serum/glucocorticoid regulated kinase family member 3

Abbreviated Name: SGK3

Family: SGK family

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 - 496 8q12 SGK3 serum/glucocorticoid regulated kinase family member 3
Mouse - 496 1 Sgk3 serum/glucocorticoid regulated kinase 3
Rat - 502 5 Sgk3 serum/glucocorticoid regulated kinase family, member 3
Previous and Unofficial Names
SGK2 | SGKL | cytokine-independent survival kinase | serine/threonine protein kinase CISK | serine/threonine-protein kinase Sgk3 | fy | serum/glucocorticoid regulated kinase family
Database Links
BRENDA
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of CISK-PX domain.
PDB Id:  1XTE
Resolution:  1.6Å
Species:  Mouse
References:  6
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of CISK-PX domain with sulfates.
PDB Id:  1XTE
Resolution:  1.6Å
Species:  Mouse
References:  6
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 14n [PMID: 25589934] Hs Inhibition 5.5 pIC50 4
pIC50 5.5 (IC50 3.1x10-6 M) [4]
Description: at high (500μM) ATP concentration
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: 2,5

Key to terms and symbols Click column headers to sort
Target used in screen: SGK3
Ligand Sp. Type Action Value Parameter
staurosporine Hs Inhibitor Inhibition 8.5 pKd
lestaurtinib Hs Inhibitor Inhibition 8.2 pKd
KW-2449 Hs Inhibitor Inhibition 7.0 pKd
AST-487 Hs Inhibitor Inhibition 6.8 pKd
sunitinib Hs Inhibitor Inhibition 6.7 pKd
SU-14813 Hs Inhibitor Inhibition 6.6 pKd
dovitinib Hs Inhibitor Inhibition 6.0 pKd
ruboxistaurin Hs Inhibitor Inhibition 5.8 pKd
midostaurin Hs Inhibitor Inhibition 5.8 pKd
linifanib 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: SGK3/SGK3
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Hs Inhibitor Inhibition 23.5 41.0 6.5
K-252a Hs Inhibitor Inhibition 53.1 47.0 13.0
JAK3 inhibitor VI Hs Inhibitor Inhibition 63.6 58.0 13.0
SB 218078 Hs Inhibitor Inhibition 71.7 98.0 80.0
GF109203X Hs Inhibitor Inhibition 72.8 101.0 65.0
H-89 Hs Inhibitor Inhibition 78.8 93.0 43.0
PKR inhibitor Hs Inhibitor Inhibition 81.2 73.0 21.0
casein kinase II inhibitor III Hs Inhibitor Inhibition 85.7 114.0 84.0
ATM/ATR kinase inhibitor Hs Inhibitor Inhibition 85.8 110.0 77.0
VEGF receptor 2 kinase inhibitor I Hs Inhibitor Inhibition 88.1 93.0 102.0
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. Halland N, Schmidt F, Weiss T, Saas J, Li Z, Czech J, Dreyer M, Hofmeister A, Mertsch K, Dietz U et al.. (2015) Discovery of N-[4-(1H-Pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides as Highly Active and Selective SGK1 Inhibitors. ACS Med Chem Lett, 6 (1): 73-8. [PMID:25589934]

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]

6. Xing Y, Liu D, Zhang R, Joachimiak A, Songyang Z, Xu W. (2004) Structural basis of membrane targeting by the Phox homology domain of cytokine-independent survival kinase (CISK-PX). J. Biol. Chem., 279 (29): 30662-9. [PMID:15126499]

How to cite this page

SGK family: serum/glucocorticoid regulated kinase family member 3. Last modified on 19/01/2017. Accessed on 25/01/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1536.