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serum/glucocorticoid regulated kinase family member 3

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Target not currently curated in GtoImmuPdb

Target id: 1536

Nomenclature: serum/glucocorticoid regulated kinase family member 3

Abbreviated Name: SGK3

Family: SGK family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 496 8q13.1 SGK3 serum/glucocorticoid regulated kinase family member 3
Mouse - 496 1 2.08 cM Sgk3 serum/glucocorticoid regulated kinase 3
Rat - 496 5 Sgk3 serum/glucocorticoid regulated kinase family, member 3
Previous and Unofficial Names Click here for help
SGK2 | SGKL | cytokine-independent survival kinase | serine/threonine protein kinase CISK | serine/threonine-protein kinase Sgk3 | fy | serum/glucocorticoid regulated kinase family
Database Links Click here for help
Alphafold Q96BR1 (Hs), Q9ERE3 (Mm), Q8R4V0 (Rn)
BRENDA 2.7.11.1
CATH/Gene3D 3.30.1520.10
ChEMBL Target CHEMBL6186 (Hs)
Ensembl Gene ENSG00000104205 (Hs), ENSMUSG00000025915 (Mm), ENSRNOG00000049052 (Rn)
Entrez Gene 23678 (Hs), 170755 (Mm)
Human Protein Atlas ENSG00000104205 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:23678 (Hs), mmu:170755 (Mm)
OMIM 607591 (Hs)
Pharos Q96BR1 (Hs)
RefSeq Nucleotide NM_001033578 (Hs), NM_001037759 (Mm), XM_003749885 (Rn)
RefSeq Protein NP_001028750 (Hs), NP_001032848 (Mm), NP_573483 (Mm), NP_808215 (Mm), XP_003749933 (Rn)
UniProtKB Q96BR1 (Hs), Q9ERE3 (Mm), Q8R4V0 (Rn)
Wikipedia SGK3 (Hs)
Selected 3D Structures Click here for help
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 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
Sanofi-14h Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 8.4 pIC50
⤷ pIC50 8.4 (IC50 4x10-9 M)
compound 14n [PMID: 25589934] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 5.5 pIC50 4
⤷ pIC50 5.5 (IC50 3.1x10-6 M) [4]
Description: at high (500μM) ATP concentration
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: 2,5
Key to terms and symbols Click column headers to sort
Target used in screen: SGK3
Ligand Sp. Type Action Value Parameter
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.5 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.2 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 7.0 pKd
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 6.8 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.7 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 6.6 pKd
dovitinib Small molecule or natural product Hs Inhibitor Inhibition 6.0 pKd
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 5.8 pKd
ruboxistaurin Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.8 pKd
linifanib 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: SGK3/SGK3
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 23.5 41.0 6.5
K-252a Small molecule or natural product Hs Inhibitor Inhibition 53.1 47.0 13.0
JAK3 inhibitor VI Small molecule or natural product Hs Inhibitor Inhibition 63.6 58.0 13.0
SB 218078 Small molecule or natural product Hs Inhibitor Inhibition 71.7 98.0 80.0
GF109203X Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 72.8 101.0 65.0
H-89 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 78.8 93.0 43.0
PKR inhibitor Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 81.2 73.0 21.0
casein kinase II inhibitor III Small molecule or natural product Hs Inhibitor Inhibition 85.7 114.0 84.0
ATM/ATR kinase inhibitor Small molecule or natural product Hs Inhibitor Inhibition 85.8 110.0 77.0
VEGF receptor 2 kinase inhibitor I Small molecule or natural product 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 04/01/2024. Accessed on 16/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=1536.