sugen kinase 110 | NKF1 family | IUPHAR/BPS Guide to PHARMACOLOGY

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sugen kinase 110

Target not currently curated in GtoImmuPdb

Target id: 2290

Nomenclature: sugen kinase 110

Abbreviated Name: SGK110

Family: NKF1 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 - 359 19q13.42 SGK110 sugen kinase 110
Mouse - 362 7 A1 Sbk3 SH3 domain binding kinase family, member 3
Previous and Unofficial Names
SG110 | Gm1078 | predicted gene 1078 | SH3 domain binding kinase family, member 3 | SH3 domain binding kinase family
Database Links
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
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 Value Parameter Reference
compound R-16 [PMID: 21967808] Hs Inhibition - - 2
[2]
Description: Measured as % inhibition using 1μM compound.
Inhibitor Comments
SGK110 activity is inhibited by 98% in the presence of 1μM compound R-16 [PMID 21967808] [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: 1,3

Key to terms and symbols Click column headers to sort
Target used in screen: SgK110
Ligand Sp. Type Action Value Parameter
staurosporine Hs Inhibitor Inhibition 7.6 pKd
NVP-TAE684 Hs Inhibitor Inhibition 7.3 pKd
lestaurtinib Hs Inhibitor Inhibition 6.9 pKd
tamatinib Hs Inhibitor Inhibition 6.7 pKd
KW-2449 Hs Inhibitor Inhibition 6.6 pKd
crizotinib Hs Inhibitor Inhibition 6.6 pKd
tozasertib Hs Inhibitor Inhibition 6.3 pKd
PD-173955 Hs Inhibitor Inhibition 6.0 pKd
JNJ-28312141 Hs Inhibitor Inhibition 6.0 pKd
sunitinib Hs Inhibitor Inhibition 5.7 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »

References

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1. 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]

2. Milkiewicz KL, Aimone LD, Albom MS, Angeles TS, Chang H, Grobelny JV, Husten J, Losardo C, Miknyoczki S, Murthy S et al.. (2011) Improvement in oral bioavailability of 2,4-diaminopyrimidine c-Met inhibitors by incorporation of a 3-amidobenzazepin-2-one group. Bioorg. Med. Chem., 19 (21): 6274-84. [PMID:21967808]

3. 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

NKF1 family: sugen kinase 110. Last modified on 24/02/2015. Accessed on 17/07/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2290.