NUAK family, SNF1-like kinase, 2 | NuaK subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

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NUAK family, SNF1-like kinase, 2

Target not currently curated in GtoImmuPdb

Target id: 2130

Nomenclature: NUAK family, SNF1-like kinase, 2

Abbreviated Name: NuaK2

Family: NuaK 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 - 628 1q32.1 NUAK2 NUAK family kinase 2
Mouse - 639 1 E4 Nuak2 NUAK family, SNF1-like kinase, 2
Rat - 630 13 q13 Nuak2 NUAK family kinase 2
Previous and Unofficial Names
Omphalocele kinase 2 | OMPHK2 | SNARK | SNF1/AMP activated protein kinase | SNF1/AMP kinase-related kinase | UV126 | NUAK family
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 Value Parameter Reference
WZ4003 Hs Inhibition 7.0 pIC50 2
pIC50 7.0 (IC50 1x10-7 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: 3-4

Key to terms and symbols Click column headers to sort
Target used in screen: SNARK
Ligand Sp. Type Action Value Parameter
staurosporine Hs Inhibitor Inhibition 10.1 pKd
lestaurtinib Hs Inhibitor Inhibition 9.0 pKd
NVP-TAE684 Hs Inhibitor Inhibition 8.9 pKd
GSK-461364A Hs Inhibitor Inhibition 7.6 pKd
fedratinib Hs Inhibitor Inhibition 7.3 pKd
KW-2449 Hs Inhibitor Inhibition 7.3 pKd
midostaurin Hs Inhibitor Inhibition 7.2 pKd
tamatinib Hs Inhibitor Inhibition 7.2 pKd
GSK690693 Hs Inhibitor Inhibition 7.1 pKd
crizotinib Hs Inhibitor Inhibition 6.9 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

Key to terms and symbols Click column headers to sort
Target used in screen: nd/SNARK(NUAK2)
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 9.7
K-252a Hs Inhibitor Inhibition 14.5
staurosporine Hs Inhibitor Inhibition 20.4
Cdk2 inhibitor IV Hs Inhibitor Inhibition 23.1
midostaurin Hs Inhibitor Inhibition 26.2
JNJ-7706621 Hs Inhibitor Inhibition 34.0
Gö 6976 Hs Inhibitor Inhibition 40.5
PKR inhibitor Hs Inhibitor Inhibition 41.2
JAK3 inhibitor VI Hs Inhibitor Inhibition 43.7
SB 218078 Hs Inhibitor Inhibition 52.0
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. Banerjee S, Buhrlage SJ, Huang HT, Deng X, Zhou W, Wang J, Traynor R, Prescott AR, Alessi DR, Gray NS. (2014) Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases. Biochem. J., 457 (1): 215-25. [PMID:24171924]

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. 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

NuaK subfamily: NUAK family, SNF1-like kinase, 2. Last modified on 30/03/2016. Accessed on 14/10/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2130.