NUAK family kinase 1 | NuaK subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

NUAK family kinase 1

Target id: 2129

Nomenclature: NUAK family kinase 1

Abbreviated Name: NuaK1

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

   GtoImmuPdb view: OFF :     Currently no data for NUAK family kinase 1 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 661 12q23.3 NUAK1 NUAK family kinase 1
Mouse - 658 10 C1 Nuak1 NUAK family, SNF1-like kinase, 1
Rat - 661 7 q13 Nuak1 NUAK family kinase 1
Previous and Unofficial Names
AMP-activated protein kinase family member 5 | AMPK-related protein kinase 5 | ARK5 | Omphalocele kinase 1 | OMPHK1 | NUAK family, SNF1-like kinase, 1 | NUAK family
Database Links
BRENDA
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 Affinity Units Reference
WZ4002 Hs Inhibition 7.0 pKd 8
pKd 7.0 (Kd 9.1x10-8 M) [8]
cerdulatinib Hs Inhibition 8.4 pIC50 3
pIC50 8.4 (IC50 4x10-9 M) [3]
WZ4003 Hs Inhibition 7.7 pIC50 2
pIC50 7.7 (IC50 2x10-8 M) [2]
compound 25b [PMID: 22564207] Hs Inhibition 7.6 pIC50 6
pIC50 7.6 (IC50 2.6x10-8 M) [6]
Description: NuaK1 is reported by its synonym ARK5 in the referencing article.
HTH-01-015 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: 4,7

Key to terms and symbols Click column headers to sort
Target used in screen: ARK5
Ligand Sp. Type Action Affinity Units
lestaurtinib Hs Inhibitor Inhibition 8.4 pKd
staurosporine Hs Inhibitor Inhibition 8.4 pKd
NVP-TAE684 Hs Inhibitor Inhibition 7.9 pKd
fedratinib Hs Inhibitor Inhibition 7.5 pKd
midostaurin Hs Inhibitor Inhibition 7.4 pKd
sunitinib Hs Inhibitor Inhibition 7.3 pKd
tamatinib Hs Inhibitor Inhibition 7.1 pKd
tozasertib Hs Inhibitor Inhibition 6.7 pKd
dovitinib Hs Inhibitor Inhibition 6.6 pKd
GSK690693 Hs Inhibitor Inhibition 6.4 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: 1,5

Key to terms and symbols Click column headers to sort
Target used in screen: ARK5/ARK5(NUAK1)
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
PKR inhibitor Hs Inhibitor Inhibition 0.8 6.0 5.0
K-252a Hs Inhibitor Inhibition 1.0 1.0 1.0
staurosporine Hs Inhibitor Inhibition 1.6 4.0 0.5
SB 218078 Hs Inhibitor Inhibition 2.1 39.0 48.0
SU11652 Hs Inhibitor Inhibition 2.1 6.0 6.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 2.1 1.0 0.0
midostaurin Hs Inhibitor Inhibition 2.7 7.0 7.0
sunitinib Hs Inhibitor Inhibition 2.7
indirubin derivative E804 Hs Inhibitor Inhibition 2.8 2.0 5.0
JAK inhibitor I Hs Inhibitor Inhibition 3.0 8.0 9.0
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. Coffey G, Betz A, DeGuzman F, Pak Y, Inagaki M, Baker DC, Hollenbach SJ, Pandey A, Sinha U. (2014) The novel kinase inhibitor PRT062070 (Cerdulatinib) demonstrates efficacy in models of autoimmunity and B-cell cancer. J. Pharmacol. Exp. Ther., 351 (3): 538-48. [PMID:25253883]

4. 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]

5. 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]

6. Gingrich DE, Lisko JG, Curry MA, Cheng M, Quail M, Lu L, Wan W, Albom MS, Angeles TS, Aimone LD et al.. (2012) Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase. J. Med. Chem., 55 (10): 4580-93. [PMID:22564207]

7. 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]

8. Zhou W, Ercan D, Chen L, Yun CH, Li D, Capelletti M, Cortot AB, Chirieac L, Iacob RE, Padera R et al.. (2009) Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. Nature, 462 (7276): 1070-4. [PMID:20033049]

How to cite this page

NuaK subfamily: NUAK family kinase 1. Last modified on 12/05/2016. Accessed on 17/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2129.