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NUAK family kinase 1

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Target not currently curated in GtoImmuPdb

Target id: 2129

Nomenclature: NUAK family kinase 1

Abbreviated Name: NuaK1

Family: NuaK subfamily

Contents:

Gene and Protein Information Click here for help
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 Click here for help
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 Click here for help
Alphafold O60285 (Hs), Q641K5 (Mm)
BRENDA 2.7.11.1
ChEMBL Target CHEMBL5784 (Hs)
Ensembl Gene ENSG00000074590 (Hs), ENSMUSG00000020032 (Mm), ENSRNOG00000008061 (Rn)
Entrez Gene 9891 (Hs), 77976 (Mm), 299694 (Rn)
Human Protein Atlas ENSG00000074590 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:9891 (Hs), mmu:77976 (Mm), rno:299694 (Rn)
OMIM 608130 (Hs)
Pharos O60285 (Hs)
RefSeq Nucleotide NM_014840 (Hs), NM_001004363 (Mm), NM_001106774 (Rn)
RefSeq Protein NP_055655 (Hs), NP_001004363 (Mm), NP_001100244 (Rn)
UniProtKB O60285 (Hs), Q641K5 (Mm)
Wikipedia NUAK1 (Hs)
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
WZ4002 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.0 pKd 10
⤷ pKd 7.0 (Kd 9.1x10-8 M) [10]
cerdulatinib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 8.4 pIC50 3
⤷ pIC50 8.4 (IC50 4x10-9 M) [3]
narazaciclib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.3 pIC50 7
⤷ pIC50 8.3 (IC50 4.95x10-9 M) [7]
HTH-02-006 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.1 pIC50 9
⤷ pIC50 8.1 (IC50 8x10-9 M) [9]
Description: Determined in a radioactive (33P-ATP) filter-binding assay.
WZ4003 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 7.7 pIC50 2
⤷ pIC50 7.7 (IC50 2x10-8 M) [2]
compound 25b [PMID: 22564207] Small molecule or natural product Click here for species-specific activity table 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 Small molecule or natural product Primary target of this compound Hs Inhibition 7.0 pIC50 2
⤷ pIC50 7.0 (IC50 1x10-7 M) [2]
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: 4,8
Key to terms and symbols Click column headers to sort
Target used in screen: ARK5
Ligand Sp. Type Action Value Parameter
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.4 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.4 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.9 pKd
fedratinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.5 pKd
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.4 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.3 pKd
tamatinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.1 pKd
tozasertib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.7 pKd
dovitinib Small molecule or natural product Hs Inhibitor Inhibition 6.6 pKd
GSK690693 Small molecule or natural product Ligand has a PDB structure 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 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: 1,5
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 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 0.8 6.0 5.0
K-252a Small molecule or natural product Hs Inhibitor Inhibition 1.0 1.0 1.0
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 1.6 4.0 0.5
SB 218078 Small molecule or natural product Hs Inhibitor Inhibition 2.1 39.0 48.0
SU11652 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 2.1 6.0 6.0
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 2.1 1.0 0.0
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 2.7 7.0 7.0
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 2.7
indirubin derivative E804 Small molecule or natural product Hs Inhibitor Inhibition 2.8 2.0 5.0
JAK inhibitor I Small molecule or natural product Ligand has a PDB structure 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. Reddy MV, Akula B, Cosenza SC, Athuluridivakar S, Mallireddigari MR, Pallela VR, Billa VK, Subbaiah DR, Bharathi EV, Vasquez-Del Carpio R et al.. (2014) Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5). J Med Chem, 57 (3): 578-99. [PMID:24417566]

8. 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]

9. Yuan WC, Pepe-Mooney B, Galli GG, Dill MT, Huang HT, Hao M, Wang Y, Liang H, Calogero RA, Camargo FD. (2018) NUAK2 is a critical YAP target in liver cancer. Nat Commun, 9 (1): 4834. [PMID:30446657]

10. 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 03/02/2022. Accessed on 20/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2129.