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unc-51 like kinase 3

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Target id: 2273

Nomenclature: unc-51 like kinase 3

Abbreviated Name: ULK3

Family: Unc-51-like kinase (ULK) family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 472 15q24.1 ULK3 unc-51 like kinase 3
Mouse - 472 9 B Ulk3 unc-51-like kinase 3
Rat - 472 8q24 Ulk3 unc-51 like kinase 3
Database Links Click here for help
Alphafold Q6PHR2 (Hs), Q3U3Q1 (Mm), D3ZHP7 (Rn)
BRENDA 2.7.11.1
ChEMBL Target CHEMBL5047 (Hs), CHEMBL3832 (Mm)
Ensembl Gene ENSG00000140474 (Hs), ENSMUSG00000032308 (Mm), ENSRNOG00000038459 (Rn)
Entrez Gene 25989 (Hs), 71742 (Mm), 691171 (Rn)
Human Protein Atlas ENSG00000140474 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:25989 (Hs), mmu:71742 (Mm), rno:691171 (Rn)
OMIM 613472 (Hs)
Pharos Q6PHR2 (Hs)
RefSeq Nucleotide NM_015518 (Hs), NM_027895 (Mm), NM_001271135 (Rn)
RefSeq Protein NP_001092906 (Hs), NP_082171 (Mm), NP_001258064 (Rn)
UniProtKB Q6PHR2 (Hs), Q3U3Q1 (Mm), D3ZHP7 (Rn)
Wikipedia ULK3 (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
compound 15 [PMID: 24900237] Small molecule or natural product Click here for species-specific activity table Hs Inhibition - - 4
⤷ [4]
Description: Measured as % inhibition using 1μM compound.
Inhibitor Comments
ULK3 activity is inhibited by 94% in the presence of 1µM compound 15 [PMID 24900237] [4].
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: ULK3
Ligand Sp. Type Action Value Parameter
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.9 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.3 pKd
tamatinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.1 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.0 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 7.4 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.4 pKd
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 7.2 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 6.9 pKd
dovitinib Small molecule or natural product Hs Inhibitor Inhibition 6.8 pKd
fedratinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.5 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: ULK3/ULK3
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 1.8 -1.0 0.5
K-252a Small molecule or natural product Hs Inhibitor Inhibition 3.2 0.0 1.0
Syk inhibitor Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 15.8 19.0 4.0
SU11652 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 21.6 17.0 2.0
SU6656 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 26.3 11.0 6.0
SB 218078 Small molecule or natural product Hs Inhibitor Inhibition 33.0 58.0 58.0
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 37.0 17.0 5.0
JAK3 inhibitor VI Small molecule or natural product Hs Inhibitor Inhibition 41.7 37.0 7.0
SU11274 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 55.3 30.0 6.0
VEGF receptor 2 kinase inhibitor II Small molecule or natural product Hs Inhibitor Inhibition 55.5 52.0 55.0
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. Ott GR, Tripathy R, Cheng M, McHugh R, Anzalone AV, Underiner TL, Curry MA, Quail MR, Lu L, Wan W et al.. (2010) Discovery of a potent inhibitor of anaplastic lymphoma kinase with in vivo antitumor activity. ACS Med Chem Lett, 1 (9): 493-8. [PMID:24900237]

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]

How to cite this page

Unc-51-like kinase (ULK) family: unc-51 like kinase 3. Last modified on 25/02/2015. Accessed on 25/10/2025. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2273.