unc-51 like kinase 3 | Unc-51-like kinase (ULK) family | IUPHAR/BPS Guide to PHARMACOLOGY

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unc-51 like kinase 3

Target not currently curated in GtoImmuPdb

Target id: 2273

Nomenclature: unc-51 like kinase 3

Abbreviated Name: ULK3

Family: Unc-51-like kinase (ULK) 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 - 472 15q24.1 ULK3 unc-51 like kinase 3
Mouse - 472 9 C Ulk3 unc-51-like kinase 3
Rat - 472 8q24 Ulk3 unc-51 like kinase 3
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
compound 15 [PMID: 24900237] 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
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 Hs Inhibitor Inhibition 8.9 pKd
lestaurtinib Hs Inhibitor Inhibition 8.3 pKd
tamatinib Hs Inhibitor Inhibition 8.1 pKd
NVP-TAE684 Hs Inhibitor Inhibition 8.0 pKd
SU-14813 Hs Inhibitor Inhibition 7.4 pKd
sunitinib Hs Inhibitor Inhibition 7.4 pKd
AST-487 Hs Inhibitor Inhibition 7.2 pKd
KW-2449 Hs Inhibitor Inhibition 6.9 pKd
dovitinib Hs Inhibitor Inhibition 6.8 pKd
fedratinib 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
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 Hs Inhibitor Inhibition 1.8 -1.0 0.5
K-252a Hs Inhibitor Inhibition 3.2 0.0 1.0
Syk inhibitor Hs Inhibitor Inhibition 15.8 19.0 4.0
SU11652 Hs Inhibitor Inhibition 21.6 17.0 2.0
SU6656 Hs Inhibitor Inhibition 26.3 11.0 6.0
SB 218078 Hs Inhibitor Inhibition 33.0 58.0 58.0
midostaurin Hs Inhibitor Inhibition 37.0 17.0 5.0
JAK3 inhibitor VI Hs Inhibitor Inhibition 41.7 37.0 7.0
SU11274 Hs Inhibitor Inhibition 55.3 30.0 6.0
VEGF receptor 2 kinase inhibitor II 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 08/12/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2273.