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unc-51 like autophagy activating kinase 2

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Target id: 2272

Nomenclature: unc-51 like autophagy activating kinase 2

Abbreviated Name: ULK2

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 - 1036 17p11.2 ULK2 unc-51 like autophagy activating kinase 2
Mouse - 1037 11 B2 Ulk2 unc-51 like kinase 2
Rat - 1037 10q23 Ulk2 unc-51 like autophagy activating kinase 2
Previous and Unofficial Names Click here for help
ATG1B
Database Links Click here for help
Alphafold Q8IYT8 (Hs), Q9QY01 (Mm)
BRENDA 2.7.11.1
ChEMBL Target CHEMBL5435 (Hs)
Ensembl Gene ENSG00000083290 (Hs), ENSMUSG00000004798 (Mm), ENSRNOG00000002763 (Rn)
Entrez Gene 9706 (Hs), 29869 (Mm), 303206 (Rn)
Human Protein Atlas ENSG00000083290 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:9706 (Hs), mmu:29869 (Mm), rno:303206 (Rn)
OMIM 608650 (Hs)
Pharos Q8IYT8 (Hs)
RefSeq Nucleotide NM_001142610 (Hs), NM_013881 (Mm), NM_001191645 (Rn)
RefSeq Protein NP_001136082 (Hs), NP_038909 (Mm), NP_001178574 (Rn)
UniProtKB Q8IYT8 (Hs), Q9QY01 (Mm)
Wikipedia ULK2 (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
SBP-7455 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 5.9 pIC50 4
⤷ pIC50 5.9 (IC50 1.158x10-6 M) [4]
Description: Inhibition determined in a NanoBRET assay.
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: ULK2
Ligand Sp. Type Action Value Parameter
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.1 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.7 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.9 pKd
tamatinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.7 pKd
dovitinib Small molecule or natural product Hs Inhibitor Inhibition 7.3 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.2 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 7.2 pKd
fedratinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.1 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 6.9 pKd
ruxolitinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.7 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: ULK2/ULK2
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 2.7 1.0 0.0
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 4.7 4.0 0.0
K-252a Small molecule or natural product Hs Inhibitor Inhibition 6.8 7.0 0.0
SU11274 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 16.8 14.0 1.0
SU6656 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 26.3 38.0 13.0
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 40.3
JAK inhibitor I Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 41.5 26.0 25.0
SU11652 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 43.0 23.0 2.0
dovitinib Small molecule or natural product Hs Inhibitor Inhibition 45.7
JAK3 inhibitor VI Small molecule or natural product Hs Inhibitor Inhibition 48.1 46.0 8.0
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. Ren H, Bakas NA, Vamos M, Chaikuad A, Limpert AS, Wimer CD, Brun SN, Lambert LJ, Tautz L, Celeridad M et al.. (2020) Design, Synthesis, and Characterization of an Orally Active Dual-Specific ULK1/2 Autophagy Inhibitor that Synergizes with the PARP Inhibitor Olaparib for the Treatment of Triple-Negative Breast Cancer. J Med Chem, 63 (23): 14609-14625. [PMID:33200929]

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 autophagy activating kinase 2. Last modified on 24/11/2020. Accessed on 10/10/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2272.