eukaryotic elongation factor 2 kinase | eEF2K subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

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eukaryotic elongation factor 2 kinase

Target not currently curated in GtoImmuPdb

Target id: 2014

Nomenclature: eukaryotic elongation factor 2 kinase

Abbreviated Name: eEF2K

Family: eEF2K subfamily

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 - 725 16p12 EEF2K eukaryotic elongation factor 2 kinase
Mouse - 724 7 F3 Eef2k eukaryotic elongation factor-2 kinase
Rat - 724 1 q35 Eef2k eukaryotic elongation factor-2 kinase
Previous and Unofficial Names
SMEF2K
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: 2.7.11.20

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 34 [PMID: 20189382] Hs Inhibition 6.8 pIC50 2
pIC50 6.8 (IC50 1.7x10-7 M) [2]
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...

Key to terms and symbols Click column headers to sort
Target used in screen: eEF-2K/nd
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
Rho kinase inhibitor IV Hs Inhibitor Inhibition 72.0 113.0
IKK-2 inhibitor IV Hs Inhibitor Inhibition 77.0 38.0
isogranulatimide Hs Inhibitor Inhibition 78.0 59.0
PKR inhibitor Hs Inhibitor Inhibition 79.0 97.0
SU11274 Hs Inhibitor Inhibition 79.0 132.0
PP3 Hs Inhibitor Inhibition 81.0 72.0
JAK inhibitor I Hs Inhibitor Inhibition 81.0 126.0
MEK1/2 inhibitor Hs Inhibitor Inhibition 81.0 82.0
Cdk1/5 inhibitor Hs Inhibitor Inhibition 82.0 110.0
AG 1296 Hs Inhibitor Inhibition 82.0 101.0
Displaying the top 10 most potent ligands  View all ligands in screen »

References

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1. 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]

2. Lockman JW, Reeder MD, Suzuki K, Ostanin K, Hoff R, Bhoite L, Austin H, Baichwal V, Adam Willardsen J. (2010) Inhibition of eEF2-K by thieno[2,3-b]pyridine analogues. Bioorg. Med. Chem. Lett., 20 (7): 2283-6. [PMID:20189382]

How to cite this page

eEF2K subfamily: eukaryotic elongation factor 2 kinase. Last modified on 10/09/2015. Accessed on 23/07/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2014.