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eukaryotic elongation factor 2 kinase

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Target not currently curated in GtoImmuPdb

Target id: 2014

Nomenclature: eukaryotic elongation factor 2 kinase

Abbreviated Name: eEF2K

Family: eEF2K subfamily

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 725 16p12.2 EEF2K eukaryotic elongation factor 2 kinase
Mouse - 724 7 F2 Eef2k eukaryotic elongation factor-2 kinase
Rat - 724 1q36 Eef2k eukaryotic elongation factor-2 kinase
Previous and Unofficial Names Click here for help
SMEF2K
Database Links Click here for help
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BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
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RefSeq Protein
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Enzyme Reaction Click here for help
EC Number: 2.7.11.20

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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] Small molecule or natural product Hs Inhibition 6.8 pIC50 2
pIC50 6.8 (IC50 1.7x10-7 M) [2]
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...

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 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 72.0 113.0
IKK-2 inhibitor IV Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 77.0 38.0
isogranulatimide Small molecule or natural product Hs Inhibitor Inhibition 78.0 59.0
PKR inhibitor Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 79.0 97.0
SU11274 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 79.0 132.0
PP3 Small molecule or natural product Hs Inhibitor Inhibition 81.0 72.0
JAK inhibitor I Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 81.0 126.0
MEK1/2 inhibitor Small molecule or natural product Hs Inhibitor Inhibition 81.0 82.0
AG 1296 Small molecule or natural product Hs Inhibitor Inhibition 82.0 101.0
Cdk1/5 inhibitor Small molecule or natural product Hs Inhibitor Inhibition 82.0 110.0
Displaying the top 10 most potent ligands  View all ligands in screen »
Immuno Process Associations
Immuno Process:  Antigen presentation

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 18/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=2014.