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Literature summary extracted from

  • Xiao, T.; Liu, R.; Proud, C.G.; Wang, M.W.
    A high-throughput screening assay for eukaryotic elongation factor 2 kinase inhibitors (2016), Acta Pharm. Sin. B, 6, 557-563 .
    View publication on PubMedView publication on EuropePMC

Activating Compound

EC Number Activating Compound Comment Organism Structure
2.7.11.20 Calmodulin
-
 Homo sapiens

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.7.11.20 expressed in Escherichia coli Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.11.20 1,1'-(cyclopropane-1,1-diyldisulfonyl)bis(4-chlorobenzene)
-
 Homo sapiens
2.7.11.20 2,6-diamino-4-(2-fluorophenyl)-4H-thiopyran-3,5-dicarbonitrile
-
 Homo sapiens
2.7.11.20 2-((3,5-dimethyl-4-hydroxyphenyl)-methylene)-4-cyclopentene-1,3-dione TX-1918 Homo sapiens
2.7.11.20 2-((3-cyano-4-(4-methoxyphenyl)pyridine-2-ylthio)-2-phenylacetic)acid
-
 Homo sapiens
2.7.11.20 3-amino-4-(furan-2-yl)-6,7,8,9,10,11-hexahydro-5H-cyclonona[b]thieno[3,2-e]pyridine-2-carboxamide
-
 Homo sapiens
2.7.11.20 3-phenyl-7-(pyrrolidin-1-yl)-2,3-dihydro-1H-inden-1-one
-
 Homo sapiens
2.7.11.20 3-[[(6-bromonaphthalen-1-yl)oxy]methyl]-1-methyl-4-phenylpiperidine
-
 Homo sapiens
2.7.11.20 4-benzyl-N-(2,4-difluorophenyl)-1,4-diazepane-1-carboxamide
-
 Homo sapiens
2.7.11.20 7-amino-1-cyclopropyl-3-ethyl-1,2,3,4-tetrahydro-2,4-dioxopyrido[2,3-d]pyrimidine-6-carboxamide A-484954, highly selective inhibitor Homo sapiens
2.7.11.20 A484954
-
 Homo sapiens
2.7.11.20 N-dodecyl-N,N-dimethyl-9H-fluoren-9-aminium bromide
-
 Homo sapiens
2.7.11.20 NH125 i.e. 1-benzyl-3-acetyl-2-methylimidazolium iodide Homo sapiens
2.7.11.20 rottlerin i.e. 1-[6-[(3-acetyl-2,4,6-trihydroxy-5-methylphenyl)methyl]-5,7-dihydroxy-2,2-dimethyl-2H-1-benzopyran-8-yl]-3-phenyl-2-propen-1-one, mallotoxin Homo sapiens
2.7.11.20 TS2 i.e. 4-ethyl-4-hydroxy-2-p-tolyl-5,6-dihydro-4H-1,3-selenazine Homo sapiens
2.7.11.20 TS4 i.e. 4-hydroxy-6-isopropyl-4-methyl-2-p-tolyl-5,6-dihydro-4H-1,3-selenazine Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.11.20 ATP + [elongation factor 2] Homo sapiens
-
 ADP + [elongation factor 2] phosphate
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.7.11.20 Homo sapiens
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.7.11.20
-
 Homo sapiens

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.7.11.20 HCT-116 cell
-
 Homo sapiens
-
2.7.11.20 MDA-MB-453 cell
-
 Homo sapiens
-
2.7.11.20 NCI-H1299 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.11.20 ATP + MH-1 peptide the MH-1 peptide amino acid sequence is RKKFGESEKTKTKEFL Homo sapiens ADP + phosphorylated MH-1 peptide
-
 ?
2.7.11.20 ATP + [elongation factor 2]
-
 Homo sapiens ADP + [elongation factor 2] phosphate
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.7.11.20 eEF2K
-
 Homo sapiens
2.7.11.20 eukaryotic elongation factor 2 kinase
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.7.11.20 0.000032
-
 at 25°C, pH not specified in the publication Homo sapiens 4-benzyl-N-(2,4-difluorophenyl)-1,4-diazepane-1-carboxamide
2.7.11.20 0.000069
-
 at 25°C, pH not specified in the publication Homo sapiens 1,1'-(cyclopropane-1,1-diyldisulfonyl)bis(4-chlorobenzene)
2.7.11.20 0.00017
-
 at 25°C, pH not specified in the publication Homo sapiens 3-amino-4-(furan-2-yl)-6,7,8,9,10,11-hexahydro-5H-cyclonona[b]thieno[3,2-e]pyridine-2-carboxamide
2.7.11.20 0.00023
-
 at 25°C, pH not specified in the publication Homo sapiens 3-phenyl-7-(pyrrolidin-1-yl)-2,3-dihydro-1H-inden-1-one
2.7.11.20 0.00023
-
 at 25°C, pH not specified in the publication Homo sapiens 7-amino-1-cyclopropyl-3-ethyl-1,2,3,4-tetrahydro-2,4-dioxopyrido[2,3-d]pyrimidine-6-carboxamide
2.7.11.20 0.00023
-
 at 25°C, pH not specified in the publication Homo sapiens A484954
2.7.11.20 0.00044
-
 at 25°C, pH not specified in the publication Homo sapiens 2-((3,5-dimethyl-4-hydroxyphenyl)-methylene)-4-cyclopentene-1,3-dione
2.7.11.20 0.01327
-
 at 25°C, pH not specified in the publication Homo sapiens N-dodecyl-N,N-dimethyl-9H-fluoren-9-aminium bromide
2.7.11.20 0.0323
-
 at 25°C, pH not specified in the publication Homo sapiens 3-[[(6-bromonaphthalen-1-yl)oxy]methyl]-1-methyl-4-phenylpiperidine