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Literature summary for 2.7.11.20 extracted from
- A high-throughput screening assay for eukaryotic elongation factor 2 kinase inhibitors (2016), Acta Pharm. Sin. B, 6, 557-563 .
Activating Compound
| Activating Compound | Comment | Organism | Structure |
|---|---|---|---|
| Calmodulin | - |
Homo sapiens |  |
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| expressed in Escherichia coli | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 1,1'-(cyclopropane-1,1-diyldisulfonyl)bis(4-chlorobenzene) | - |
Homo sapiens | |
| 2,6-diamino-4-(2-fluorophenyl)-4H-thiopyran-3,5-dicarbonitrile | - |
Homo sapiens | |
| 2-((3,5-dimethyl-4-hydroxyphenyl)-methylene)-4-cyclopentene-1,3-dione | TX-1918 | Homo sapiens | |
| 2-((3-cyano-4-(4-methoxyphenyl)pyridine-2-ylthio)-2-phenylacetic)acid | - |
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 | - |
Homo sapiens | |
| 3-phenyl-7-(pyrrolidin-1-yl)-2,3-dihydro-1H-inden-1-one | - |
Homo sapiens | |
| 3-[[(6-bromonaphthalen-1-yl)oxy]methyl]-1-methyl-4-phenylpiperidine | - |
Homo sapiens | |
| 4-benzyl-N-(2,4-difluorophenyl)-1,4-diazepane-1-carboxamide | - |
Homo sapiens | |
| 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 | |
| A484954 | - |
Homo sapiens | |
| N-dodecyl-N,N-dimethyl-9H-fluoren-9-aminium bromide | - |
Homo sapiens | |
| NH125 | i.e. 1-benzyl-3-acetyl-2-methylimidazolium iodide | Homo sapiens | |
| 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 | |
| TS2 | i.e. 4-ethyl-4-hydroxy-2-p-tolyl-5,6-dihydro-4H-1,3-selenazine | Homo sapiens | |
| 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)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + [elongation factor 2] | Homo sapiens | - |
ADP + [elongation factor 2] phosphate | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
- |
Homo sapiens |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| HCT-116 cell | - |
Homo sapiens | - |
| MDA-MB-453 cell | - |
Homo sapiens | - |
| NCI-H1299 cell | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + MH-1 peptide | the MH-1 peptide amino acid sequence is RKKFGESEKTKTKEFL | Homo sapiens | ADP + phosphorylated MH-1 peptide | - |
? | |
| ATP + [elongation factor 2] | - |
Homo sapiens | ADP + [elongation factor 2] phosphate | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| eEF2K | - |
Homo sapiens |
| eukaryotic elongation factor 2 kinase | - |
Homo sapiens |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.000032 | - |
at 25°C, pH not specified in the publication | Homo sapiens | 4-benzyl-N-(2,4-difluorophenyl)-1,4-diazepane-1-carboxamide | |
| 0.000069 | - |
at 25°C, pH not specified in the publication | Homo sapiens | 1,1'-(cyclopropane-1,1-diyldisulfonyl)bis(4-chlorobenzene) | |
| 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 | |
| 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 | |
| 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 | |
| 0.00023 | - |
at 25°C, pH not specified in the publication | Homo sapiens | A484954 | |
| 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 | |
| 0.01327 | - |
at 25°C, pH not specified in the publication | Homo sapiens | N-dodecyl-N,N-dimethyl-9H-fluoren-9-aminium bromide | |
| 0.0323 | - |
at 25°C, pH not specified in the publication | Homo sapiens | 3-[[(6-bromonaphthalen-1-yl)oxy]methyl]-1-methyl-4-phenylpiperidine | |
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