Any feedback?
Literature summary for 2.7.11.21 extracted from
- Identification of indole-3-carboxylic acids as non-ATP-competitive Polo-like kinase 1 (Plk1) inhibitors (2015), Bioorg. Med. Chem. Lett., 25, 431-434.
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| (4E)-4-(hydroxyimino)-5-methyl-2-(propan-2-yl)cyclohexa-2,5-dien-1-one | - |
Homo sapiens |  |
| (4E)-5-methyl-4-{[(2-methylbenzoyl)oxy]imino}-2-(propan-2-yl)cyclohexa-2,5-dien-1-one | - |
Homo sapiens | |
| 1-[2-hydroxy-3-(4-methylpiperazin-1-yl)propyl]-1H-indole-3-carboxylic acid | - |
Homo sapiens | |
| 1-[2-hydroxy-3-(piperidin-1-yl)propyl]-1H-indole-3-carboxylic acid | - |
Homo sapiens | |
| 1-[2-hydroxy-3-(pyrrolidin-1-yl)propyl]-1H-indole-3-carboxylic acid | - |
Homo sapiens | |
| 1-[3-(diethylamino)-2-hydroxypropyl]-1H-indole-3-carboxylic acid | - |
Homo sapiens | |
| 2-methyl-5-(propan-2-yl)cyclohexa-2,5-diene-1,4-dione | - |
Homo sapiens | |
| 3-[1-[2-hydroxy-3-(piperidin-1-yl)propyl]-1H-indol-3-yl]propanoic acid | - |
Homo sapiens | |
| 3-[1-[2-hydroxy-3-(pyrrolidin-1-yl)propyl]-1H-indol-3-yl]propanoic acid | - |
Homo sapiens | |
| CJ-054 | - |
Homo sapiens | |
| additional information | identification of indole-3-carboxylic acids as non-ATP-competitive Plk1 inhibitors | Homo sapiens | |
| N-[2-methoxy-5-({[(E)-2-(2,4,6-trimethoxyphenyl)ethenyl]sulfonyl}methyl)phenyl]glycine | - |
Homo sapiens | |
| thymoquinone | - |
Homo sapiens | |
| [1-[2-hydroxy-3-(4-methylpiperazin-1-yl)propyl]-1H-indol-3-yl]acetic acid | a highly selective inhibitor of Plk1, poor inhibition of Plk2 and Plk3 | Homo sapiens | |
| [1-[2-hydroxy-3-(morpholin-4-yl)propyl]-1H-indol-3-yl]acetic acid | - |
Homo sapiens | |
| [1-[2-hydroxy-3-(piperidin-1-yl)propyl]-1H-indol-3-yl]acetic acid | - |
Homo sapiens | |
| [1-[2-hydroxy-3-(pyrrolidin-1-yl)propyl]-1H-indol-3-yl]acetic acid | - |
Homo sapiens | |
| [1-[3-(diethylamino)-2-hydroxypropyl]-1H-indol-3-yl]acetic acid | - |
Homo sapiens | |
Metals/Ions
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Mg2+ | required | Homo sapiens | |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + a protein | Homo sapiens | - |
ADP + a phosphoprotein | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | P53350 | - |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| carcinoma cell | - |
Homo sapiens | - |
| HeLa cell | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + a protein | - |
Homo sapiens | ADP + a phosphoprotein | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| Plk1 | - |
Homo sapiens |
| Polo-like kinase 1 | - |
Homo sapiens |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 30 | - |
assay at | Homo sapiens |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 7.5 | - |
assay at | Homo sapiens |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| ATP | - |
Homo sapiens | |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| additional information | - |
IC50 values for cell growth inhibition of HeLa and MCF-7 cells | Homo sapiens | additional information | |
| 0.00013 | - |
pH 7.5, 30°C | Homo sapiens | [1-[2-hydroxy-3-(pyrrolidin-1-yl)propyl]-1H-indol-3-yl]acetic acid | |
| 0.00041 | - |
pH 7.5, 30°C | Homo sapiens | [1-[2-hydroxy-3-(piperidin-1-yl)propyl]-1H-indol-3-yl]acetic acid | |
| 0.00096 | - |
pH 7.5, 30°C | Homo sapiens | [1-[2-hydroxy-3-(morpholin-4-yl)propyl]-1H-indol-3-yl]acetic acid | |
| 0.00188 | - |
pH 7.5, 30°C | Homo sapiens | [1-[2-hydroxy-3-(4-methylpiperazin-1-yl)propyl]-1H-indol-3-yl]acetic acid | |
| 0.00191 | - |
pH 7.5, 30°C | Homo sapiens | 1-[3-(diethylamino)-2-hydroxypropyl]-1H-indole-3-carboxylic acid | |
| 0.0021 | - |
pH 7.5, 30°C | Homo sapiens | 1-[2-hydroxy-3-(piperidin-1-yl)propyl]-1H-indole-3-carboxylic acid | |
| 0.00218 | - |
pH 7.5, 30°C | Homo sapiens | thymoquinone | |
| 0.00264 | - |
pH 7.5, 30°C | Homo sapiens | [1-[3-(diethylamino)-2-hydroxypropyl]-1H-indol-3-yl]acetic acid | |
| 0.0029 | - |
pH 7.5, 30°C | Homo sapiens | 3-[1-[2-hydroxy-3-(pyrrolidin-1-yl)propyl]-1H-indol-3-yl]propanoic acid | |
| 0.00347 | - |
pH 7.5, 30°C | Homo sapiens | 1-[2-hydroxy-3-(4-methylpiperazin-1-yl)propyl]-1H-indole-3-carboxylic acid | |
| 0.00484 | - |
pH 7.5, 30°C | Homo sapiens | 1-[2-hydroxy-3-(pyrrolidin-1-yl)propyl]-1H-indole-3-carboxylic acid | |
| 0.00571 | - |
pH 7.5, 30°C | Homo sapiens | 3-[1-[2-hydroxy-3-(piperidin-1-yl)propyl]-1H-indol-3-yl]propanoic acid | |
General Information
| General Information | Comment | Organism |
|---|---|---|
| evolution | the serine/threonine kinase Polo-like kinase 1 (Plk1) is a member of the Polo-like kinases family | Homo sapiens |
Use of this online version of BRENDA is free under the CC BY 4.0 license. See terms of use for full details.
Release 2023.1 (January 2023)
Legal
Curated at
Member of
