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Literature summary for 3.1.1.4 extracted from
- 1-(5-Carboxyindol-1-yl)propan-2-ones as inhibitors of human cytosolic phospholipase A2alpha: synthesis and properties of bioisosteric benzimidazole, benzotriazole and indazole analogues (2009), Bioorg. Med. Chem. Lett., 19, 2107-2111.
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-benzotriazole-5-carboxylic acid | 43% metabolic stability in an assay with rat liver microsomes. Thermodynamic solubility is less than 1 microg/ml at pH 7.4 | Homo sapiens |  |
| 1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-benzotriazole-6-carboxylic acid | 44% metabolic stability in an assay with rat liver microsomes. Thermodynamic solubility is 2 microg/ml at pH 7.4 | Homo sapiens | |
| 1-[3-(4-octylphenoxy)-2-oxopropyl]benzimidazole-5-carboxylic acid | 49% metabolic stability in an assay with rat liver microsomes, possesses the best thermodynamic solubility (22 microg/ml at pH 7.4) | Homo sapiens | |
| 1-[3-(4-octylphenoxy)-2-oxopropyl]benzimidazole-6-carboxylic acid | 40% metabolic stability in an assay with rat liver microsomes. Thermodynamic solubility is 7 microg/ml at pH 7.4 | Homo sapiens | |
| 1-[3-(4-octylphenoxy)-2-oxopropyl]indazole-5-carboxylic acid | reveals the highest cPLA2a inhibitory potency, is 7fold more active than the lead 1-[3-(4-octylphenoxy)-2-oxopropyl]indole-5-carboxylic acid, is the metabolically most stable compound in an assay with rat liver microsomes (64% stability). Thermodynamic solubility is less than 1 microg/ml at pH 7.4 | Homo sapiens | |
| 1-[3-(4-octylphenoxy)-2-oxopropyl]indazole-6-carboxylic acid | 36% metabolic stability in an assay with rat liver microsomes. Thermodynamic solubility is 5 microg/ml at pH 7.4 | Homo sapiens | |
| 1-[3-(4-octylphenoxy)-2-oxopropyl]indole-5-carboxylic acid | is 7fold less active than 1-[3-(4-octylphenoxy)-2-oxopropyl]indazole-5-carboxylic acid, is the metabolically most stable compound in an assay with rat liver microsomes (65% stability). Thermodynamic solubility is less than 1 microg/ml at pH 7.4 | Homo sapiens | |
| 1-[3-(4-octylphenoxy)-2-oxopropyl]indole-6-carboxylic acid | 39% metabolic stability in an assay with rat liver microsomes. Thermodynamic solubility is less than 1 microg/ml at pH 7.4 | Homo sapiens | |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| cPLA2alpha | - |
Homo sapiens |
| cytosolic phospholipase A2alpha | - |
Homo sapiens |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.000005 | - |
- |
Homo sapiens | 1-[3-(4-octylphenoxy)-2-oxopropyl]indazole-5-carboxylic acid | |
| 0.000016 | - |
- |
Homo sapiens | 1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-benzotriazole-6-carboxylic acid | |
| 0.000026 | - |
- |
Homo sapiens | 1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-benzotriazole-5-carboxylic acid | |
| 0.000026 | - |
- |
Homo sapiens | 1-[3-(4-octylphenoxy)-2-oxopropyl]indazole-6-carboxylic acid | |
| 0.000035 | - |
- |
Homo sapiens | 1-[3-(4-octylphenoxy)-2-oxopropyl]indole-5-carboxylic acid | |
| 0.000085 | - |
- |
Homo sapiens | 1-[3-(4-octylphenoxy)-2-oxopropyl]benzimidazole-6-carboxylic acid | |
| 0.00015 | - |
- |
Homo sapiens | 1-[3-(4-octylphenoxy)-2-oxopropyl]benzimidazole-5-carboxylic acid | |
| 0.0011 | - |
- |
Homo sapiens | 1-[3-(4-octylphenoxy)-2-oxopropyl]indole-6-carboxylic acid | |
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