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Literature summary for 2.5.1.58 extracted from
- Discovery of a new class of protein farnesyltransferase inhibitors in the arylthiophene series (2009), J. Med. Chem., 52, 6205-6208.
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 3-(4-chlorophenyl)-4-cyano-1-methyl-5-[(1-methylethyl)sulfanyl]-1H-pyrrole-2-carboxylic acid | - |
Saccharomyces cerevisiae |  |
| 3-(4-chlorophenyl)-4-cyano-5-(cyclohexylsulfanyl)thiophene-2-carboxylic acid | - |
Saccharomyces cerevisiae | |
| 3-(4-chlorophenyl)-4-cyano-5-(ethylsulfanyl)thiophene-2-carboxylic acid | - |
Saccharomyces cerevisiae | |
| 3-(4-chlorophenyl)-4-cyano-5-(methylsulfanyl)thiophene-2-carboxylic acid | - |
Saccharomyces cerevisiae | |
| 3-(4-chlorophenyl)-4-cyano-5-(morpholin-4-ylsulfanyl)thiophene-2-carboxylic acid | - |
Saccharomyces cerevisiae | |
| 3-(4-chlorophenyl)-4-cyano-5-[(1-methylethyl)sulfanyl]furan-2-carboxylic acid | - |
Saccharomyces cerevisiae | |
| 3-(4-chlorophenyl)-4-cyano-5-[(1-methylethyl)sulfanyl]thiophene-2-carboxamide | - |
Saccharomyces cerevisiae | |
| 3-(4-chlorophenyl)-4-cyano-5-[(1-methylethyl)sulfanyl]thiophene-2-carboxylic acid | - |
Saccharomyces cerevisiae | |
| 3-(4-chlorophenyl)-4-cyano-5-[(1-methylpropyl)sulfanyl]thiophene-2-carboxylic acid | - |
Saccharomyces cerevisiae | |
| 3-(4-chlorophenyl)-4-cyano-5-[(2-methylpropyl)sulfanyl]thiophene-2-carboxylic acid | - |
Saccharomyces cerevisiae | |
| 3-(4-chlorophenyl)-4-cyano-N-cyclopropyl-5-[(1-methylethyl)sulfanyl]thiophene-2-carboxamide | - |
Saccharomyces cerevisiae | |
| 4-(4-chlorophenyl)-2-[(1-methylethyl)sulfanyl]-1,3-thiazole-5-carboxylic acid | - |
Saccharomyces cerevisiae | |
| 4-(4-chlorophenyl)-5-(hydroxyacetyl)-2-[(1-methylethyl)sulfanyl]thiophene-3-carbonitrile | - |
Saccharomyces cerevisiae | |
| 4-(4-chlorophenyl)-5-(methoxyacetyl)-2-[(1-methylethyl)sulfanyl]thiophene-3-carbonitrile | - |
Saccharomyces cerevisiae | |
| 5-(butylsulfanyl)-3-(4-chlorophenyl)-4-cyanothiophene-2-carboxylic acid | - |
Saccharomyces cerevisiae | |
| 5-acetyl-4-(4-chlorophenyl)-2-[(1-methylethyl)sulfanyl]thiophene-3-carbonitrile | - |
Saccharomyces cerevisiae | |
| ethyl 3-(4-chlorophenyl)-4-cyano-5-[(1-methylethyl)sulfanyl]thiophene-2-carboxylate | - |
Saccharomyces cerevisiae | |
| [3-(4-chlorophenyl)-4-cyano-5-[(1-methylethyl)sulfanyl]thiophen-2-yl]methyl acetate | - |
Saccharomyces cerevisiae | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Saccharomyces cerevisiae | - |
- |
- |
Subunits
| Subunits | Comment | Organism |
|---|---|---|
| heterodimer | - |
Saccharomyces cerevisiae |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| FTase | - |
Saccharomyces cerevisiae |
| protein farnesyltransferase | - |
Saccharomyces cerevisiae |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.0000075 | - |
30°C, pH 7.5 | Saccharomyces cerevisiae | 4-(4-chlorophenyl)-5-(hydroxyacetyl)-2-[(1-methylethyl)sulfanyl]thiophene-3-carbonitrile | |
| 0.00011 | - |
30°C, pH 7.5 | Saccharomyces cerevisiae | 3-(4-chlorophenyl)-4-cyano-5-[(1-methylethyl)sulfanyl]thiophene-2-carboxylic acid | |
| 0.000325 | - |
30°C, pH 7.5 | Saccharomyces cerevisiae | 3-(4-chlorophenyl)-4-cyano-5-(ethylsulfanyl)thiophene-2-carboxylic acid | |
| 0.000345 | - |
30°C, pH 7.5 | Saccharomyces cerevisiae | 3-(4-chlorophenyl)-4-cyano-5-[(1-methylpropyl)sulfanyl]thiophene-2-carboxylic acid | |
| 0.00061 | - |
30°C, pH 7.5 | Saccharomyces cerevisiae | 3-(4-chlorophenyl)-4-cyano-5-(methylsulfanyl)thiophene-2-carboxylic acid | |
| 0.00079 | - |
30°C, pH 7.5 | Saccharomyces cerevisiae | 5-acetyl-4-(4-chlorophenyl)-2-[(1-methylethyl)sulfanyl]thiophene-3-carbonitrile | |
| 0.00089 | - |
30°C, pH 7.5 | Saccharomyces cerevisiae | 3-(4-chlorophenyl)-4-cyano-5-[(2-methylpropyl)sulfanyl]thiophene-2-carboxylic acid | |
| 0.0011 | - |
30°C, pH 7.5 | Saccharomyces cerevisiae | 3-(4-chlorophenyl)-4-cyano-5-[(1-methylethyl)sulfanyl]thiophene-2-carboxamide | |
| 0.00124 | - |
30°C, pH 7.5 | Saccharomyces cerevisiae | 5-(butylsulfanyl)-3-(4-chlorophenyl)-4-cyanothiophene-2-carboxylic acid | |
| 0.00145 | - |
30°C, pH 7.5 | Saccharomyces cerevisiae | 3-(4-chlorophenyl)-4-cyano-5-(cyclohexylsulfanyl)thiophene-2-carboxylic acid | |
| 0.002 | - |
30°C, pH 7.5 | Saccharomyces cerevisiae | 3-(4-chlorophenyl)-4-cyano-5-[(1-methylethyl)sulfanyl]furan-2-carboxylic acid | |
| 0.0038 | - |
30°C, pH 7.5 | Saccharomyces cerevisiae | ethyl 3-(4-chlorophenyl)-4-cyano-5-[(1-methylethyl)sulfanyl]thiophene-2-carboxylate | |
| 0.0057 | - |
30°C, pH 7.5 | Saccharomyces cerevisiae | 4-(4-chlorophenyl)-5-(methoxyacetyl)-2-[(1-methylethyl)sulfanyl]thiophene-3-carbonitrile | |
| 0.022 | - |
30°C, pH 7.5 | Saccharomyces cerevisiae | 3-(4-chlorophenyl)-4-cyano-N-cyclopropyl-5-[(1-methylethyl)sulfanyl]thiophene-2-carboxamide | |
| 0.028 | - |
30°C, pH 7.5 | Saccharomyces cerevisiae | 3-(4-chlorophenyl)-4-cyano-5-(morpholin-4-ylsulfanyl)thiophene-2-carboxylic acid | |
| 0.045 | - |
30°C, pH 7.5 | Saccharomyces cerevisiae | [3-(4-chlorophenyl)-4-cyano-5-[(1-methylethyl)sulfanyl]thiophen-2-yl]methyl acetate | |
| 0.047 | - |
30°C, pH 7.5 | Saccharomyces cerevisiae | 3-(4-chlorophenyl)-4-cyano-1-methyl-5-[(1-methylethyl)sulfanyl]-1H-pyrrole-2-carboxylic acid | |
| 0.051 | - |
30°C, pH 7.5 | Saccharomyces cerevisiae | 4-(4-chlorophenyl)-2-[(1-methylethyl)sulfanyl]-1,3-thiazole-5-carboxylic acid | |
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