Inhibitors | Comment | Organism | Structure |
---|---|---|---|
1-[4-benzoyl-1-(1-hydroxy-1H-pyrazol-4-yl)-1H-pyrrol-2-yl]-2,2,2-trifluoroethan-1-one | 413fold selectivity for isoform ALR2 over ALR1 | Rattus norvegicus | |
2,2,2-trifluoro-1-[1-(1-hydroxy-1H-pyrazol-4-yl)-4-(3-methoxybenzoyl)-1H-pyrrol-2-yl]ethan-1-one | 370fold selectivity for isoform ALR2 over ALR1 | Rattus norvegicus | |
2,2,2-trifluoro-1-[1-(1-hydroxy-1H-pyrazol-4-yl)-4-(4-methoxybenzoyl)-1H-pyrrol-2-yl]ethan-1-one | 468fold selectivity for isoform ALR2 over ALR1 | Rattus norvegicus | |
2,2,2-trifluoro-1-[1-(1-hydroxy-1H-pyrazol-4-yl)-4-(4-phenoxybenzoyl)-1H-pyrrol-2-yl]ethan-1-one | 190fold selectivity for isoform ALR2 over ALR1 | Rattus norvegicus | |
2,2,2-trifluoro-1-[1-(1-hydroxy-1H-pyrazol-4-yl)-4-[4-(methanesulfonyl)benzoyl]-1H-pyrrol-2-yl]ethan-1-one | 775fold selectivity for isoform ALR2 over ALR1 | Rattus norvegicus | |
2,2,2-trifluoro-1-[1-(1-hydroxy-1H-pyrazol-4-yl)-4-[4-(methylsulfanyl)benzoyl]-1H-pyrrol-2-yl]ethan-1-one | mixed-type inhibition | Homo sapiens | |
2,2,2-trifluoro-1-[1-(1-hydroxy-1H-pyrazol-4-yl)-4-[4-(methylsulfanyl)benzoyl]-1H-pyrrol-2-yl]ethan-1-one | 650fold selectivity for isoform ALR2 over ALR1 | Rattus norvegicus | |
2,2,2-trifluoro-1-[4-(3-fluorobenzoyl)-1-(1-hydroxy-1H-pyrazol-4-yl)-1H-pyrrol-2-yl]ethan-1-one | 339fold selectivity for isoform ALR2 over ALR1 | Rattus norvegicus | |
2,2,2-trifluoro-1-[4-(4-fluorobenzoyl)-1-(1-hydroxy-1H-pyrazol-4-yl)-1H-pyrrol-2-yl]ethan-1-one | mixed-type inhibition | Homo sapiens | |
2,2,2-trifluoro-1-[4-(4-fluorobenzoyl)-1-(1-hydroxy-1H-pyrazol-4-yl)-1H-pyrrol-2-yl]ethan-1-one | 858fold selectivity for isoform ALR2 over ALR1 | Rattus norvegicus | |
sorbinil | - |
Rattus norvegicus | |
Valproic acid | - |
Rattus norvegicus |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P15121 | - |
- |
Rattus norvegicus | - |
- |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
kidney | isoform ALR1 | Rattus norvegicus | - |
lens | isoform ALR2 | Rattus norvegicus | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
4-hydroxynonenal + NADPH + H+ | - |
Homo sapiens | 4-hydroxynonanol + NADP+ | - |
? | |
DL-glyceraldehyde + NAD(P)H + H+ | - |
Homo sapiens | glycerol + NAD(P)+ | - |
? | |
L-idose + NADPH + H+ | - |
Homo sapiens | alditol + NADP+ | - |
? |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.000043 | - |
pH 7.4, 37°C | Rattus norvegicus | 2,2,2-trifluoro-1-[1-(1-hydroxy-1H-pyrazol-4-yl)-4-[4-(methylsulfanyl)benzoyl]-1H-pyrrol-2-yl]ethan-1-one | |
0.000064 | - |
pH 7.4, 37°C | Rattus norvegicus | 2,2,2-trifluoro-1-[1-(1-hydroxy-1H-pyrazol-4-yl)-4-(3-methoxybenzoyl)-1H-pyrrol-2-yl]ethan-1-one | |
0.000073 | - |
pH 7.4, 37°C | Rattus norvegicus | 2,2,2-trifluoro-1-[1-(1-hydroxy-1H-pyrazol-4-yl)-4-(4-methoxybenzoyl)-1H-pyrrol-2-yl]ethan-1-one | |
0.000078 | - |
pH 7.4, 37°C | Rattus norvegicus | 2,2,2-trifluoro-1-[4-(4-fluorobenzoyl)-1-(1-hydroxy-1H-pyrazol-4-yl)-1H-pyrrol-2-yl]ethan-1-one | |
0.000094 | - |
pH 7.4, 37°C | Rattus norvegicus | 2,2,2-trifluoro-1-[1-(1-hydroxy-1H-pyrazol-4-yl)-4-[4-(methanesulfonyl)benzoyl]-1H-pyrrol-2-yl]ethan-1-one | |
0.00014 | - |
pH 7.4, 37°C | Rattus norvegicus | 2,2,2-trifluoro-1-[4-(3-fluorobenzoyl)-1-(1-hydroxy-1H-pyrazol-4-yl)-1H-pyrrol-2-yl]ethan-1-one | |
0.000242 | - |
pH 7.4, 37°C | Rattus norvegicus | 1-[4-benzoyl-1-(1-hydroxy-1H-pyrazol-4-yl)-1H-pyrrol-2-yl]-2,2,2-trifluoroethan-1-one | |
0.00025 | - |
isoform ALR2, pH 7.4, 37°C | Rattus norvegicus | sorbinil | |
0.00074 | - |
pH 7.4, 37°C | Rattus norvegicus | 2,2,2-trifluoro-1-[1-(1-hydroxy-1H-pyrazol-4-yl)-4-(4-phenoxybenzoyl)-1H-pyrrol-2-yl]ethan-1-one | |
0.056 | - |
isoform ALR1, pH 7.4, 37°C | Rattus norvegicus | Valproic acid |