Inhibitors | Comment | Organism | Structure |
---|---|---|---|
1-(4-nitrobenzyl)-3-(4-(2-morpholinoethyl) piperazin-1-yl)quinoxalin-2(1H)-one | 23% inhibition | Rattus norvegicus | |
1-(4-nitrobenzyl)-3-(4-(3-(trifluoromethyl) phenyl)piperazin-1-yl) quinoxalin-2(1H)-one | 43% inhibition | Rattus norvegicus | |
1-(4-nitrobenzyl)-3-(4-(4-methoxyphenyl) piperazin-1-yl)quinoxalin-2(1H)-one | 26% inhibition | Rattus norvegicus | |
1-(4-nitrobenzyl)-3-(4-(pyrazin-2-yl) piperazin-1-yl)quinoxalin-2(1H)-one | 24% inhibition | Rattus norvegicus | |
1-(4-nitrobenzyl)-3-styrylquinoxalin-2(1H)-one | 30% inhibition | Rattus norvegicus | |
2-(2-oxo-3-phenethylquinoxalin-1(2H)-yl) acetic acid | - |
Rattus norvegicus | |
2-(2-oxo-3-styrylquinoxalin-1(2H)-yl) acetic acid | - |
Rattus norvegicus | |
2-(3-(2,4-difluorophenylamino)-6-nitro-2-oxoquinoxalin-1(2H)-yl) acetic acid | - |
Rattus norvegicus | |
2-(3-(3-(tert-butylamino)-3-oxoprop-1-en-1-yl)-2-oxoquinoxalin-1(2H)-yl) acetic acid | - |
Rattus norvegicus | |
2-(3-(4-(4-methoxyphenyl) piperazin-1-yl)-2-oxoquinoxalin-1(2H)-yl) acetic acid | - |
Rattus norvegicus | |
2-(3-(4-fluorophenethyl)-2-oxoquinoxalin-1(2H)-yl) acetic acid | - |
Rattus norvegicus | |
2-(3-(4-fluorostyryl)-2-oxoquinoxalin-1(2H)-yl) acetic acid | - |
Rattus norvegicus | |
2-(3-(4-fluorostyryl)-6-nitro-2-oxoquinoxalin-1(2H)-yl)acetic acid | - |
Rattus norvegicus | |
2-(6-chloro-3-(4-fluorostyryl)-2-oxoquinoxalin-1(2H)-yl)acetic acid | - |
Rattus norvegicus | |
2-(7-chloro-2-oxo-3-styrylquinoxalin-1(2H)-yl) acetic acid | - |
Rattus norvegicus | |
3-(4-fluorostyryl)-1-(4-nitrobenzyl) quinoxalin-2(1H)-one | 24% inhibition | Rattus norvegicus | |
3-(benzo[b] thiophen-3-yl)-1-(4-nitrobenzyl)quinoxalin-2(1H)-one | 32% inhibition | Rattus norvegicus | |
additional information | structure-activity relationships study of quinoxalinone derivatives as aldose reductase inhibitors. Among them, N1-acetate derivatives have significant activity, molecular modeling and docking, overview. Both C3-phenethyl and C6-NO2 groups play an important role in enhancing the activity and selectivity of the quinoxalinone based inhibitors | Rattus norvegicus | |
N-(tert-butyl)-3-(4-(4-nitrobenzyl)-3-oxo-3, 4-dihydroquinoxalin-2-yl) acryl amide | 36% inhibition | Rattus norvegicus |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Rattus norvegicus | P51635 | - |
- |
Rattus norvegicus Wistar | P51635 | - |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
additional information | ALR1 is present in all tissues | Rattus norvegicus | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
D-glucuronate + NADPH + H+ | - |
Rattus norvegicus | ? + NADP+ | - |
r | |
D-glucuronate + NADPH + H+ | - |
Rattus norvegicus Wistar | ? + NADP+ | - |
r |
Synonyms | Comment | Organism |
---|---|---|
alcohol dehydrogenase [NADP(+)] | UniProt | Rattus norvegicus |
aldehyde reductase | - |
Rattus norvegicus |
ALR1 | - |
Rattus norvegicus |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
assay at, ALR1 | Rattus norvegicus |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.2 | - |
assay at, ALR1 | Rattus norvegicus |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
NADPH | - |
Rattus norvegicus |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.000143 | - |
pH 7.2, 37°C, ALR1 | Rattus norvegicus | 2-(2-oxo-3-phenethylquinoxalin-1(2H)-yl) acetic acid | |
0.000283 | - |
pH 7.2, 37°C, ALR1 | Rattus norvegicus | 2-(3-(2,4-difluorophenylamino)-6-nitro-2-oxoquinoxalin-1(2H)-yl) acetic acid | |
0.000362 | - |
pH 7.2, 37°C, ALR1 | Rattus norvegicus | 2-(3-(4-fluorostyryl)-6-nitro-2-oxoquinoxalin-1(2H)-yl)acetic acid | |
0.00066 | - |
pH 7.2, 37°C, ALR1 | Rattus norvegicus | 2-(6-chloro-3-(4-fluorostyryl)-2-oxoquinoxalin-1(2H)-yl)acetic acid | |
0.00082 | - |
pH 7.2, 37°C, ALR1 | Rattus norvegicus | 2-(2-oxo-3-styrylquinoxalin-1(2H)-yl) acetic acid | |
0.00114 | - |
pH 7.2, 37°C, ALR1 | Rattus norvegicus | 2-(3-(4-fluorophenethyl)-2-oxoquinoxalin-1(2H)-yl) acetic acid | |
0.00143 | - |
pH 7.2, 37°C, ALR1 | Rattus norvegicus | 2-(3-(4-fluorostyryl)-2-oxoquinoxalin-1(2H)-yl) acetic acid | |
0.00186 | - |
pH 7.2, 37°C, ALR1 | Rattus norvegicus | 2-(3-(3-(tert-butylamino)-3-oxoprop-1-en-1-yl)-2-oxoquinoxalin-1(2H)-yl) acetic acid | |
0.00388 | - |
pH 7.2, 37°C, ALR1 | Rattus norvegicus | 2-(7-chloro-2-oxo-3-styrylquinoxalin-1(2H)-yl) acetic acid | |
0.00753 | - |
pH 7.2, 37°C, ALR1 | Rattus norvegicus | 2-(3-(4-(4-methoxyphenyl) piperazin-1-yl)-2-oxoquinoxalin-1(2H)-yl) acetic acid |
General Information | Comment | Organism |
---|---|---|
physiological function | ALR1 is present in all tissues and plays an important role in detoxification | Rattus norvegicus |