EC Number | Inhibitors | Comment | Organism | Structure |
---|---|---|---|---|
1.1.1.2 | 1-(4-nitrobenzyl)-3-(4-(2-morpholinoethyl) piperazin-1-yl)quinoxalin-2(1H)-one | 23% inhibition | Rattus norvegicus | |
1.1.1.2 | 1-(4-nitrobenzyl)-3-(4-(3-(trifluoromethyl) phenyl)piperazin-1-yl) quinoxalin-2(1H)-one | 43% inhibition | Rattus norvegicus | |
1.1.1.2 | 1-(4-nitrobenzyl)-3-(4-(4-methoxyphenyl) piperazin-1-yl)quinoxalin-2(1H)-one | 26% inhibition | Rattus norvegicus | |
1.1.1.2 | 1-(4-nitrobenzyl)-3-(4-(pyrazin-2-yl) piperazin-1-yl)quinoxalin-2(1H)-one | 24% inhibition | Rattus norvegicus | |
1.1.1.2 | 1-(4-nitrobenzyl)-3-styrylquinoxalin-2(1H)-one | 30% inhibition | Rattus norvegicus | |
1.1.1.2 | 2-(2-oxo-3-phenethylquinoxalin-1(2H)-yl) acetic acid | - |
Rattus norvegicus | |
1.1.1.2 | 2-(2-oxo-3-styrylquinoxalin-1(2H)-yl) acetic acid | - |
Rattus norvegicus | |
1.1.1.2 | 2-(3-(2,4-difluorophenylamino)-6-nitro-2-oxoquinoxalin-1(2H)-yl) acetic acid | - |
Rattus norvegicus | |
1.1.1.2 | 2-(3-(3-(tert-butylamino)-3-oxoprop-1-en-1-yl)-2-oxoquinoxalin-1(2H)-yl) acetic acid | - |
Rattus norvegicus | |
1.1.1.2 | 2-(3-(4-(4-methoxyphenyl) piperazin-1-yl)-2-oxoquinoxalin-1(2H)-yl) acetic acid | - |
Rattus norvegicus | |
1.1.1.2 | 2-(3-(4-fluorophenethyl)-2-oxoquinoxalin-1(2H)-yl) acetic acid | - |
Rattus norvegicus | |
1.1.1.2 | 2-(3-(4-fluorostyryl)-2-oxoquinoxalin-1(2H)-yl) acetic acid | - |
Rattus norvegicus | |
1.1.1.2 | 2-(3-(4-fluorostyryl)-6-nitro-2-oxoquinoxalin-1(2H)-yl)acetic acid | - |
Rattus norvegicus | |
1.1.1.2 | 2-(6-chloro-3-(4-fluorostyryl)-2-oxoquinoxalin-1(2H)-yl)acetic acid | - |
Rattus norvegicus | |
1.1.1.2 | 2-(7-chloro-2-oxo-3-styrylquinoxalin-1(2H)-yl) acetic acid | - |
Rattus norvegicus | |
1.1.1.2 | 3-(4-fluorostyryl)-1-(4-nitrobenzyl) quinoxalin-2(1H)-one | 24% inhibition | Rattus norvegicus | |
1.1.1.2 | 3-(benzo[b] thiophen-3-yl)-1-(4-nitrobenzyl)quinoxalin-2(1H)-one | 32% inhibition | Rattus norvegicus | |
1.1.1.2 | 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 | |
1.1.1.2 | N-(tert-butyl)-3-(4-(4-nitrobenzyl)-3-oxo-3, 4-dihydroquinoxalin-2-yl) acryl amide | 36% inhibition | Rattus norvegicus | |
1.1.1.21 | 1-(4-nitrobenzyl)-3-(4-(2-morpholinoethyl)piperazin-1-yl)quinoxalin-2(1H)-one | - |
Rattus norvegicus | |
1.1.1.21 | 1-(4-nitrobenzyl)-3-(4-(4-methoxyphenyl)piperazin-1-yl)quinoxalin-2(1H)-one | - |
Rattus norvegicus | |
1.1.1.21 | 1-(4-nitrobenzyl)-3-(4-(pyrazin-2-yl)piperazin-1-yl)quinoxalin-2(1H)-one} | - |
Rattus norvegicus | |
1.1.1.21 | 1-(4-nitrobenzyl)-3-styryl-quinoxalin-2(1H)-one | - |
Rattus norvegicus | |
1.1.1.21 | 2-(2-oxo-3-phenethylquinoxalin-1(2H)-yl)acetic acid | 22% inhibition | Rattus norvegicus | |
1.1.1.21 | 2-(2-oxo-3-styrylquinoxalin-1(2H)-yl)acetic acid | 32% inhibition | Rattus norvegicus | |
1.1.1.21 | 2-(3-(2,4-difluorophenylamino)-6-nitro-2-oxoquinoxalin-1(2H)-yl) acetic acid} | 41% inhibition | Rattus norvegicus | |
1.1.1.21 | 2-(3-(3-(tert-butylamino)-3-oxoprop-1-en-1-yl)-2-oxoquinoxalin-1(2H)-yl)acetic acid | 25% inhibition | Rattus norvegicus | |
1.1.1.21 | 2-(3-(4-(4-methoxyphenyl) piperazin-1-yl)-2-oxoquinoxalin-1(2H)-yl)acetic acid | 48% inhibition | Rattus norvegicus | |
1.1.1.21 | 2-(3-(4-fluorophenethyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid | 40% inhibition | Rattus norvegicus | |
1.1.1.21 | 2-(3-(4-fluorostyryl)-2-oxoquinoxalin-1(2H)-yl)acetic acid | 47% inhibition | Rattus norvegicus | |
1.1.1.21 | 2-(3-(4-fluorostyryl)-6-nitro-2-oxoquinoxalin-1(2H)-yl)acetic acid} | 25% inhibition | Rattus norvegicus | |
1.1.1.21 | 2-(6-chloro-3-(4-fluoro-styryl)-2-oxoquinoxalin-1(2H)-yl)acetic acid | 25% inhibition | Rattus norvegicus | |
1.1.1.21 | 2-(7-chloro-2-oxo-3-styrylquinoxalin-1(2H)-yl) acetic acid} | 35% inhibition | Rattus norvegicus | |
1.1.1.21 | 3-(4-fluorostyryl)-1-(4-nitrobenzyl)quinoxalin-2(1H)-one | - |
Rattus norvegicus | |
1.1.1.21 | 3-(benzo[b] thiophen-3-yl)-1-(4-nitrobenzylquinoxalin-2(1H)-one | - |
Rattus norvegicus | |
1.1.1.21 | 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 | |
1.1.1.21 | N-(tert-butyl)-3-(4-(4-nitrobenzyl)-3-oxo-3,4-dihydroquinoxalin-2-ylacryl amide | - |
Rattus norvegicus |
EC Number | Organism | UniProt | Comment | Textmining |
---|---|---|---|---|
1.1.1.2 | Rattus norvegicus | P51635 | - |
- |
1.1.1.2 | Rattus norvegicus Wistar | P51635 | - |
- |
1.1.1.21 | Rattus norvegicus | P07943 | - |
- |
1.1.1.21 | Rattus norvegicus Wistar | P07943 | - |
- |
EC Number | Source Tissue | Comment | Organism | Textmining |
---|---|---|---|---|
1.1.1.2 | additional information | ALR1 is present in all tissues | Rattus norvegicus | - |
EC Number | Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|---|
1.1.1.2 | D-glucuronate + NADPH + H+ | - |
Rattus norvegicus | ? + NADP+ | - |
r | |
1.1.1.2 | D-glucuronate + NADPH + H+ | - |
Rattus norvegicus Wistar | ? + NADP+ | - |
r | |
1.1.1.21 | D-glyceraldehyde + NADPH + H+ | - |
Rattus norvegicus | glycerol + NADP+ | - |
r | |
1.1.1.21 | D-glyceraldehyde + NADPH + H+ | - |
Rattus norvegicus Wistar | glycerol + NADP+ | - |
r |
EC Number | Synonyms | Comment | Organism |
---|---|---|---|
1.1.1.2 | alcohol dehydrogenase [NADP(+)] | UniProt | Rattus norvegicus |
1.1.1.2 | aldehyde reductase | - |
Rattus norvegicus |
1.1.1.2 | ALR1 | - |
Rattus norvegicus |
1.1.1.21 | ALR2 | - |
Rattus norvegicus |
EC Number | Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|---|
1.1.1.2 | 37 | - |
assay at, ALR1 | Rattus norvegicus |
1.1.1.21 | 30 | - |
assay at, ALR2 | Rattus norvegicus |
EC Number | pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|---|
1.1.1.2 | 7.2 | - |
assay at, ALR1 | Rattus norvegicus |
1.1.1.21 | 6.2 | - |
assay at, ALR2 | Rattus norvegicus |
EC Number | Cofactor | Comment | Organism | Structure |
---|---|---|---|---|
1.1.1.2 | NADPH | - |
Rattus norvegicus |
EC Number | IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|---|
1.1.1.2 | 0.000143 | - |
pH 7.2, 37°C, ALR1 | Rattus norvegicus | 2-(2-oxo-3-phenethylquinoxalin-1(2H)-yl) acetic acid | |
1.1.1.2 | 0.000283 | - |
pH 7.2, 37°C, ALR1 | Rattus norvegicus | 2-(3-(2,4-difluorophenylamino)-6-nitro-2-oxoquinoxalin-1(2H)-yl) acetic acid | |
1.1.1.2 | 0.000362 | - |
pH 7.2, 37°C, ALR1 | Rattus norvegicus | 2-(3-(4-fluorostyryl)-6-nitro-2-oxoquinoxalin-1(2H)-yl)acetic acid | |
1.1.1.2 | 0.00066 | - |
pH 7.2, 37°C, ALR1 | Rattus norvegicus | 2-(6-chloro-3-(4-fluorostyryl)-2-oxoquinoxalin-1(2H)-yl)acetic acid | |
1.1.1.2 | 0.00082 | - |
pH 7.2, 37°C, ALR1 | Rattus norvegicus | 2-(2-oxo-3-styrylquinoxalin-1(2H)-yl) acetic acid | |
1.1.1.2 | 0.00114 | - |
pH 7.2, 37°C, ALR1 | Rattus norvegicus | 2-(3-(4-fluorophenethyl)-2-oxoquinoxalin-1(2H)-yl) acetic acid | |
1.1.1.2 | 0.00143 | - |
pH 7.2, 37°C, ALR1 | Rattus norvegicus | 2-(3-(4-fluorostyryl)-2-oxoquinoxalin-1(2H)-yl) acetic acid | |
1.1.1.2 | 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 | |
1.1.1.2 | 0.00388 | - |
pH 7.2, 37°C, ALR1 | Rattus norvegicus | 2-(7-chloro-2-oxo-3-styrylquinoxalin-1(2H)-yl) acetic acid | |
1.1.1.2 | 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 |
EC Number | General Information | Comment | Organism |
---|---|---|---|
1.1.1.2 | physiological function | ALR1 is present in all tissues and plays an important role in detoxification | Rattus norvegicus |
1.1.1.21 | evolution | aldose reductase (ALR2) is a member of aldo-keto reductase superfamily | Rattus norvegicus |