Inhibitors | Comment | Organism | Structure |
---|---|---|---|
6-(2,3-dichlorobenzenesulfonyl)-2H-pyridazin-3-one | IC50: 55 nM | Rattus norvegicus | |
6-(2,3-dichlorophenylmethanesulfonyl)-2H-pyridazin-3-one | IC50: 35 nM | Rattus norvegicus | |
6-(2,3-difluorobenzenesulfonyl)-2H-pyridazin-3-one | IC50: 390 nM | Rattus norvegicus | |
6-(2,3-difluorophenylmethanesulfonyl)-2H-pyridazin-3-one | IC50: 257 nM | Rattus norvegicus | |
6-(2,4-dichlorobenzenesulfonyl)-2H-pyridazin-3-one | IC50: 190 nM | Rattus norvegicus | |
6-(2,4-dichlorophenylsulfonyl)-2H-pyridazin-3-one | - |
Rattus norvegicus | |
6-(2,4-difluorobenzenesulfonyl)-2H-pyridazin-3-one | IC50: 870 nM | Rattus norvegicus | |
6-(2,5-dichlorobenzenesulfonyl)-2H-pyridazin-3-one | IC50: 73 nM | Rattus norvegicus | |
6-(2,6-dichlorobenzenesulfonyl)-2H-pyridazin-3-one | IC50: 50 nM | Rattus norvegicus | |
6-(2,6-dichlorophenylmethanesulfonyl)-2H-pyridazin-3-one | IC50: 52 nM | Rattus norvegicus | |
6-(2-bromobenzenesulfonyl)-2H-pyridazin-3-one | IC50: 210 nM | Rattus norvegicus | |
6-(2-chloro-4-fluorobenzenesulfonyl)-2H-pyridazin-3-one | IC50: 280 nM | Rattus norvegicus | |
6-(2-chloro-6-fluorophenylmethanesulfonyl)-2H-pyridazin-3-one | IC50: 26 nM | Rattus norvegicus | |
6-(2-chlorobenzenesulfonyl)-2H-pyridazin-3-one | IC50: 170 nM | Rattus norvegicus | |
6-(2-chlorophenylmethanesulfonyl)-2H-pyridazin-3-one | IC50: 118 nM | Rattus norvegicus | |
6-(2-fluoro-3-chlorophenylmethanesulfonyl)-2H-pyridazin-3-one | IC50: 54 nM | Rattus norvegicus | |
6-(2-fluoro-3-trifluoromethylphenylmethanesulfonyl)-2H-pyridazin-3-one | IC50: 44 nM | Rattus norvegicus | |
6-(2-fluoro-4-bromophenylmethanesulfonyl)-2H-pyridazin-3-one | IC50: 667 nM | Rattus norvegicus | |
6-(2-fluorobenzenesulfonyl)-2H-pyridazin-3-one | IC50: 540 nM | Rattus norvegicus | |
6-(2-fluorophenylmethanesulfonyl)-2H-pyridazin-3-one | IC50: 422 nM | Rattus norvegicus | |
6-(2-trifluoromethylphenylmethanesulfonyl)-2H-pyridazin-3-one | IC50: 500 nM | Rattus norvegicus | |
6-(3,4-dichlorobenzenesulfonyl)-2H-pyridazin-3-one | - |
Rattus norvegicus | |
6-(3,5-dichlorobenzenesulfonyl)-2H-pyridazin-3-one | - |
Rattus norvegicus | |
6-(3,5-dimethylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one | IC50: 13 nM | Rattus norvegicus | |
6-(3-chlorobenzenesulfonyl)-2H-pyridazin-3-one | IC50: 240 nM | Rattus norvegicus | |
6-(3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one | IC50: 140 nM | Rattus norvegicus | |
6-(3-phenylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one | IC50: 23 nM | Rattus norvegicus | |
6-(3-trifluoromethylbenzenesulfonyl)-2H-pyridazin-3-one | IC50: 175 nM | Rattus norvegicus | |
6-(3-trifluoromethylphenylmethanesulfonyl)-2H-pyridazin-3-one | IC50: 72 nM | Rattus norvegicus | |
6-(3-[4-fluorophenyl]benzofuran-2-sulfonyl)-2H-pyridazin-3-one | IC50: 49 nM | Rattus norvegicus | |
6-(4-bromo-2-fluorobenzenesulfonyl)-2H-pyridazin-3-one | IC50: 140 nM | Rattus norvegicus | |
6-(4-bromobenzenesulfonyl)-2H-pyridazin-3-one | IC50: 350 nM | Rattus norvegicus | |
6-(4-chlorobenzenesulfonyl)-2H-pyridazin-3-one | IC50: 380 nM | Rattus norvegicus | |
6-(4-fluorobenzenesulfonyl)-2H-pyridazin-3-one | IC50: 474 nM | Rattus norvegicus | |
6-(4-methoxybenzenesulfonyl)-2H-pyridazin-3-one | IC50: 0.002 mM | Rattus norvegicus | |
6-(4-trifluoromethylbenzenesulfonyl)-2H-pyridazin-3-one | IC50: 360 nM | Rattus norvegicus | |
6-(5,6-methylenedioxyindole-2-sulfonyl)-2H-pyridazin-3-one | IC50: 0.0038 mM | Rattus norvegicus | |
6-(5,7-dichlorobenzofuran-2-sulfonyl)-2H-pyridazin-3-one | IC50: 87 nM | Rattus norvegicus | |
6-(5,7-dichloroindole-2-sulfonyl)-2H-pyridazin-3-one | IC50: 200 nM | Rattus norvegicus | |
6-(5-chloro-3-ethylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one | IC50: 6 nM | Rattus norvegicus | |
6-(5-chloro-3-isopropylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one | IC50: 92 nM | Rattus norvegicus | |
6-(5-chloro-3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one | IC50: 0.001 mM | Rattus norvegicus | |
6-(5-chloro-3-methylbenzothiophene-2-sulfonyl)-2H-pyridazin-3-one | IC50: 55 nM | Rattus norvegicus | |
6-(5-chloro-3-phenylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one | IC50: 34 nM | Rattus norvegicus | |
6-(5-chlorobenzofuran-2-sulfonyl)-2H-pyridazin-3-one | IC50: 25 nM | Rattus norvegicus | |
6-(5-chloroindole-2-sulfonyl)-2H-pyridazin-3-one | IC50: 0.0011 mM | Rattus norvegicus | |
6-(5-fluoro-3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one | IC50: 3 nM | Rattus norvegicus | |
6-(5-methoxybenzofuran-2-sulfonyl)-2H-pyridazin-3-one | IC50: 230 nM | Rattus norvegicus | |
6-(5-methylbenzothiophene-2-sulfonyl)-2H-pyridazin-3-one | IC50: 160 nM | Rattus norvegicus | |
6-(5-trifluoromethyl-3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one | IC50: 5 nM | Rattus norvegicus | |
6-(6-chloro-3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one | IC50: 190 nM | Rattus norvegicus | |
6-(6-chloroindole-2-sulfonyl)-2H-pyridazin-3-one | IC50: 645 nM | Rattus norvegicus | |
6-(6-fluoroindole-2-sulfonyl)-2H-pyridazin-3-one | IC50: 0.0014 mM | Rattus norvegicus | |
6-(7-chloroindole-2-sulfonyl)-2H-pyridazin-3-one | IC50: 450 nM | Rattus norvegicus | |
6-(alpha-naphthylmethylbenzenesulfonyl)-2H-pyridazin-3-one | IC50: 150 nM | Rattus norvegicus | |
6-(benzofuran-2-sulfonyl)-2H-pyridazin-3-one | IC50: 150 nM | Rattus norvegicus | |
6-(benzothiazole-2-sulfonyl)-2H-pyridazin-3-one | IC50: 450 nM | Rattus norvegicus | |
6-(benzothiophene-2-sulfonyl)-2H-pyridazin-3-one | IC50: 180 nM | Rattus norvegicus | |
6-(beta-naphthylmethylbenzenesulfonyl)-2H-pyridazin-3-one | IC50: 360 nM | Rattus norvegicus | |
6-(biphenyl-2-sulfonyl)-2H-pyridazin-3-one | IC50: 0.0022 mM | Rattus norvegicus | |
6-(indole-2-sulfonyl)-2H-pyridazin-3-one | IC50: 590 nM | Rattus norvegicus | |
8-phenylsulfonylphthalazin-2H-3-one | IC50: 55 nM | Rattus norvegicus | |
minalrestat | - |
Rattus norvegicus | |
additional information | synthesis and structure-activity relationship study of inhibitors, overview | Rattus norvegicus | |
ponalrestat | - |
Rattus norvegicus | |
ranirestat | - |
Rattus norvegicus | |
sorbinil | IC50: 140 nM | Rattus norvegicus | |
Tolrestat | - |
Rattus norvegicus | |
zopolrestat | IC50: 4 nM | Rattus norvegicus |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
aldose + NADPH + H+ | Rattus norvegicus | first and rate-limiting step in the polyol pathway, pathway network overview | alditol + NADP+ | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Rattus norvegicus | - |
diabetic rats | - |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
lens | of diabetic rats | Rattus norvegicus | - |
nerve | of diabetic rats | Rattus norvegicus | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
aldose + NADPH + H+ | - |
Rattus norvegicus | alditol + NADP+ | - |
? | |
aldose + NADPH + H+ | first and rate-limiting step in the polyol pathway, pathway network overview | Rattus norvegicus | alditol + NADP+ | - |
? |
Synonyms | Comment | Organism |
---|---|---|
aldose reductase | - |
Rattus norvegicus |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
24 | - |
assay at | Rattus norvegicus |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7 | - |
assay at | Rattus norvegicus |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
NADPH | - |
Rattus norvegicus |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.000003 | - |
IC50: 3 nM | Rattus norvegicus | 6-(5-fluoro-3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one | |
0.000004 | - |
IC50: 4 nM | Rattus norvegicus | zopolrestat | |
0.000005 | - |
IC50: 5 nM | Rattus norvegicus | 6-(5-trifluoromethyl-3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one | |
0.000006 | - |
IC50: 6 nM | Rattus norvegicus | 6-(5-chloro-3-ethylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one | |
0.000013 | - |
IC50: 13 nM | Rattus norvegicus | 6-(3,5-dimethylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one | |
0.000023 | - |
IC50: 23 nM | Rattus norvegicus | 6-(3-phenylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one | |
0.000025 | - |
IC50: 25 nM | Rattus norvegicus | 6-(5-chlorobenzofuran-2-sulfonyl)-2H-pyridazin-3-one | |
0.000026 | - |
IC50: 26 nM | Rattus norvegicus | 6-(2-chloro-6-fluorophenylmethanesulfonyl)-2H-pyridazin-3-one | |
0.000034 | - |
IC50: 34 nM | Rattus norvegicus | 6-(5-chloro-3-phenylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one | |
0.000035 | - |
IC50: 35 nM | Rattus norvegicus | 6-(2,3-dichlorophenylmethanesulfonyl)-2H-pyridazin-3-one | |
0.000044 | - |
IC50: 44 nM | Rattus norvegicus | 6-(2-fluoro-3-trifluoromethylphenylmethanesulfonyl)-2H-pyridazin-3-one | |
0.000049 | - |
IC50: 49 nM | Rattus norvegicus | 6-(3-[4-fluorophenyl]benzofuran-2-sulfonyl)-2H-pyridazin-3-one | |
0.00005 | - |
IC50: 50 nM | Rattus norvegicus | 6-(2,6-dichlorobenzenesulfonyl)-2H-pyridazin-3-one | |
0.000052 | - |
IC50: 52 nM | Rattus norvegicus | 6-(2,6-dichlorophenylmethanesulfonyl)-2H-pyridazin-3-one | |
0.000054 | - |
IC50: 54 nM | Rattus norvegicus | 6-(2-fluoro-3-chlorophenylmethanesulfonyl)-2H-pyridazin-3-one | |
0.000055 | - |
IC50: 55 nM | Rattus norvegicus | 6-(2,3-dichlorobenzenesulfonyl)-2H-pyridazin-3-one | |
0.000055 | - |
IC50: 55 nM | Rattus norvegicus | 8-phenylsulfonylphthalazin-2H-3-one | |
0.000055 | - |
IC50: 55 nM | Rattus norvegicus | 6-(5-chloro-3-methylbenzothiophene-2-sulfonyl)-2H-pyridazin-3-one | |
0.000072 | - |
IC50: 72 nM | Rattus norvegicus | 6-(3-trifluoromethylphenylmethanesulfonyl)-2H-pyridazin-3-one | |
0.000073 | - |
IC50: 73 nM | Rattus norvegicus | 6-(2,5-dichlorobenzenesulfonyl)-2H-pyridazin-3-one | |
0.000087 | - |
IC50: 87 nM | Rattus norvegicus | 6-(5,7-dichlorobenzofuran-2-sulfonyl)-2H-pyridazin-3-one | |
0.000092 | - |
IC50: 92 nM | Rattus norvegicus | 6-(5-chloro-3-isopropylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one | |
0.000118 | - |
IC50: 118 nM | Rattus norvegicus | 6-(2-chlorophenylmethanesulfonyl)-2H-pyridazin-3-one | |
0.00014 | - |
IC50: 140 nM | Rattus norvegicus | sorbinil | |
0.00014 | - |
IC50: 140 nM | Rattus norvegicus | 6-(4-bromo-2-fluorobenzenesulfonyl)-2H-pyridazin-3-one | |
0.00014 | - |
IC50: 140 nM | Rattus norvegicus | 6-(3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one | |
0.00015 | - |
IC50: 150 nM | Rattus norvegicus | 6-(alpha-naphthylmethylbenzenesulfonyl)-2H-pyridazin-3-one | |
0.00015 | - |
IC50: 150 nM | Rattus norvegicus | 6-(benzofuran-2-sulfonyl)-2H-pyridazin-3-one | |
0.00016 | - |
IC50: 160 nM | Rattus norvegicus | 6-(5-methylbenzothiophene-2-sulfonyl)-2H-pyridazin-3-one | |
0.00017 | - |
IC50: 170 nM | Rattus norvegicus | 6-(2-chlorobenzenesulfonyl)-2H-pyridazin-3-one | |
0.000175 | - |
IC50: 175 nM | Rattus norvegicus | 6-(3-trifluoromethylbenzenesulfonyl)-2H-pyridazin-3-one | |
0.00018 | - |
IC50: 180 nM | Rattus norvegicus | 6-(benzothiophene-2-sulfonyl)-2H-pyridazin-3-one | |
0.00019 | - |
IC50: 190 nM | Rattus norvegicus | 6-(2,4-dichlorobenzenesulfonyl)-2H-pyridazin-3-one | |
0.00019 | - |
IC50: 190 nM | Rattus norvegicus | 6-(6-chloro-3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one | |
0.0002 | - |
IC50: 200 nM | Rattus norvegicus | 6-(5,7-dichloroindole-2-sulfonyl)-2H-pyridazin-3-one | |
0.00021 | - |
IC50: 210 nM | Rattus norvegicus | 6-(2-bromobenzenesulfonyl)-2H-pyridazin-3-one | |
0.00023 | - |
IC50: 230 nM | Rattus norvegicus | 6-(5-methoxybenzofuran-2-sulfonyl)-2H-pyridazin-3-one | |
0.00024 | - |
IC50: 240 nM | Rattus norvegicus | 6-(3-chlorobenzenesulfonyl)-2H-pyridazin-3-one | |
0.000257 | - |
IC50: 257 nM | Rattus norvegicus | 6-(2,3-difluorophenylmethanesulfonyl)-2H-pyridazin-3-one | |
0.00028 | - |
IC50: 280 nM | Rattus norvegicus | 6-(2-chloro-4-fluorobenzenesulfonyl)-2H-pyridazin-3-one | |
0.00035 | - |
IC50: 350 nM | Rattus norvegicus | 6-(4-bromobenzenesulfonyl)-2H-pyridazin-3-one | |
0.00036 | - |
IC50: 360 nM | Rattus norvegicus | 6-(4-trifluoromethylbenzenesulfonyl)-2H-pyridazin-3-one | |
0.00036 | - |
IC50: 360 nM | Rattus norvegicus | 6-(beta-naphthylmethylbenzenesulfonyl)-2H-pyridazin-3-one | |
0.00038 | - |
IC50: 380 nM | Rattus norvegicus | 6-(4-chlorobenzenesulfonyl)-2H-pyridazin-3-one | |
0.00039 | - |
IC50: 390 nM | Rattus norvegicus | 6-(2,3-difluorobenzenesulfonyl)-2H-pyridazin-3-one | |
0.000422 | - |
IC50: 422 nM | Rattus norvegicus | 6-(2-fluorophenylmethanesulfonyl)-2H-pyridazin-3-one | |
0.00045 | - |
IC50: 450 nM | Rattus norvegicus | 6-(7-chloroindole-2-sulfonyl)-2H-pyridazin-3-one | |
0.00045 | - |
IC50: 450 nM | Rattus norvegicus | 6-(benzothiazole-2-sulfonyl)-2H-pyridazin-3-one | |
0.000474 | - |
IC50: 474 nM | Rattus norvegicus | 6-(4-fluorobenzenesulfonyl)-2H-pyridazin-3-one | |
0.0005 | - |
IC50: 500 nM | Rattus norvegicus | 6-(2-trifluoromethylphenylmethanesulfonyl)-2H-pyridazin-3-one | |
0.00054 | - |
IC50: 540 nM | Rattus norvegicus | 6-(2-fluorobenzenesulfonyl)-2H-pyridazin-3-one | |
0.00059 | - |
IC50: 590 nM | Rattus norvegicus | 6-(indole-2-sulfonyl)-2H-pyridazin-3-one | |
0.000645 | - |
IC50: 645 nM | Rattus norvegicus | 6-(6-chloroindole-2-sulfonyl)-2H-pyridazin-3-one | |
0.000667 | - |
IC50: 667 nM | Rattus norvegicus | 6-(2-fluoro-4-bromophenylmethanesulfonyl)-2H-pyridazin-3-one | |
0.00087 | - |
IC50: 870 nM | Rattus norvegicus | 6-(2,4-difluorobenzenesulfonyl)-2H-pyridazin-3-one | |
0.001 | - |
IC50: 0.001 mM | Rattus norvegicus | 6-(5-chloro-3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one | |
0.0011 | - |
IC50: 0.0011 mM | Rattus norvegicus | 6-(5-chloroindole-2-sulfonyl)-2H-pyridazin-3-one | |
0.0014 | - |
IC50: 0.0014 mM | Rattus norvegicus | 6-(6-fluoroindole-2-sulfonyl)-2H-pyridazin-3-one | |
0.002 | - |
IC50: 0.002 mM | Rattus norvegicus | 6-(4-methoxybenzenesulfonyl)-2H-pyridazin-3-one | |
0.0022 | - |
IC50: 0.0022 mM | Rattus norvegicus | 6-(biphenyl-2-sulfonyl)-2H-pyridazin-3-one | |
0.0038 | - |
IC50: 0.0038 mM | Rattus norvegicus | 6-(5,6-methylenedioxyindole-2-sulfonyl)-2H-pyridazin-3-one |