Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(6-chloro-5,7-dimethyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)acetic acid | - |
Mus musculus | |
2-(3,4-dichlorobenzoyl)cyclopropane-1-carboxylic acid | PNU-168754 | Mus musculus | |
3,4-dimethoxy-N-[4-(3-nitrophenyl)-1,3-thiazol-2-yl]benzene-1-sulfonamide | Ro-61-8048 | Mus musculus | |
3,4-dimethoxy-N-[5-(3-nitrophenyl)-4-[(piperidin-1-yl)methyl]-1,3-thiazol-2-yl]benzene-1-sulfonamide | JM-6 | Mus musculus | |
3-(5-chloro-6-[(1R)-1-(pyridin-2-yl)ethoxy]-1,2-benzoxazol-3-yl)propanoic acid | GSK-065 | Mus musculus | |
3-(dimethylamino)-N-(6-[2-(pyrrolidin-1-yl)phenyl]pyridazin-3-yl)benzene-1-sulfonamide | - |
Mus musculus | |
4-methyl-N-(6-[2-(4-methylpiperazin-1-yl)phenyl]pyridazin-3-yl)benzene-1-sulfonamide | - |
Mus musculus | |
4-methyl-N-(6-[2-(morpholin-4-yl)phenyl]pyridazin-3-yl)benzene-1-sulfonamide | - |
Mus musculus | |
4-methyl-N-(6-[2-(piperidin-1-yl)phenyl]pyridazin-3-yl)benzene-1-sulfonamide | - |
Mus musculus | |
4-methyl-N-(6-[2-(pyrrolidin-1-yl)phenyl]pyridazin-3-yl)benzene-1-sulfonamide | - |
Mus musculus | |
4-methyl-N-[6-(1-methyl-1H-indol-7-yl)pyridazin-3-yl]benzene-1-sulfonamide | - |
Mus musculus | |
4-methyl-N-[6-(1-methyl-2,3-dihydro-1H-indol-7-yl)pyridazin-3-yl]benzene-1-sulfonamide | - |
Mus musculus | |
4-methyl-N-[6-(quinolin-8-yl)pyridazin-3-yl]benzene-1-sulfonamide | - |
Mus musculus | |
6-[4-chloro-3-(cyclopropyloxy)phenyl]pyrimidine-4-carboxylic acid | CHDI-340246 | Mus musculus | |
CHDI-340246 | - |
Mus musculus | |
additional information | synthesis and evaluation of enzyme inhibitors | Mus musculus | |
N-(6-[2-(dimethylamino)phenyl]pyridazin-3-yl)-4-methylbenzene-1-sulfonamide | - |
Mus musculus | |
N-(6-[3-(dimethylamino)phenyl]pyridazin-3-yl)-4-methylbenzene-1-sulfonamide | - |
Mus musculus | |
N-(6-[4-(dimethylamino)phenyl]pyridazin-3-yl)-4-methylbenzene-1-sulfonamide | - |
Mus musculus | |
N-[6-(2-ethylphenyl)pyridazin-3-yl]-4-methylbenzene-1-sulfonamide | - |
Mus musculus | |
N-[6-(2-methoxyphenyl)pyridazin-3-yl]-4-methylbenzene-1-sulfonamide | - |
Mus musculus | |
N-[6-(3-chlorophenyl)pyridazin-3-yl]-2-(dimethylamino)benzene-1-sulfonamide | - |
Mus musculus | |
N-[6-(3-chlorophenyl)pyridazin-3-yl]-3-(dimethylamino)benzene-1-sulfonamide | - |
Mus musculus | |
N-[6-(3-chlorophenyl)pyridazin-3-yl]-3-methylbenzene-1-sulfonamide | - |
Mus musculus | |
N-[6-(3-chlorophenyl)pyridazin-3-yl]-4-(dimethylamino)benzene-1-sulfonamide | - |
Mus musculus | |
N-[6-(3-chlorophenyl)pyridazin-3-yl]pyridine-2-sulfonamide | - |
Mus musculus | |
N-[6-(3-chlorophenyl)pyridazin-3-yl]pyridine-3-sulfonamide | - |
Mus musculus | |
N-[6-(isoquinolin-8-yl)pyridazin-3-yl]-4-methylbenzene-1-sulfonamide | - |
Mus musculus |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
microsome | - |
Mus musculus | - |
- |
mitochondrial membrane | - |
Mus musculus | 31966 | - |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
L-kynurenine + NADPH + H+ + O2 | Mus musculus | - |
3-hydroxy-L-kynurenine + NADP+ + H2O | - |
? | |
L-kynurenine + NADPH + H+ + O2 | Mus musculus R6/2 | - |
3-hydroxy-L-kynurenine + NADP+ + H2O | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Mus musculus | Q91WN4 | - |
- |
Mus musculus R6/2 | Q91WN4 | - |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
brain | - |
Mus musculus | - |
liver | - |
Mus musculus | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
L-kynurenine + NADPH + H+ + O2 | - |
Mus musculus | 3-hydroxy-L-kynurenine + NADP+ + H2O | - |
? | |
L-kynurenine + NADPH + H+ + O2 | - |
Mus musculus R6/2 | 3-hydroxy-L-kynurenine + NADP+ + H2O | - |
? |
Synonyms | Comment | Organism |
---|---|---|
KMO | - |
Mus musculus |
kynurenine monooxygenase | - |
Mus musculus |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
FAD | - |
Mus musculus | |
NADPH | - |
Mus musculus |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.0000005 | - |
pH and temperature not specified in the publication | Mus musculus | 6-[4-chloro-3-(cyclopropyloxy)phenyl]pyrimidine-4-carboxylic acid | |
0.0000014 | - |
brain enzyme, pH and temperature not specified in the publication | Mus musculus | 4-methyl-N-(6-[2-(piperidin-1-yl)phenyl]pyridazin-3-yl)benzene-1-sulfonamide | |
0.0000023 | - |
pH and temperature not specified in the publication | Mus musculus | 3-(5-chloro-6-[(1R)-1-(pyridin-2-yl)ethoxy]-1,2-benzoxazol-3-yl)propanoic acid | |
0.0000026 | - |
brain enzyme, pH and temperature not specified in the publication | Mus musculus | (6-chloro-5,7-dimethyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)acetic acid | |
0.0000027 | - |
brain enzyme, pH and temperature not specified in the publication | Mus musculus | 4-methyl-N-(6-[2-(pyrrolidin-1-yl)phenyl]pyridazin-3-yl)benzene-1-sulfonamide | |
0.0000033 | - |
brain enzyme, pH and temperature not specified in the publication | Mus musculus | 3-(dimethylamino)-N-(6-[2-(pyrrolidin-1-yl)phenyl]pyridazin-3-yl)benzene-1-sulfonamide | |
0.0000039 | - |
brain enzyme, pH and temperature not specified in the publication | Mus musculus | 4-methyl-N-(6-[2-(morpholin-4-yl)phenyl]pyridazin-3-yl)benzene-1-sulfonamide | |
0.0000045 | - |
brain enzyme, pH and temperature not specified in the publication | Mus musculus | N-(6-[2-(dimethylamino)phenyl]pyridazin-3-yl)-4-methylbenzene-1-sulfonamide | |
0.0000087 | - |
brain enzyme, pH and temperature not specified in the publication | Mus musculus | 4-methyl-N-[6-(quinolin-8-yl)pyridazin-3-yl]benzene-1-sulfonamide | |
0.0000169 | - |
brain enzyme, pH and temperature not specified in the publication | Mus musculus | 4-methyl-N-[6-(1-methyl-2,3-dihydro-1H-indol-7-yl)pyridazin-3-yl]benzene-1-sulfonamide | |
0.0000291 | - |
brain enzyme, pH and temperature not specified in the publication | Mus musculus | 4-methyl-N-[6-(1-methyl-1H-indol-7-yl)pyridazin-3-yl]benzene-1-sulfonamide | |
0.0000292 | - |
brain enzyme, pH and temperature not specified in the publication | Mus musculus | N-[6-(2-ethylphenyl)pyridazin-3-yl]-4-methylbenzene-1-sulfonamide | |
0.0000317 | - |
brain enzyme, pH and temperature not specified in the publication | Mus musculus | N-[6-(3-chlorophenyl)pyridazin-3-yl]-3-(dimethylamino)benzene-1-sulfonamide | |
0.000034 | - |
pH and temperature not specified in the publication | Mus musculus | 3,4-dimethoxy-N-[4-(3-nitrophenyl)-1,3-thiazol-2-yl]benzene-1-sulfonamide | |
0.0000365 | - |
brain enzyme, pH and temperature not specified in the publication | Mus musculus | N-[6-(2-methoxyphenyl)pyridazin-3-yl]-4-methylbenzene-1-sulfonamide | |
0.00004 | - |
pH and temperature not specified in the publication | Mus musculus | 2-(3,4-dichlorobenzoyl)cyclopropane-1-carboxylic acid | |
0.0000472 | - |
brain enzyme, pH and temperature not specified in the publication | Mus musculus | N-[6-(isoquinolin-8-yl)pyridazin-3-yl]-4-methylbenzene-1-sulfonamide | |
0.0000825 | - |
brain enzyme, pH and temperature not specified in the publication | Mus musculus | N-(6-[3-(dimethylamino)phenyl]pyridazin-3-yl)-4-methylbenzene-1-sulfonamide | |
0.0001 | - |
brain enzyme, pH and temperature not specified in the publication | Mus musculus | 4-methyl-N-(6-[2-(4-methylpiperazin-1-yl)phenyl]pyridazin-3-yl)benzene-1-sulfonamide | |
0.000101 | - |
brain enzyme, pH and temperature not specified in the publication | Mus musculus | N-[6-(3-chlorophenyl)pyridazin-3-yl]-3-methylbenzene-1-sulfonamide | |
0.000118 | - |
brain enzyme, pH and temperature not specified in the publication | Mus musculus | N-[6-(3-chlorophenyl)pyridazin-3-yl]-2-(dimethylamino)benzene-1-sulfonamide | |
0.000402 | - |
brain enzyme, pH and temperature not specified in the publication | Mus musculus | N-[6-(3-chlorophenyl)pyridazin-3-yl]-4-(dimethylamino)benzene-1-sulfonamide | |
0.000546 | - |
brain enzyme, pH and temperature not specified in the publication | Mus musculus | N-(6-[4-(dimethylamino)phenyl]pyridazin-3-yl)-4-methylbenzene-1-sulfonamide | |
0.02 | - |
pH and temperature not specified in the publication | Mus musculus | 3,4-dimethoxy-N-[5-(3-nitrophenyl)-4-[(piperidin-1-yl)methyl]-1,3-thiazol-2-yl]benzene-1-sulfonamide |
General Information | Comment | Organism |
---|---|---|
malfunction | kynurenine monooxygenase (KMO) is the ideal target for an inhibitor because its inhibition is expected to reduce the toxic metabolites and increase kynurenic acid (KYNA), which is neuroprotective. KMO inhibitors can correct the 3-HK/KYNA unbalance | Mus musculus |
physiological function | the kynurenine pathway (KP) is the major route for tryptophan metabolism in mammals. Several metabolites in the KP, however, are potentially toxic, particularly 3-hydroxykynurenine (3-HK) and quinolinic acid (QA). QA is an excitotoxic agonist at the NMDA receptor, and 3-HK and QA are reported to increase in Huntington's disease (HD) | Mus musculus |