EC Number | Inhibitors | Comment | Organism | Structure |
---|---|---|---|---|
1.14.13.9 | (6-chloro-5,7-dimethyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)acetic acid | KMO-inhibitor 1 | Homo sapiens | |
1.14.13.9 | 1-cyclopentyl-N-(6-[4-fluoro-2-(piperidin-1-yl)phenyl]pyridazin-3-yl)methanesulfonamide | - |
Homo sapiens | |
1.14.13.9 | 2,2,2-trifluoro-N-(6-[4-fluoro-2-(piperidin-1-yl)phenyl]pyridazin-3-yl)ethane-1-sulfonamide | - |
Homo sapiens | |
1.14.13.9 | 2-(3,4-dichlorobenzoyl)cyclopropane-1-carboxylic acid | - |
Homo sapiens | |
1.14.13.9 | 3,4-dimethoxy-N-[4-(3-nitrophenyl)-1,3-thiazol-2-yl]benzene-1-sulfonamide | Ro 61-8048 | Homo sapiens | |
1.14.13.9 | 3,4-dimethoxy-N-[5-(3-nitrophenyl)-4-[(piperidin-1-yl)methyl]-1,3-thiazol-2-yl]benzene-1-sulfonamide | JM-6 | Homo sapiens | |
1.14.13.9 | 3-(5-chloro-6-[(1R)-1-(pyridin-2-yl)ethoxy]-1,2-benzoxazol-3-yl)propanoic acid | GSK-065 | Homo sapiens | |
1.14.13.9 | 4-methyl-N-(6-[2-(piperidin-1-yl)phenyl]pyridazin-3-yl)benzene-1-sulfonamide | permeable and strong KMO inhibitor | Homo sapiens | |
1.14.13.9 | 6-[4-chloro-3-(cyclopropyloxy)phenyl]pyrimidine-4-carboxylic acid | CHDI-340246 | Homo sapiens | |
1.14.13.9 | additional information | pyridazine derivatives as KMO inhibitors, structure-activity relationship, overview | Homo sapiens | |
1.14.13.9 | additional information | pyridazine derivatives as KMO inhibitors, structure-activity relationship, overview | Mus musculus | |
1.14.13.9 | N-(6-(5-fluoro-2-(piperidin-1-yl)phenyl)pyridazin-3-yl)-1-(tetrahydro-2H-pyran-4-yl)methanesulfonamide | a brain-permeable and metabolically stable kynurenine monooxygenase inhibitor. The compound exhibits high brain permeability and a long-lasting pharmacokinetics profile in monkeys. Enzyme inhibition leads to production of neuroprotective kynurenic acid in the brain | Homo sapiens | |
1.14.13.9 | N-(6-(5-fluoro-2-(piperidin-1-yl)phenyl)pyridazin-3-yl)-1-(tetrahydro-2H-pyran-4-yl)methanesulfonamide | a brain-permeable and metabolically stable kynurenine monooxygenase inhibitor. The compound exhibits high brain permeability and a long-lasting pharmacokinetics profile in monkeys, and neuroprotective kynurenic acid is increased by a single administration of the inhibitor in R6/2 mouse brain | Mus musculus | |
1.14.13.9 | N-(6-[2-fluoro-6-(piperidin-1-yl)phenyl]pyridazin-3-yl)-4-methylbenzene-1-sulfonamide | - |
Homo sapiens | |
1.14.13.9 | N-(6-[3-fluoro-2-(piperidin-1-yl)phenyl]pyridazin-3-yl)-4-methylbenzene-1-sulfonamide | - |
Homo sapiens | |
1.14.13.9 | N-(6-[4-fluoro-2-(piperidin-1-yl)phenyl]pyridazin-3-yl)-1-(oxan-2-yl)methanesulfonamide | - |
Homo sapiens | |
1.14.13.9 | N-(6-[4-fluoro-2-(piperidin-1-yl)phenyl]pyridazin-3-yl)-1-(oxan-3-yl)methanesulfonamide | - |
Homo sapiens | |
1.14.13.9 | N-(6-[4-fluoro-2-(piperidin-1-yl)phenyl]pyridazin-3-yl)-1-(oxan-4-yl)methanesulfonamide | - |
Homo sapiens | |
1.14.13.9 | N-(6-[4-fluoro-2-(piperidin-1-yl)phenyl]pyridazin-3-yl)-1-(oxolan-2-yl)methanesulfonamide | - |
Homo sapiens | |
1.14.13.9 | N-(6-[4-fluoro-2-(piperidin-1-yl)phenyl]pyridazin-3-yl)-2-methoxyethane-1-sulfonamide | - |
Homo sapiens | |
1.14.13.9 | N-(6-[4-fluoro-2-(piperidin-1-yl)phenyl]pyridazin-3-yl)-3-methoxypropane-1-sulfonamide | - |
Homo sapiens | |
1.14.13.9 | N-(6-[4-fluoro-2-(piperidin-1-yl)phenyl]pyridazin-3-yl)-4-methylbenzene-1-sulfonamide | - |
Homo sapiens | |
1.14.13.9 | N-(6-[4-fluoro-2-(piperidin-1-yl)phenyl]pyridazin-3-yl)butane-2-sulfonamide | - |
Homo sapiens | |
1.14.13.9 | N-(6-[4-fluoro-2-(piperidin-1-yl)phenyl]pyridazin-3-yl)ethanesulfonamide | - |
Homo sapiens | |
1.14.13.9 | N-(6-[4-fluoro-2-(piperidin-1-yl)phenyl]pyridazin-3-yl)propane-1-sulfonamide | - |
Homo sapiens | |
1.14.13.9 | N-(6-[5-fluoro-2-(piperidin-1-yl)phenyl]pyridazin-3-yl)-4-methylbenzene-1-sulfonamide | - |
Homo sapiens |
EC Number | Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|---|
1.14.13.9 | membrane | - |
Homo sapiens | 16020 | - |
1.14.13.9 | membrane | - |
Mus musculus | 16020 | - |
1.14.13.9 | microsome | - |
Homo sapiens | - |
- |
1.14.13.9 | microsome | - |
Mus musculus | - |
- |
EC Number | Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|---|
1.14.13.9 | L-kynurenine + NADPH + H+ + O2 | Homo sapiens | - |
3-hydroxy-L-kynurenine + NADP+ + H2O | - |
? | |
1.14.13.9 | L-kynurenine + NADPH + H+ + O2 | Mus musculus | - |
3-hydroxy-L-kynurenine + NADP+ + H2O | - |
? |
EC Number | Organism | UniProt | Comment | Textmining |
---|---|---|---|---|
1.14.13.9 | Homo sapiens | O15229 | - |
- |
1.14.13.9 | Mus musculus | Q91WN4 | - |
- |
EC Number | Source Tissue | Comment | Organism | Textmining |
---|---|---|---|---|
1.14.13.9 | brain | - |
Homo sapiens | - |
1.14.13.9 | brain | - |
Mus musculus | - |
1.14.13.9 | liver | - |
Homo sapiens | - |
1.14.13.9 | liver | - |
Mus musculus | - |
EC Number | Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|---|
1.14.13.9 | L-kynurenine + NADPH + H+ + O2 | - |
Homo sapiens | 3-hydroxy-L-kynurenine + NADP+ + H2O | - |
? | |
1.14.13.9 | L-kynurenine + NADPH + H+ + O2 | - |
Mus musculus | 3-hydroxy-L-kynurenine + NADP+ + H2O | - |
? |
EC Number | Synonyms | Comment | Organism |
---|---|---|---|
1.14.13.9 | KMO | - |
Homo sapiens |
1.14.13.9 | KMO | - |
Mus musculus |
EC Number | Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|---|
1.14.13.9 | 37 | - |
assay at | Homo sapiens |
1.14.13.9 | 37 | - |
assay at | Mus musculus |
EC Number | Cofactor | Comment | Organism | Structure |
---|---|---|---|---|
1.14.13.9 | FAD | - |
Homo sapiens | |
1.14.13.9 | FAD | - |
Mus musculus | |
1.14.13.9 | NADPH | - |
Homo sapiens | |
1.14.13.9 | NADPH | - |
Mus musculus |
EC Number | IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|---|
1.14.13.9 | 0.0000005 | - |
pH not specified in the publication, 37°C | Homo sapiens | 6-[4-chloro-3-(cyclopropyloxy)phenyl]pyrimidine-4-carboxylic acid | |
1.14.13.9 | 0.0000023 | - |
pH not specified in the publication, 37°C | Homo sapiens | 3-(5-chloro-6-[(1R)-1-(pyridin-2-yl)ethoxy]-1,2-benzoxazol-3-yl)propanoic acid | |
1.14.13.9 | 0.0000024 | - |
pH not specified in the publication, 37°C | Homo sapiens | 4-methyl-N-(6-[2-(piperidin-1-yl)phenyl]pyridazin-3-yl)benzene-1-sulfonamide | |
1.14.13.9 | 0.0000042 | - |
pH not specified in the publication, 37°C | Homo sapiens | N-(6-[5-fluoro-2-(piperidin-1-yl)phenyl]pyridazin-3-yl)-4-methylbenzene-1-sulfonamide | |
1.14.13.9 | 0.0000061 | - |
pH not specified in the publication, 37°C | Homo sapiens | N-(6-[2-fluoro-6-(piperidin-1-yl)phenyl]pyridazin-3-yl)-4-methylbenzene-1-sulfonamide | |
1.14.13.9 | 0.0000091 | - |
pH not specified in the publication, 37°C | Homo sapiens | N-(6-[4-fluoro-2-(piperidin-1-yl)phenyl]pyridazin-3-yl)-4-methylbenzene-1-sulfonamide | |
1.14.13.9 | 0.0000128 | - |
pH not specified in the publication, 37°C | Homo sapiens | N-(6-[4-fluoro-2-(piperidin-1-yl)phenyl]pyridazin-3-yl)-1-(oxan-4-yl)methanesulfonamide | |
1.14.13.9 | 0.0000179 | - |
pH not specified in the publication, 37°C | Homo sapiens | N-(6-[4-fluoro-2-(piperidin-1-yl)phenyl]pyridazin-3-yl)-1-(oxan-3-yl)methanesulfonamide | |
1.14.13.9 | 0.0000272 | - |
pH not specified in the publication, 37°C | Homo sapiens | N-(6-[4-fluoro-2-(piperidin-1-yl)phenyl]pyridazin-3-yl)butane-2-sulfonamide | |
1.14.13.9 | 0.0000286 | - |
pH not specified in the publication, 37°C | Homo sapiens | 1-cyclopentyl-N-(6-[4-fluoro-2-(piperidin-1-yl)phenyl]pyridazin-3-yl)methanesulfonamide | |
1.14.13.9 | 0.000034 | - |
pH not specified in the publication, 37°C | Homo sapiens | 3,4-dimethoxy-N-[4-(3-nitrophenyl)-1,3-thiazol-2-yl]benzene-1-sulfonamide | |
1.14.13.9 | 0.0000341 | - |
pH not specified in the publication, 37°C | Homo sapiens | N-(6-[4-fluoro-2-(piperidin-1-yl)phenyl]pyridazin-3-yl)-1-(oxan-2-yl)methanesulfonamide | |
1.14.13.9 | 0.0000371 | - |
pH not specified in the publication, 37°C | Homo sapiens | N-(6-[4-fluoro-2-(piperidin-1-yl)phenyl]pyridazin-3-yl)propane-1-sulfonamide | |
1.14.13.9 | 0.0000387 | - |
pH not specified in the publication, 37°C | Homo sapiens | 2,2,2-trifluoro-N-(6-[4-fluoro-2-(piperidin-1-yl)phenyl]pyridazin-3-yl)ethane-1-sulfonamide | |
1.14.13.9 | 0.000041 | - |
pH not specified in the publication, 37°C | Homo sapiens | N-(6-[4-fluoro-2-(piperidin-1-yl)phenyl]pyridazin-3-yl)-1-(oxolan-2-yl)methanesulfonamide | |
1.14.13.9 | 0.0000616 | - |
pH not specified in the publication, 37°C | Homo sapiens | N-(6-[4-fluoro-2-(piperidin-1-yl)phenyl]pyridazin-3-yl)-3-methoxypropane-1-sulfonamide | |
1.14.13.9 | 0.0000839 | - |
pH not specified in the publication, 37°C | Homo sapiens | N-(6-[4-fluoro-2-(piperidin-1-yl)phenyl]pyridazin-3-yl)-2-methoxyethane-1-sulfonamide | |
1.14.13.9 | 0.000116 | - |
pH not specified in the publication, 37°C | Homo sapiens | N-(6-[4-fluoro-2-(piperidin-1-yl)phenyl]pyridazin-3-yl)ethanesulfonamide | |
1.14.13.9 | 0.02 | - |
pH not specified in the publication, 37°C | Homo sapiens | 3,4-dimethoxy-N-[5-(3-nitrophenyl)-4-[(piperidin-1-yl)methyl]-1,3-thiazol-2-yl]benzene-1-sulfonamide | |
1.14.13.9 | 0.02 | - |
pH not specified in the publication, 37°C | Homo sapiens | N-(6-[3-fluoro-2-(piperidin-1-yl)phenyl]pyridazin-3-yl)-4-methylbenzene-1-sulfonamide |