Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(6-chloro-5,7-dimethyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)acetic acid | KMO-inhibitor 1 | Homo sapiens | |
1-cyclopentyl-N-(6-[4-fluoro-2-(piperidin-1-yl)phenyl]pyridazin-3-yl)methanesulfonamide | - |
Homo sapiens | |
2,2,2-trifluoro-N-(6-[4-fluoro-2-(piperidin-1-yl)phenyl]pyridazin-3-yl)ethane-1-sulfonamide | - |
Homo sapiens | |
2-(3,4-dichlorobenzoyl)cyclopropane-1-carboxylic acid | - |
Homo sapiens | |
3,4-dimethoxy-N-[4-(3-nitrophenyl)-1,3-thiazol-2-yl]benzene-1-sulfonamide | Ro 61-8048 | Homo sapiens | |
3,4-dimethoxy-N-[5-(3-nitrophenyl)-4-[(piperidin-1-yl)methyl]-1,3-thiazol-2-yl]benzene-1-sulfonamide | JM-6 | Homo sapiens | |
3-(5-chloro-6-[(1R)-1-(pyridin-2-yl)ethoxy]-1,2-benzoxazol-3-yl)propanoic acid | GSK-065 | Homo sapiens | |
4-methyl-N-(6-[2-(piperidin-1-yl)phenyl]pyridazin-3-yl)benzene-1-sulfonamide | permeable and strong KMO inhibitor | Homo sapiens | |
6-[4-chloro-3-(cyclopropyloxy)phenyl]pyrimidine-4-carboxylic acid | CHDI-340246 | Homo sapiens | |
additional information | pyridazine derivatives as KMO inhibitors, structure-activity relationship, overview | Homo sapiens | |
additional information | pyridazine derivatives as KMO inhibitors, structure-activity relationship, overview | Mus musculus | |
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 | |
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 | |
N-(6-[2-fluoro-6-(piperidin-1-yl)phenyl]pyridazin-3-yl)-4-methylbenzene-1-sulfonamide | - |
Homo sapiens | |
N-(6-[3-fluoro-2-(piperidin-1-yl)phenyl]pyridazin-3-yl)-4-methylbenzene-1-sulfonamide | - |
Homo sapiens | |
N-(6-[4-fluoro-2-(piperidin-1-yl)phenyl]pyridazin-3-yl)-1-(oxan-2-yl)methanesulfonamide | - |
Homo sapiens | |
N-(6-[4-fluoro-2-(piperidin-1-yl)phenyl]pyridazin-3-yl)-1-(oxan-3-yl)methanesulfonamide | - |
Homo sapiens | |
N-(6-[4-fluoro-2-(piperidin-1-yl)phenyl]pyridazin-3-yl)-1-(oxan-4-yl)methanesulfonamide | - |
Homo sapiens | |
N-(6-[4-fluoro-2-(piperidin-1-yl)phenyl]pyridazin-3-yl)-1-(oxolan-2-yl)methanesulfonamide | - |
Homo sapiens | |
N-(6-[4-fluoro-2-(piperidin-1-yl)phenyl]pyridazin-3-yl)-2-methoxyethane-1-sulfonamide | - |
Homo sapiens | |
N-(6-[4-fluoro-2-(piperidin-1-yl)phenyl]pyridazin-3-yl)-3-methoxypropane-1-sulfonamide | - |
Homo sapiens | |
N-(6-[4-fluoro-2-(piperidin-1-yl)phenyl]pyridazin-3-yl)-4-methylbenzene-1-sulfonamide | - |
Homo sapiens | |
N-(6-[4-fluoro-2-(piperidin-1-yl)phenyl]pyridazin-3-yl)butane-2-sulfonamide | - |
Homo sapiens | |
N-(6-[4-fluoro-2-(piperidin-1-yl)phenyl]pyridazin-3-yl)ethanesulfonamide | - |
Homo sapiens | |
N-(6-[4-fluoro-2-(piperidin-1-yl)phenyl]pyridazin-3-yl)propane-1-sulfonamide | - |
Homo sapiens | |
N-(6-[5-fluoro-2-(piperidin-1-yl)phenyl]pyridazin-3-yl)-4-methylbenzene-1-sulfonamide | - |
Homo sapiens |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
membrane | - |
Homo sapiens | 16020 | - |
membrane | - |
Mus musculus | 16020 | - |
microsome | - |
Homo sapiens | - |
- |
microsome | - |
Mus musculus | - |
- |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
L-kynurenine + NADPH + H+ + O2 | Homo sapiens | - |
3-hydroxy-L-kynurenine + NADP+ + H2O | - |
? | |
L-kynurenine + NADPH + H+ + O2 | Mus musculus | - |
3-hydroxy-L-kynurenine + NADP+ + H2O | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | O15229 | - |
- |
Mus musculus | Q91WN4 | - |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
brain | - |
Homo sapiens | - |
brain | - |
Mus musculus | - |
liver | - |
Homo sapiens | - |
liver | - |
Mus musculus | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
L-kynurenine + NADPH + H+ + O2 | - |
Homo sapiens | 3-hydroxy-L-kynurenine + NADP+ + H2O | - |
? | |
L-kynurenine + NADPH + H+ + O2 | - |
Mus musculus | 3-hydroxy-L-kynurenine + NADP+ + H2O | - |
? |
Synonyms | Comment | Organism |
---|---|---|
KMO | - |
Homo sapiens |
KMO | - |
Mus musculus |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
assay at | Homo sapiens |
37 | - |
assay at | Mus musculus |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
FAD | - |
Homo sapiens | |
FAD | - |
Mus musculus | |
NADPH | - |
Homo sapiens | |
NADPH | - |
Mus musculus |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.0000005 | - |
pH not specified in the publication, 37°C | Homo sapiens | 6-[4-chloro-3-(cyclopropyloxy)phenyl]pyrimidine-4-carboxylic acid | |
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 | |
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 | |
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 | |
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 | |
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 | |
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 | |
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 | |
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 | |
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 | |
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 | |
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 | |
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 | |
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 | |
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 | |
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 | |
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 | |
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 | |
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 | |
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 |