Application | Comment | Organism |
---|---|---|
medicine | inhibition of the enzyme shows benefit in neurodegenerative diseases such as Huntington's and Alzheimer's. It is a target for acute pancreatitis multiple organ dysfunction syndrome | Homo sapiens |
medicine | inhibition of the enzyme shows benefit in neurodegenerative diseases such as Huntington's and Alzheimer's. It is a target for acute pancreatitis multiple organ dysfunction syndrome (AP-MODS) | Pseudomonas fluorescens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
GSK065 | suitable for preclinical evaluation | Homo sapiens | |
GSK065 | suitable for preclinical evaluation | Pseudomonas fluorescens | |
GSK366 | suitable for preclinical evaluation | Homo sapiens | |
GSK366 | suitable for preclinical evaluation | Pseudomonas fluorescens | |
GSK428 | - |
Homo sapiens | |
GSK428 | - |
Pseudomonas fluorescens | |
GSK775 | - |
Homo sapiens | |
GSK775 | - |
Pseudomonas fluorescens | |
GSK891 | - |
Homo sapiens | |
GSK891 | - |
Pseudomonas fluorescens | |
additional information | the molecular mechanism of action of three classes of inhibitors with differentiated binding modes and kinetics is reported. Two inhibitor classes trap the catalytic flavin in a tilting conformation. This correlates with picomolar affinities, increased residence times and an absence of the peroxide production | Homo sapiens | |
additional information | the molecular mechanism of action of three classes of inhibitors with differentiated binding modes and kinetics is reported. Two inhibitor classes trap the catalytic flavin in a tilting conformation. This correlates with picomolar affinities, increased residence times and an absence of the peroxide production | Pseudomonas fluorescens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | O15229 | - |
- |
Pseudomonas fluorescens | Q84HF5 | - |
- |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
FAD | flavoprotein | Pseudomonas fluorescens | |
FAD | flavoprotein | Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.0000007 | - |
pH 7.5, temperature not specified in the publication | Pseudomonas fluorescens | GSK366 | |
0.0000023 | - |
pH 7.5, temperature not specified in the publication | Homo sapiens | GSK366 | |
0.0000027 | - |
pH 7.5, temperature not specified in the publication | Homo sapiens | GSK775 | |
0.000003 | - |
pH 7.5, temperature not specified in the publication | Pseudomonas fluorescens | GSK775 | |
0.0000036 | - |
pH 7.5, temperature not specified in the publication | Homo sapiens | GSK891 | |
0.0000043 | - |
pH 7.5, temperature not specified in the publication | Pseudomonas fluorescens | GSK891 | |
0.00001 | - |
pH 7.5, temperature not specified in the publication | Homo sapiens | GSK428 | |
0.00006 | - |
pH 7.5, temperature not specified in the publication | Pseudomonas fluorescens | GSK428 |
General Information | Comment | Organism |
---|---|---|
drug target | inhibition of the enzyme shows benefit in neurodegenerative diseases such as Huntingtons and Alzheimers. It is a target for acute pancreatitis multiple organ dysfunction syndrome | Homo sapiens |
metabolism | key enzyme of tryptophan metabolism | Pseudomonas fluorescens |
metabolism | key enzyme of tryptophan metabolism | Homo sapiens |