Application | Comment | Organism |
---|---|---|
drug development | the enzyme is a promising therapeutic target of cancer | Homo sapiens |
Cloned (Comment) | Organism |
---|---|
expression in Escherichia coli | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
1-methyl-tryptophan | competitive | Homo sapiens | |
1H-benzotriazole | - |
Homo sapiens | |
3-(1H-1,2,3-triazol-5-yl)pyridine | - |
Homo sapiens | |
4-bromo-5-(4-methylphenyl)-1H-1,2,3-triazole | - |
Homo sapiens | |
4-iodo-5-phenyl-1H-1,2,3-triazole | - |
Homo sapiens | |
4-nitro-5-(4-nitrophenyl)-1H-1,2,3-triazole | - |
Homo sapiens | |
5-(2-bromophenyl)-1H-1,2,3-triazole | - |
Homo sapiens | |
5-(2-chlorophenyl)-1H-1,2,3-triazole | - |
Homo sapiens | |
5-(2-methoxyphenyl)-1H-1,2,3-triazole | - |
Homo sapiens | |
5-(4-bromophenyl)-1H-1,2,3-triazole | - |
Homo sapiens | |
5-(4-chlorophenyl)-1H-1,2,3-triazole | - |
Homo sapiens | |
5-(4-fluorophenyl)-1H-1,2,3-triazole | - |
Homo sapiens | |
5-(4-methoxyphenyl)-1H-1,2,3-triazole | - |
Homo sapiens | |
5-phenyl-1H-1,2,3-triazole | - |
Homo sapiens | |
ethyl 1-(4-chlorophenyl)-1H-1,2,3-triazole-4-carboxylate | - |
Homo sapiens | |
additional information | structure-activity relationship and enzyme kinetics of 4-aryl-1H-1,2,3-triazoles as indoleamine 2,3-dioxygenase inhibitors, molecular docking studies, overview. An electron-withdrawing group with low steric hindrance near the NH group of triazoles is necessary for the IDO inhibition. No inhibition by 5-(4-methylphenyl)-1H-1,2,3-triazole, methyl 4-(1H-1,2,3-triazol-5-yl)benzoate, 4-bromo-5-phenyl-1H-1,2,3-triazole, 4-chloro-5-phenyl-1H-1,2,3-triazole, 1H-benzotriazol-1-ol, and 5-(4-bromophenyl)-1H-tetrazole | Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
D-tryptophan + O2 | Homo sapiens | - |
N-formyl-D-kynurenine | - |
? | |
L-tryptophan + O2 | Homo sapiens | - |
N-formyl-L-kynurenine | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
HEK-293 cell | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
D-tryptophan + O2 | - |
Homo sapiens | N-formyl-D-kynurenine | - |
? | |
L-tryptophan + O2 | - |
Homo sapiens | N-formyl-L-kynurenine | - |
? |
Synonyms | Comment | Organism |
---|---|---|
IDO | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
assay at | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
6.5 | - |
assay at | Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.0145 | - |
5-(2-chlorophenyl)-1H-1,2,3-triazole | pH 6.5, 37°C, recombinant enzyme | Homo sapiens | |
0.018 | - |
5-(2-bromophenyl)-1H-1,2,3-triazole | pH 6.5, 37°C, recombinant enzyme | Homo sapiens | |
0.0225 | - |
5-phenyl-1H-1,2,3-triazole | pH 6.5, 37°C, recombinant enzyme | Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.086 | - |
pH 6.5, 37°C, recombinant enzyme | Homo sapiens | 5-(2-chlorophenyl)-1H-1,2,3-triazole | |
0.143 | - |
pH 6.5, 37°C, recombinant enzyme | Homo sapiens | 5-phenyl-1H-1,2,3-triazole | |
0.148 | - |
pH 6.5, 37°C, recombinant enzyme | Homo sapiens | 5-(2-bromophenyl)-1H-1,2,3-triazole | |
0.533 | - |
pH 6.5, 37°C, recombinant enzyme | Homo sapiens | 4-nitro-5-(4-nitrophenyl)-1H-1,2,3-triazole | |
0.58 | - |
pH 6.5, 37°C, recombinant enzyme | Homo sapiens | 5-(4-fluorophenyl)-1H-1,2,3-triazole | |
0.708 | - |
pH 6.5, 37°C, recombinant enzyme | Homo sapiens | 3-(1H-1,2,3-triazol-5-yl)pyridine | |
0.817 | - |
pH 6.5, 37°C, recombinant enzyme | Homo sapiens | 5-(4-chlorophenyl)-1H-1,2,3-triazole | |
1.028 | - |
pH 6.5, 37°C, recombinant enzyme | Homo sapiens | 5-(2-methoxyphenyl)-1H-1,2,3-triazole | |
1.028 | - |
pH 6.5, 37°C, recombinant enzyme | Homo sapiens | 4-bromo-5-(4-methylphenyl)-1H-1,2,3-triazole | |
1.256 | - |
pH 6.5, 37°C, recombinant enzyme | Homo sapiens | 5-(4-bromophenyl)-1H-1,2,3-triazole | |
1.371 | - |
pH 6.5, 37°C, recombinant enzyme | Homo sapiens | 4-iodo-5-phenyl-1H-1,2,3-triazole | |
2 | - |
pH 6.5, 37°C, recombinant enzyme | Homo sapiens | ethyl 1-(4-chlorophenyl)-1H-1,2,3-triazole-4-carboxylate | |
2.57 | - |
pH 6.5, 37°C, recombinant enzyme | Homo sapiens | 1H-benzotriazole | |
6 | - |
pH 6.5, 37°C, recombinant enzyme | Homo sapiens | 5-(4-methoxyphenyl)-1H-1,2,3-triazole |