Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(1R,2S)-2-([[6-(trifluoromethyl)-1H-indazol-4-yl]amino]methyl)cyclohexan-1-ol | - |
Homo sapiens | |
(1R,2S)-2-[[(5-bromo-1H-indazol-4-yl)amino]methyl]cyclohexan-1-ol | - |
Homo sapiens | |
(1R,2S)-2-[[(5-bromo-1H-indazol-7-yl)amino]methyl]cyclohexan-1-ol | - |
Homo sapiens | |
(1R,2S)-2-[[(5-chloro-1H-indazol-7-yl)amino]methyl]cyclohexan-1-ol | - |
Homo sapiens | |
(1R,2S)-2-[[(6-bromo-1-methyl-1H-indazol-4-yl)amino]methyl]cyclohexan-1-ol | - |
Homo sapiens | |
(1R,2S)-2-[[(6-bromo-1H-indazol-4-yl)amino]methyl]cyclohexan-1-ol | - |
Homo sapiens | |
(1R,2S)-2-[[(6-bromo-1H-indazol-4-yl)amino]methyl]cyclohexyl acetate | - |
Homo sapiens | |
(1R,2S)-2-[[(6-chloro-1H-indazol-4-yl)amino]methyl]cyclohexan-1-ol | - |
Homo sapiens | |
(1R,2S)-2-[[(6-methyl-1H-indazol-4-yl)amino]methyl]cyclohexan-1-ol | - |
Homo sapiens | |
(1S,2R)-2-[[(6-bromo-1H-indazol-4-yl)amino]methyl]cyclohexan-1-ol | - |
Homo sapiens | |
1-cyclohexyl-2-(5H-imidazo[5,1-a]isoindol-5-yl)ethan-1-ol | - |
Homo sapiens | |
2-[(6-bromo-1H-indazol-4-yl)amino]-1-(3-chlorophenyl)ethan-1-ol | - |
Homo sapiens | |
2-[(6-bromo-1H-indazol-4-yl)amino]-1-(4-hydroxyphenyl)ethan-1-one | - |
Homo sapiens | |
2-[(6-bromo-1H-indazol-4-yl)amino]-2-(3-chlorophenyl)ethan-1-ol | - |
Homo sapiens | |
2-[(6-bromo-1H-indazol-4-yl)amino]-2-phenylethan-1-ol | - |
Homo sapiens | |
2-[[(6-bromo-1H-indazol-4-yl)amino]methyl]cyclohexan-1-ol | - |
Homo sapiens | |
4-([[(1S,2R)-2-hydroxycyclohexyl]methyl]amino)-1H-indazole-6-carboxylic acid | - |
Homo sapiens | |
4-[(1Z)-2-[(6-bromo-1H-indazol-4-yl)amino]-N-hydroxyethanimidoyl]phenol | - |
Homo sapiens | |
4-[[(6-bromo-1H-indazol-4-yl)amino]methyl]phenol | - |
Homo sapiens | |
6-bromo-1H-indazol-4-amine | - |
Homo sapiens | |
6-bromo-N-(cyclohexylmethyl)-1H-indazol-4-amine | - |
Homo sapiens | |
6-bromo-N-[(1,4-dioxaspiro[4.5]decan-6-yl)methyl]-1H-indazol-4-amine | - |
Homo sapiens | |
6-bromo-N-[(1R,2R)-2-hydroxycyclohexyl]-1H-indazole-4-carboxamide | - |
Homo sapiens | |
6-bromo-N-[(pyridin-2-yl)methyl]-1H-indazol-4-amine | - |
Homo sapiens | |
6-bromo-N-[(pyrrolidin-3-yl)methyl]-1H-indazol-4-amine | - |
Homo sapiens | |
6-bromo-N-[[(1S,2S)-2-chlorocyclohexyl]methyl]-1H-indazol-4-amine | - |
Homo sapiens | |
6-bromo-N-[[(2R)-piperidin-2-yl]methyl]-1H-indazol-4-amine | - |
Homo sapiens | |
6-bromo-N-[[(2R)-pyrrolidin-2-yl]methyl]-1H-indazol-4-amine | - |
Homo sapiens | |
6-bromo-N-[[(2S)-piperidin-2-yl]methyl]-1H-indazol-4-amine | - |
Homo sapiens | |
6-bromo-N-[[(2S)-pyrrolidin-2-yl]methyl]-1H-indazol-4-amine | - |
Homo sapiens | |
methyl 4-([[(1S,2R)-2-hydroxycyclohexyl]methyl]amino)-1H-indazole-6-carboxylate | - |
Homo sapiens | |
additional information | 1H-indazole-4-amines inhibit both human indoleamine 2,3-dioxygenase 1 (hIDO1) and tryptophan 2,3-dioxygenase (hTDO) by a mechanism involving direct coordination with the heme ferrous and ferric states | Homo sapiens | |
N-(3-bromo-4-fluorophenyl)-N'-hydroxy-4-[[2-(sulfamoylamino)ethyl]amino]-1,2,5-oxadiazole-3-carboximidamide | - |
Homo sapiens | |
N-(4-[[(6-bromo-1H-indazol-4-yl)amino]methyl]cyclohexylidene)hydroxylamine | - |
Homo sapiens | |
N-[(azetidin-3-yl)methyl]-6-bromo-1H-indazol-4-amine | - |
Homo sapiens | |
N-[[(1S,2R)-2-aminocyclohexyl]methyl]-6-bromo-1H-indazol-4-amine | - |
Homo sapiens | |
N-[[(1S,2S)-2-aminocyclohexyl]methyl]-6-bromo-1H-indazol-4-amine | - |
Homo sapiens | |
tert-butyl 3-[[(6-bromo-1H-indazol-4-yl)amino]methyl]pyrrolidine-1-carboxylate | - |
Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P48775 | - |
- |
Synonyms | Comment | Organism |
---|---|---|
TDO | - |
Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
heme | - |
Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.00004 | - |
shows efficacy against the 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-induced mouse motor coordination deficits, comparable to Madopar, an anti-Parkinson's disease medicine, 22°C, pH 6.5 | Homo sapiens | (1R,2S)-2-[[(6-bromo-1H-indazol-4-yl)amino]methyl]cyclohexan-1-ol | |
0.00009 | - |
22°C, pH 6.5 | Homo sapiens | (1S,2R)-2-[[(6-bromo-1H-indazol-4-yl)amino]methyl]cyclohexan-1-ol | |
0.00012 | - |
22°C, pH 6.5 | Homo sapiens | 2-[[(6-bromo-1H-indazol-4-yl)amino]methyl]cyclohexan-1-ol | |
0.00013 | - |
22°C, pH 6.5 | Homo sapiens | (1R,2S)-2-[[(6-chloro-1H-indazol-4-yl)amino]methyl]cyclohexan-1-ol | |
0.00015 | - |
22°C, pH 6.5 | Homo sapiens | 1-cyclohexyl-2-(5H-imidazo[5,1-a]isoindol-5-yl)ethan-1-ol | |
0.00019 | - |
22°C, pH 6.5 | Homo sapiens | (1R,2S)-2-[[(6-bromo-1H-indazol-4-yl)amino]methyl]cyclohexyl acetate | |
0.00022 | - |
22°C, pH 6.5 | Homo sapiens | 6-bromo-N-[[(1S,2S)-2-chlorocyclohexyl]methyl]-1H-indazol-4-amine | |
0.00033 | - |
22°C, pH 6.5 | Homo sapiens | 2-[(6-bromo-1H-indazol-4-yl)amino]-2-phenylethan-1-ol | |
0.00036 | - |
22°C, pH 6.5 | Homo sapiens | N-[[(1S,2R)-2-aminocyclohexyl]methyl]-6-bromo-1H-indazol-4-amine | |
0.0004 | - |
22°C, pH 6.5 | Homo sapiens | (1R,2S)-2-([[6-(trifluoromethyl)-1H-indazol-4-yl]amino]methyl)cyclohexan-1-ol | |
0.00041 | - |
22°C, pH 6.5 | Homo sapiens | (1R,2S)-2-[[(6-methyl-1H-indazol-4-yl)amino]methyl]cyclohexan-1-ol | |
0.00045 | - |
22°C, pH 6.5 | Homo sapiens | N-(4-[[(6-bromo-1H-indazol-4-yl)amino]methyl]cyclohexylidene)hydroxylamine | |
0.00086 | - |
22°C, pH 6.5 | Homo sapiens | 6-bromo-N-(cyclohexylmethyl)-1H-indazol-4-amine | |
0.00091 | - |
22°C, pH 6.5 | Homo sapiens | N-[[(1S,2S)-2-aminocyclohexyl]methyl]-6-bromo-1H-indazol-4-amine | |
0.00136 | - |
22°C, pH 6.5 | Homo sapiens | tert-butyl 3-[[(6-bromo-1H-indazol-4-yl)amino]methyl]pyrrolidine-1-carboxylate | |
0.0017 | - |
22°C, pH 6.5 | Homo sapiens | 6-bromo-1H-indazol-4-amine | |
0.00185 | - |
22°C, pH 6.5 | Homo sapiens | 4-[[(6-bromo-1H-indazol-4-yl)amino]methyl]phenol | |
0.00185 | - |
22°C, pH 6.5 | Homo sapiens | 6-bromo-N-[[(2R)-piperidin-2-yl]methyl]-1H-indazol-4-amine | |
0.00204 | - |
22°C, pH 6.5 | Homo sapiens | 2-[(6-bromo-1H-indazol-4-yl)amino]-2-(3-chlorophenyl)ethan-1-ol | |
0.00204 | - |
22°C, pH 6.5 | Homo sapiens | 6-bromo-N-[(1,4-dioxaspiro[4.5]decan-6-yl)methyl]-1H-indazol-4-amine | |
0.00311 | - |
22°C, pH 6.5 | Homo sapiens | 6-bromo-N-[(pyridin-2-yl)methyl]-1H-indazol-4-amine | |
0.00338 | - |
22°C, pH 6.5 | Homo sapiens | 2-[(6-bromo-1H-indazol-4-yl)amino]-1-(3-chlorophenyl)ethan-1-ol | |
0.00417 | - |
22°C, pH 6.5 | Homo sapiens | 6-bromo-N-[[(2S)-pyrrolidin-2-yl]methyl]-1H-indazol-4-amine | |
0.00606 | - |
22°C, pH 6.5 | Homo sapiens | 6-bromo-N-[[(2S)-piperidin-2-yl]methyl]-1H-indazol-4-amine | |
0.00745 | - |
22°C, pH 6.5 | Homo sapiens | 6-bromo-N-[[(2R)-pyrrolidin-2-yl]methyl]-1H-indazol-4-amine | |
0.00777 | - |
22°C, pH 6.5 | Homo sapiens | N-(3-bromo-4-fluorophenyl)-N'-hydroxy-4-[[2-(sulfamoylamino)ethyl]amino]-1,2,5-oxadiazole-3-carboximidamide | |
0.01044 | - |
22°C, pH 6.5 | Homo sapiens | 6-bromo-N-[(pyrrolidin-3-yl)methyl]-1H-indazol-4-amine | |
0.01124 | - |
22°C, pH 6.5 | Homo sapiens | (1R,2S)-2-[[(5-bromo-1H-indazol-4-yl)amino]methyl]cyclohexan-1-ol | |
0.01259 | - |
22°C, pH 6.5 | Homo sapiens | methyl 4-([[(1S,2R)-2-hydroxycyclohexyl]methyl]amino)-1H-indazole-6-carboxylate | |
0.01286 | - |
22°C, pH 6.5 | Homo sapiens | 4-[(1Z)-2-[(6-bromo-1H-indazol-4-yl)amino]-N-hydroxyethanimidoyl]phenol | |
0.02702 | - |
22°C, pH 6.5 | Homo sapiens | 4-([[(1S,2R)-2-hydroxycyclohexyl]methyl]amino)-1H-indazole-6-carboxylic acid | |
0.03324 | - |
22°C, pH 6.5 | Homo sapiens | (1R,2S)-2-[[(6-bromo-1-methyl-1H-indazol-4-yl)amino]methyl]cyclohexan-1-ol | |
0.03916 | - |
22°C, pH 6.5 | Homo sapiens | (1R,2S)-2-[[(5-bromo-1H-indazol-7-yl)amino]methyl]cyclohexan-1-ol | |
0.04487 | - |
22°C, pH 6.5 | Homo sapiens | N-[(azetidin-3-yl)methyl]-6-bromo-1H-indazol-4-amine | |
0.05841 | - |
22°C, pH 6.5 | Homo sapiens | 6-bromo-N-[(1R,2R)-2-hydroxycyclohexyl]-1H-indazole-4-carboxamide | |
0.08419 | - |
22°C, pH 6.5 | Homo sapiens | (1R,2S)-2-[[(5-chloro-1H-indazol-7-yl)amino]methyl]cyclohexan-1-ol | |
0.1477 | - |
22°C, pH 6.5 | Homo sapiens | 2-[(6-bromo-1H-indazol-4-yl)amino]-1-(4-hydroxyphenyl)ethan-1-one |
General Information | Comment | Organism |
---|---|---|
drug target | human indoleamine 2,3-dioxygenase 1 (hIDO1) and tryptophan 2,3-dioxygenase (hTDO) are closely linked to the pathogenesis of Parkinson's disease | Homo sapiens |