1.13.11.11: tryptophan 2,3-dioxygenase
This is an abbreviated version!
For detailed information about tryptophan 2,3-dioxygenase, go to the full flat file.
Word Map on EC 1.13.11.11
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1.13.11.11
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indoleamine
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kynurenine
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immunotherapy
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heme
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serotonin
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checkpoint
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l-trp
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n-formylkynurenine
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quinolinic
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tolerogenic
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3-monooxygenase
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3,4-dioxygenase
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heme-containing
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2,3-dioxygenase-1
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tryptophan-degrading
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3-hydroxyanthranilate
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indoleamine-2,3-dioxygenase
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picolinic
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tryptophan-catabolizing
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pyrrolase
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3-hydroxykynurenine
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medicine
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drug development
- 1.13.11.11
- indoleamine
- kynurenine
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immunotherapy
- heme
- serotonin
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checkpoint
- l-trp
- n-formylkynurenine
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quinolinic
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tolerogenic
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3-monooxygenase
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3,4-dioxygenase
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heme-containing
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2,3-dioxygenase-1
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tryptophan-degrading
- 3-hydroxyanthranilate
- indoleamine-2,3-dioxygenase
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picolinic
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tryptophan-catabolizing
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pyrrolase
- 3-hydroxykynurenine
- medicine
- drug development
Reaction
Synonyms
33737, BRAFLDRAFT_210874, C28H8.11, EC 1.11.1.4, hTDO, IDO-1, IDO-2, IDO1, IDO2, indoleamine 2,3-dioxygenase 1, indoleamine 2,3-dioxygenase 2, TDO, TDO2, TDOa, tryptophan 2,3-dioxygenase, tryptophan 2,3-dioxygenase 2, tryptophan 2,3-dioxygenase-2, tryptophan-2,3-dioxygenase, v1g157887, vCG5163, XcTDO
ECTree
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Inhibitors
Inhibitors on EC 1.13.11.11 - tryptophan 2,3-dioxygenase
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(1R,2S)-2-([[6-(trifluoromethyl)-1H-indazol-4-yl]amino]methyl)cyclohexan-1-ol
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(1R,2S)-2-[[(6-bromo-1-methyl-1H-indazol-4-yl)amino]methyl]cyclohexan-1-ol
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(2E)-3-(8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazolin-2-yl)prop-2-enoic acid
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(8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazolin-2-yl)boronic acid
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1-(2-hydroxy-4-methylphenyl)-3-{2-[(propan-2-yl)oxy]phenyl}propane-1,3-dione
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1-(3-bromothiophen-2-yl)-2-(3-methyl-1,4-dihydronaphthalen-2-yl)ethan-1-one
most potent inhibitor capable of blocking both indoleamine 2,3-dioxygenase 1 (IDO1) and tryptophan 2,3-dioxygenase (TDO2) activity, with the IC50 value for BT-549 cells at 0.00342 mM
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1-(3-[(4-acetyl-1-piperazinyl)carbonyl]benzyl)-1H-naphtho-[2,3-d][1,2,3]triazole-4,9-dione
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1-(3-[(4-methyl-1-piperazinyl)carbonyl]benzyl)-1H-naphtho-[2,3-d][1,2,3]triazole-4,9-dione
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1-(4-[(4-acetylpiperazin-1-yl)carbonyl]benzyl)-1H-naphtho-[2,3-d][1,2,3]triazole-4,9-dione
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1-(4-[(4-methoxypiperidin-1-yl)carbonyl]benzyl)-1Hnaphtho[2,3-d][1,2,3]triazole-4,9-dione
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1-[(8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazolin-2-yl)methyl]piperidine-3-carboxylic acid
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1-[(8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazolin-2-yl)methyl]piperidine-4-carboxylic acid
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1-[(8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazolin-2-yl)methyl]proline
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1-[3-(4-morpholinylcarbonyl)benzyl]-1H-naphtho[2,3-d]-[1,2,3]triazole-4,9-dione
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1-[4-(morpholin-4-ylcarbonyl)benzyl]-1H-naphtho[2,3-d]-[1,2,3]triazole-4,9-dione
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1-[4-[(4-methylpiperazin-1-yl)carbonyl]benzyl]-1H-naphtho-[2,3-d][1,2,3]triazole-4,9-dione
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2-(4-[(4,9-dioxo-4,9-dihydro-1H-naphtho[2,3-d][1,2,3]-triazol-1-yl)methyl]phenyl)-N,N-diethylacetamide
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3-[(4,9-dioxo-4,9-dihydro-1H-naphtho[2,3-d][1,2,3]triazol-1-yl)methyl]-N,N-diethylbenzamide
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3-[(4,9-dioxo-4,9-dihydro-1H-naphtho[2,3-d][1,2,3]triazol-1-yl)methyl]benzoic acid
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4-([[(1S,2R)-2-hydroxycyclohexyl]methyl]amino)-1H-indazole-6-carboxylic acid
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4-[(1Z)-2-[(6-bromo-1H-indazol-4-yl)amino]-N-hydroxyethanimidoyl]phenol
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4-[(4,9-dioxo-4,9-dihydro-1H-naphtho[2,3-d][1,2,3]triazol-1-yl)methyl]-N,N-diethylbenzamide
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4-[(4,9-dioxo-4,9-dihydro-1H-naphtho[2,3-d][1,2,3]triazol-1-yl)methyl]benzoic acid
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5-(6-fluoro-1H-indol-3-yl)-1-[2-(piperazin-1-yl)ethyl]-1H-benzotriazole
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5-phenyl-1,2,3-thiadiazol-4-amine
potent tryptophan 2,3-dioxygenase 2 inhibitor with modest selectivity over indolamine 2,3-dioxygenase 1 and with improved human whole blood stability
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8-fluoro-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)indolo[2,1-b]quinazoline-6,12-dione
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8-fluoro-2-[(1H-1,2,3-triazol-1-yl)methyl]indolo[2,1-b]quinazoline-6,12-dione
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8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazoline-2-carbaldehyde
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ethyl (2E)-3-(8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazolin-2-yl)prop-2-enoate
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methyl 1-[(8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazolin-2-yl)methyl]piperidine-3-carboxylate
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methyl 1-[(8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazolin-2-yl)methyl]piperidine-4-carboxylate
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methyl 1-[(8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazolin-2-yl)methyl]prolinate
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methyl 4-([[(1S,2R)-2-hydroxycyclohexyl]methyl]amino)-1H-indazole-6-carboxylate
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N-(3-bromo-4-fluorophenyl)-N'-hydroxy-4-[[2-(sulfamoylamino)ethyl]amino]-1,2,5-oxadiazole-3-carboximidamide
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N-(4-[[(6-bromo-1H-indazol-4-yl)amino]methyl]cyclohexylidene)hydroxylamine
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tert-butyl 3-[[(6-bromo-1H-indazol-4-yl)amino]methyl]pyrrolidine-1-carboxylate
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isatin derivatives analysis as a class of TDO inhibitors, structure-activity relationships and molecular docking studies, and optimized the inhibition potency of isatin derivatives by over 130fold, overview. Hydrogen bond interactions between the compound and key active site residues of TDO, freedom upon rotation of the C3 chemical moiety and the presence of chlorines in the benzene ring of the compound comprise the properties that an isatin-based inhibitor requires to effectively inhibit the enzymatic activity of enzyme TDO
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additional information
identification of substituted naphthotriazolediones as tryptophan 2,3-dioxygenase (TDO) inhibitors through structure-based virtual screening, homology modeling and virtual screening, ligand docking analysis, overview
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additional information
the enzymatic and cellular assays are influenced by many factors including detection product, reaction time and culture medium, which may cause the inconsistency of enzymatic and cellular inhibitory activities of test compounds. The TDO IC50 values of all the test compounds derived from NFK assay are 2-3 times higher than that of Kyn adduct assay
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additional information
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the enzymatic and cellular assays are influenced by many factors including detection product, reaction time and culture medium, which may cause the inconsistency of enzymatic and cellular inhibitory activities of test compounds. The TDO IC50 values of all the test compounds derived from NFK assay are 2-3 times higher than that of Kyn adduct assay
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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
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additional information
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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
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