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Literature summary for 1.8.1.12 extracted from

  • Spinks, D.; Shanks, E.J.; Cleghorn, L.A.; McElroy, S.; Jones, D.; James, D.; Fairlamb, A.H.; Frearson, J.A.; Wyatt, P.G.; Gilbert, I.H.
    Investigation of trypanothione reductase as a drug target in Trypanosoma brucei (2009), ChemMedChem, 4, 2060-2069.
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
1,6-dimethyl-3-(4-methylphenyl)pyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione linear uncompetitive mode of inhibition Trypanosoma brucei
1-ethyl-6-methyl-3-(pyridin-3-yl)pyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione
-
Trypanosoma brucei
1-ethyl-6-methyl-3-(thiophen-2-yl)pyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione linear uncompetitive mode of inhibition Trypanosoma brucei
1-ethyl-6-methyl-3-phenylpyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione
-
Trypanosoma brucei
1-ethyl-6-methyl-3-[(Z)-2-phenylethenyl]pyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione
-
Trypanosoma brucei
1-ethyl-6-methyl-3-[4-(trifluoromethyl)phenyl]pyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione
-
Trypanosoma brucei
2-(5-methylfuran-2-yl)-N-(2-morpholinoethyl)quinoline-4-carboxamide
-
Trypanosoma brucei
2-(5-methylfuran-2-yl)-N-(pyridin-2-ylmethyl)quinoline-4-carboxamide
-
Trypanosoma brucei
3-(5-bromo-2-fluorophenyl)-1-butyl-6-methylpyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione
-
Trypanosoma brucei
3-(5-bromo-2-fluorophenyl)-1-cyclopentyl-6-methylpyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione
-
Trypanosoma brucei
3-(5-bromo-2-fluorophenyl)-1-ethyl-6-methylpyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione
-
Trypanosoma brucei
3-(5-bromo-2-fluorophenyl)-1-[2-(dimethylamino)ethyl]-6-methylpyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione
-
Trypanosoma brucei
3-(5-bromo-2-fluorophenyl)-6-methyl-1-(propan-2-yl)pyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione
-
Trypanosoma brucei
3-(5-bromo-2-fluorophenyl)-6-methylpyrimido[5,4-e,1,2,4]triazine-5,7(1H,6H)dione
-
Trypanosoma brucei
3-(5-bromo-2-fluorophenyl)-6-methylpyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione
-
Trypanosoma brucei
3-(5-bromothiophen-2-yl)-1-ethyl-6-methylpyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione
-
Trypanosoma brucei
6-bromo-2-(5-methylfuran-2-yl)-N-(2-morpholinoethyl)quinoline-4-carboxamide linear mixed-type inhibition Trypanosoma brucei
6-bromo-2-(5-methylfuran-2-yl)-N-(4-sulfamoylbenzyl)quinoline-4-carboxamide
-
Trypanosoma brucei
6-bromo-2-(5-methylfuran-2-yl)-N-(morpholin-4-yl)quinoline-4-carboxamide
-
Trypanosoma brucei
6-bromo-2-(5-methylfuran-2-yl)-N-(pyridin-2-ylmethyl)quinoline-4-carboxamide linear mixed-type inhibition Trypanosoma brucei
6-bromo-2-(5-methylfuran-2-yl)-N-(pyridin-3-yl)quinoline-4-carboxamide
-
Trypanosoma brucei
6-bromo-2-(5-methylfuran-2-yl)-N-phenethylquinoline-4-carboxamide
-
Trypanosoma brucei
6-bromo-N,N,N-trimethyl-2-(2-(5-methylfuran-2-yl)quinoline-4-carboxamido)ethanaminium iodide
-
Trypanosoma brucei
6-bromo-N-(2-(dimethylamino)ethyl)-2-(5-methylfuran-2-yl)quinoline-4-carboxamide linear mixed-type inhibition Trypanosoma brucei
6-bromo-N-(2-(dimethylamino)ethyl)-2-(5-methylthiophen-2-yl)-quinoline-4-carboxamide
-
Trypanosoma brucei
6-bromo-N-(2-(dimethylamino)ethyl)-2-(furan-2-yl)quinoline-4-carboxamide
-
Trypanosoma brucei
6-bromo-N-(2-(methylamino)ethyl)-2-(5-methylfuran-2-yl)quinoline-4-carboxamide
-
Trypanosoma brucei
6-bromo-N-(furan-2-ylmethyl)-2-(5-methylfuran-2-yl)quinoline-4-carboxamide
-
Trypanosoma brucei
6-bromo-N-[2-(dimethylamino)ethyl]-2-(pyridin-4-yl)quinoline-4-carboxamide
-
Trypanosoma brucei
6-bromo-N-[2-(dimethylamino)ethyl]-2-phenylquinoline-4-carboxamide
-
Trypanosoma brucei
6-bromo-N-[3-(1H-imidazol-1-ylamino)propyl]-2-(5-methylfuran-2-yl)quinoline-4-carboxamide
-
Trypanosoma brucei
6-chloro-2-(5-methylfuran-2-yl)-N-[3-(morpholin-4-yl)propyl]quinoline-4-carboxamide
-
Trypanosoma brucei
6-chloro-N-(2-(dimethylamino)ethyl)-2-(5-methylfuran-2-yl)quinoline-4-carboxamide
-
Trypanosoma brucei
6-chloro-N-[2-(dimethylamino)ethyl]-3-methyl-2-(4-methylphenyl)quinoline-4-carboxamide
-
Trypanosoma brucei
7-bromo-N-(2-(dimethylamino)ethyl)-2-(5-methylfuran-2-yl)quinoline-4-carboxamide
-
Trypanosoma brucei
8-bromo-N-(2-(dimethylamino)ethyl)-2-(5-methylfuran-2-yl)quinoline-4-carboxamide
-
Trypanosoma brucei
N-(2-(dimethylamino)ethyl)-2-(5-methylfuran-2-yl)quinoline-4-carboxamide
-
Trypanosoma brucei
N-(2-(dimethylamino)ethyl)-6-fluoro-2-(5-methylfuran-2-yl)quinoline-4-carboxamide
-
Trypanosoma brucei
N-benzyl-6-bromo-2-(5-methylfuran-2-yl)quinoline-4-carboxamide
-
Trypanosoma brucei

Organism

Organism UniProt Comment Textmining
Trypanosoma brucei
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
trypanothione disulfide + NADPH + H+
-
Trypanosoma brucei trypanothione + NADP+
-
?

Synonyms

Synonyms Comment Organism
trypanothione reductase
-
Trypanosoma brucei
TryR
-
Trypanosoma brucei

Cofactor

Cofactor Comment Organism Structure
FAD
-
Trypanosoma brucei
NADPH
-
Trypanosoma brucei

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0011
-
40 mM HEPES, 1 mM EDTA, pH 7.4, at 22°C Trypanosoma brucei 6-bromo-N-(2-(methylamino)ethyl)-2-(5-methylfuran-2-yl)quinoline-4-carboxamide
0.0012
-
40 mM HEPES, 1 mM EDTA, pH 7.4, at 22°C Trypanosoma brucei 6-bromo-N,N,N-trimethyl-2-(2-(5-methylfuran-2-yl)quinoline-4-carboxamido)ethanaminium iodide
0.0017
-
40 mM HEPES, 1 mM EDTA, pH 7.4, at 22°C Trypanosoma brucei 6-bromo-N-(2-(dimethylamino)ethyl)-2-(5-methylfuran-2-yl)quinoline-4-carboxamide
0.0026
-
in 40 mM HEPES, 1 mM EDTA, pH 7.4, at 22°C Trypanosoma brucei 1-ethyl-6-methyl-3-[(Z)-2-phenylethenyl]pyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione
0.0042
-
40 mM HEPES, 1 mM EDTA, pH 7.4, at 22°C Trypanosoma brucei 6-bromo-2-(5-methylfuran-2-yl)-N-(2-morpholinoethyl)quinoline-4-carboxamide
0.0047
-
40 mM HEPES, 1 mM EDTA, pH 7.4, at 22°C Trypanosoma brucei 6-bromo-2-(5-methylfuran-2-yl)-N-(pyridin-2-ylmethyl)quinoline-4-carboxamide
0.0051
-
40 mM HEPES, 1 mM EDTA, pH 7.4, at 22°C Trypanosoma brucei 8-bromo-N-(2-(dimethylamino)ethyl)-2-(5-methylfuran-2-yl)quinoline-4-carboxamide
0.0051
-
in 40 mM HEPES, 1 mM EDTA, pH 7.4, at 22°C Trypanosoma brucei 6-bromo-N-[3-(1H-imidazol-1-ylamino)propyl]-2-(5-methylfuran-2-yl)quinoline-4-carboxamide
0.0072
-
in 40 mM HEPES, 1 mM EDTA, pH 7.4, at 22°C Trypanosoma brucei 6-bromo-2-(5-methylfuran-2-yl)-N-(pyridin-3-yl)quinoline-4-carboxamide
0.0084
-
in 40 mM HEPES, 1 mM EDTA, pH 7.4, at 22°C Trypanosoma brucei 6-bromo-2-(5-methylfuran-2-yl)-N-(4-sulfamoylbenzyl)quinoline-4-carboxamide
0.0086
-
in 40 mM HEPES, 1 mM EDTA, pH 7.4, at 22°C Trypanosoma brucei 1,6-dimethyl-3-(4-methylphenyl)pyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione
0.0102
-
in 40 mM HEPES, 1 mM EDTA, pH 7.4, at 22°C Trypanosoma brucei 3-(5-bromo-2-fluorophenyl)-1-ethyl-6-methylpyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione
0.0113
-
in 40 mM HEPES, 1 mM EDTA, pH 7.4, at 22°C Trypanosoma brucei 1-ethyl-6-methyl-3-phenylpyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione
0.0116
-
in 40 mM HEPES, 1 mM EDTA, pH 7.4, at 22°C Trypanosoma brucei 6-chloro-2-(5-methylfuran-2-yl)-N-[3-(morpholin-4-yl)propyl]quinoline-4-carboxamide
0.0128
-
in 40 mM HEPES, 1 mM EDTA, pH 7.4, at 22°C Trypanosoma brucei 1-ethyl-6-methyl-3-(thiophen-2-yl)pyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione
0.013
-
in 40 mM HEPES, 1 mM EDTA, pH 7.4, at 22°C Trypanosoma brucei 3-(5-bromothiophen-2-yl)-1-ethyl-6-methylpyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione
0.0144
-
40 mM HEPES, 1 mM EDTA, pH 7.4, at 22°C Trypanosoma brucei N-(2-(dimethylamino)ethyl)-2-(5-methylfuran-2-yl)quinoline-4-carboxamide
0.0152
-
in 40 mM HEPES, 1 mM EDTA, pH 7.4, at 22°C Trypanosoma brucei 1-ethyl-6-methyl-3-[4-(trifluoromethyl)phenyl]pyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione
0.0265
-
in 40 mM HEPES, 1 mM EDTA, pH 7.4, at 22°C Trypanosoma brucei 6-chloro-N-[2-(dimethylamino)ethyl]-3-methyl-2-(4-methylphenyl)quinoline-4-carboxamide
0.0324
-
40 mM HEPES, 1 mM EDTA, pH 7.4, at 22°C Trypanosoma brucei 6-bromo-N-(2-(dimethylamino)ethyl)-2-(furan-2-yl)quinoline-4-carboxamide
0.05
-
IC50 above 0.05 mM, 40 mM HEPES, 1 mM EDTA, pH 7.4, at 22°C Trypanosoma brucei 3-(5-bromo-2-fluorophenyl)-6-methyl-1-(propan-2-yl)pyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione
0.092
-
40 mM HEPES, 1 mM EDTA, pH 7.4, at 22°C Trypanosoma brucei 3-(5-bromo-2-fluorophenyl)-6-methylpyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione
0.0963
-
in 40 mM HEPES, 1 mM EDTA, pH 7.4, at 22°C Trypanosoma brucei 6-bromo-N-[2-(dimethylamino)ethyl]-2-(pyridin-4-yl)quinoline-4-carboxamide
0.1
-
40 mM HEPES, 1 mM EDTA, pH 7.4, at 22°C Trypanosoma brucei 2-(5-methylfuran-2-yl)-N-(2-morpholinoethyl)quinoline-4-carboxamide
0.1
-
IC50 above 0.1 mM, 40 mM HEPES, 1 mM EDTA, pH 7.4, at 22°C Trypanosoma brucei N-benzyl-6-bromo-2-(5-methylfuran-2-yl)quinoline-4-carboxamide
0.1
-
IC50 above 0.1 mM, 40 mM HEPES, 1 mM EDTA, pH 7.4, at 22°C Trypanosoma brucei 6-bromo-N-(2-(dimethylamino)ethyl)-2-(5-methylthiophen-2-yl)-quinoline-4-carboxamide
0.1
-
IC50 above 0.1 mM, 40 mM HEPES, 1 mM EDTA, pH 7.4, at 22°C Trypanosoma brucei 6-bromo-2-(5-methylfuran-2-yl)-N-phenethylquinoline-4-carboxamide
0.1
-
IC50 above 0.1 mM, 40 mM HEPES, 1 mM EDTA, pH 7.4, at 22°C Trypanosoma brucei N-(2-(dimethylamino)ethyl)-6-fluoro-2-(5-methylfuran-2-yl)quinoline-4-carboxamide
0.1
-
IC50 above 0.1 mM, 40 mM HEPES, 1 mM EDTA, pH 7.4, at 22°C Trypanosoma brucei 3-(5-bromo-2-fluorophenyl)-6-methylpyrimido[5,4-e,1,2,4]triazine-5,7(1H,6H)dione
0.1
-
IC50 above 0.1 mM, 40 mM HEPES, 1 mM EDTA, pH 7.4, at 22°C Trypanosoma brucei 3-(5-bromo-2-fluorophenyl)-1-[2-(dimethylamino)ethyl]-6-methylpyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione
0.1
-
IC50 above 0.1 mM, 40 mM HEPES, 1 mM EDTA, pH 7.4, at 22°C Trypanosoma brucei 3-(5-bromo-2-fluorophenyl)-1-butyl-6-methylpyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione
0.1
-
IC50 above 0.1 mM, 40 mM HEPES, 1 mM EDTA, pH 7.4, at 22°C Trypanosoma brucei 3-(5-bromo-2-fluorophenyl)-1-cyclopentyl-6-methylpyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione
0.1
-
IC50 above 0.1 mM, in 40 mM HEPES, 1 mM EDTA, pH 7.4, at 22°C Trypanosoma brucei 6-bromo-N-[3-(1H-imidazol-1-ylamino)propyl]-2-(5-methylfuran-2-yl)quinoline-4-carboxamide
0.1
-
IC50 above 0.1 mM, in 40 mM HEPES, 1 mM EDTA, pH 7.4, at 22°C Trypanosoma brucei 6-bromo-N-[2-(dimethylamino)ethyl]-2-phenylquinoline-4-carboxamide
0.1
-
IC50 above 0.1 mM, in 40 mM HEPES, 1 mM EDTA, pH 7.4, at 22°C Trypanosoma brucei 6-bromo-2-(5-methylfuran-2-yl)-N-(morpholin-4-yl)quinoline-4-carboxamide
0.1
-
IC50 above 0.1 mM, in 40 mM HEPES, 1 mM EDTA, pH 7.4, at 22°C Trypanosoma brucei 6-bromo-N-(furan-2-ylmethyl)-2-(5-methylfuran-2-yl)quinoline-4-carboxamide
0.1
-
IC50 above 0.1 mM, in 40 mM HEPES, 1 mM EDTA, pH 7.4, at 22°C Trypanosoma brucei 1-ethyl-6-methyl-3-(pyridin-3-yl)pyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione