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Literature summary for 1.8.1.12 extracted from

  • Richardson, J.L.; Nett, I.R.; Jones, D.C.; Abdille, M.H.; Gilbert, I.H.; Fairlamb, A.H.
    Improved tricyclic inhibitors of trypanothione reductase by screening and chemical synthesis (2009), ChemMedChem, 4, 1333-1340.
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
(2-chloroethoxy)diphenylmethane
-
Trypanosoma brucei
1-((2-benzhydryloxy)ethyl)piperazine
-
Trypanosoma brucei
1-(1-benzo[b]thiophen-2-yl-cyclohexyl)-piperidine
-
Trypanosoma brucei
1-(2-(benzhydryloxy)ethyl)-4-(3-phenylpropyl)piperazine GBR-12935 Trypanosoma brucei
1-(3-phenylpropyl)piperazine
-
Trypanosoma brucei
1-propylbenzene
-
Trypanosoma brucei
1-[2-(10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-yloxy)ethyl]-4-(3-phenyl-propyl)piperazine
-
Trypanosoma brucei
1-[2-(10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-yloxy)ethyl]-4-(E)-(3-phenyl-allyl)piperazine
-
Trypanosoma brucei
1-[2-(10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-yloxy)ethyl]-piperazine
-
Trypanosoma brucei
2-chloro-10-(3-(4-(3-phenylpropyl)piperazin-1-yl)propyl)-10H-phenothiazine
-
Trypanosoma brucei
3-Phenylpropylamine
-
Trypanosoma brucei
4-chloromercuribenzoic acid
-
Trypanosoma brucei
5-(2-chloroethoxy)-10,11-dihydro-5H-dibenzo[a,d]cycloheptene
-
Trypanosoma brucei
Bay 11-7085
-
Trypanosoma brucei
bromoacetyl alprenolol menthane
-
Trypanosoma brucei
chlorpromazoine
-
Trypanosoma brucei
clomipramine
-
Trypanosoma brucei
ebselen
-
Trypanosoma brucei
indatraline
-
Trypanosoma brucei
perphenazine
-
Trypanosoma brucei
pindobind
-
Trypanosoma brucei
prochlorperazine
-
Trypanosoma brucei
triflupromazine
-
Trypanosoma brucei

Organism

Organism UniProt Comment Textmining
Trypanosoma brucei
-
-
-

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
0.000251
-
in 40 mM HEPES pH 7.4, 1 mM EDTA, at 25°C Trypanosoma brucei 4-chloromercuribenzoic acid
0.00075
-
in 40 mM HEPES pH 7.4, 1 mM EDTA, at 25°C Trypanosoma brucei 2-chloro-10-(3-(4-(3-phenylpropyl)piperazin-1-yl)propyl)-10H-phenothiazine
0.00136
-
in 40 mM HEPES pH 7.4, 1 mM EDTA, at 25°C Trypanosoma brucei ebselen
0.00194
-
in 40 mM HEPES pH 7.4, 1 mM EDTA, at 25°C Trypanosoma brucei 1-[2-(10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-yloxy)ethyl]-4-(3-phenyl-propyl)piperazine
0.0021
-
in 40 mM HEPES pH 7.4, 1 mM EDTA, at 25°C Trypanosoma brucei bromoacetyl alprenolol menthane
0.00369
-
in 40 mM HEPES pH 7.4, 1 mM EDTA, at 25°C Trypanosoma brucei 1-(1-benzo[b]thiophen-2-yl-cyclohexyl)-piperidine
0.0038
-
in 40 mM HEPES pH 7.4, 1 mM EDTA, at 25°C Trypanosoma brucei clomipramine
0.00488
-
in 40 mM HEPES pH 7.4, 1 mM EDTA, at 25°C Trypanosoma brucei perphenazine
0.00494
-
in 40 mM HEPES pH 7.4, 1 mM EDTA, at 25°C Trypanosoma brucei Bay 11-7085
0.00632
-
in 40 mM HEPES pH 7.4, 1 mM EDTA, at 25°C Trypanosoma brucei chlorpromazoine
0.00689
-
in 40 mM HEPES pH 7.4, 1 mM EDTA, at 25°C Trypanosoma brucei pindobind
0.00726
-
in 40 mM HEPES pH 7.4, 1 mM EDTA, at 25°C Trypanosoma brucei indatraline
0.00746
-
in 40 mM HEPES pH 7.4, 1 mM EDTA, at 25°C Trypanosoma brucei prochlorperazine
0.00753
-
in 40 mM HEPES pH 7.4, 1 mM EDTA, at 25°C Trypanosoma brucei triflupromazine
0.0109
-
in 40 mM HEPES pH 7.4, 1 mM EDTA, at 25°C Trypanosoma brucei 1-(2-(benzhydryloxy)ethyl)-4-(3-phenylpropyl)piperazine
0.0269
-
in 40 mM HEPES pH 7.4, 1 mM EDTA, at 25°C Trypanosoma brucei 1-[2-(10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-yloxy)ethyl]-4-(E)-(3-phenyl-allyl)piperazine
0.0297
-
in 40 mM HEPES pH 7.4, 1 mM EDTA, at 25°C Trypanosoma brucei 5-(2-chloroethoxy)-10,11-dihydro-5H-dibenzo[a,d]cycloheptene
0.0345
-
in 40 mM HEPES pH 7.4, 1 mM EDTA, at 25°C Trypanosoma brucei 1-(3-phenylpropyl)piperazine
0.0487
-
in 40 mM HEPES pH 7.4, 1 mM EDTA, at 25°C Trypanosoma brucei 1-((2-benzhydryloxy)ethyl)piperazine
0.0515
-
in 40 mM HEPES pH 7.4, 1 mM EDTA, at 25°C Trypanosoma brucei 1-[2-(10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-yloxy)ethyl]-piperazine
0.0829
-
in 40 mM HEPES pH 7.4, 1 mM EDTA, at 25°C Trypanosoma brucei (2-chloroethoxy)diphenylmethane
0.1
-
IC50 above 0.1 mM, in 40 mM HEPES pH 7.4, 1 mM EDTA, at 25°C Trypanosoma brucei 3-Phenylpropylamine
0.1
-
IC50 above 0.1 mM, in 40 mM HEPES pH 7.4, 1 mM EDTA, at 25°C Trypanosoma brucei 1-propylbenzene