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Assay Detail

CHEMBL818116

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Binding
Concentration required for inhibition of Trypanothione reductase (TcTR) from Trypanosoma cruzi in the presence of 50 uM TS2 as substrate
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Trypanosoma cruzi
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Trypanothione reductase (CHEMBL5131)
Type SINGLE PROTEIN
Organism Trypanosoma cruzi

Publication

Parallel synthesis of a library of 1,4-naphthoquinones and automated screening of potential inhibitors of trypanothione reductase from Trypanosoma cruzi.
Salmon-Chemin L, Lemaire A, De Freitas S, Deprez B, Sergheraert C, Davioud-Charvet E.
Bioorg Med Chem Lett (2000) 10 : 631 -635
PubMed 10762041 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.64 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL160637 1 6.52
CHEMBL358636 1 6.30
CHEMBL159006 1 6.22
CHEMBL155801 1 5.96
CHEMBL295316 PLUMBAGIN 1.0 1 4.55
CHEMBL590 MENADIONE 4.0 1 4.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL160637 IC50 = 300.0 nM 6.52
CHEMBL358636 IC50 = 500.0 nM 6.30
CHEMBL159006 IC50 = 600.0 nM 6.22
CHEMBL155801 IC50 = 1100.0 nM 5.96
CHEMBL295316 PLUMBAGIN IC50 = 28000.0 nM 4.55
CHEMBL590 MENADIONE IC50 = 55000.0 nM 4.26