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Assay Detail

CHEMBL878025

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Binding
The competitive inhibitory activity against trypanothione reductase was evaluated from Lineweaver Burk plots
10
Total Activities
10
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

Inhibition of Trypanosoma cruzi trypanothione reductase by acridines: kinetic studies and structure-activity relationships.
Bonse S, Santelli-Rouvier C, Barbe J, Krauth-Siegel RL.
J Med Chem (1999) 42 : 5448 -5454
PubMed 10639286 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 4.73 5.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL151228 1 5.26
CHEMBL76954 1 5.16
CHEMBL153790 1 5.00
CHEMBL151397 1 4.96
CHEMBL7568 QUINACRINE 4.0 1 4.72
CHEMBL152023 1 4.57
CHEMBL43184 AMINACRINE 2.0 1 4.42
CHEMBL146512 1 4.37
CHEMBL292314 1 4.10
CHEMBL95 TACRINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL151228 Ki = 5500.0 nM 5.26
CHEMBL76954 Ki = 7000.0 nM 5.16
CHEMBL153790 Ki = 10000.0 nM 5.00
CHEMBL151397 Ki = 11000.0 nM 4.96
CHEMBL7568 QUINACRINE Ki = 19000.0 nM 4.72
CHEMBL152023 Ki = 27000.0 nM 4.57
CHEMBL43184 AMINACRINE Ki = 38000.0 nM 4.42
CHEMBL146512 Ki = 43000.0 nM 4.37
CHEMBL292314 Ki = 80000.0 nM 4.10
CHEMBL95 TACRINE Ki = 140000.0 nM -