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Assay Detail

CHEMBL830275

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Binding
Inhibitory concentration against cruzain of Trypanosoma cruzi
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cruzipain (CHEMBL3563)
Type SINGLE PROTEIN
Organism Trypanosoma cruzi

Publication

Discovery of potent thiosemicarbazone inhibitors of rhodesain and cruzain.
Fujii N, Mallari JP, Hansell EJ, Mackey Z, Doyle P, Zhou YM, Gut J, Rosenthal PJ, McKerrow JH, Guy RK.
Bioorg Med Chem Lett (2005) 15 : 121 -123
PubMed 15582423 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.17 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL181504 1 7.72
CHEMBL92099 1 7.52
CHEMBL181752 1 7.52
CHEMBL183396 1 7.52
CHEMBL182790 1 7.52
CHEMBL182795 1 7.40
CHEMBL183005 1 7.40
CHEMBL183767 1 7.10
CHEMBL313679 1 6.51
CHEMBL181902 1 5.52
CHEMBL367811 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL181504 IC50 = 19.0 nM 7.72
CHEMBL92099 IC50 = 30.0 nM 7.52
CHEMBL181752 IC50 = 30.0 nM 7.52
CHEMBL183396 IC50 = 30.0 nM 7.52
CHEMBL182790 IC50 = 30.0 nM 7.52
CHEMBL182795 IC50 = 40.0 nM 7.40
CHEMBL183005 IC50 = 40.0 nM 7.40
CHEMBL183767 IC50 = 80.0 nM 7.10
CHEMBL313679 IC50 = 310.0 nM 6.51
CHEMBL181902 IC50 = 3000.0 nM 5.52
CHEMBL367811 IC50 > 10000.0 nM -