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Assay Detail

CHEMBL4812898

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of recombinant Trypanosoma cruzi cruzain using Z-FR-AMC as substrate preincubated for 10 mins followed by substrate addition measured for 5 mins by fluorimetric analysis relative to control
4
Total Activities
4
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

Cruzipain (CHEMBL3563)
Type SINGLE PROTEIN
Organism Trypanosoma cruzi

Publication

Computer-aided design of 1,4-naphthoquinone-based inhibitors targeting cruzain and rhodesain cysteine proteases.
Silva LR, Guimarães AS, do Nascimento J, do Santos Nascimento IJ, da Silva EB, McKerrow JH, Cardoso SH, da Silva-Júnior EF.
Bioorg Med Chem (2021) 41 : 116213 -116213
PubMed 33992862 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.46 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL374508 E-64 1 7.70
CHEMBL4877896 1 5.20
CHEMBL4845877 1 4.48
CHEMBL4859457 1 4.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL374508 E-64 IC50 = 20.0 nM 7.70
CHEMBL4877896 IC50 = 6300.0 nM 5.20
CHEMBL4845877 IC50 = 33000.0 nM 4.48
CHEMBL4859457 IC50 = 34000.0 nM 4.47