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Assay Detail

CHEMBL5326511

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

Binding
Inhibition of recombinant Trypanosoma cruzi Cruzipain using Z-FR-AMC as substrate preincubated for 20 mins followed by substrate addition and measured for 45 mins by fluorescence analysis
12
Total Activities
9
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

Design, synthesis and biological evaluation of novel thiosemicarbazones as cruzipain inhibitors.
Jasinski G, Salas-Sarduy E, Vega D, Fabian L, Florencia Martini M, Moglioni AG.
Eur J Med Chem (2023) 254 : 115345 -115345
PubMed 37054562 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.32 8.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5437573 2 8.54
CHEMBL5394366 2 8.48
CHEMBL5403163 2 8.17
CHEMBL181504 1 7.72
CHEMBL89973 1 7.22
CHEMBL183767 1 7.10
CHEMBL313679 1 6.75
CHEMBL91844 1 5.87
CHEMBL108035 1 5.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5437573 IC50 = 2.86 nM 8.54
CHEMBL5394366 IC50 = 3.34 nM 8.48
CHEMBL5403163 IC50 = 6.76 nM 8.17
CHEMBL5437573 IC50 = 8.54 nM 8.07
CHEMBL5394366 IC50 = 8.48 nM 8.07
CHEMBL181504 IC50 = 19.01 nM 7.72
CHEMBL89973 IC50 = 59.98 nM 7.22
CHEMBL183767 IC50 = 79.98 nM 7.10
CHEMBL5403163 IC50 = 175.0 nM 6.76
CHEMBL313679 IC50 = 176.2 nM 6.75
CHEMBL91844 IC50 = 1361.44 nM 5.87
CHEMBL108035 IC50 = 7998.34 nM 5.10