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Assay Detail

CHEMBL4700265

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

Binding
Covalent inhibition of Trypanosoma cruzi cruzipain using Z-Phe-Arg-7-amidomethylcoumarin as substrate measured after 30 mins by fluorometric analysis
2
Total Activities
2
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

On the intrinsic reactivity of highly potent trypanocidal cruzain inhibitors
Bonatto, Vinicius, Batista, Pedro Henrique Jatai, Cianni, Lorenzo, De Vita, Daniela, Silva, Daniel G., Cedron, Rodrigo, Tezuka, Daiane Y., de Albuquerque, Sergio, Moraes, Carolina Borsoi, Franco, Caio Haddad, Lameira, Jeronimo, Leitao, Andrei, Montanari, Carlos A.
RSC Med Chem (2020) 11 : 1275 -1284
PubMed 34095840 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 8.75 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4217414 1 8.80
CHEMBL604281 1 8.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4217414 Ki = 1.585 nM 8.80
CHEMBL604281 Ki = 1.995 nM 8.70