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Assay Detail

CHEMBL4700264

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 5 mins by fluorometric analysis
14
Total Activities
14
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 14 5.28 6.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4463665 1 6.60
CHEMBL344174 1 6.30
CHEMBL371466 1 6.30
CHEMBL4213247 1 5.40
CHEMBL4217658 1 5.20
CHEMBL4208861 1 5.00
CHEMBL4789329 1 5.00
CHEMBL4776689 1 5.00
CHEMBL4750144 1 4.70
CHEMBL4209401 1 4.60
CHEMBL4747490 1 4.00
CHEMBL4203721 1 -
CHEMBL4213366 1 -
CHEMBL4208600 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4463665 Ki = 251.19 nM 6.60
CHEMBL344174 Ki = 501.19 nM 6.30
CHEMBL371466 Ki = 501.19 nM 6.30
CHEMBL4213247 Ki = 3981.07 nM 5.40
CHEMBL4217658 Ki = 6309.57 nM 5.20
CHEMBL4208861 Ki = 10000.0 nM 5.00
CHEMBL4789329 Ki = 10000.0 nM 5.00
CHEMBL4776689 Ki = 10000.0 nM 5.00
CHEMBL4750144 Ki = 19952.62 nM 4.70
CHEMBL4209401 Ki = 25118.86 nM 4.60
CHEMBL4747490 Ki = 100000.0 nM 4.00
CHEMBL4203721 Ki = 199526.23 nM -
CHEMBL4213366 Ki = 125892.54 nM -
CHEMBL4208600 Ki = 398107.17 nM -