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Assay Detail

CHEMBL4308358

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

Functional
Antitrypanosomal activity against Trypanosoma cruzi Y strain amastigotes infected in human U2OS cells assessed as parasite growth inhibition after 72 hrs post infection by DRAQ5 staining based analysis
27
Total Activities
27
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Trypanosoma cruzi
Confidence 1 — Organism
Curated By Autocuration

Target

Trypanosoma cruzi (CHEMBL368)
Type ORGANISM
Organism Trypanosoma cruzi

Publication

Synthesis and structure-activity relationship of nitrile-based cruzain inhibitors incorporating a trifluoroethylamine-based P2 amide replacement.
Gomes JC, Cianni L, Ribeiro J, Dos Reis Rocho F, da Costa Martins Silva S, Batista PHJ, Moraes CB, Franco CH, Freitas-Junior LHG, Kenny PW, Leitão A, Burtoloso ACB, de Vita D, Montanari CA.
Bioorg Med Chem (2019) 27 : 115083 -115083
PubMed 31561938 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Activity 23 - -
EC50 4 4.77 4.94

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4515535 1 4.94
CHEMBL4535973 1 4.59
CHEMBL4519995 1 -
CHEMBL4546133 1 -
CHEMBL4579894 1 -
CHEMBL4543467 1 -
CHEMBL4580196 1 -
CHEMBL4544254 1 -
CHEMBL4446278 1 -
CHEMBL4514540 1 -
CHEMBL4582238 1 -
CHEMBL4439127 1 -
CHEMBL4455305 1 -
CHEMBL4471896 1 -
CHEMBL4591985 1 -
CHEMBL4565840 1 -
CHEMBL4473385 1 -
CHEMBL4452562 1 -
CHEMBL4456233 1 -
CHEMBL4586752 1 -
CHEMBL4441186 1 -
CHEMBL4440148 1 -
CHEMBL481611 ODANACATIB 3.0 1 -
CHEMBL4442543 1 -
CHEMBL4463665 1 -
CHEMBL4578891 1 -
CHEMBL4451757 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4515535 EC50 = 11500.0 nM 4.94
CHEMBL4535973 EC50 = 25600.0 nM 4.59
CHEMBL4519995 Activity - -
CHEMBL4546133 Activity - -
CHEMBL4579894 Activity - -
CHEMBL4543467 Activity - -
CHEMBL4580196 Activity - -
CHEMBL4544254 Activity - -
CHEMBL4446278 Activity - -
CHEMBL4514540 Activity - -
CHEMBL4582238 EC50 - -
CHEMBL4439127 Activity - -
CHEMBL4455305 Activity - -
CHEMBL4471896 Activity - -
CHEMBL4591985 Activity - -
CHEMBL4565840 Activity - -
CHEMBL4473385 Activity - -
CHEMBL4452562 Activity - -
CHEMBL4456233 Activity - -
CHEMBL4586752 Activity - -
CHEMBL4441186 Activity - -
CHEMBL4440148 Activity - -
CHEMBL481611 ODANACATIB Activity - -
CHEMBL4442543 Activity - -
CHEMBL4463665 EC50 - -
CHEMBL4578891 Activity - -
CHEMBL4451757 Activity - -