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Assay Detail

CHEMBL4261102

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

Functional
Antiparasitic activity against GFP-expressing Trypanosoma cruzi Tulahuen amastigote formss infected in cardiomyocytes assessed as reduction in rate of parasite multiplication within infected cardiomyocytes measured at 72 hrs post infection by fluorescence microscopy
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Trypanosoma cruzi (CHEMBL368)
Type ORGANISM
Organism Trypanosoma cruzi

Publication

Sterol 14α-Demethylase Structure-Based Optimization of Drug Candidates for Human Infections with the Protozoan Trypanosomatidae.
Friggeri L, Hargrove TY, Rachakonda G, Blobaum AL, Fisher P, de Oliveira GM, da Silva CF, Soeiro MNC, Nes WD, Lindsley CW, Villalta F, Guengerich FP, Lepesheva GI.
J Med Chem (2018) 61 : 10910 -10921
PubMed 30451500 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 9.00 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4276822 1 9.30
CHEMBL3629567 1 9.00
CHEMBL1236677 1 8.89
CHEMBL4129161 1 8.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4276822 EC50 = 0.5 nM 9.30
CHEMBL3629567 EC50 = 1.0 nM 9.00
CHEMBL1236677 EC50 = 1.3 nM 8.89
CHEMBL4129161 EC50 = 1.6 nM 8.80