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Assay Detail

CHEMBL4771962

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

Functional
Antitrypanosomal activity against Trypanosoma cruzi trypomastigotes infected in African green monkey Vero cells incubated for 120 hrs measured on day 6 cells followed by trypomastigotes release by haemocytometer-based light microscopy
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Trypanosoma cruzi (CHEMBL368)
Type ORGANISM
Organism Trypanosoma cruzi

Publication

8-Alkynyl-3-nitroimidazopyridines display potent antitrypanosomal activity against both T. b. brucei and cruzi.
Fersing C,Boudot C,Castera-Ducros C,Pinault E,Hutter S,Paoli-Lombardo R,Primas N,Pedron J,Seguy L,Bourgeade-Delmas S,Sournia-Saquet A,Stigliani JL,Brossas JY,Paris L,Valentin A,Wyllie S,Fairlamb AH,Boutet-Robinet É,Corvaisier S,Since M,Malzert-Fréon A,Destere A,Mazier D,Rathelot P,Courtioux B,Azas N,Verhaeghe P,Vanelle P
Eur J Med Chem (2020) 202 : 112558 -112558
PubMed 32652409 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 5.91 6.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL110 BENZNIDAZOLE 4.0 1 6.30
CHEMBL4787217 1 5.92
CHEMBL1631694 FEXINIDAZOLE 4.0 1 5.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL110 BENZNIDAZOLE EC50 = 500.0 nM 6.30
CHEMBL4787217 EC50 = 1200.0 nM 5.92
CHEMBL1631694 FEXINIDAZOLE EC50 = 3000.0 nM 5.52