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Assay Detail

CHEMBL3860281

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Functional
Antitrypanosomal activity against amastigote stage of Trypanosoma cruzi Y infected in human U2OS cells after 96 hrs by Draq5 staining-based high content screening assay
16
Total Activities
8
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Trypanosoma cruzi
Cell Type U2OS
Confidence 1 — Organism
Curated By Autocuration

Publication

Design, synthesis and antitrypanosomal activity of some nitrofurazone 1,2,4-triazolic bioisosteric analogues.
Silva FT, Franco CH, Favaro DC, Freitas-Junior LH, Moraes CB, Ferreira EI.
Eur J Med Chem (2016) 121 : 553 -560
PubMed 27318979 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 5.14 6.47
Emax 8 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL290960 NIFURTIMOX 4.0 2 6.47
CHEMBL110 BENZNIDAZOLE 4.0 2 5.40
CHEMBL3410627 2 5.26
CHEMBL3961604 2 4.81
CHEMBL3936285 2 4.67
CHEMBL3927334 2 4.20
CHEMBL2063495 2 -
CHEMBL3908348 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL290960 NIFURTIMOX EC50 = 340.0 nM 6.47
CHEMBL110 BENZNIDAZOLE EC50 = 3960.0 nM 5.40
CHEMBL3410627 EC50 = 5530.0 nM 5.26
CHEMBL3961604 EC50 = 15370.0 nM 4.81
CHEMBL3936285 EC50 = 21570.0 nM 4.67
CHEMBL3927334 EC50 = 63100.0 nM 4.20
CHEMBL2063495 EC50 = 144000.0 nM -
CHEMBL3908348 EC50 = 101300.0 nM -
CHEMBL110 BENZNIDAZOLE Emax = 103.5 % -
CHEMBL290960 NIFURTIMOX Emax = 101.5 % -
CHEMBL3410627 Emax = 86.99 % -
CHEMBL3908348 Emax = 95.23 % -
CHEMBL3936285 Emax = 92.75 % -
CHEMBL2063495 Emax = 68.7 % -
CHEMBL3927334 Emax = 96.6 % -
CHEMBL3961604 Emax = 95.22 % -