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Assay Detail

CHEMBL3366950

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

Functional
Antitrypanosomal activity against Trypanosoma cruzi amastigotes infected in mouse C2C12 cells after 72 hrs by DAPI staining method
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Trypanosoma cruzi
Cell Type C2C12
Confidence 1 — Organism
Curated By Autocuration

Target

Trypanosoma cruzi (CHEMBL368)
Type ORGANISM
Organism Trypanosoma cruzi

Publication

4-Aminopyridyl-based CYP51 inhibitors as anti-Trypanosoma cruzi drug leads with improved pharmacokinetic profile and in vivo potency.
Calvet CM, Vieira DF, Choi JY, Kellar D, Cameron MD, Siqueira-Neto JL, Gut J, Johnston JB, Lin L, Khan S, McKerrow JH, Roush WR, Podust LM.
J Med Chem (2014) 57 : 6989 -7005
PubMed 25101801 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 14 7.76 10.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3259946 1 10.77
CHEMBL3259944 1 9.92
CHEMBL3259945 1 8.89
CHEMBL3337539 1 8.17
CHEMBL3337540 1 7.77
CHEMBL3337534 1 7.68
CHEMBL3337541 1 7.54
CHEMBL3337532 1 7.41
CHEMBL3337537 1 7.23
CHEMBL3337536 1 7.11
CHEMBL3337535 1 6.77
CHEMBL3337538 1 6.64
CHEMBL3337533 1 6.55
CHEMBL507264 1 6.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3259946 EC50 = 0.017 nM 10.77
CHEMBL3259944 EC50 = 0.12 nM 9.92
CHEMBL3259945 EC50 = 1.3 nM 8.89
CHEMBL3337539 EC50 = 6.8 nM 8.17
CHEMBL3337540 EC50 = 17.0 nM 7.77
CHEMBL3337534 EC50 = 21.0 nM 7.68
CHEMBL3337541 EC50 = 29.0 nM 7.54
CHEMBL3337532 EC50 = 39.0 nM 7.41
CHEMBL3337537 EC50 = 59.0 nM 7.23
CHEMBL3337536 EC50 = 78.0 nM 7.11
CHEMBL3337535 EC50 = 170.0 nM 6.77
CHEMBL3337538 EC50 = 230.0 nM 6.64
CHEMBL3337533 EC50 = 280.0 nM 6.55
CHEMBL507264 EC50 = 650.0 nM 6.19