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Assay Detail

CHEMBL3365080

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

Functional
Antitrypanosomal activity against Trypanosoma cruzi Tulahuen trypomastigotes expressing green florescent protein infected in cardiomyocytes assessed as inhibition of parasite growth after 72 hrs by fluorescence microscopy
13
Total Activities
13
Compounds Tested
1
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

Structural basis for rational design of inhibitors targeting Trypanosoma cruzi sterol 14α-demethylase: two regions of the enzyme molecule potentiate its inhibition.
Friggeri L, Hargrove TY, Rachakonda G, Williams AD, Wawrzak Z, Di Santo R, De Vita D, Waterman MR, Tortorella S, Villalta F, Lepesheva GI.
J Med Chem (2014) 57 : 6704 -6717
PubMed 25033013 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 13 8.44 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2385091 1 9.00
CHEMBL2386135 1 8.92
CHEMBL3318325 1 8.92
CHEMBL3318326 1 8.89
CHEMBL3318324 1 8.82
CHEMBL3318323 1 8.60
CHEMBL1397 POSACONAZOLE 4.0 1 8.30
CHEMBL3318310 1 8.26
CHEMBL2386134 1 7.82
CHEMBL3318309 1 7.70
CHEMBL2386136 1 7.66
CHEMBL3318311 1 -
CHEMBL3318322 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2385091 EC50 = 1.0 nM 9.00
CHEMBL2386135 EC50 = 1.2 nM 8.92
CHEMBL3318325 EC50 = 1.2 nM 8.92
CHEMBL3318326 EC50 = 1.3 nM 8.89
CHEMBL3318324 EC50 = 1.5 nM 8.82
CHEMBL3318323 EC50 = 2.5 nM 8.60
CHEMBL1397 POSACONAZOLE EC50 = 5.0 nM 8.30
CHEMBL3318310 EC50 = 5.5 nM 8.26
CHEMBL2386134 EC50 = 15.0 nM 7.82
CHEMBL3318309 EC50 = 20.0 nM 7.70
CHEMBL2386136 EC50 = 22.0 nM 7.66
CHEMBL3318311 EC50 - -
CHEMBL3318322 EC50 - -