Assay Detail

CHEMBL4313836

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

Functional

Antitrypanosomal activity against intracellular amastigote stage of Trypanosoma cruzi CL Brener infected in human U2OS cells measured after 96 hrs by DRAQ5 dye based microscopic analysis

ChEMBL ↗

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Target

Trypanosoma cruzi (CHEMBL368) ↗

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Trypanosoma cruzi (CHEMBL368) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Trypanosoma cruzi

CHEMBL368

Anchored from Assay target.

Protein identity Trypanosoma cruzi

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

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

Discovery of a benzothiophene-flavonol halting miltefosine and antimonial drug resistance in Leishmania parasites through the application of medicinal chemistry, screening and genomics.

Borsari C, Jiménez-Antón MD, Eick J, Bifeld E, Torrado JJ, Olías-Molero AI, Corral MJ, Santarem N, Baptista C, Severi L, Gul S, Wolf M, Kuzikov M, Ellinger B, Reinshagen J, Witt G, Linciano P, Tait A, Costantino L, Luciani R, Tejera Nevado P, Zander-Dinse D, Franco CH, Ferrari S, Moraes CB, Cordeiro-da-Silva A, Ponterini G, Clos J, Alunda JM, Costi MP.
Eur J Med Chem (2019) 183 : 111676 -111676
PubMed 31542713 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
EC50	2	6.11	6.22
Inhibition	1	-	-

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL4464312	—	—	1	6.22
CHEMBL110	BENZNIDAZOLE	4.0	1	6.00
CHEMBL125	MILTEFOSINE	4.0	1	-

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL4464312	—	EC50	=	600.0	nM	6.22
CHEMBL110	BENZNIDAZOLE	EC50	=	1000.0	nM	6.00
CHEMBL125	MILTEFOSINE	Inhibition		-	%	-