Assay Detail

CHEMBL4771967

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Functional

Antitrypanosomal activity against bloodstream form of wild type Trypanosoma brucei brucei S427 trypomastigotes incubated for 72 hrs

ChEMBL ↗

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Target

Trypanosoma brucei brucei (CHEMBL612851) ↗

Open DB target context

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Trypanosoma brucei brucei (CHEMBL612851) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Trypanosoma brucei brucei

CHEMBL612851

Anchored from Assay target.

Protein identity Trypanosoma brucei brucei

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 brucei brucei
Confidence	1 — Organism
Curated By	Autocuration

Target

Trypanosoma brucei brucei (CHEMBL612851) ↗

Type	ORGANISM
Organism	Trypanosoma brucei brucei

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	6.45	6.91

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL4787217	—	—	1	6.91
CHEMBL4780415	—	—	1	6.70
CHEMBL290960	NIFURTIMOX	4.0	1	5.73

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL4787217	—	EC50	=	124.3	nM	6.91
CHEMBL4780415	—	EC50	=	200.0	nM	6.70
CHEMBL290960	NIFURTIMOX	EC50	=	1870.0	nM	5.73