Assay Detail

CHEMBL4773775

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Functional

Antitrypanosomal activity against blood stream form of Trypanosoma brucei brucei S427 trypomastigotes overexpressing NTR1 assessed as inhibition of parasite growth

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

Antikinetoplastid SAR study in 3-nitroimidazopyridine series: Identification of a novel non-genotoxic and potent anti-T. b. brucei hit-compound with improved pharmacokinetic properties.

Fersing C,Boudot C,Paoli-Lombardo R,Primas N,Pinault E,Hutter S,Castera-Ducros C,Kabri Y,Pedron J,Bourgeade-Delmas S,Sournia-Saquet A,Stigliani JL,Valentin A,Azqueta A,Muruzabal D,Destere A,Wyllie S,Fairlamb AH,Corvaisier S,Since M,Malzert-Fréon A,Di Giorgio C,Rathelot P,Azas N,Courtioux B,Vanelle P,Verhaeghe P
Eur J Med Chem (2020) 206 : 112668 -112668
PubMed 32795774 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
EC50	2	7.01	7.80

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL4776584	—	—	1	7.80
CHEMBL290960	NIFURTIMOX	4.0	1	6.22

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL4776584	—	EC50	=	16.0	nM	7.80
CHEMBL290960	NIFURTIMOX	EC50	=	600.0	nM	6.22