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Assay Detail

CHEMBL4274075

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

ADMET
Substrate activity at recombinant type-1 nitroreductase in bloodstream form of Trypanosoma brucei brucei S427 assessed as inhibition of parasite growth after 72 hrs
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Trypanosoma brucei brucei
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

8-Aryl-6-chloro-3-nitro-2-(phenylsulfonylmethyl)imidazo[1,2-a]pyridines as potent antitrypanosomatid molecules bioactivated by type 1 nitroreductases.
Fersing C, Boudot C, Pedron J, Hutter S, Primas N, Castera-Ducros C, Bourgeade-Delmas S, Sournia-Saquet A, Moreau A, Cohen A, Stigliani JL, Pratviel G, Crozet MD, Wyllie S, Fairlamb A, Valentin A, Rathelot P, Azas N, Courtioux B, Verhaeghe P, Vanelle P.
Eur J Med Chem (2018) 157 : 115 -126
PubMed 30092366 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.78 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4288624 1 7.40
CHEMBL4280330 1 6.72
CHEMBL290960 NIFURTIMOX 4.0 1 6.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4288624 IC50 = 40.0 nM 7.40
CHEMBL4280330 IC50 = 190.0 nM 6.72
CHEMBL290960 NIFURTIMOX IC50 = 600.0 nM 6.22