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Assay Detail

CHEMBL4345834

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

Functional
Antitrypanosomal activity against bloodstream form of wild type Trypanosoma brucei brucei S427 trypomastigotes assessed as inhibition of parasite growth
6
Total Activities
6
Compounds Tested
1
Activity Types
0
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

New 8-Nitroquinolinone Derivative Displaying Submicromolar in Vitro Activities against Both Trypanosoma brucei and cruzi.
Pedron J, Boudot C, Brossas JY, Pinault E, Bourgeade-Delmas S, Sournia-Saquet A, Boutet-Robinet E, Destere A, Tronnet A, Bergé J, Bonduelle C, Deraeve C, Pratviel G, Stigliani JL, Paris L, Mazier D, Corvaisier S, Since M, Malzert-Fréon A, Wyllie S, Milne R, Fairlamb AH, Valentin A, Courtioux B, Verhaeghe P.
ACS Med Chem Lett (2020) 11 : 464 -472
PubMed 32292551 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 5.47 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4565434 1 6.52
CHEMBL290960 NIFURTIMOX 4.0 1 5.72
CHEMBL4559873 1 5.40
CHEMBL4547155 1 5.27
CHEMBL4556532 1 5.17
CHEMBL4170207 1 4.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4565434 EC50 = 300.0 nM 6.52
CHEMBL290960 NIFURTIMOX EC50 = 1900.0 nM 5.72
CHEMBL4559873 EC50 = 4000.0 nM 5.40
CHEMBL4547155 EC50 = 5400.0 nM 5.27
CHEMBL4556532 EC50 = 6700.0 nM 5.17
CHEMBL4170207 EC50 = 17700.0 nM 4.75