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Assay Detail

CHEMBL5533716

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

Functional
Antitrypanosomal activity against bloodstream forms of Trypanosoma brucei gambiense 130R assessed as growth inhibition incubated for 68 hrs followed by treated with resazurin 4 to 6 hrs by resazurin based fluorescence assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Trypanosoma brucei gambiense
Confidence 1 — Organism
Curated By Autocuration

Target

Trypanosoma brucei gambiense (CHEMBL613768)
Type ORGANISM
Organism Trypanosoma brucei gambiense

Publication

Discovery of an orally active nitrothiophene-based antitrypanosomal agent.
Ajayi O, Metibemu DS, Crown O, Adeyinka OS, Kaiser M, Shoji N, Silva M, Rodriguez A, Ogungbe IV.
Eur J Med Chem (2024) 263 : 115954 -115954
PubMed 37984297 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 11 6.90 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL166 MELARSOPROL 3.0 1 8.00
CHEMBL5573874 1 7.52
CHEMBL5573369 1 7.22
CHEMBL5571920 1 7.22
CHEMBL4642933 1 7.16
CHEMBL5579771 1 6.89
CHEMBL5564036 1 6.70
CHEMBL5564546 1 6.60
CHEMBL5571750 1 6.50
CHEMBL5572856 1 6.33
CHEMBL5563629 1 5.73

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL166 MELARSOPROL EC50 = 10.0 nM 8.00
CHEMBL5573874 EC50 = 30.0 nM 7.52
CHEMBL5573369 EC50 = 60.0 nM 7.22
CHEMBL5571920 EC50 = 60.0 nM 7.22
CHEMBL4642933 EC50 = 70.0 nM 7.16
CHEMBL5579771 EC50 = 130.0 nM 6.89
CHEMBL5564036 EC50 = 200.0 nM 6.70
CHEMBL5564546 EC50 = 250.0 nM 6.60
CHEMBL5571750 EC50 = 320.0 nM 6.50
CHEMBL5572856 EC50 = 470.0 nM 6.33
CHEMBL5563629 EC50 = 1880.0 nM 5.73