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Assay Detail

CHEMBL3398946

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

Functional
Trypanocidal activity against pentamidine and melarsoprol-resistant Trypanosoma brucei rhodesiense K 243-As-10-3 assessed as inhibition of trypanosomes after 48 hrs
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Trypanosoma brucei rhodesiense (CHEMBL612348)
Type ORGANISM
Organism Trypanosoma brucei rhodesiense

Publication

Dibenzosuberyl substituted polyamines and analogs of clomipramine as effective inhibitors of trypanothione reductase; molecular docking, and assessment of trypanocidal activities.
O'Sullivan MC, Durham TB, Valdes HE, Dauer KL, Karney NJ, Forrestel AC, Bacchi CJ, Baker JF.
Bioorg Med Chem (2015) 23 : 996 -1010
PubMed 25661449 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.05 5.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3398187 1 5.40
CHEMBL378650 1 5.08
CHEMBL3398189 1 4.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3398187 IC50 = 4000.0 nM 5.40
CHEMBL378650 IC50 = 8300.0 nM 5.08
CHEMBL3398189 IC50 = 22000.0 nM 4.66