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Assay Detail

CHEMBL814912

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

Functional
Tested in vitro for trypanocidal activity against KETRI 243 an uncloned clinical isolate of Trypanosoma brucei. rhodesiense
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Trypanosoma brucei
Confidence 1 — Organism
Curated By Intermediate

Target

Trypanosoma brucei (CHEMBL612849)
Type ORGANISM
Organism Trypanosoma brucei

Publication

Polyamines with N-(3-phenylpropyl) substituents are effective competitive inhibitors of trypanothione reductase and trypanocidal agents.
Li Z, Fennie MW, Ganem B, Hancock MT, Kobaslija M, Rattendi D, Bacchi CJ, O'Sullivan MC.
Bioorg Med Chem Lett (2001) 11 : 251 -254
PubMed 11206471 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.11 6.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL86281 1 6.85
CHEMBL85189 1 6.80
CHEMBL84221 1 6.80
CHEMBL82641 1 6.44
CHEMBL85198 1 6.28
CHEMBL62048 1 6.10
CHEMBL86096 1 5.82
CHEMBL85161 1 5.47
CHEMBL310207 1 4.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL86281 IC50 = 140.0 nM 6.85
CHEMBL85189 IC50 = 160.0 nM 6.80
CHEMBL84221 IC50 = 160.0 nM 6.80
CHEMBL82641 IC50 = 360.0 nM 6.44
CHEMBL85198 IC50 = 530.0 nM 6.28
CHEMBL62048 IC50 = 790.0 nM 6.10
CHEMBL86096 IC50 = 1500.0 nM 5.82
CHEMBL85161 IC50 = 3350.0 nM 5.47
CHEMBL310207 IC50 = 35000.0 nM 4.46