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Assay Detail

CHEMBL3868093

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

Functional
Antitrypanosomal against bloostream forms of Trypanosoma brucei gambiense FeoITMAP/1893 trypomastigotes after 72 hrs in the dark by resazurin assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Synthesis and in vitro antikinetoplastid activity of polyamine-hydroxybenzotriazole conjugates.
Jagu E, Pomel S, Diez-Martinez A, Ramiandrasoa F, Krauth-Siegel RL, Pethe S, Blonski C, Labruère R, Loiseau PM.
Bioorg Med Chem (2017) 25 : 84 -90
PubMed 27793448 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 5.36 8.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL55 PENTAMIDINE 4.0 1 8.68
CHEMBL3911154 1 5.92
CHEMBL3938030 1 5.70
CHEMBL3929012 1 5.50
CHEMBL19612 SPERMIDINE 3.0 1 5.48
CHEMBL3982145 1 5.46
CHEMBL3892084 1 5.02
CHEMBL3935427 1 4.86
CHEMBL3901047 1 4.60
CHEMBL3973073 1 4.54
CHEMBL3899791 1 4.41
CHEMBL3981165 1 4.14
CHEMBL3974072 1 -
CHEMBL3963859 1 -
CHEMBL3920101 1 -
CHEMBL125 MILTEFOSINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL55 PENTAMIDINE IC50 = 2.1 nM 8.68
CHEMBL3911154 IC50 = 1200.0 nM 5.92
CHEMBL3938030 IC50 = 2000.0 nM 5.70
CHEMBL3929012 IC50 = 3200.0 nM 5.50
CHEMBL19612 SPERMIDINE IC50 = 3300.0 nM 5.48
CHEMBL3982145 IC50 = 3500.0 nM 5.46
CHEMBL3892084 IC50 = 9500.0 nM 5.02
CHEMBL3935427 IC50 = 13800.0 nM 4.86
CHEMBL3901047 IC50 = 25300.0 nM 4.60
CHEMBL3973073 IC50 = 28800.0 nM 4.54
CHEMBL3899791 IC50 = 38700.0 nM 4.41
CHEMBL3981165 IC50 = 72000.0 nM 4.14
CHEMBL3974072 IC50 > 100000.0 nM -
CHEMBL3963859 IC50 > 100000.0 nM -
CHEMBL3920101 IC50 > 100000.0 nM -
CHEMBL125 MILTEFOSINE IC50 - -