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Assay Detail

CHEMBL3815295

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

Functional
Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB 900 bloodstream forms after 72 hrs by Alamar blue assay
21
Total Activities
21
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

Antiprotozoal activity of bicycles featuring a dimethylamino group at their bridgehead.
Faist J, Seebacher W, Saf R, Brun R, Kaiser M, Weis R.
Bioorg Med Chem (2016) 24 : 3781 -3789
PubMed 27344215 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 6.16 8.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL166 MELARSOPROL 3.0 1 8.41
CHEMBL3814328 1 6.96
CHEMBL3814914 1 6.92
CHEMBL3814549 1 6.82
CHEMBL3815012 1 6.80
CHEMBL3813814 1 6.57
CHEMBL3813761 1 6.34
CHEMBL3814468 1 6.32
CHEMBL3814637 1 6.27
CHEMBL3814373 1 5.91
CHEMBL3813987 1 5.84
CHEMBL3814817 1 5.83
CHEMBL3814553 1 5.83
CHEMBL3814274 1 5.82
CHEMBL3814114 1 5.80
CHEMBL3814792 1 5.75
CHEMBL3814194 1 5.67
CHEMBL3814403 1 5.62
CHEMBL3814996 1 5.58
CHEMBL3813828 1 5.28
CHEMBL3814558 1 5.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL166 MELARSOPROL IC50 = 3.9 nM 8.41
CHEMBL3814328 IC50 = 110.0 nM 6.96
CHEMBL3814914 IC50 = 120.0 nM 6.92
CHEMBL3814549 IC50 = 150.0 nM 6.82
CHEMBL3815012 IC50 = 160.0 nM 6.80
CHEMBL3813814 IC50 = 270.0 nM 6.57
CHEMBL3813761 IC50 = 460.0 nM 6.34
CHEMBL3814468 IC50 = 480.0 nM 6.32
CHEMBL3814637 IC50 = 540.0 nM 6.27
CHEMBL3814373 IC50 = 1230.0 nM 5.91
CHEMBL3813987 IC50 = 1460.0 nM 5.84
CHEMBL3814817 IC50 = 1470.0 nM 5.83
CHEMBL3814553 IC50 = 1490.0 nM 5.83
CHEMBL3814274 IC50 = 1520.0 nM 5.82
CHEMBL3814114 IC50 = 1570.0 nM 5.80
CHEMBL3814792 IC50 = 1790.0 nM 5.75
CHEMBL3814194 IC50 = 2160.0 nM 5.67
CHEMBL3814403 IC50 = 2400.0 nM 5.62
CHEMBL3814996 IC50 = 2620.0 nM 5.58
CHEMBL3813828 IC50 = 5210.0 nM 5.28
CHEMBL3814558 IC50 = 9470.0 nM 5.02