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Assay Detail

CHEMBL3118185

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

Functional
Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 assessed as parasite growth inhibition after 70 hrs by Alamar blue assay
16
Total Activities
16
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

Activity of diimidazoline amides against African trypanosomiasis.
Dong Y, Wang X, Cal M, Kaiser M, Vennerstrom JL.
Bioorg Med Chem Lett (2014) 24 : 944 -948
PubMed 24398295 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 7.23 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL361506 PENTAMIDINE ISETHIONATE 4.0 1 8.82
CHEMBL3113731 1 8.82
CHEMBL3113730 1 8.66
CHEMBL166 MELARSOPROL 3.0 1 8.42
CHEMBL3113720 1 8.33
CHEMBL3113724 1 7.96
CHEMBL3113727 1 7.72
CHEMBL3113732 1 7.64
CHEMBL3113721 1 7.29
CHEMBL3113729 1 7.07
CHEMBL3113726 1 6.92
CHEMBL3113725 1 6.92
CHEMBL3113728 1 6.16
CHEMBL3113733 1 5.66
CHEMBL3113722 1 5.02
CHEMBL3113723 1 4.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL361506 PENTAMIDINE ISETHIONATE IC50 = 1.5 nM 8.82
CHEMBL3113731 IC50 = 1.5 nM 8.82
CHEMBL3113730 IC50 = 2.2 nM 8.66
CHEMBL166 MELARSOPROL IC50 = 3.8 nM 8.42
CHEMBL3113720 IC50 = 4.7 nM 8.33
CHEMBL3113724 IC50 = 11.0 nM 7.96
CHEMBL3113727 IC50 = 19.0 nM 7.72
CHEMBL3113732 IC50 = 23.0 nM 7.64
CHEMBL3113721 IC50 = 51.0 nM 7.29
CHEMBL3113729 IC50 = 86.0 nM 7.07
CHEMBL3113726 IC50 = 120.0 nM 6.92
CHEMBL3113725 IC50 = 120.0 nM 6.92
CHEMBL3113728 IC50 = 690.0 nM 6.16
CHEMBL3113733 IC50 = 2200.0 nM 5.66
CHEMBL3113722 IC50 = 9500.0 nM 5.02
CHEMBL3113723 IC50 = 64000.0 nM 4.19