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Assay Detail

CHEMBL1105850

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

Functional
Antitrypanosomal activity against Multidrug-resistant Trypanosoma brucei rhodesiense KETRI 243
14
Total Activities
14
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

Synthesis and SAR of alkanediamide-linked bisbenzamidines with anti-trypanosomal and anti-pneumocystis activity.
Huang TL, Vanden Eynde JJ, Mayence A, Collins MS, Cushion MT, Rattendi D, Londono I, Mazumder L, Bacchi CJ, Yarlett N.
Bioorg Med Chem Lett (2009) 19 : 5884 -5886
PubMed 19736009 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 7.40 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1081709 1 9.00
CHEMBL185175 1 8.70
CHEMBL1081708 1 8.70
CHEMBL55 PENTAMIDINE 4.0 1 8.70
CHEMBL1081887 1 8.40
CHEMBL1079366 1 8.15
CHEMBL1080776 1 8.15
CHEMBL1081522 1 7.68
CHEMBL185063 1 7.02
CHEMBL1081886 1 6.62
CHEMBL1081521 1 5.96
CHEMBL1078223 1 5.71
CHEMBL1080610 1 5.66
CHEMBL1080611 1 5.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1081709 IC50 = 1.0 nM 9.00
CHEMBL185175 IC50 = 2.0 nM 8.70
CHEMBL1081708 IC50 = 2.0 nM 8.70
CHEMBL55 PENTAMIDINE IC50 = 2.0 nM 8.70
CHEMBL1081887 IC50 = 4.0 nM 8.40
CHEMBL1079366 IC50 = 7.0 nM 8.15
CHEMBL1080776 IC50 = 7.0 nM 8.15
CHEMBL1081522 IC50 = 21.0 nM 7.68
CHEMBL185063 IC50 = 96.0 nM 7.02
CHEMBL1081886 IC50 = 240.0 nM 6.62
CHEMBL1081521 IC50 = 1100.0 nM 5.96
CHEMBL1078223 IC50 = 1970.0 nM 5.71
CHEMBL1080610 IC50 = 2190.0 nM 5.66
CHEMBL1080611 IC50 = 7900.0 nM 5.10