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Assay Detail

CHEMBL4424079

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

Functional
Antitrypanosomal activity against pentamidine/diminazene/melaminophenyl arsenical resistant Trypanosoma brucei B48 after 48 hrs by alamar blue assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Trypanosoma brucei (CHEMBL612849)
Type ORGANISM
Organism Trypanosoma brucei

Publication

Revisiting tubercidin against kinetoplastid parasites: Aromatic substitutions at position 7 improve activity and reduce toxicity.
Hulpia F, Campagnaro GD, Scortichini M, Van Hecke K, Maes L, de Koning HP, Caljon G, Van Calenbergh S.
Eur J Med Chem (2019) 164 : 689 -705
PubMed 30677668 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 5.87 6.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4581647 1 6.57
CHEMBL2111043 ISOMETAMIDIUM 2.0 1 6.25
CHEMBL55 PENTAMIDINE 4.0 1 6.00
CHEMBL267099 TUBERCIDIN 1 5.37
CHEMBL35241 DIMINAZENE 2.0 1 5.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4581647 EC50 = 270.0 nM 6.57
CHEMBL2111043 ISOMETAMIDIUM EC50 = 560.0 nM 6.25
CHEMBL55 PENTAMIDINE EC50 = 990.0 nM 6.00
CHEMBL267099 TUBERCIDIN EC50 = 4300.0 nM 5.37
CHEMBL35241 DIMINAZENE EC50 = 7200.0 nM 5.14