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Assay Detail

CHEMBL1781268

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

Functional
Antiparasitic activity against Trypanosoma brucei rhodesiense STIB900
11
Total Activities
11
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, DNA binding, fluorescence measurements and antiparasitic activity of DAPI related diamidines.
Farahat AA, Kumar A, Say M, Barghash Ael-D, Goda FE, Eisa HM, Wenzler T, Brun R, Liu Y, Mickelson L, Wilson WD, Boykin DW.
Bioorg Med Chem (2010) 18 : 557 -566
PubMed 20031421 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.86 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3216973 1 8.70
CHEMBL55 PENTAMIDINE 4.0 1 8.66
CHEMBL3216515 1 8.52
CHEMBL3216972 1 8.40
CHEMBL24057 FURAMIDINE -1.0 1 8.35
CHEMBL3216091 1 8.22
CHEMBL1232057 1 8.11
CHEMBL3217179 1 8.05
CHEMBL48217 DAPI 1 7.75
CHEMBL3216750 1 6.67
CHEMBL1780243 1 5.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3216973 IC50 = 2.0 nM 8.70
CHEMBL55 PENTAMIDINE IC50 = 2.2 nM 8.66
CHEMBL3216515 IC50 = 3.0 nM 8.52
CHEMBL3216972 IC50 = 4.0 nM 8.40
CHEMBL24057 FURAMIDINE IC50 = 4.5 nM 8.35
CHEMBL3216091 IC50 = 6.0 nM 8.22
CHEMBL1232057 IC50 = 7.7 nM 8.11
CHEMBL3217179 IC50 = 9.0 nM 8.05
CHEMBL48217 DAPI IC50 = 18.0 nM 7.75
CHEMBL3216750 IC50 = 215.0 nM 6.67
CHEMBL1780243 IC50 = 8723.0 nM 5.06