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Assay Detail

CHEMBL5362064

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

Functional
Antiprotozoal activity against long slender blood stream form Trypanosoma brucei rhodesiense STIB900 assessed as parasite growth inhibition incubated for 70 hrs by resazurin based microplate fluorometer analysis
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

Investigation of the effect of structure modification of furamidine on the DNA minor groove binding and antiprotozoal activity.
Farahat AA, Kumar A, Wenzler T, Brun R, Paul A, Guo P, Wilson WD, Boykin DW.
Eur J Med Chem (2023) 252 : 115287 -115287
PubMed 36958267 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 7.98 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4854793 1 8.70
CHEMBL5438713 1 8.52
CHEMBL24057 FURAMIDINE -1.0 1 8.35
CHEMBL4866022 1 8.22
CHEMBL5440966 1 8.22
CHEMBL5426298 1 8.22
CHEMBL5414878 1 8.15
CHEMBL4868476 1 7.92
CHEMBL4853880 1 7.92
CHEMBL4856398 1 7.82
CHEMBL5398487 1 7.77
CHEMBL1232046 1 7.57
CHEMBL4851823 1 7.41
CHEMBL62071 1 6.91

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4854793 IC50 = 2.0 nM 8.70
CHEMBL5438713 IC50 = 3.0 nM 8.52
CHEMBL24057 FURAMIDINE IC50 = 4.5 nM 8.35
CHEMBL4866022 IC50 = 6.0 nM 8.22
CHEMBL5440966 IC50 = 6.0 nM 8.22
CHEMBL5426298 IC50 = 6.0 nM 8.22
CHEMBL5414878 IC50 = 7.0 nM 8.15
CHEMBL4868476 IC50 = 12.0 nM 7.92
CHEMBL4853880 IC50 = 12.0 nM 7.92
CHEMBL4856398 IC50 = 15.0 nM 7.82
CHEMBL5398487 IC50 = 17.0 nM 7.77
CHEMBL1232046 IC50 = 27.0 nM 7.57
CHEMBL4851823 IC50 = 39.0 nM 7.41
CHEMBL62071 IC50 = 122.0 nM 6.91