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Assay Detail

CHEMBL4827164

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

Functional
Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 measured after 72 hrs by alamar blue dye based fluorimetry analysis
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

New antiparasitic flexible triaryl diamidines, their prodrugs and aza analogues: Synthesis, in vitro and in vivo biological evaluation, and molecular modelling studies.
Arafa RK, Ismail MA, Wenzler T, Brun R, Paul A, Wilson WD, Alakhdar AA, Boykin DW.
Eur J Med Chem (2021) 222 : 113625 -113625
PubMed 34146914 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 6.67 8.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL55 PENTAMIDINE 4.0 1 8.66
CHEMBL24057 FURAMIDINE -1.0 1 8.35
CHEMBL4862097 1 7.96
CHEMBL4877093 1 7.82
CHEMBL4867511 1 7.57
CHEMBL4859955 1 7.46
CHEMBL4877388 1 7.39
CHEMBL4854237 1 7.14
CHEMBL4849091 1 7.14
CHEMBL4875142 1 6.98
CHEMBL298415 1 6.42
CHEMBL4865149 1 4.90
CHEMBL4846149 1 4.84
CHEMBL4867790 1 4.78
CHEMBL4878609 1 4.73
CHEMBL4850544 1 4.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL55 PENTAMIDINE IC50 = 2.2 nM 8.66
CHEMBL24057 FURAMIDINE IC50 = 4.5 nM 8.35
CHEMBL4862097 IC50 = 11.0 nM 7.96
CHEMBL4877093 IC50 = 15.0 nM 7.82
CHEMBL4867511 IC50 = 27.0 nM 7.57
CHEMBL4859955 IC50 = 35.0 nM 7.46
CHEMBL4877388 IC50 = 41.0 nM 7.39
CHEMBL4854237 IC50 = 73.0 nM 7.14
CHEMBL4849091 IC50 = 72.0 nM 7.14
CHEMBL4875142 IC50 = 105.0 nM 6.98
CHEMBL298415 IC50 = 378.0 nM 6.42
CHEMBL4865149 IC50 = 12600.0 nM 4.90
CHEMBL4846149 IC50 = 14400.0 nM 4.84
CHEMBL4867790 IC50 = 16600.0 nM 4.78
CHEMBL4878609 IC50 = 18700.0 nM 4.73
CHEMBL4850544 IC50 = 26100.0 nM 4.58