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Assay Detail

CHEMBL812088

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

Functional
In vitro inhibitory activity against T. b. rhodesiense
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Trypanosoma brucei rhodesiense
Confidence 1 — Organism
Curated By Expert

Target

Trypanosoma brucei rhodesiense (CHEMBL612348)
Type ORGANISM
Organism Trypanosoma brucei rhodesiense

Publication

Synthesis and antiprotozoal activity of aza-analogues of furamidine.
Ismail MA, Brun R, Easterbrook JD, Tanious FA, Wilson WD, Boykin DW.
J Med Chem (2003) 46 : 4761 -4769
PubMed 14561095 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 6.39 8.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL55 PENTAMIDINE 4.0 1 8.66
CHEMBL424121 1 8.51
CHEMBL24057 FURAMIDINE -1.0 1 8.35
CHEMBL145251 1 8.15
CHEMBL145572 1 8.15
CHEMBL358287 1 7.68
CHEMBL144893 1 7.39
CHEMBL141719 1 6.83
CHEMBL146273 1 5.19
CHEMBL357661 1 5.08
CHEMBL356072 1 5.03
CHEMBL145654 1 4.96
CHEMBL145627 1 4.88
CHEMBL144950 1 4.72
CHEMBL264664 1 4.43
CHEMBL145118 1 4.25
CHEMBL146548 1 -
CHEMBL344103 1 -
CHEMBL343253 1 -
CHEMBL342961 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL55 PENTAMIDINE IC50 = 2.2 nM 8.66
CHEMBL424121 IC50 = 3.1 nM 8.51
CHEMBL24057 FURAMIDINE IC50 = 4.5 nM 8.35
CHEMBL145251 IC50 = 7.0 nM 8.15
CHEMBL145572 IC50 = 7.0 nM 8.15
CHEMBL358287 IC50 = 21.0 nM 7.68
CHEMBL144893 IC50 = 40.7 nM 7.39
CHEMBL141719 IC50 = 147.0 nM 6.83
CHEMBL146273 IC50 = 6500.0 nM 5.19
CHEMBL357661 IC50 = 8400.0 nM 5.08
CHEMBL356072 IC50 = 9400.0 nM 5.03
CHEMBL145654 IC50 = 11100.0 nM 4.96
CHEMBL145627 IC50 = 13300.0 nM 4.88
CHEMBL144950 IC50 = 19100.0 nM 4.72
CHEMBL264664 IC50 = 37100.0 nM 4.43
CHEMBL145118 IC50 = 55800.0 nM 4.25
CHEMBL146548 IC50 = 200000.0 nM -
CHEMBL344103 IC50 = 120000.0 nM -
CHEMBL343253 IC50 > 187000.0 nM -
CHEMBL342961 IC50 > 21000.0 nM -