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Assay Detail

CHEMBL1073224

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

Functional
Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900
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 Autocuration

Target

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

Publication

Synthesis and activity of azaterphenyl diamidines against Trypanosoma brucei rhodesiense and Plasmodium falciparum.
Hu L, Arafa RK, Ismail MA, Patel A, Munde M, Wilson WD, Wenzler T, Brun R, Boykin DW.
Bioorg Med Chem (2009) 17 : 6651 -6658
PubMed 19699098 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 7.99 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL258320 1 9.00
CHEMBL215484 1 8.70
CHEMBL55 PENTAMIDINE 4.0 1 8.66
CHEMBL256247 1 8.52
CHEMBL402847 1 8.40
CHEMBL24057 FURAMIDINE -1.0 1 8.35
CHEMBL215692 1 8.30
CHEMBL255539 1 8.22
CHEMBL257422 1 8.22
CHEMBL145251 1 8.19
CHEMBL256795 1 8.15
CHEMBL258319 1 7.96
CHEMBL256797 1 7.92
CHEMBL272090 1 7.85
CHEMBL273018 1 7.85
CHEMBL211920 1 7.80
CHEMBL403091 1 7.75
CHEMBL594198 1 7.50
CHEMBL213259 1 7.33
CHEMBL255758 1 5.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL258320 IC50 = 1.0 nM 9.00
CHEMBL215484 IC50 = 2.0 nM 8.70
CHEMBL55 PENTAMIDINE IC50 = 2.2 nM 8.66
CHEMBL256247 IC50 = 3.0 nM 8.52
CHEMBL402847 IC50 = 4.0 nM 8.40
CHEMBL24057 FURAMIDINE IC50 = 4.5 nM 8.35
CHEMBL215692 IC50 = 5.0 nM 8.30
CHEMBL255539 IC50 = 6.0 nM 8.22
CHEMBL257422 IC50 = 6.0 nM 8.22
CHEMBL145251 IC50 = 6.5 nM 8.19
CHEMBL256795 IC50 = 7.0 nM 8.15
CHEMBL258319 IC50 = 11.0 nM 7.96
CHEMBL256797 IC50 = 12.0 nM 7.92
CHEMBL272090 IC50 = 14.0 nM 7.85
CHEMBL273018 IC50 = 14.0 nM 7.85
CHEMBL211920 IC50 = 16.0 nM 7.80
CHEMBL403091 IC50 = 18.0 nM 7.75
CHEMBL594198 IC50 = 32.0 nM 7.50
CHEMBL213259 IC50 = 47.0 nM 7.33
CHEMBL255758 IC50 = 7131.0 nM 5.15