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Assay Detail

CHEMBL1768090

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

Functional
Antiparasitic activity against Plasmodium falciparum K1
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Plasmodium falciparum
Confidence 1 — Organism
Curated By Autocuration

Target

Plasmodium falciparum (CHEMBL364)
Type ORGANISM
Organism Plasmodium falciparum

Publication

Exploration of larger central ring linkers in furamidine analogues: synthesis and evaluation of their DNA binding, antiparasitic and fluorescence properties.
Farahat AA, Paliakov E, Kumar A, Barghash AE, Goda FE, Eisa HM, Wenzler T, Brun R, Liu Y, Wilson WD, Boykin DW.
Bioorg Med Chem (2011) 19 : 2156 -2167
PubMed 21421317 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 8.19 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1232057 1 9.30
CHEMBL3216295 1 8.89
CHEMBL48217 DAPI 1 8.52
CHEMBL1765480 1 8.48
CHEMBL3216971 1 8.43
CHEMBL3215856 1 8.28
CHEMBL3216088 1 8.24
CHEMBL3216087 1 8.15
CHEMBL3216970 1 8.01
CHEMBL3216747 1 7.96
CHEMBL3216513 1 7.90
CHEMBL24057 FURAMIDINE -1.0 1 7.81
CHEMBL3217178 1 7.75
CHEMBL3216089 1 7.75
CHEMBL55 PENTAMIDINE 4.0 1 7.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1232057 IC50 = 0.5 nM 9.30
CHEMBL3216295 IC50 = 1.3 nM 8.89
CHEMBL48217 DAPI IC50 = 3.0 nM 8.52
CHEMBL1765480 IC50 = 3.3 nM 8.48
CHEMBL3216971 IC50 = 3.7 nM 8.43
CHEMBL3215856 IC50 = 5.2 nM 8.28
CHEMBL3216088 IC50 = 5.7 nM 8.24
CHEMBL3216087 IC50 = 7.1 nM 8.15
CHEMBL3216970 IC50 = 9.8 nM 8.01
CHEMBL3216747 IC50 = 11.1 nM 7.96
CHEMBL3216513 IC50 = 12.5 nM 7.90
CHEMBL24057 FURAMIDINE IC50 = 15.5 nM 7.81
CHEMBL3217178 IC50 = 18.0 nM 7.75
CHEMBL3216089 IC50 = 18.0 nM 7.75
CHEMBL55 PENTAMIDINE IC50 = 46.4 nM 7.33