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Assay Detail

CHEMBL760274

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

Functional
In vitro antiparasitic activity against chloroquine-sensitive Plasmodium falciparum Haiti 135
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Plasmodium falciparum (CHEMBL364)
Type ORGANISM
Organism Plasmodium falciparum

Publication

Parallel solution-phase synthesis of conformationally restricted congeners of pentamidine and evaluation of their antiplasmodial activities.
Mayence A, Vanden Eynde JJ, Krogstad FM, Krogstad DJ, Cushion MT, Huang TL.
J Med Chem (2004) 47 : 2700 -2705
PubMed 15115412 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 7.84 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL537672 1 8.52
CHEMBL540380 1 8.52
CHEMBL539512 1 8.52
CHEMBL539613 1 8.52
CHEMBL539612 1 8.40
CHEMBL3216192 1 8.30
CHEMBL538481 1 8.22
CHEMBL76 CHLOROQUINE 4.0 1 8.22
CHEMBL55 PENTAMIDINE 4.0 1 7.82
CHEMBL541808 1 7.40
CHEMBL558206 1 7.00
CHEMBL540527 1 6.82
CHEMBL3215536 1 5.70
CHEMBL328338 1 -
CHEMBL90753 1 -
CHEMBL44144 1 -
CHEMBL421358 1 -
CHEMBL290691 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL537672 IC50 = 3.0 nM 8.52
CHEMBL540380 IC50 = 3.0 nM 8.52
CHEMBL539512 IC50 = 3.0 nM 8.52
CHEMBL539613 IC50 = 3.0 nM 8.52
CHEMBL539612 IC50 = 4.0 nM 8.40
CHEMBL3216192 IC50 = 5.0 nM 8.30
CHEMBL538481 IC50 = 6.0 nM 8.22
CHEMBL76 CHLOROQUINE IC50 = 6.0 nM 8.22
CHEMBL55 PENTAMIDINE IC50 = 15.0 nM 7.82
CHEMBL541808 IC50 = 40.0 nM 7.40
CHEMBL558206 IC50 = 100.0 nM 7.00
CHEMBL540527 IC50 = 150.0 nM 6.82
CHEMBL3215536 IC50 = 2000.0 nM 5.70
CHEMBL328338 IC50 > 500.0 nM -
CHEMBL90753 IC50 > 500.0 nM -
CHEMBL44144 IC50 > 500.0 nM -
CHEMBL421358 IC50 > 500.0 nM -
CHEMBL290691 IC50 > 500.0 nM -