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Assay Detail

CHEMBL985931

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Functional
Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 by [3H]hypoxanthine uptake
11
Total Activities
11
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

Synthesis and biological evaluation of extraordinarily potent C-10 carba artemisinin dimers against P. falciparum malaria parasites and HL-60 cancer cells.
Chadwick J, Chadwick J, Mercer AE, Park BK, Cosstick R, O'Neill PM.
Bioorg Med Chem (2009) 17 : 1325 -1338
PubMed 19136263 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 8.86 10.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL506075 1 10.52
CHEMBL505378 1 9.68
CHEMBL450980 1 9.34
CHEMBL507226 1 9.30
CHEMBL566534 ARTEMETHER 4.0 1 8.68
CHEMBL446048 1 8.34
CHEMBL449370 1 8.32
CHEMBL510943 1 8.32
CHEMBL504137 1 8.22
CHEMBL269671 ARTEMISININ 3.0 1 7.91
CHEMBL445951 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL506075 IC50 = 0.03 nM 10.52
CHEMBL505378 IC50 = 0.21 nM 9.68
CHEMBL450980 IC50 = 0.46 nM 9.34
CHEMBL507226 IC50 = 0.5 nM 9.30
CHEMBL566534 ARTEMETHER IC50 = 2.11 nM 8.68
CHEMBL446048 IC50 = 4.6 nM 8.34
CHEMBL449370 IC50 = 4.8 nM 8.32
CHEMBL510943 IC50 = 4.8 nM 8.32
CHEMBL504137 IC50 = 6.0 nM 8.22
CHEMBL269671 ARTEMISININ IC50 = 12.3 nM 7.91
CHEMBL445951 IC50 > 60.0 nM -