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Assay Detail

CHEMBL1658385

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Functional
Antimalarial activity against Plasmodium falciparum D6 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter
6
Total Activities
6
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

Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
Briolant S, Henry M, Oeuvray C, Amalvict R, Baret E, Didillon E, Rogier C, Pradines B.
Antimicrob Agents Chemother (2010) 54 : 3537 -3544
PubMed 20547801 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.26 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL307261 ARTENIMOL 3.0 1 8.85
CHEMBL1235 DESETHYL AMODIAQUINE 1 7.64
CHEMBL76 CHLOROQUINE 4.0 1 7.60
CHEMBL170 QUININE 4.0 1 7.32
CHEMBL303933 PIPERAQUINE 3.0 1 7.24
CHEMBL1200699 DOXYCYCLINE 4.0 1 4.88

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL307261 ARTENIMOL IC50 = 1.4 nM 8.85
CHEMBL1235 DESETHYL AMODIAQUINE IC50 = 23.0 nM 7.64
CHEMBL76 CHLOROQUINE IC50 = 25.0 nM 7.60
CHEMBL170 QUININE IC50 = 48.0 nM 7.32
CHEMBL303933 PIPERAQUINE IC50 = 58.0 nM 7.24
CHEMBL1200699 DOXYCYCLINE IC50 = 13200.0 nM 4.88