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Assay Detail

CHEMBL5239934

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

Functional
Antiplasmodial activity against liver stage Plasmodium berghei ANKA sporozoites expressing GFP infected in HepG2 cells pre-infected with cells for 1 hr prior to compound addition and measured after 48 hrs by flow cytometry analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Plasmodium berghei
Cell Type HepG2
Confidence 1 — Organism
Curated By Autocuration

Target

Plasmodium berghei (CHEMBL612653)
Type ORGANISM
Organism Plasmodium berghei

Publication

Novel 3-Trifluoromethyl-1,2,4-oxadiazole Analogues of Astemizole with Multi-stage Antiplasmodium Activity and <i>In Vivo</i> Efficacy in a <i>Plasmodium berghei</i> Mouse Malaria Infection Model.
Mambwe D, Korkor CM, Mabhula A, Ngqumba Z, Cloete C, Kumar M, Barros PL, Leshabane M, Coertzen D, Taylor D, Gibhard L, Njoroge M, Lawrence N, Reader J, Moreira DR, Birkholtz LM, Wittlin S, Egan TJ, Chibale K.
J Med Chem (2022) 65 : 16695 -16715
PubMed 36507890 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.11 6.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5267563 1 6.68
CHEMBL5273140 1 6.31
CHEMBL296419 ASTEMIZOLE 4.0 1 6.23
CHEMBL506 PRIMAQUINE 4.0 1 5.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5267563 IC50 = 210.0 nM 6.68
CHEMBL5273140 IC50 = 490.0 nM 6.31
CHEMBL296419 ASTEMIZOLE IC50 = 590.0 nM 6.23
CHEMBL506 PRIMAQUINE IC50 = 6000.0 nM 5.22