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Assay Detail

CHEMBL5239933

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

Functional
Antiplasmodial activity against early stage (I to III) Plasmodium falciparum incubated for 48 hrs by bioluminescence assay
4
Total Activities
4
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

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 6.06 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL405110 METHYLENE BLUE ANHYDROUS 4.0 1 6.70
CHEMBL5286751 1 5.93
CHEMBL5273140 1 5.82
CHEMBL5267563 1 5.78

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL405110 METHYLENE BLUE ANHYDROUS IC50 = 200.0 nM 6.70
CHEMBL5286751 IC50 = 1180.0 nM 5.93
CHEMBL5273140 IC50 = 1520.0 nM 5.82
CHEMBL5267563 IC50 = 1670.0 nM 5.78