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Assay Detail

CHEMBL5239928

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

Functional
Antiplasmodial activity against multidrug resistant Plasmodium falciparum K1 incubated for 72 hrs by microplate reader assay
19
Total Activities
19
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 19 6.89 7.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5283963 1 7.57
CHEMBL5273140 1 7.40
CHEMBL5267563 1 7.32
CHEMBL5286466 1 7.31
CHEMBL4845682 1 7.28
CHEMBL5280818 1 7.09
CHEMBL5267878 1 6.98
CHEMBL76 CHLOROQUINE 4.0 1 6.85
CHEMBL5285111 1 6.81
CHEMBL5270015 1 6.76
CHEMBL5275583 1 6.76
CHEMBL5273046 1 6.75
CHEMBL5274888 1 6.75
CHEMBL5272240 1 6.58
CHEMBL5286751 1 6.52
CHEMBL5271875 1 6.45
CHEMBL296419 ASTEMIZOLE 4.0 1 6.43
CHEMBL5265992 1 6.40
CHEMBL5287948 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5283963 IC50 = 27.0 nM 7.57
CHEMBL5273140 IC50 = 40.0 nM 7.40
CHEMBL5267563 IC50 = 48.0 nM 7.32
CHEMBL5286466 IC50 = 49.0 nM 7.31
CHEMBL4845682 IC50 = 52.0 nM 7.28
CHEMBL5280818 IC50 = 82.0 nM 7.09
CHEMBL5267878 IC50 = 104.0 nM 6.98
CHEMBL76 CHLOROQUINE IC50 = 140.0 nM 6.85
CHEMBL5285111 IC50 = 156.0 nM 6.81
CHEMBL5270015 IC50 = 174.0 nM 6.76
CHEMBL5275583 IC50 = 173.0 nM 6.76
CHEMBL5273046 IC50 = 178.0 nM 6.75
CHEMBL5274888 IC50 = 176.0 nM 6.75
CHEMBL5272240 IC50 = 263.0 nM 6.58
CHEMBL5286751 IC50 = 300.0 nM 6.52
CHEMBL5271875 IC50 = 352.0 nM 6.45
CHEMBL296419 ASTEMIZOLE IC50 = 370.0 nM 6.43
CHEMBL5265992 IC50 = 399.0 nM 6.40
CHEMBL5287948 IC50 - -