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Assay Detail

CHEMBL5506813

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

Functional
Antiplasmodial activity against sorbitol-synchronized ring stage atovaquone resistant Plasmodium falciparum TM90C6B harboring Y268S mutation in CYTB gene, Y184F mutation in MDR1 gene, N51I/C59R/S108N mutation in DHFR gene and S436F/A437G/A581G mutation in DHPS gene infected in erythrocytes measured after 48 hrs by SYBR green dye based fluorescence analysis
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Plasmodium falciparum
Cell Type Erythrocyte
Confidence 1 — Organism
Curated By Autocuration

Target

Plasmodium falciparum (CHEMBL364)
Type ORGANISM
Organism Plasmodium falciparum

Publication

Discovery of new piperaquine hybrid analogs linked by triazolopyrimidine and pyrazolopyrimidine scaffolds with antiplasmodial and transmission blocking activities.
Feitosa LM, Franca RRF, Ferreira MLG, Aguiar ACC, de Souza GE, Maluf SEC, de Souza JO, Zapata L, Duarte D, Morais I, Nogueira F, Nonato MC, Pinheiro LCS, Guido RVC, Boechat N.
Eur J Med Chem (2024) 267 : 116163 -116163
PubMed 38290351 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.95 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5557769 1 7.40
CHEMBL5559121 1 6.75
CHEMBL5560017 1 6.70
CHEMBL5559610 1 -
CHEMBL5563645 1 -
CHEMBL76 CHLOROQUINE 4.0 1 -
CHEMBL1956285 DSM-265 2.0 1 -
CHEMBL1450 ATOVAQUONE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5557769 IC50 = 40.0 nM 7.40
CHEMBL5559121 IC50 = 180.0 nM 6.75
CHEMBL5560017 IC50 = 200.0 nM 6.70
CHEMBL5559610 IC50 - -
CHEMBL5563645 IC50 - -
CHEMBL76 CHLOROQUINE IC50 - -
CHEMBL1956285 DSM-265 IC50 - -
CHEMBL1450 ATOVAQUONE IC50 > 1000.0 nM -