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Assay Detail

CHEMBL5637580

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

Functional
Antiplasmodial activity against erythrocytic stage of chloroquine, pyrimethamine and sulfadoxine resistant Plasmodium falciparum K1 infected in human erythrocytes assessed as reduction in parasite growth incubated for 72 hrs by SYBR green I fluorescence based spectrophotometric analysis
19
Total Activities
19
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

Novel thienopyrimidones targeting hepatic and erythrocytic stages of Plasmodium parasites with increased microsomal stability.
Lagardère P, Mustière R, Amanzougaghene N, Hutter S, Casanova M, Franetich JF, Tajeri S, Malzert-Fréon A, Corvaisier S, Since M, Azas N, Vanelle P, Verhaeghe P, Primas N, Mazier D, Masurier N, Lisowski V.
Eur J Med Chem (2023) 261 : 115873 -115873
PubMed 37857143 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 19 5.92 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5646444 1 7.00
CHEMBL5639596 1 6.70
CHEMBL76 CHLOROQUINE 4.0 1 6.10
CHEMBL5639348 1 6.05
CHEMBL5647138 1 5.96
CHEMBL5641686 1 5.85
CHEMBL5641867 1 5.85
CHEMBL5639982 1 5.38
CHEMBL1433 DOXYCYCLINE ANHYDROUS 4.0 1 5.30
CHEMBL5639093 1 5.01
CHEMBL5641821 1 -
CHEMBL5647344 1 -
CHEMBL5639413 1 -
CHEMBL5641912 1 -
CHEMBL5639392 1 -
CHEMBL5639558 1 -
CHEMBL5647059 1 -
CHEMBL5639706 1 -
CHEMBL5641835 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5646444 EC50 = 100.0 nM 7.00
CHEMBL5639596 EC50 = 200.0 nM 6.70
CHEMBL76 CHLOROQUINE EC50 = 800.0 nM 6.10
CHEMBL5639348 EC50 = 900.0 nM 6.05
CHEMBL5647138 EC50 = 1100.0 nM 5.96
CHEMBL5641686 EC50 = 1400.0 nM 5.85
CHEMBL5641867 EC50 = 1400.0 nM 5.85
CHEMBL5639982 EC50 = 4200.0 nM 5.38
CHEMBL1433 DOXYCYCLINE ANHYDROUS EC50 = 5000.0 nM 5.30
CHEMBL5639093 EC50 = 9800.0 nM 5.01
CHEMBL5641821 EC50 > 12500.0 nM -
CHEMBL5647344 EC50 > 25000.0 nM -
CHEMBL5639413 EC50 > 25000.0 nM -
CHEMBL5641912 EC50 > 10000.0 nM -
CHEMBL5639392 EC50 > 25000.0 nM -
CHEMBL5639558 EC50 > 31250.0 nM -
CHEMBL5647059 EC50 > 12500.0 nM -
CHEMBL5639706 EC50 > 12500.0 nM -
CHEMBL5641835 EC50 > 10000.0 nM -