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Assay Detail

CHEMBL989659

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

Functional
Antimalarial activity against Plasmodium falciparum 3D7A infected erythrocytes by [3H]hypoxanthine uptake
16
Total Activities
16
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

Synthesis and structure-activity relationships of 4-pyridones as potential antimalarials.
Yeates CL, Batchelor JF, Capon EC, Cheesman NJ, Fry M, Hudson AT, Pudney M, Trimming H, Woolven J, Bueno JM, Chicharro J, Fernández E, Fiandor JM, Gargallo-Viola D, Gómez de las Heras F, Herreros E, León ML.
J Med Chem (2008) 51 : 2845 -2852
PubMed 18396855 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 7.45 9.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1450 ATOVAQUONE 4.0 1 9.57
CHEMBL467584 1 8.30
CHEMBL469011 1 8.30
CHEMBL444503 1 8.15
CHEMBL512802 1 8.10
CHEMBL468638 1 7.52
CHEMBL468637 1 7.52
CHEMBL58510 CHLOROQUINE PHOSPHATE 4.0 1 7.51
CHEMBL511932 1 6.96
CHEMBL467583 1 6.80
CHEMBL468343 1 6.70
CHEMBL468639 1 6.52
CHEMBL513164 1 6.40
CHEMBL468990 1 5.89
CHEMBL513677 1 -
CHEMBL468344 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1450 ATOVAQUONE IC50 = 0.27 nM 9.57
CHEMBL467584 IC50 = 5.0 nM 8.30
CHEMBL469011 IC50 = 5.0 nM 8.30
CHEMBL444503 IC50 = 7.0 nM 8.15
CHEMBL512802 IC50 = 8.0 nM 8.10
CHEMBL468638 IC50 = 30.0 nM 7.52
CHEMBL468637 IC50 = 30.0 nM 7.52
CHEMBL58510 CHLOROQUINE PHOSPHATE IC50 = 31.0 nM 7.51
CHEMBL511932 IC50 = 110.0 nM 6.96
CHEMBL467583 IC50 = 160.0 nM 6.80
CHEMBL468343 IC50 = 200.0 nM 6.70
CHEMBL468639 IC50 = 300.0 nM 6.52
CHEMBL513164 IC50 = 400.0 nM 6.40
CHEMBL468990 IC50 = 1290.0 nM 5.89
CHEMBL513677 IC50 > 1000.0 nM -
CHEMBL468344 IC50 > 1000.0 nM -