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Assay Detail

CHEMBL1032136

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

Functional
Antimalarial activity after 48 hrs against atovaquone-resistant Plasmodium falciparum FCR3 by [3H]hypoxanthine uptake
23
Total Activities
23
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

Design, synthesis and structure-activity relationships of (1H-pyridin-4-ylidene)amines as potential antimalarials.
Rodrigues T, Guedes RC, dos Santos DJ, Carrasco M, Gut J, Rosenthal PJ, Moreira R, Lopes F.
Bioorg Med Chem Lett (2009) 19 : 3476 -3480
PubMed 19467600 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 5.59 7.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL76 CHLOROQUINE 4.0 1 7.29
CHEMBL559643 1 5.77
CHEMBL565121 1 5.74
CHEMBL549945 1 5.73
CHEMBL1450 ATOVAQUONE 4.0 1 5.72
CHEMBL555880 1 5.68
CHEMBL564704 1 5.66
CHEMBL562098 1 5.66
CHEMBL560430 1 5.65
CHEMBL557075 1 5.55
CHEMBL556259 1 5.54
CHEMBL564346 1 5.50
CHEMBL446918 CLOPIDOL 2.0 1 5.47
CHEMBL561221 1 5.45
CHEMBL551552 1 5.43
CHEMBL564236 1 5.40
CHEMBL556672 1 5.29
CHEMBL559073 1 5.10
CHEMBL556257 1 5.09
CHEMBL565089 1 5.01
CHEMBL551494 1 -
CHEMBL560557 1 -
CHEMBL556258 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL76 CHLOROQUINE IC50 = 51.0 nM 7.29
CHEMBL559643 IC50 = 1700.0 nM 5.77
CHEMBL565121 IC50 = 1830.0 nM 5.74
CHEMBL549945 IC50 = 1870.0 nM 5.73
CHEMBL1450 ATOVAQUONE IC50 = 1890.0 nM 5.72
CHEMBL555880 IC50 = 2080.0 nM 5.68
CHEMBL564704 IC50 = 2210.0 nM 5.66
CHEMBL562098 IC50 = 2170.0 nM 5.66
CHEMBL560430 IC50 = 2250.0 nM 5.65
CHEMBL557075 IC50 = 2800.0 nM 5.55
CHEMBL556259 IC50 = 2890.0 nM 5.54
CHEMBL564346 IC50 = 3190.0 nM 5.50
CHEMBL446918 CLOPIDOL IC50 = 3370.0 nM 5.47
CHEMBL561221 IC50 = 3530.0 nM 5.45
CHEMBL551552 IC50 = 3740.0 nM 5.43
CHEMBL564236 IC50 = 3950.0 nM 5.40
CHEMBL556672 IC50 = 5120.0 nM 5.29
CHEMBL559073 IC50 = 7900.0 nM 5.10
CHEMBL556257 IC50 = 8090.0 nM 5.09
CHEMBL565089 IC50 = 9860.0 nM 5.01
CHEMBL551494 IC50 > 10000.0 nM -
CHEMBL560557 IC50 > 8900000.0 nM -
CHEMBL556258 IC50 > 10000.0 nM -