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Assay Detail

CHEMBL3376036

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

Functional
Antimalarial activity against chloroquine /mefloquine/pyrimethamine-resistant Plasmodium falciparum C235 by malaria SYBR green 1-based fluorescence (MSF) assay
24
Total Activities
24
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

The synthesis, antimalarial activity and CoMFA analysis of novel aminoalkylated quercetin analogs.
Helgren TR, Sciotti RJ, Lee P, Duffy S, Avery VM, Igbinoba O, Akoto M, Hagen TJ.
Bioorg Med Chem Lett (2015) 25 : 327 -332
PubMed 25488841 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 6.42 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL269671 ARTEMISININ 3.0 1 7.89
CHEMBL172 (S,R)-MEFLOQUINE 1 7.11
CHEMBL3354445 1 7.10
CHEMBL3354446 1 7.10
CHEMBL3354447 1 7.06
CHEMBL3354449 1 6.82
CHEMBL3354450 1 6.82
CHEMBL3354448 1 6.75
CHEMBL3354454 1 6.66
CHEMBL76 CHLOROQUINE 4.0 1 6.64
CHEMBL3354451 1 6.58
CHEMBL3354455 1 6.37
CHEMBL297453 EPIGALOCATECHIN GALLATE 3.0 1 6.21
CHEMBL3354457 1 6.21
CHEMBL3354456 1 6.16
CHEMBL3354452 1 5.92
CHEMBL3354460 1 5.51
CHEMBL518280 1 5.28
CHEMBL311498 CIANIDANOL 4.0 1 5.23
CHEMBL50 QUERCETIN 3.0 1 4.89
CHEMBL3354453 1 -
CHEMBL3354458 1 -
CHEMBL3354459 1 -
CHEMBL3354444 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL269671 ARTEMISININ IC50 = 13.0 nM 7.89
CHEMBL172 (S,R)-MEFLOQUINE IC50 = 77.0 nM 7.11
CHEMBL3354445 IC50 = 79.0 nM 7.10
CHEMBL3354446 IC50 = 80.0 nM 7.10
CHEMBL3354447 IC50 = 88.0 nM 7.06
CHEMBL3354449 IC50 = 150.0 nM 6.82
CHEMBL3354450 IC50 = 150.0 nM 6.82
CHEMBL3354448 IC50 = 180.0 nM 6.75
CHEMBL3354454 IC50 = 220.0 nM 6.66
CHEMBL76 CHLOROQUINE IC50 = 230.0 nM 6.64
CHEMBL3354451 IC50 = 260.0 nM 6.58
CHEMBL3354455 IC50 = 430.0 nM 6.37
CHEMBL297453 EPIGALOCATECHIN GALLATE IC50 = 610.0 nM 6.21
CHEMBL3354457 IC50 = 620.0 nM 6.21
CHEMBL3354456 IC50 = 700.0 nM 6.16
CHEMBL3354452 IC50 = 1200.0 nM 5.92
CHEMBL3354460 IC50 = 3100.0 nM 5.51
CHEMBL518280 IC50 = 5300.0 nM 5.28
CHEMBL311498 CIANIDANOL IC50 = 5900.0 nM 5.23
CHEMBL50 QUERCETIN IC50 = 13000.0 nM 4.89
CHEMBL3354453 IC50 > 2180.0 nM -
CHEMBL3354458 IC50 > 2230.0 nM -
CHEMBL3354459 IC50 > 2210.0 nM -
CHEMBL3354444 IC50 > 2120.0 nM -