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Assay Detail

CHEMBL3266494

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Functional
Antimalarial activity against multidrug-resistant Plasmodium falciparum Dd2 MRA-156 infected in human red blood cells assessed as suppression of parasitemia after 72 hrs by SYBR Green I-based fluorescence method
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Plasmodium falciparum Dd2
Confidence 1 — Organism
Curated By Autocuration

Publication

Discovery, synthesis, and optimization of antimalarial 4(1H)-quinolone-3-diarylethers.
Nilsen A, Miley GP, Forquer IP, Mather MW, Katneni K, Li Y, Pou S, Pershing AM, Stickles AM, Ryan E, Kelly JX, Doggett JS, White KL, Hinrichs DJ, Winter RW, Charman SA, Zakharov LN, Bathurst I, Burrows JN, Vaidya AB, Riscoe MK.
J Med Chem (2014) 57 : 3818 -3834
PubMed 24720377 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 24 8.67 10.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3261732 1 10.52
CHEMBL1450 ATOVAQUONE 4.0 1 10.00
CHEMBL3261738 1 9.70
CHEMBL3261733 1 9.52
CHEMBL3259839 1 9.30
CHEMBL3261736 1 9.30
CHEMBL3261731 1 8.85
CHEMBL3261734 1 8.74
CHEMBL1258013 1 8.64
CHEMBL3261730 1 8.62
CHEMBL2431810 1 8.60
CHEMBL527822 1 8.51
CHEMBL3261728 1 8.47
CHEMBL3261735 1 8.42
CHEMBL3261727 1 8.25
CHEMBL3261741 1 8.24
CHEMBL2030049 1 8.23
CHEMBL3261740 1 8.21
CHEMBL3261953 1 8.17
CHEMBL3261737 1 7.92
CHEMBL3261726 1 7.92
CHEMBL3261952 1 7.89
CHEMBL3261729 1 7.37
CHEMBL3261739 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3261732 EC50 = 0.03 nM 10.52
CHEMBL1450 ATOVAQUONE EC50 = 0.1 nM 10.00
CHEMBL3261738 EC50 = 0.2 nM 9.70
CHEMBL3261733 EC50 = 0.3 nM 9.52
CHEMBL3259839 EC50 = 0.5 nM 9.30
CHEMBL3261736 EC50 = 0.5 nM 9.30
CHEMBL3261731 EC50 = 1.4 nM 8.85
CHEMBL3261734 EC50 = 1.8 nM 8.74
CHEMBL1258013 EC50 = 2.3 nM 8.64
CHEMBL3261730 EC50 = 2.4 nM 8.62
CHEMBL2431810 EC50 = 2.5 nM 8.60
CHEMBL527822 EC50 = 3.1 nM 8.51
CHEMBL3261728 EC50 = 3.4 nM 8.47
CHEMBL3261735 EC50 = 3.8 nM 8.42
CHEMBL3261727 EC50 = 5.6 nM 8.25
CHEMBL3261741 EC50 = 5.8 nM 8.24
CHEMBL2030049 EC50 = 5.9 nM 8.23
CHEMBL3261740 EC50 = 6.1 nM 8.21
CHEMBL3261953 EC50 = 6.8 nM 8.17
CHEMBL3261737 EC50 = 12.0 nM 7.92
CHEMBL3261726 EC50 = 12.0 nM 7.92
CHEMBL3261952 EC50 = 13.0 nM 7.89
CHEMBL3261729 EC50 = 43.0 nM 7.37
CHEMBL3261739 EC50 > 2500.0 nM -