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Assay Detail

CHEMBL4008052

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Functional
Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 assessed as reduction in [3H]-hypoxanthine incorporation preincubated for 24 hrs followed by [3H]-hypoxanthine addition measured after 18 hrs by liquid scintillation counting
50
Total Activities
50
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

Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).
Dong Y, Wang X, Kamaraj S, Bulbule VJ, Chiu FC, Chollet J, Dhanasekaran M, Hein CD, Papastogiannidis P, Morizzi J, Shackleford DM, Barker H, Ryan E, Scheurer C, Tang Y, Zhao Q, Zhou L, White KL, Urwyler H, Charman WN, Matile H, Wittlin S, Charman SA, Vennerstrom JL.
J Med Chem (2017) 60 : 2654 -2668
PubMed 28052200 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 50 8.61 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4092270 1 9.05
CHEMBL4069159 1 9.00
CHEMBL4089705 1 9.00
CHEMBL4093865 1 8.89
CHEMBL4097433 1 8.85
CHEMBL4077302 1 8.82
CHEMBL4100778 1 8.82
CHEMBL4066300 1 8.82
CHEMBL4070429 1 8.80
CHEMBL4069135 1 8.80
CHEMBL4074912 1 8.77
CHEMBL4092098 1 8.77
CHEMBL4085085 1 8.74
CHEMBL4064284 1 8.74
CHEMBL4100499 1 8.74
CHEMBL4081536 1 8.74
CHEMBL4084042 1 8.72
CHEMBL580910 1 8.70
CHEMBL1828820 ARTEFENOMEL 2.0 1 8.70
CHEMBL4101597 1 8.70
CHEMBL4104032 1 8.70
CHEMBL4101516 1 8.70
CHEMBL4070954 1 8.70
CHEMBL4091361 1 8.68
CHEMBL4063456 1 8.68
CHEMBL4061808 1 8.68
CHEMBL4099838 1 8.66
CHEMBL4100572 1 8.64
CHEMBL4078151 1 8.64
CHEMBL4083579 1 8.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4092270 IC50 = 0.9 nM 9.05
CHEMBL4069159 IC50 = 1.0 nM 9.00
CHEMBL4089705 IC50 = 1.0 nM 9.00
CHEMBL4093865 IC50 = 1.3 nM 8.89
CHEMBL4097433 IC50 = 1.4 nM 8.85
CHEMBL4077302 IC50 = 1.5 nM 8.82
CHEMBL4100778 IC50 = 1.5 nM 8.82
CHEMBL4066300 IC50 = 1.5 nM 8.82
CHEMBL4070429 IC50 = 1.6 nM 8.80
CHEMBL4069135 IC50 = 1.6 nM 8.80
CHEMBL4074912 IC50 = 1.7 nM 8.77
CHEMBL4092098 IC50 = 1.7 nM 8.77
CHEMBL4100499 IC50 = 1.8 nM 8.74
CHEMBL4085085 IC50 = 1.8 nM 8.74
CHEMBL4064284 IC50 = 1.8 nM 8.74
CHEMBL4081536 IC50 = 1.8 nM 8.74
CHEMBL4084042 IC50 = 1.9 nM 8.72
CHEMBL580910 IC50 = 2.0 nM 8.70
CHEMBL1828820 ARTEFENOMEL IC50 = 2.0 nM 8.70
CHEMBL4101597 IC50 = 2.0 nM 8.70
CHEMBL4104032 IC50 = 2.0 nM 8.70
CHEMBL4101516 IC50 = 2.0 nM 8.70
CHEMBL4070954 IC50 = 2.0 nM 8.70
CHEMBL4061808 IC50 = 2.1 nM 8.68
CHEMBL4091361 IC50 = 2.1 nM 8.68
CHEMBL4063456 IC50 = 2.1 nM 8.68
CHEMBL4099838 IC50 = 2.2 nM 8.66
CHEMBL4100572 IC50 = 2.3 nM 8.64
CHEMBL4078151 IC50 = 2.3 nM 8.64
CHEMBL4083579 IC50 = 2.3 nM 8.64
CHEMBL4082552 IC50 = 2.4 nM 8.62
CHEMBL4071302 IC50 = 2.5 nM 8.60
CHEMBL4074019 IC50 = 2.6 nM 8.59
CHEMBL4092834 IC50 = 2.8 nM 8.55
CHEMBL4068615 IC50 = 2.9 nM 8.54
CHEMBL4091290 IC50 = 2.9 nM 8.54
CHEMBL4072076 IC50 = 2.9 nM 8.54
CHEMBL4062891 IC50 = 3.2 nM 8.49
CHEMBL4081835 IC50 = 3.2 nM 8.49
CHEMBL4070246 IC50 = 3.6 nM 8.44
CHEMBL4101605 IC50 = 3.7 nM 8.43
CHEMBL4077597 IC50 = 3.8 nM 8.42
CHEMBL4091806 IC50 = 4.8 nM 8.32
CHEMBL4073682 IC50 = 5.2 nM 8.28
CHEMBL4074836 IC50 = 5.5 nM 8.26
CHEMBL4062326 IC50 = 5.8 nM 8.24
CHEMBL4099546 IC50 = 5.7 nM 8.24
CHEMBL4092772 IC50 = 6.5 nM 8.19
CHEMBL4065089 IC50 = 9.2 nM 8.04
CHEMBL4096204 IC50 = 9.5 nM 8.02