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Assay Detail

CHEMBL4008053

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Functional
Antimalarial activity against chloroquine-sensitive Plasmodium falciparum NF54 assessed as reduction in [3H]-hypoxanthine incorporation preincubated for 24 hrs followed by [3H]-hypoxanthine addition measured after 18 hrs by liquid scintillation counting
ChEMBL ↗
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 8.54 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4092270 — — 1 8.96
CHEMBL4069159 — — 1 8.89
CHEMBL4070429 — — 1 8.89
CHEMBL4092098 — — 1 8.89
CHEMBL4077302 — — 1 8.82
CHEMBL4082552 — — 1 8.80
CHEMBL4091361 — — 1 8.77
CHEMBL4100572 — — 1 8.77
CHEMBL4066300 — — 1 8.77
CHEMBL580910 — — 1 8.74
CHEMBL4104032 — — 1 8.72
CHEMBL4069135 — — 1 8.70
CHEMBL4093865 — — 1 8.70
CHEMBL4097433 — — 1 8.68
CHEMBL4081536 — — 1 8.68
CHEMBL4099838 — — 1 8.66
CHEMBL4072076 — — 1 8.64
CHEMBL4083579 — — 1 8.64
CHEMBL4074912 — — 1 8.64
CHEMBL4074019 — — 1 8.64
CHEMBL4089705 — — 1 8.62
CHEMBL4100778 — — 1 8.62
CHEMBL4084042 — — 1 8.60
CHEMBL4071302 — — 1 8.60
CHEMBL4064284 — — 1 8.59
CHEMBL4085085 — — 1 8.57
CHEMBL4100499 — — 1 8.54
CHEMBL4092834 — — 1 8.54
CHEMBL4061808 — — 1 8.54
CHEMBL4081835 — — 1 8.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4092270 — IC50 = 1.1 nM 8.96
CHEMBL4069159 — IC50 = 1.3 nM 8.89
CHEMBL4092098 — IC50 = 1.3 nM 8.89
CHEMBL4070429 — IC50 = 1.3 nM 8.89
CHEMBL4077302 — IC50 = 1.5 nM 8.82
CHEMBL4082552 — IC50 = 1.6 nM 8.80
CHEMBL4091361 — IC50 = 1.7 nM 8.77
CHEMBL4100572 — IC50 = 1.7 nM 8.77
CHEMBL4066300 — IC50 = 1.7 nM 8.77
CHEMBL580910 — IC50 = 1.8 nM 8.74
CHEMBL4104032 — IC50 = 1.9 nM 8.72
CHEMBL4069135 — IC50 = 2.0 nM 8.70
CHEMBL4093865 — IC50 = 2.0 nM 8.70
CHEMBL4081536 — IC50 = 2.1 nM 8.68
CHEMBL4097433 — IC50 = 2.1 nM 8.68
CHEMBL4099838 — IC50 = 2.2 nM 8.66
CHEMBL4072076 — IC50 = 2.3 nM 8.64
CHEMBL4083579 — IC50 = 2.3 nM 8.64
CHEMBL4074912 — IC50 = 2.3 nM 8.64
CHEMBL4074019 — IC50 = 2.3 nM 8.64
CHEMBL4089705 — IC50 = 2.4 nM 8.62
CHEMBL4100778 — IC50 = 2.4 nM 8.62
CHEMBL4084042 — IC50 = 2.5 nM 8.60
CHEMBL4071302 — IC50 = 2.5 nM 8.60
CHEMBL4064284 — IC50 = 2.6 nM 8.59
CHEMBL4085085 — IC50 = 2.7 nM 8.57
CHEMBL4092834 — IC50 = 2.9 nM 8.54
CHEMBL4061808 — IC50 = 2.9 nM 8.54
CHEMBL4081835 — IC50 = 2.9 nM 8.54
CHEMBL4100499 — IC50 = 2.9 nM 8.54
CHEMBL1828820 ARTEFENOMEL IC50 = 3.2 nM 8.49
CHEMBL4101516 — IC50 = 3.2 nM 8.49
CHEMBL4101605 — IC50 = 3.3 nM 8.48
CHEMBL4070246 — IC50 = 3.3 nM 8.48
CHEMBL4063456 — IC50 = 3.3 nM 8.48
CHEMBL4070954 — IC50 = 3.4 nM 8.47
CHEMBL4068615 — IC50 = 3.6 nM 8.44
CHEMBL4101597 — IC50 = 3.8 nM 8.42
CHEMBL4062891 — IC50 = 3.9 nM 8.41
CHEMBL4073682 — IC50 = 4.1 nM 8.39
CHEMBL4077597 — IC50 = 4.4 nM 8.36
CHEMBL4091290 — IC50 = 4.7 nM 8.33
CHEMBL4091806 — IC50 = 4.8 nM 8.32
CHEMBL4078151 — IC50 = 5.0 nM 8.30
CHEMBL4062326 — IC50 = 5.4 nM 8.27
CHEMBL4099546 — IC50 = 5.9 nM 8.23
CHEMBL4065089 — IC50 = 8.5 nM 8.07
CHEMBL4096204 — IC50 = 8.7 nM 8.06
CHEMBL4074836 — IC50 = 9.7 nM 8.01
CHEMBL4092772 — IC50 = 12.2 nM 7.91