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Assay Detail

CHEMBL4391970

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Functional
Antimalarial activity against multidrug-resistant Plasmodium falciparum Dd2 infected in human erythrocytes by SYBR green 1-based fluorescence assay
ChEMBL ↗
77
Total Activities
77
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

Discovery and Structural Optimization of Acridones as Broad-Spectrum Antimalarials.
Dodean RA, Kancharla P, Li Y, Melendez V, Read L, Bane CE, Vesely B, Kreishman-Deitrick M, Black C, Li Q, Sciotti RJ, Olmeda R, Luong TL, Gaona H, Potter B, Sousa J, Marcsisin S, Caridha D, Xie L, Vuong C, Zeng Q, Zhang J, Zhang P, Lin H, Butler K, Roncal N, Gaynor-Ohnstad L, Leed SE, Nolan C, Huezo SJ, Rasmussen SA, Stephens MT, Tan JC, Cooper RA, Smilkstein MJ, Pou S, Winter RW, Riscoe MK, Kelly JX.
J Med Chem (2019) 62 : 3475 -3502
PubMed 30852885 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 77 7.57 10.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4464660 — — 1 10.82
CHEMBL4586210 — — 1 10.48
CHEMBL4457749 — — 1 10.39
CHEMBL4471348 — — 1 10.39
CHEMBL4457910 — — 1 10.30
CHEMBL1450 ATOVAQUONE 4.0 1 10.00
CHEMBL4465617 — — 1 9.89
CHEMBL4553286 — — 1 9.80
CHEMBL4513754 — — 1 9.52
CHEMBL4458629 — — 1 9.36
CHEMBL4532218 — — 1 9.31
CHEMBL4513569 — — 1 9.00
CHEMBL4573274 — — 1 8.77
CHEMBL4517602 — — 1 8.54
CHEMBL4472705 — — 1 8.38
CHEMBL38827 LUMEFANTRINE 4.0 1 8.24
CHEMBL4439514 — — 1 8.15
CHEMBL4454647 — — 1 8.11
CHEMBL4461187 — — 1 8.05
CHEMBL303933 PIPERAQUINE 3.0 1 8.05
CHEMBL4557331 — — 1 7.96
CHEMBL4438847 — — 1 7.96
CHEMBL4517848 — — 1 7.92
CHEMBL4544660 — — 1 7.92
CHEMBL3261733 — — 1 7.89
CHEMBL4437915 — — 1 7.82
CHEMBL4529933 — — 1 7.80
CHEMBL4476110 — — 1 7.77
CHEMBL4451413 — — 1 7.77
CHEMBL4574985 — — 1 7.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4464660 — IC50 = 0.015 nM 10.82
CHEMBL4586210 — IC50 = 0.033 nM 10.48
CHEMBL4471348 — IC50 = 0.041 nM 10.39
CHEMBL4457749 — IC50 = 0.041 nM 10.39
CHEMBL4457910 — IC50 = 0.05 nM 10.30
CHEMBL1450 ATOVAQUONE IC50 = 0.1 nM 10.00
CHEMBL4465617 — IC50 = 0.13 nM 9.89
CHEMBL4553286 — IC50 = 0.16 nM 9.80
CHEMBL4513754 — IC50 = 0.3 nM 9.52
CHEMBL4458629 — IC50 = 0.44 nM 9.36
CHEMBL4532218 — IC50 = 0.49 nM 9.31
CHEMBL4513569 — IC50 = 1.0 nM 9.00
CHEMBL4573274 — IC50 = 1.7 nM 8.77
CHEMBL4517602 — IC50 = 2.9 nM 8.54
CHEMBL4472705 — IC50 = 4.2 nM 8.38
CHEMBL38827 LUMEFANTRINE IC50 = 5.7 nM 8.24
CHEMBL4439514 — IC50 = 7.0 nM 8.15
CHEMBL4454647 — IC50 = 7.8 nM 8.11
CHEMBL4461187 — IC50 = 8.9 nM 8.05
CHEMBL303933 PIPERAQUINE IC50 = 9.0 nM 8.05
CHEMBL4557331 — IC50 = 11.0 nM 7.96
CHEMBL4438847 — IC50 = 11.0 nM 7.96
CHEMBL4517848 — IC50 = 12.0 nM 7.92
CHEMBL4544660 — IC50 = 12.0 nM 7.92
CHEMBL3261733 — IC50 = 13.0 nM 7.89
CHEMBL4437915 — IC50 = 15.0 nM 7.82
CHEMBL4529933 — IC50 = 16.0 nM 7.80
CHEMBL4476110 — IC50 = 17.0 nM 7.77
CHEMBL4451413 — IC50 = 17.0 nM 7.77
CHEMBL4574985 — IC50 = 17.0 nM 7.77
CHEMBL172 (S,R)-MEFLOQUINE IC50 = 18.0 nM 7.75
CHEMBL4579700 — IC50 = 22.0 nM 7.66
CHEMBL4435084 — IC50 = 27.0 nM 7.57
CHEMBL7568 QUINACRINE IC50 = 29.0 nM 7.54
CHEMBL4591302 — IC50 = 34.0 nM 7.47
CHEMBL4554608 — IC50 = 37.0 nM 7.43
CHEMBL4551172 — IC50 = 38.0 nM 7.42
CHEMBL4474607 — IC50 = 38.0 nM 7.42
CHEMBL4547527 — IC50 = 41.0 nM 7.39
CHEMBL4569227 — IC50 = 45.0 nM 7.35
CHEMBL4535380 — IC50 = 63.0 nM 7.20
CHEMBL3188523 — IC50 = 77.0 nM 7.11
CHEMBL4571858 — IC50 = 77.0 nM 7.11
CHEMBL4440690 — IC50 = 92.0 nM 7.04
CHEMBL4560448 — IC50 = 105.0 nM 6.98
CHEMBL4544761 — IC50 = 132.0 nM 6.88
CHEMBL4536883 — IC50 = 132.0 nM 6.88
CHEMBL4469013 — IC50 = 139.0 nM 6.86
CHEMBL4436121 — IC50 = 145.0 nM 6.84
CHEMBL76 CHLOROQUINE IC50 = 163.0 nM 6.79