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Assay Detail

CHEMBL4391972

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Functional
Antimalarial activity against atovaquone-resistant Plasmodium falciparum Tm90-C2B infected in human erythrocytes by SYBR green 1-based fluorescence assay
ChEMBL ↗
71
Total Activities
71
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 71 6.51 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4464660 — — 1 8.70
CHEMBL4471348 — — 1 8.27
CHEMBL4436307 — — 1 8.17
CHEMBL4586210 — — 1 7.40
CHEMBL4553286 — — 1 7.40
CHEMBL4439514 — — 1 7.34
CHEMBL4465617 — — 1 7.33
CHEMBL4574985 — — 1 7.24
CHEMBL4554608 — — 1 7.17
CHEMBL4517602 — — 1 7.16
CHEMBL3188523 — — 1 7.15
CHEMBL4472705 — — 1 7.09
CHEMBL4545135 — — 1 7.09
CHEMBL4513754 — — 1 7.05
CHEMBL4557331 — — 1 7.02
CHEMBL4544761 — — 1 7.01
CHEMBL4457910 — — 1 6.85
CHEMBL4467034 — — 1 6.82
CHEMBL4571858 — — 1 6.79
CHEMBL4436121 — — 1 6.75
CHEMBL4474607 — — 1 6.71
CHEMBL76 CHLOROQUINE 4.0 1 6.68
CHEMBL4457749 — — 1 6.64
CHEMBL4569227 — — 1 6.64
CHEMBL4447569 — — 1 6.57
CHEMBL4513569 — — 1 6.57
CHEMBL4476110 — — 1 6.56
CHEMBL4449707 — — 1 6.53
CHEMBL4437915 — — 1 6.50
CHEMBL4573274 — — 1 6.45

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4464660 — IC50 = 2.0 nM 8.70
CHEMBL4471348 — IC50 = 5.4 nM 8.27
CHEMBL4436307 — IC50 = 6.8 nM 8.17
CHEMBL4586210 — IC50 = 40.0 nM 7.40
CHEMBL4553286 — IC50 = 40.0 nM 7.40
CHEMBL4439514 — IC50 = 46.0 nM 7.34
CHEMBL4465617 — IC50 = 47.0 nM 7.33
CHEMBL4574985 — IC50 = 58.0 nM 7.24
CHEMBL4554608 — IC50 = 68.0 nM 7.17
CHEMBL4517602 — IC50 = 70.0 nM 7.16
CHEMBL3188523 — IC50 = 71.0 nM 7.15
CHEMBL4472705 — IC50 = 81.0 nM 7.09
CHEMBL4545135 — IC50 = 82.0 nM 7.09
CHEMBL4513754 — IC50 = 89.0 nM 7.05
CHEMBL4557331 — IC50 = 96.0 nM 7.02
CHEMBL4544761 — IC50 = 97.0 nM 7.01
CHEMBL4457910 — IC50 = 142.0 nM 6.85
CHEMBL4467034 — IC50 = 153.0 nM 6.82
CHEMBL4571858 — IC50 = 163.0 nM 6.79
CHEMBL4436121 — IC50 = 177.0 nM 6.75
CHEMBL4474607 — IC50 = 196.0 nM 6.71
CHEMBL76 CHLOROQUINE IC50 = 208.0 nM 6.68
CHEMBL4457749 — IC50 = 228.0 nM 6.64
CHEMBL4569227 — IC50 = 228.0 nM 6.64
CHEMBL4513569 — IC50 = 270.0 nM 6.57
CHEMBL4447569 — IC50 = 270.0 nM 6.57
CHEMBL4476110 — IC50 = 274.0 nM 6.56
CHEMBL4449707 — IC50 = 297.0 nM 6.53
CHEMBL4437915 — IC50 = 317.0 nM 6.50
CHEMBL4573274 — IC50 = 356.0 nM 6.45
CHEMBL4551172 — IC50 = 371.0 nM 6.43
CHEMBL4562828 — IC50 = 368.0 nM 6.43
CHEMBL4457727 — IC50 = 386.0 nM 6.41
CHEMBL4517848 — IC50 = 409.0 nM 6.39
CHEMBL4532218 — IC50 = 440.0 nM 6.36
CHEMBL4579700 — IC50 = 465.0 nM 6.33
CHEMBL4536883 — IC50 = 507.0 nM 6.29
CHEMBL4437347 — IC50 = 551.0 nM 6.26
CHEMBL4535380 — IC50 = 563.0 nM 6.25
CHEMBL4440690 — IC50 = 558.0 nM 6.25
CHEMBL4547527 — IC50 = 589.0 nM 6.23
CHEMBL4444698 — IC50 = 622.0 nM 6.21
CHEMBL4454647 — IC50 = 705.0 nM 6.15
CHEMBL4464872 — IC50 = 945.0 nM 6.03
CHEMBL4591302 — IC50 = 968.0 nM 6.01
CHEMBL4451413 — IC50 = 1045.0 nM 5.98
CHEMBL4444991 — IC50 = 1044.0 nM 5.98
CHEMBL4563655 — IC50 = 1163.0 nM 5.93
CHEMBL4544660 — IC50 = 1259.0 nM 5.90
CHEMBL4435084 — IC50 = 1377.0 nM 5.86