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Assay Detail

CHEMBL4392007

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Antimalarial activity against Plasmodium falciparum 3D7 infected in human erythrocytes after 72 hrs by SYBR green 1-based fluorescence assay
21
Total Activities
21
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 21 7.92 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4436307 1 9.52
CHEMBL1450 ATOVAQUONE 4.0 1 9.30
CHEMBL38827 LUMEFANTRINE 4.0 1 8.52
CHEMBL303933 PIPERAQUINE 3.0 1 8.14
CHEMBL76 CHLOROQUINE 4.0 1 8.02
CHEMBL4451413 1 7.96
CHEMBL3261733 1 7.96
CHEMBL4529933 1 7.82
CHEMBL4579700 1 7.80
CHEMBL4544660 1 7.55
CHEMBL4547527 1 7.08
CHEMBL4573274 1 6.75
CHEMBL4544761 1 6.58
CHEMBL7568 QUINACRINE 4.0 1 -
CHEMBL172 (S,R)-MEFLOQUINE 1 -
CHEMBL170 QUININE 4.0 1 -
CHEMBL4571858 1 -
CHEMBL4469013 1 -
CHEMBL4562828 1 -
CHEMBL4457749 1 -
CHEMBL4457910 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4436307 IC50 = 0.3 nM 9.52
CHEMBL1450 ATOVAQUONE IC50 = 0.5 nM 9.30
CHEMBL38827 LUMEFANTRINE IC50 = 3.0 nM 8.52
CHEMBL303933 PIPERAQUINE IC50 = 7.2 nM 8.14
CHEMBL76 CHLOROQUINE IC50 = 9.6 nM 8.02
CHEMBL4451413 IC50 = 11.1 nM 7.96
CHEMBL3261733 IC50 = 11.0 nM 7.96
CHEMBL4529933 IC50 = 15.0 nM 7.82
CHEMBL4579700 IC50 = 16.0 nM 7.80
CHEMBL4544660 IC50 = 28.0 nM 7.55
CHEMBL4547527 IC50 = 84.0 nM 7.08
CHEMBL4573274 IC50 = 178.0 nM 6.75
CHEMBL4544761 IC50 = 262.0 nM 6.58
CHEMBL7568 QUINACRINE IC50 - -
CHEMBL172 (S,R)-MEFLOQUINE IC50 - -
CHEMBL170 QUININE IC50 - -
CHEMBL4571858 IC50 - -
CHEMBL4469013 IC50 - -
CHEMBL4562828 IC50 - -
CHEMBL4457749 IC50 - -
CHEMBL4457910 IC50 - -