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Assay Detail

CHEMBL4606282

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Functional
Antimalarial activity against Plasmodium falciparum clinical isolates measured after 72 hrs by SYBR green dye based fluorescence assay
7
Total Activities
7
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

Lead Optimization of Second-Generation Acridones as Broad-Spectrum Antimalarials.
Kancharla P, Dodean RA, Li Y, Pou S, Pybus B, 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, Ceja FG, Rasmussen SA, Tumwebaze PK, Rosenthal PJ, Mu J, Bayles BR, Cooper RA, Reynolds KA, Smilkstein MJ, Riscoe MK, Kelly JX.
J Med Chem (2020) 63 : 6179 -6202
PubMed 32390431 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 8.45 9.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1450 ATOVAQUONE 4.0 1 9.57
CHEMBL307261 ARTENIMOL 3.0 1 8.85
CHEMBL4634377 1 8.41
CHEMBL38827 LUMEFANTRINE 4.0 1 8.38
CHEMBL4639326 1 8.27
CHEMBL303933 PIPERAQUINE 3.0 1 8.23
CHEMBL76 CHLOROQUINE 4.0 1 7.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1450 ATOVAQUONE IC50 = 0.27 nM 9.57
CHEMBL307261 ARTENIMOL IC50 = 1.4 nM 8.85
CHEMBL4634377 IC50 = 3.9 nM 8.41
CHEMBL38827 LUMEFANTRINE IC50 = 4.2 nM 8.38
CHEMBL4639326 IC50 = 5.4 nM 8.27
CHEMBL303933 PIPERAQUINE IC50 = 5.9 nM 8.23
CHEMBL76 CHLOROQUINE IC50 = 34.0 nM 7.47