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Assay Detail

CHEMBL4680972

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

Functional
Antiplasmodial activity against late stage (IV/V) Plasmodium falciparum NF54 gametocytes transfected with GFP-LUC assessed as growth inhibition incubated for 72 hrs by mitotracker Red-CMXROS dye based fluorescence microscopic analysis
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

Discovery of a Quinoline-4-carboxamide Derivative with a Novel Mechanism of Action, Multistage Antimalarial Activity, and Potent in Vivo Efficacy.
Baragaña B,Norcross NR,Wilson C,Porzelle A,Hallyburton I,Grimaldi R,Osuna-Cabello M,Norval S,Riley J,Stojanovski L,Simeons FR,Wyatt PG,Delves MJ,Meister S,Duffy S,Avery VM,Winzeler EA,Sinden RE,Wittlin S,Frearson JA,Gray DW,Fairlamb AH,Waterson D,Campbell SF,Willis P,Read KD,Gilbert IH
J Med Chem (2016) 59 : 9672 -9685
PubMed 27631715 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 6.96 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL269671 ARTEMISININ 3.0 1 9.10
CHEMBL4091762 CABAMIQUINE 2.0 1 7.62
CHEMBL4764214 1 7.41
CHEMBL4781713 1 6.98
CHEMBL4783407 1 6.82
CHEMBL35228 PYRONARIDINE 3.0 1 5.51
CHEMBL298470 TAFENOQUINE 4.0 1 5.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL269671 ARTEMISININ EC50 = 0.8 nM 9.10
CHEMBL4091762 CABAMIQUINE EC50 = 24.0 nM 7.62
CHEMBL4764214 EC50 = 39.0 nM 7.41
CHEMBL4781713 EC50 = 104.0 nM 6.98
CHEMBL4783407 EC50 = 152.0 nM 6.82
CHEMBL35228 PYRONARIDINE EC50 = 3108.0 nM 5.51
CHEMBL298470 TAFENOQUINE EC50 = 5250.0 nM 5.28