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Assay Detail

CHEMBL4013660

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

Functional
Gametocytocidal activity against transgenic GFP-fused Plasmodium falciparum NF54 ring stage gametocytes after 72 hrs by Mitotracker Red CMH2XRos staining based confocal microscopic method
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

3-Hydroxy-N'-arylidenepropanehydrazonamides with Halo-Substituted Phenanthrene Scaffolds Cure P. berghei Infected Mice When Administered Perorally.
Leven M, Knaab TC, Held J, Duffy S, Meister S, Fischli C, Meitzner D, Lehmann U, Lungerich B, Kuna K, Stahlke P, Delves MJ, Buchholz M, Winzeler EA, Avery VM, Mordmüller B, Wittlin S, Kurz T.
J Med Chem (2017) 60 : 6036 -6044
PubMed 28653845 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.39 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL361497 ARTESUNATE 4.0 1 8.52
CHEMBL76 CHLOROQUINE 4.0 1 7.77
CHEMBL4070451 1 7.44
CHEMBL4081080 1 7.18
CHEMBL4105332 1 6.96
CHEMBL4097624 1 6.46
CHEMBL1450 ATOVAQUONE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL361497 ARTESUNATE IC50 = 3.0 nM 8.52
CHEMBL76 CHLOROQUINE IC50 = 17.0 nM 7.77
CHEMBL4070451 IC50 = 36.0 nM 7.44
CHEMBL4081080 IC50 = 66.0 nM 7.18
CHEMBL4105332 IC50 = 110.0 nM 6.96
CHEMBL4097624 IC50 = 345.0 nM 6.46
CHEMBL1450 ATOVAQUONE IC50 - -