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Assay Detail

CHEMBL4056787

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

Functional
Antiplasmodial activity against chloroquine-sensitive IEF stage of Plasmodium falciparum NF54 infected in human RBC assessed as reduction in [3H]hypoxanthine incorporation preincubated for 48 hrs followed by [3H]hypoxanthine addition measured after 24 hrs by liquid scintillation counting method
12
Total Activities
12
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

Structure-activity relationship studies on thiaplidiaquinones A and B as novel inhibitors of Plasmodium falciparum and farnesyltransferase.
Cadelis MM, Bourguet-Kondracki ML, Dubois J, Kaiser M, Brunel JM, Barker D, Copp BR.
Bioorg Med Chem (2017) 25 : 4433 -4443
PubMed 28666857 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.56 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL76 CHLOROQUINE 4.0 1 8.22
CHEMBL4098096 1 6.54
CHEMBL4075066 1 5.70
CHEMBL4104673 1 5.54
CHEMBL4086502 1 5.47
CHEMBL4076843 1 5.40
CHEMBL4075495 1 5.32
CHEMBL4090877 1 5.14
CHEMBL4105597 1 5.13
CHEMBL4095500 1 5.10
CHEMBL4063801 1 4.69
CHEMBL4096919 1 4.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL76 CHLOROQUINE IC50 = 6.0 nM 8.22
CHEMBL4098096 IC50 = 290.0 nM 6.54
CHEMBL4075066 IC50 = 2000.0 nM 5.70
CHEMBL4104673 IC50 = 2900.0 nM 5.54
CHEMBL4086502 IC50 = 3400.0 nM 5.47
CHEMBL4076843 IC50 = 4000.0 nM 5.40
CHEMBL4075495 IC50 = 4800.0 nM 5.32
CHEMBL4090877 IC50 = 7200.0 nM 5.14
CHEMBL4105597 IC50 = 7400.0 nM 5.13
CHEMBL4095500 IC50 = 8000.0 nM 5.10
CHEMBL4063801 IC50 = 20400.0 nM 4.69
CHEMBL4096919 IC50 = 33900.0 nM 4.47