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Assay Detail

CHEMBL4194451

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Functional
Antiplasmodial activity against chloroquine and pyrimethamine resistant Plasmodium falciparum K1 assessed as reduction in [3H]-hypoxanthine incorporation incubated for 48 hrs by liquid scintillation counting method
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Plasmodium falciparum
Confidence 1 — Organism
Curated By Intermediate

Target

Plasmodium falciparum (CHEMBL364)
Type ORGANISM
Organism Plasmodium falciparum

Publication

Synthesis and antimalarial evaluation of artesunate-polyamine and trioxolane-polyamine conjugates.
Pearce AN, Kaiser M, Copp BR.
Eur J Med Chem (2017) 140 : 595 -603
PubMed 28988153 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 8.27 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL361497 ARTESUNATE 4.0 1 9.30
CHEMBL4205016 1 9.22
CHEMBL4205524 1 9.22
CHEMBL4217237 1 9.22
CHEMBL4213779 1 9.10
CHEMBL4214291 1 9.10
CHEMBL4209396 1 9.10
CHEMBL4218712 1 9.05
CHEMBL4217759 1 8.96
CHEMBL1830032 1 8.55
CHEMBL4209154 1 8.30
CHEMBL4212555 1 8.21
CHEMBL4212811 1 8.04
CHEMBL4208833 1 7.96
CHEMBL4210583 1 7.96
CHEMBL4215412 1 7.52
CHEMBL4214072 1 7.49
CHEMBL4213553 1 7.23
CHEMBL4218487 1 7.22
CHEMBL4205722 1 7.12
CHEMBL76 CHLOROQUINE 4.0 1 5.74
CHEMBL4214244 1 -
CHEMBL4208197 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL361497 ARTESUNATE IC50 = 0.5 nM 9.30
CHEMBL4205016 IC50 = 0.6 nM 9.22
CHEMBL4205524 IC50 = 0.6 nM 9.22
CHEMBL4217237 IC50 = 0.6 nM 9.22
CHEMBL4213779 IC50 = 0.8 nM 9.10
CHEMBL4214291 IC50 = 0.8 nM 9.10
CHEMBL4209396 IC50 = 0.8 nM 9.10
CHEMBL4218712 IC50 = 0.9 nM 9.05
CHEMBL4217759 IC50 = 1.1 nM 8.96
CHEMBL1830032 IC50 = 2.8 nM 8.55
CHEMBL4209154 IC50 = 5.0 nM 8.30
CHEMBL4212555 IC50 = 6.2 nM 8.21
CHEMBL4212811 IC50 = 9.2 nM 8.04
CHEMBL4208833 IC50 = 11.0 nM 7.96
CHEMBL4210583 IC50 = 11.0 nM 7.96
CHEMBL4215412 IC50 = 30.0 nM 7.52
CHEMBL4214072 IC50 = 32.2 nM 7.49
CHEMBL4213553 IC50 = 59.0 nM 7.23
CHEMBL4218487 IC50 = 60.0 nM 7.22
CHEMBL4205722 IC50 = 76.0 nM 7.12
CHEMBL76 CHLOROQUINE IC50 = 1828.0 nM 5.74
CHEMBL4214244 IC50 - -
CHEMBL4208197 IC50 - -