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Assay Detail

CHEMBL4045493

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Functional
Antiparasitic activity against intraerythrocytic form of chloroquine/pyrimethamine-resistant Plasmodium falciparum K1 infected in human RBC preincubated for 48 hrs followed by [3H]-hypoxanthine addition measured after 24 hrs by liquid scintillation counting analysis
11
Total Activities
11
Compounds Tested
2
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 selection of antiparasitic compounds from a focused library of benzenesulfonyl derivatives of heterocycles.
Pagliero RJ, Kaiser M, Brun R, Nieto MJ, Mazzieri MR.
Bioorg Med Chem Lett (2017) 27 : 3945 -3949
PubMed 28789893 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Activity 8 - -
IC50 3 6.08 6.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL76 CHLOROQUINE 4.0 1 6.60
CHEMBL4075894 1 5.82
CHEMBL4094002 1 5.82
CHEMBL1885822 1 -
CHEMBL4072453 1 -
CHEMBL517496 1 -
CHEMBL4064884 1 -
CHEMBL4102778 1 -
CHEMBL4095965 1 -
CHEMBL4076450 1 -
CHEMBL82224 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL76 CHLOROQUINE IC50 = 250.0 nM 6.60
CHEMBL4075894 IC50 = 1500.0 nM 5.82
CHEMBL4094002 IC50 = 1500.0 nM 5.82
CHEMBL1885822 Activity - -
CHEMBL4072453 Activity - -
CHEMBL517496 Activity - -
CHEMBL4064884 Activity - -
CHEMBL4102778 Activity - -
CHEMBL4095965 Activity - -
CHEMBL4076450 Activity - -
CHEMBL82224 Activity - -