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Assay Detail

CHEMBL3241789

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Binding
Inhibition of Plasmodium falciparum plasmepsin 2
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Plasmodium falciparum
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Plasmepsin II (CHEMBL4414)
Type SINGLE PROTEIN
Organism Plasmodium falciparum

Publication

Optimization of plasmepsin inhibitor by focusing on similar structural feature with chloroquine to avoid drug-resistant mechanism of Plasmodium falciparum.
Miura T, Hidaka K, Azai Y, Kashimoto K, Kawasaki Y, Chen SE, de Freitas RF, Freire E, Kiso Y.
Bioorg Med Chem Lett (2014) 24 : 1698 -1701
PubMed 24631188 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 8.46 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3236067 1 9.00
CHEMBL3236066 1 8.96
CHEMBL3236064 1 8.92
CHEMBL3236063 1 8.77
CHEMBL3236065 1 8.64
CHEMBL3236069 1 8.37
CHEMBL3236061 1 8.36
CHEMBL3236062 1 8.32
CHEMBL3236058 1 8.26
CHEMBL3236068 1 8.24
CHEMBL3236059 1 7.96
CHEMBL3236060 1 7.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3236067 Ki = 1.0 nM 9.00
CHEMBL3236066 Ki = 1.1 nM 8.96
CHEMBL3236064 Ki = 1.2 nM 8.92
CHEMBL3236063 Ki = 1.7 nM 8.77
CHEMBL3236065 Ki = 2.3 nM 8.64
CHEMBL3236069 Ki = 4.3 nM 8.37
CHEMBL3236061 Ki = 4.4 nM 8.36
CHEMBL3236062 Ki = 4.8 nM 8.32
CHEMBL3236058 Ki = 5.5 nM 8.26
CHEMBL3236068 Ki = 5.7 nM 8.24
CHEMBL3236059 Ki = 11.0 nM 7.96
CHEMBL3236060 Ki = 22.0 nM 7.66