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Assay Detail

CHEMBL764684

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Binding
Inhibitory activity against plasmepsin-2
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Plasmepsin II (CHEMBL4414)
Type SINGLE PROTEIN
Organism Plasmodium falciparum

Publication

Potent, low-molecular-weight non-peptide inhibitors of malarial aspartyl protease plasmepsin II.
Haque TS, Skillman AG, Lee CE, Habashita H, Gluzman IY, Ewing TJ, Goldberg DE, Kuntz ID, Ellman JA.
J Med Chem (1999) 42 : 1428 -1440
PubMed 10212129 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 7.97 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL285133 1 8.70
CHEMBL285177 1 8.70
CHEMBL34323 1 8.52
CHEMBL290115 1 8.40
CHEMBL32684 1 8.39
CHEMBL33989 1 8.37
CHEMBL284534 1 8.32
CHEMBL284955 1 8.05
CHEMBL32997 1 7.00
CHEMBL34051 1 6.66
CHEMBL284151 1 6.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL285133 Ki = 2.0 nM 8.70
CHEMBL285177 Ki = 2.0 nM 8.70
CHEMBL34323 Ki = 3.0 nM 8.52
CHEMBL290115 Ki = 4.0 nM 8.40
CHEMBL32684 Ki = 4.1 nM 8.39
CHEMBL33989 Ki = 4.3 nM 8.37
CHEMBL284534 Ki = 4.8 nM 8.32
CHEMBL284955 Ki = 9.0 nM 8.05
CHEMBL32997 Ki = 100.0 nM 7.00
CHEMBL34051 Ki = 220.0 nM 6.66
CHEMBL284151 Ki = 300.0 nM 6.52