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Assay Detail

CHEMBL832831

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

Binding
Inhibitory activity against beta-secretase 1 (BACE1)
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Beta-secretase 1 (CHEMBL4822)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of highly active Alzheimer's beta-secretase (BACE1) inhibitors, KMI-420 and KMI-429, with enhanced chemical stability.
Kimura T, Shuto D, Hamada Y, Igawa N, Kasai S, Liu P, Hidaka K, Hamada T, Hayashi Y, Kiso Y.
Bioorg Med Chem Lett (2005) 15 : 211 -215
PubMed 15582441 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.94 8.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL183546 1 8.41
CHEMBL181826 1 8.33
CHEMBL183494 1 8.09
CHEMBL367139 1 7.80
CHEMBL183059 1 7.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL183546 IC50 = 3.9 nM 8.41
CHEMBL181826 IC50 = 4.7 nM 8.33
CHEMBL183494 IC50 = 8.2 nM 8.09
CHEMBL367139 IC50 = 16.0 nM 7.80
CHEMBL183059 IC50 = 84.0 nM 7.08