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Assay Detail

CHEMBL2154188

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Binding
Inhibition of BACE by TR-FRET assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Compounds and Their Use as BACE Inhibitors: Patent Highlight.
Blass B.
ACS Med Chem Lett (2012) 3 : 875 -876
PubMed 24900397 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 8.64 9.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2152921 1 9.14
CHEMBL2151058 1 8.85
CHEMBL2152919 1 8.85
CHEMBL2152915 1 8.80
CHEMBL2152918 1 8.80
CHEMBL2152914 1 8.66
CHEMBL2152920 1 8.64
CHEMBL2152916 1 8.32
CHEMBL2152917 1 7.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2152921 IC50 = 0.72 nM 9.14
CHEMBL2151058 IC50 = 1.4 nM 8.85
CHEMBL2152919 IC50 = 1.4 nM 8.85
CHEMBL2152915 IC50 = 1.6 nM 8.80
CHEMBL2152918 IC50 = 1.6 nM 8.80
CHEMBL2152914 IC50 = 2.2 nM 8.66
CHEMBL2152920 IC50 = 2.3 nM 8.64
CHEMBL2152916 IC50 = 4.8 nM 8.32
CHEMBL2152917 IC50 = 20.0 nM 7.70