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Assay Detail

CHEMBL830893

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Binding
Inhibitory concentration against beta-site APP cleaving enzyme (BACE-1) by fluorescence resonance energy transfer assay
4
Total Activities
4
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

Discovery of cell-permeable non-peptide inhibitors of beta-secretase by high-throughput docking and continuum electrostatics calculations.
Huang D, Lüthi U, Kolb P, Edler K, Cecchini M, Audetat S, Barberis A, Caflisch A.
J Med Chem (2005) 48 : 5108 -5111
PubMed 16078830 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.13 7.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL370043 1 7.24
CHEMBL190644 1 7.01
CHEMBL190346 1 -
CHEMBL363539 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL370043 IC50 = 57.8 nM 7.24
CHEMBL190644 IC50 = 97.0 nM 7.01
CHEMBL190346 IC50 > 25.0 nM -
CHEMBL363539 IC50 = 283900.0 nM -