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Assay Detail

CHEMBL4260388

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

Binding
Inhibition of BACE1 in human SH-SY5Y cells harboring wild type APP695 assessed as reduction in amyloid beta (1 to 42) level after 24 hrs by ELISA method
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type SH-SY5Y
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

A phenotypic approach to the discovery of compounds that promote non-amyloidogenic processing of the amyloid precursor protein: Toward a new profile of indirect β-secretase inhibitors.
Gay M, Evrard C, Descamps F, Carato P, Renault N, Coevoet M, Eddarkaoui S, Baud C, Larchanché PE, Buée L, El Bakali J, Vingtdeux V, Sergeant N, Melnyk P.
Eur J Med Chem (2018) 159 : 104 -125
PubMed 30268822 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 5.49 5.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4291231 1 5.92
CHEMBL4281005 1 5.92
CHEMBL4290806 1 5.80
CHEMBL4282946 1 5.80
CHEMBL4293890 1 5.77
CHEMBL4280586 1 5.75
CHEMBL4284039 1 5.70
CHEMBL419432 1 5.68
CHEMBL4291976 1 5.57
CHEMBL4294633 1 5.55
CHEMBL4282611 1 5.48
CHEMBL4284107 1 5.47
CHEMBL4288906 1 5.44
CHEMBL4279482 1 5.40
CHEMBL4278741 1 5.39
CHEMBL4289410 1 5.38
CHEMBL4285991 1 5.32
CHEMBL4279857 1 5.19
CHEMBL167970 1 4.95
CHEMBL76 CHLOROQUINE 4.0 1 4.90
CHEMBL4287392 1 4.86

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4291231 IC50 = 1200.0 nM 5.92
CHEMBL4281005 IC50 = 1200.0 nM 5.92
CHEMBL4290806 IC50 = 1600.0 nM 5.80
CHEMBL4282946 IC50 = 1600.0 nM 5.80
CHEMBL4293890 IC50 = 1700.0 nM 5.77
CHEMBL4280586 IC50 = 1800.0 nM 5.75
CHEMBL4284039 IC50 = 2000.0 nM 5.70
CHEMBL419432 IC50 = 2100.0 nM 5.68
CHEMBL4291976 IC50 = 2700.0 nM 5.57
CHEMBL4294633 IC50 = 2800.0 nM 5.55
CHEMBL4282611 IC50 = 3300.0 nM 5.48
CHEMBL4284107 IC50 = 3400.0 nM 5.47
CHEMBL4288906 IC50 = 3600.0 nM 5.44
CHEMBL4279482 IC50 = 4000.0 nM 5.40
CHEMBL4278741 IC50 = 4100.0 nM 5.39
CHEMBL4289410 IC50 = 4200.0 nM 5.38
CHEMBL4285991 IC50 = 4800.0 nM 5.32
CHEMBL4279857 IC50 = 6500.0 nM 5.19
CHEMBL167970 IC50 = 11200.0 nM 4.95
CHEMBL76 CHLOROQUINE IC50 = 12700.0 nM 4.90
CHEMBL4287392 IC50 = 13700.0 nM 4.86