Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL5336813

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

Binding
Inhibition of human recombinant BACE1 using Rh-EVNLDAEFK-quencher as substrate incubated for 60 mins by FRET assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of novel multifunctional ligands targeting GABA transporters, butyrylcholinesterase, β-secretase, and amyloid β aggregation as potential treatment of Alzheimer's disease.
Zaręba P, Łątka K, Mazur G, Gryzło B, Pasieka A, Godyń J, Panek D, Skrzypczak-Wiercioch A, Höfner GC, Latacz G, Maj M, Espargaró A, Sabaté R, Jóźwiak K, Wanner KT, Sałat K, Malawska B, Kulig K, Bajda M.
Eur J Med Chem (2023) 261 : 115832 -115832
PubMed 37837674 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 5.26 7.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL378225 1 7.23
CHEMBL5423316 1 5.80
CHEMBL4861574 1 5.39
CHEMBL4852705 1 5.31
CHEMBL5423337 1 5.29
CHEMBL4859850 1 5.29
CHEMBL5404846 1 5.27
CHEMBL5411905 1 5.27
CHEMBL4854550 1 5.17
CHEMBL5440565 1 5.03
CHEMBL4849009 1 4.76
CHEMBL4868987 1 4.71
CHEMBL5411369 1 4.64
CHEMBL4873878 1 4.54
CHEMBL502 DONEPEZIL 4.0 1 -
CHEMBL95 TACRINE 4.0 1 -
CHEMBL1428 NIMODIPINE 4.0 1 -
CHEMBL5411893 1 -
CHEMBL5419680 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL378225 IC50 = 59.0 nM 7.23
CHEMBL5423316 IC50 = 1570.0 nM 5.80
CHEMBL4861574 IC50 = 4030.0 nM 5.39
CHEMBL4852705 IC50 = 4880.0 nM 5.31
CHEMBL5423337 IC50 = 5170.0 nM 5.29
CHEMBL4859850 IC50 = 5130.0 nM 5.29
CHEMBL5404846 IC50 = 5410.0 nM 5.27
CHEMBL5411905 IC50 = 5350.0 nM 5.27
CHEMBL4854550 IC50 = 6680.0 nM 5.17
CHEMBL5440565 IC50 = 9420.0 nM 5.03
CHEMBL4849009 IC50 = 17300.0 nM 4.76
CHEMBL4868987 IC50 = 19500.0 nM 4.71
CHEMBL5411369 IC50 = 22900.0 nM 4.64
CHEMBL4873878 IC50 = 29000.0 nM 4.54
CHEMBL502 DONEPEZIL IC50 - -
CHEMBL95 TACRINE IC50 - -
CHEMBL1428 NIMODIPINE IC50 - -
CHEMBL5411893 IC50 - -
CHEMBL5419680 IC50 - -