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Assay Detail

CHEMBL3379807

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

Binding
Inhibition of beta-secretase (unknown origin) using 150 nM Rhodamine-EVNLDAEFK-quencher substrate proteolysis by fluorescence resonance energy transfer assay
7
Total Activities
7
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

Syntheses of coumarin-tacrine hybrids as dual-site acetylcholinesterase inhibitors and their activity against butylcholinesterase, Aβ aggregation, and β-secretase.
Sun Q, Peng DY, Yang SG, Zhu XL, Yang WC, Yang GF.
Bioorg Med Chem (2014) 22 : 4784 -4791
PubMed 25088549 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 4.69 5.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL140 CURCUMIN 3.0 1 5.28
CHEMBL3326704 1 4.76
CHEMBL3327246 1 4.70
CHEMBL3326709 1 4.65
CHEMBL3326698 1 4.40
CHEMBL3327247 1 4.37
CHEMBL3326707 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL140 CURCUMIN IC50 = 5300.0 nM 5.28
CHEMBL3326704 IC50 = 17200.0 nM 4.76
CHEMBL3327246 IC50 = 20200.0 nM 4.70
CHEMBL3326709 IC50 = 22600.0 nM 4.65
CHEMBL3326698 IC50 = 40100.0 nM 4.40
CHEMBL3327247 IC50 = 42800.0 nM 4.37
CHEMBL3326707 IC50 > 100000.0 nM -