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Assay Detail

CHEMBL4274267

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

Binding
Inhibition of human serum BuChE using butyrylthiocholine iodide as substrate incubated for 5 mins followed by substrate addition measured after 180 secs by Ellman's method
16
Total Activities
16
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

Cholinesterase (CHEMBL1914)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Donepezil-butylated hydroxytoluene (BHT) hybrids as Anti-Alzheimer's disease agents with cholinergic, antioxidant, and neuroprotective properties.
Cai P, Fang SQ, Yang HL, Yang XL, Liu QH, Kong LY, Wang XB.
Eur J Med Chem (2018) 157 : 161 -176
PubMed 30096650 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 5.17 5.91

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3819320 1 5.91
CHEMBL3819548 1 5.78
CHEMBL502 DONEPEZIL 4.0 1 5.50
CHEMBL4286736 1 5.02
CHEMBL4279488 1 4.71
CHEMBL4283390 1 4.07
CHEMBL4288282 1 -
CHEMBL4284895 1 -
CHEMBL4295126 1 -
CHEMBL4284475 1 -
CHEMBL4291697 1 -
CHEMBL4281066 1 -
CHEMBL4293155 1 -
CHEMBL4282558 1 -
CHEMBL4281727 1 -
CHEMBL4292349 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3819320 IC50 = 1220.0 nM 5.91
CHEMBL3819548 IC50 = 1670.0 nM 5.78
CHEMBL502 DONEPEZIL IC50 = 3170.0 nM 5.50
CHEMBL4286736 IC50 = 9610.0 nM 5.02
CHEMBL4279488 IC50 = 19560.0 nM 4.71
CHEMBL4283390 IC50 = 84810.0 nM 4.07
CHEMBL4288282 IC50 - -
CHEMBL4284895 IC50 - -
CHEMBL4295126 IC50 - -
CHEMBL4284475 IC50 - -
CHEMBL4291697 IC50 - -
CHEMBL4281066 IC50 - -
CHEMBL4293155 IC50 - -
CHEMBL4282558 IC50 - -
CHEMBL4281727 IC50 - -
CHEMBL4292349 IC50 - -