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Assay Detail

CHEMBL4048100

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

ADMET
Inhibition of equine serum BuChE incubated for 15 mins by Ellman's method
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Equus caballus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cholinesterase (CHEMBL5763)
Type SINGLE PROTEIN
Organism Equus caballus

Publication

Design, synthesis and biological evaluation of 2-acetyl-5-O-(amino-alkyl)phenol derivatives as multifunctional agents for the treatment of Alzheimer's disease.
Sang Z, Wang K, Wang H, Wang H, Ma Q, Han X, Ye M, Yu L, Liu W.
Bioorg Med Chem Lett (2017) 27 : 5046 -5052
PubMed 29033233 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 4.48 5.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL502 DONEPEZIL 4.0 1 5.32
CHEMBL4093622 1 4.50
CHEMBL4069471 1 4.43
CHEMBL4090497 1 4.34
CHEMBL4099142 1 4.34
CHEMBL4072178 1 4.33
CHEMBL4065727 1 4.12
CHEMBL4082669 1 -
CHEMBL8706 CLORGILINE 2.0 1 -
CHEMBL887 RASAGILINE 4.0 1 -
CHEMBL92401 IPRONIAZID 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL502 DONEPEZIL IC50 = 4760.0 nM 5.32
CHEMBL4093622 IC50 = 31400.0 nM 4.50
CHEMBL4069471 IC50 = 37200.0 nM 4.43
CHEMBL4090497 IC50 = 46100.0 nM 4.34
CHEMBL4099142 IC50 = 45700.0 nM 4.34
CHEMBL4072178 IC50 = 46500.0 nM 4.33
CHEMBL4065727 IC50 = 75400.0 nM 4.12
CHEMBL4082669 IC50 = 137000.0 nM -
CHEMBL8706 CLORGILINE IC50 - -
CHEMBL887 RASAGILINE IC50 - -
CHEMBL92401 IPRONIAZID IC50 - -