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Assay Detail

CHEMBL4048097

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

Binding
Inhibition of electric eel AChE using acetylthiocholine as substrate incubated for 15 mins by Ellman's method
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Electrophorus electricus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Acetylcholinesterase (CHEMBL4078)
Type SINGLE PROTEIN
Organism Electrophorus electricus

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 24 5.04 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL502 DONEPEZIL 4.0 1 7.72
CHEMBL4093622 1 6.02
CHEMBL4088328 1 5.66
CHEMBL4099142 1 5.54
CHEMBL4072178 1 5.41
CHEMBL4098208 1 5.26
CHEMBL4069471 1 5.20
CHEMBL4090497 1 5.07
CHEMBL4084930 1 5.06
CHEMBL4092686 1 4.82
CHEMBL4063278 1 4.78
CHEMBL4065727 1 4.78
CHEMBL4067057 1 4.74
CHEMBL4067550 1 4.66
CHEMBL4087146 1 4.59
CHEMBL4071909 1 4.58
CHEMBL4080179 1 4.56
CHEMBL4101356 1 4.54
CHEMBL4066052 1 4.38
CHEMBL4082669 1 4.29
CHEMBL4077921 1 4.24
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 = 19.0 nM 7.72
CHEMBL4093622 IC50 = 960.0 nM 6.02
CHEMBL4088328 IC50 = 2200.0 nM 5.66
CHEMBL4099142 IC50 = 2900.0 nM 5.54
CHEMBL4072178 IC50 = 3900.0 nM 5.41
CHEMBL4098208 IC50 = 5500.0 nM 5.26
CHEMBL4069471 IC50 = 6300.0 nM 5.20
CHEMBL4090497 IC50 = 8500.0 nM 5.07
CHEMBL4084930 IC50 = 8800.0 nM 5.06
CHEMBL4092686 IC50 = 15200.0 nM 4.82
CHEMBL4063278 IC50 = 16700.0 nM 4.78
CHEMBL4065727 IC50 = 16800.0 nM 4.78
CHEMBL4067057 IC50 = 18400.0 nM 4.74
CHEMBL4067550 IC50 = 21900.0 nM 4.66
CHEMBL4087146 IC50 = 25800.0 nM 4.59
CHEMBL4071909 IC50 = 26300.0 nM 4.58
CHEMBL4080179 IC50 = 27500.0 nM 4.56
CHEMBL4101356 IC50 = 29200.0 nM 4.54
CHEMBL4066052 IC50 = 41300.0 nM 4.38
CHEMBL4082669 IC50 = 51800.0 nM 4.29
CHEMBL4077921 IC50 = 57000.0 nM 4.24
CHEMBL8706 CLORGILINE IC50 - -
CHEMBL887 RASAGILINE IC50 - -
CHEMBL92401 IPRONIAZID IC50 - -