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Assay Detail

CHEMBL2346192

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

Binding
Inhibition of electric eel AChE using acetylthiocholine chloride as substrate after 15 mins by Ellman's method
16
Total Activities
16
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

A novel series of tacrine-selegiline hybrids with cholinesterase and monoamine oxidase inhibition activities for the treatment of Alzheimer's disease.
Lu C, Zhou Q, Yan J, Du Z, Huang L, Li X.
Eur J Med Chem (2013) 62 : 745 -753
PubMed 23454517 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 7.18 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2333927 1 7.85
CHEMBL2333925 1 7.65
CHEMBL2333926 1 7.63
CHEMBL2333933 1 7.44
CHEMBL2333934 1 7.28
CHEMBL2333930 1 7.26
CHEMBL2333935 1 7.11
CHEMBL2333929 1 7.10
CHEMBL2333928 1 7.09
CHEMBL2333932 1 7.08
CHEMBL95 TACRINE 4.0 1 6.96
CHEMBL2333936 1 6.86
CHEMBL2333937 1 6.83
CHEMBL2333931 1 6.34
CHEMBL673 PARGYLINE 4.0 1 -
CHEMBL8706 CLORGILINE 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2333927 IC50 = 14.2 nM 7.85
CHEMBL2333925 IC50 = 22.6 nM 7.65
CHEMBL2333926 IC50 = 23.2 nM 7.63
CHEMBL2333933 IC50 = 36.1 nM 7.44
CHEMBL2333934 IC50 = 53.0 nM 7.28
CHEMBL2333930 IC50 = 55.4 nM 7.26
CHEMBL2333935 IC50 = 77.6 nM 7.11
CHEMBL2333929 IC50 = 79.3 nM 7.10
CHEMBL2333928 IC50 = 82.0 nM 7.09
CHEMBL2333932 IC50 = 83.1 nM 7.08
CHEMBL95 TACRINE IC50 = 110.2 nM 6.96
CHEMBL2333936 IC50 = 138.0 nM 6.86
CHEMBL2333937 IC50 = 147.0 nM 6.83
CHEMBL2333931 IC50 = 456.0 nM 6.34
CHEMBL673 PARGYLINE IC50 - -
CHEMBL8706 CLORGILINE IC50 - -