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Assay Detail

CHEMBL3095598

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 preincubated for 15 mins by Ellman's method
11
Total Activities
11
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

Novel tacrine-ebselen hybrids with improved cholinesterase inhibitory, hydrogen peroxide and peroxynitrite scavenging activity.
Mao F, Chen J, Zhou Q, Luo Z, Huang L, Li X.
Bioorg Med Chem Lett (2013) 23 : 6737 -6742
PubMed 24220172 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.52 9.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL32823 1 9.77
CHEMBL3093791 1 8.59
CHEMBL3093787 1 8.20
CHEMBL3093789 1 7.62
CHEMBL3093788 1 7.58
CHEMBL3093790 1 7.50
CHEMBL3093786 1 7.15
CHEMBL95 TACRINE 4.0 1 6.96
CHEMBL3093785 1 6.82
CHEMBL3093793 1 6.37
CHEMBL3093792 1 6.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL32823 IC50 = 0.17 nM 9.77
CHEMBL3093791 IC50 = 2.55 nM 8.59
CHEMBL3093787 IC50 = 6.32 nM 8.20
CHEMBL3093789 IC50 = 24.14 nM 7.62
CHEMBL3093788 IC50 = 26.49 nM 7.58
CHEMBL3093790 IC50 = 31.98 nM 7.50
CHEMBL3093786 IC50 = 70.77 nM 7.15
CHEMBL95 TACRINE IC50 = 109.0 nM 6.96
CHEMBL3093785 IC50 = 152.0 nM 6.82
CHEMBL3093793 IC50 = 423.0 nM 6.37
CHEMBL3093792 IC50 = 657.0 nM 6.18