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Assay Detail

CHEMBL3390449

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

Binding
Inhibition of electric eel AChE using acetylthiocholine iodide as substrate incubated for 6 mins by spectrophotometric method
20
Total Activities
20
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 evaluation of novel tacrine-(β-carboline) hybrids as multifunctional agents for the treatment of Alzheimer's disease.
Lan JS, Xie SS, Li SY, Pan LF, Wang XB, Kong LY.
Bioorg Med Chem (2014) 22 : 6089 -6104
PubMed 25282654 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 6.71 7.67

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3343927 1 7.67
CHEMBL3343922 1 7.49
CHEMBL3343885 1 7.39
CHEMBL3343931 1 7.29
CHEMBL3343882 1 7.29
CHEMBL3343930 1 7.17
CHEMBL3343925 1 7.01
CHEMBL3343920 1 6.97
CHEMBL3343932 1 6.94
CHEMBL3343923 1 6.90
CHEMBL3343926 1 6.85
CHEMBL3343929 1 6.81
CHEMBL3343924 1 6.64
CHEMBL95 TACRINE 4.0 1 6.58
CHEMBL3343884 1 6.57
CHEMBL3343928 1 6.41
CHEMBL3343883 1 6.31
CHEMBL3343921 1 6.11
CHEMBL659 GALANTAMINE 4.0 1 5.57
CHEMBL453066 BETA-CCM 1 4.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3343927 IC50 = 21.6 nM 7.67
CHEMBL3343922 IC50 = 32.4 nM 7.49
CHEMBL3343885 IC50 = 40.6 nM 7.39
CHEMBL3343931 IC50 = 51.6 nM 7.29
CHEMBL3343882 IC50 = 51.7 nM 7.29
CHEMBL3343930 IC50 = 67.3 nM 7.17
CHEMBL3343925 IC50 = 97.7 nM 7.01
CHEMBL3343920 IC50 = 107.0 nM 6.97
CHEMBL3343932 IC50 = 115.0 nM 6.94
CHEMBL3343923 IC50 = 127.0 nM 6.90
CHEMBL3343926 IC50 = 141.0 nM 6.85
CHEMBL3343929 IC50 = 156.0 nM 6.81
CHEMBL3343924 IC50 = 230.0 nM 6.64
CHEMBL95 TACRINE IC50 = 260.0 nM 6.58
CHEMBL3343884 IC50 = 268.0 nM 6.57
CHEMBL3343928 IC50 = 389.0 nM 6.41
CHEMBL3343883 IC50 = 485.0 nM 6.31
CHEMBL3343921 IC50 = 783.0 nM 6.11
CHEMBL659 GALANTAMINE IC50 = 2670.0 nM 5.57
CHEMBL453066 BETA-CCM IC50 = 63000.0 nM 4.20