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Assay Detail

CHEMBL3868644

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

Binding
Inhibition of Electrophorus electricus AChE using acetylthiocholine iodide as substrate incubated for 15 mins followed by substrate addition by Ellman's method
9
Total Activities
9
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

Avarol derivatives as competitive AChE inhibitors, non hepatotoxic and neuroprotective agents for Alzheimer's disease.
Tommonaro G, García-Font N, Vitale RM, Pejin B, Iodice C, Cañadas S, Marco-Contelles J, Oset-Gasque MJ.
Eur J Med Chem (2016) 122 : 326 -338
PubMed 27376495 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.37 7.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL95 TACRINE 4.0 1 7.21
CHEMBL659 GALANTAMINE 4.0 1 6.21
CHEMBL3958859 1 5.17
CHEMBL3920392 1 5.10
CHEMBL3907011 1 4.88
CHEMBL3922437 1 4.86
CHEMBL238756 1 4.82
CHEMBL3945723 1 4.74
CHEMBL459814 AVAROL 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL95 TACRINE IC50 = 61.0 nM 7.21
CHEMBL659 GALANTAMINE IC50 = 610.0 nM 6.21
CHEMBL3958859 IC50 = 6770.0 nM 5.17
CHEMBL3920392 IC50 = 7880.0 nM 5.10
CHEMBL3907011 IC50 = 13090.0 nM 4.88
CHEMBL3922437 IC50 = 13790.0 nM 4.86
CHEMBL238756 IC50 = 15110.0 nM 4.82
CHEMBL3945723 IC50 = 18100.0 nM 4.74
CHEMBL459814 AVAROL IC50 = 285630.0 nM -