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Assay Detail

CHEMBL3784772

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 by Ellman's method
7
Total Activities
7
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

In silico to in vitro screening of hydroxypyridinones as acetylcholinesterase inhibitors.
Telpoukhovskaia MA, Patrick BO, Rodríguez-Rodríguez C, Orvig C.
Bioorg Med Chem Lett (2016) 26 : 1624 -1628
PubMed 26869193 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.98 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL95 TACRINE 4.0 1 8.70
CHEMBL636 RIVASTIGMINE 4.0 1 5.26
CHEMBL2288699 P-TOLYL DIMETHYLCARBAMATE 1 -
CHEMBL3781763 1 -
CHEMBL3781438 1 -
CHEMBL3780941 1 -
CHEMBL326815 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL95 TACRINE IC50 = 2.0 nM 8.70
CHEMBL636 RIVASTIGMINE IC50 = 5500.0 nM 5.26
CHEMBL2288699 P-TOLYL DIMETHYLCARBAMATE IC50 = 1282000.0 nM -
CHEMBL3781763 IC50 = 216500.0 nM -
CHEMBL3781438 IC50 = 252300.0 nM -
CHEMBL3780941 IC50 = 347600.0 nM -
CHEMBL326815 IC50 = 219900.0 nM -