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Assay Detail

CHEMBL5353744

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

Binding
Inhibition of human BChE using butyrylthiocholine iodide as substrate measured for 3 mins by Ellman's method
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cholinesterase (CHEMBL1914)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and biological evaluation of aromatic tertiary amine derivatives as selective butyrylcholinesterase inhibitors for the treatment of Alzheimer's disease.
Lu X, Qin N, Liu Y, Du C, Feng F, Liu W, Chen Y, Sun H.
Eur J Med Chem (2022) 243 : 114729 -114729
PubMed 36084535 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.54 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL95 TACRINE 4.0 1 8.52
CHEMBL5416136 1 7.96
CHEMBL5403451 1 7.80
CHEMBL5405011 1 7.62
CHEMBL5414031 1 7.57
CHEMBL5435700 1 7.52
CHEMBL5425810 1 6.75
CHEMBL5436125 1 6.54
CHEMBL5421870 1 -
CHEMBL5414945 1 -
CHEMBL5439234 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL95 TACRINE IC50 = 3.0 nM 8.52
CHEMBL5416136 IC50 = 11.0 nM 7.96
CHEMBL5403451 IC50 = 16.0 nM 7.80
CHEMBL5405011 IC50 = 24.0 nM 7.62
CHEMBL5414031 IC50 = 27.0 nM 7.57
CHEMBL5435700 IC50 = 30.0 nM 7.52
CHEMBL5425810 IC50 = 180.0 nM 6.75
CHEMBL5436125 IC50 = 290.0 nM 6.54
CHEMBL5421870 IC50 - -
CHEMBL5414945 IC50 - -
CHEMBL5439234 IC50 - -