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Assay Detail

CHEMBL4307302

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

Binding
Inhibition of human recombinant AChE expressed in HEK293 cells using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition by spectrophotometry analysis
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Acetylcholinesterase (CHEMBL220)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A novel class of multitarget anti-Alzheimer benzohomoadamantane‒chlorotacrine hybrids modulating cholinesterases and glutamate NMDA receptors.
Pérez-Areales FJ, Turcu AL, Barniol-Xicota M, Pont C, Pivetta D, Espargaró A, Bartolini M, De Simone A, Andrisano V, Pérez B, Sabate R, Sureda FX, Vázquez S, Muñoz-Torrero D.
Eur J Med Chem (2019) 180 : 613 -626
PubMed 31351393 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 8.75 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4471659 1 9.52
CHEMBL4462369 1 8.89
CHEMBL4558495 1 8.85
CHEMBL4438626 1 8.85
CHEMBL4469343 1 8.70
CHEMBL4591167 1 8.60
CHEMBL292314 1 7.84
CHEMBL807 MEMANTINE 4.0 1 -
CHEMBL3259988 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4471659 IC50 = 0.3 nM 9.52
CHEMBL4462369 IC50 = 1.3 nM 8.89
CHEMBL4558495 IC50 = 1.4 nM 8.85
CHEMBL4438626 IC50 = 1.4 nM 8.85
CHEMBL4469343 IC50 = 2.0 nM 8.70
CHEMBL4591167 IC50 = 2.5 nM 8.60
CHEMBL292314 IC50 = 14.5 nM 7.84
CHEMBL807 MEMANTINE IC50 - -
CHEMBL3259988 IC50 - -