Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL5635997

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

Binding
Inhibition of recombinant human AChE using acetylthiocholine as substrate preincubated for 20 mins followed by substrate addition measured for 3 mins by Ellman's method
7
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Acetylcholinesterase (CHEMBL220)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Galantamine-memantine hybrids for Alzheimer's disease: The influence of linker rigidity in biological activity and pharmacokinetic properties.
Basagni F, Ortega JA, Bertozzi SM, Armirotti A, Summa M, Bertorelli R, Bartolini M, Mellor IR, Bedeschi M, Bottegoni G, Lembo V, Minarini A, Cavalli A, Rosini M.
Eur J Med Chem (2023) 261 : 115803 -115803
PubMed 37734258 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.34 6.94
T1/2 3 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5646469 2 6.94
CHEMBL5641542 2 6.12
CHEMBL2178782 2 5.95
CHEMBL807 MEMANTINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5646469 IC50 = 115.0 nM 6.94
CHEMBL5641542 IC50 = 762.0 nM 6.12
CHEMBL2178782 IC50 = 1130.0 nM 5.95
CHEMBL807 MEMANTINE IC50 - -
CHEMBL2178782 T1/2 > 1.0 hr -
CHEMBL5646469 T1/2 > 1.0 hr -
CHEMBL5641542 t1/2 - -