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Assay Detail

CHEMBL5338149

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

Binding
Inhibition of human erythrocyte AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition and measured every min for 10 mins by Ellman's method
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Acetylcholinesterase (CHEMBL220)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis and preliminary biological evaluation of rivastigmine-INDY hybrids as multitarget ligands against Alzheimer's disease by targeting butyrylcholinesterase and DYRK1A/CLK1 kinases.
Ţînţaş ML, Peauger L, Barré A, Papamicaël C, Besson T, Sopkovà-de Oliveira Santos J, Gembus V, Levacher V.
RSC Med Chem (2024) 15 : 963 -980
PubMed 38516603 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.48 8.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL502 DONEPEZIL 4.0 1 8.41
CHEMBL5414144 1 4.96
CHEMBL5407180 1 4.85
CHEMBL5407164 1 4.70
CHEMBL5434888 1 4.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL502 DONEPEZIL IC50 = 3.9 nM 8.41
CHEMBL5414144 IC50 = 11000.0 nM 4.96
CHEMBL5407180 IC50 = 14000.0 nM 4.85
CHEMBL5407164 IC50 = 20000.0 nM 4.70
CHEMBL5434888 IC50 = 34000.0 nM 4.47