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Assay Detail

CHEMBL4376479

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

Binding
Inhibition of recombinant human AChE using acetylthiocholine iodide as substrate preincubated with enzyme for 5 mins prior to substrate addition measured after 5 mins by Ellman's method
4
Total Activities
4
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

Acetylcholinesterase (CHEMBL220)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Search for new multi-target compounds against Alzheimer's disease among histamine H3 receptor ligands.
Bajda M, Łażewska D, Godyń J, Zaręba P, Kuder K, Hagenow S, Łątka K, Stawarska E, Stark H, Kieć-Kononowicz K, Malawska B.
Eur J Med Chem (2020) 185 : 111785 -111785
PubMed 31669851 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.97 8.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL502 DONEPEZIL 4.0 1 8.25
CHEMBL95 TACRINE 4.0 1 6.88
CHEMBL4474399 1 6.44
CHEMBL4455690 1 6.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL502 DONEPEZIL IC50 = 5.59 nM 8.25
CHEMBL95 TACRINE IC50 = 131.0 nM 6.88
CHEMBL4474399 IC50 = 360.0 nM 6.44
CHEMBL4455690 IC50 = 480.0 nM 6.32