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Assay Detail

CHEMBL960589

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

Binding
Inhibition of human erythrocyte AChE by Ellman's assay
12
Total Activities
12
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

Novel donepezil-based inhibitors of acetyl- and butyrylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation.
Camps P, Formosa X, Galdeano C, Gómez T, Muñoz-Torrero D, Scarpellini M, Viayna E, Badia A, Clos MV, Camins A, Pallàs M, Bartolini M, Mancini F, Andrisano V, Estelrich J, Lizondo M, Bidon-Chanal A, Luque FJ.
J Med Chem (2008) 51 : 3588 -3598
PubMed 18517184 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 8.49 9.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3216655 1 9.57
CHEMBL3216422 1 9.17
CHEMBL3216886 1 9.06
CHEMBL3217103 1 8.97
CHEMBL3216209 1 8.67
CHEMBL3216210 1 8.59
CHEMBL2448138 9-[(2-{4-[(5,6-Dimethoxy-1-oxoindan-2-yl)methyl]piperidin-1-yl}ethyl)amino]-1,2,3,4-tetrahydroacridine dihydrochloride 1 8.39
CHEMBL3216208 1 8.29
CHEMBL486698 1 8.08
CHEMBL1678 DONEPEZIL HYDROCHLORIDE 4.0 1 7.94
CHEMBL1677 TACRINE HYDROCHLORIDE 4.0 1 6.69
CHEMBL486699 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3216655 IC50 = 0.27 nM 9.57
CHEMBL3216422 IC50 = 0.67 nM 9.17
CHEMBL3216886 IC50 = 0.88 nM 9.06
CHEMBL3217103 IC50 = 1.06 nM 8.97
CHEMBL3216209 IC50 = 2.16 nM 8.67
CHEMBL3216210 IC50 = 2.6 nM 8.59
CHEMBL2448138 9-[(2-{4-[(5,6-Dimethoxy-1-oxoindan-2-yl)methyl]piperidin-1-yl}ethyl)amino]-1,2,3,4-tetrahydroacridine dihydrochloride IC50 = 4.04 nM 8.39
CHEMBL3216208 IC50 = 5.13 nM 8.29
CHEMBL486698 IC50 = 8.32 nM 8.08
CHEMBL1678 DONEPEZIL HYDROCHLORIDE IC50 = 11.6 nM 7.94
CHEMBL1677 TACRINE HYDROCHLORIDE IC50 = 205.0 nM 6.69
CHEMBL486699 IC50 - -