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Assay Detail

CHEMBL967995

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

Binding
Inhibition of human erythrocyte AChE by Ellman's method
10
Total Activities
10
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

New tacrine-dihydropyridine hybrids that inhibit acetylcholinesterase, calcium entry, and exhibit neuroprotection properties.
León R, de los Ríos C, Marco-Contelles J, Huertas O, Barril X, Luque FJ, López MG, García AG, Villarroya M.
Bioorg Med Chem (2008) 16 : 7759 -7769
PubMed 18640842 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.43 6.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL374184 1 6.96
CHEMBL218939 1 6.92
CHEMBL95 TACRINE 4.0 1 6.82
CHEMBL219406 1 6.77
CHEMBL219172 1 6.72
CHEMBL468001 1 6.43
CHEMBL513161 1 6.17
CHEMBL512096 1 6.15
CHEMBL468000 1 5.80
CHEMBL468002 1 5.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL374184 IC50 = 110.0 nM 6.96
CHEMBL218939 IC50 = 120.0 nM 6.92
CHEMBL95 TACRINE IC50 = 150.0 nM 6.82
CHEMBL219406 IC50 = 170.0 nM 6.77
CHEMBL219172 IC50 = 190.0 nM 6.72
CHEMBL468001 IC50 = 370.0 nM 6.43
CHEMBL513161 IC50 = 670.0 nM 6.17
CHEMBL512096 IC50 = 710.0 nM 6.15
CHEMBL468000 IC50 = 1600.0 nM 5.80
CHEMBL468002 IC50 = 2800.0 nM 5.55