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Assay Detail

CHEMBL913361

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Binding
Inhibition of Electrophorus electricus AChE
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Electrophorus electricus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Acetylcholinesterase (CHEMBL4078)
Type SINGLE PROTEIN
Organism Electrophorus electricus

Publication

Novel multipotent tacrine-dihydropyridine hybrids with improved acetylcholinesterase inhibitory and neuroprotective activities as potential drugs for the treatment of Alzheimer's disease.
Marco-Contelles J, León R, de Los Ríos C, Guglietta A, Terencio J, López MG, García AG, Villarroya M.
J Med Chem (2006) 49 : 7607 -7610
PubMed 17181144 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.92 7.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL374184 1 7.35
CHEMBL219172 1 7.28
CHEMBL218940 1 7.21
CHEMBL218939 1 7.10
CHEMBL219406 1 7.04
CHEMBL220294 1 6.96
CHEMBL436302 1 6.80
CHEMBL95 TACRINE 4.0 1 6.75
CHEMBL219400 1 6.52
CHEMBL219405 1 6.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL374184 IC50 = 45.0 nM 7.35
CHEMBL219172 IC50 = 52.0 nM 7.28
CHEMBL218940 IC50 = 61.0 nM 7.21
CHEMBL218939 IC50 = 80.0 nM 7.10
CHEMBL219406 IC50 = 91.0 nM 7.04
CHEMBL220294 IC50 = 110.0 nM 6.96
CHEMBL436302 IC50 = 160.0 nM 6.80
CHEMBL95 TACRINE IC50 = 180.0 nM 6.75
CHEMBL219400 IC50 = 304.0 nM 6.52
CHEMBL219405 IC50 = 600.0 nM 6.22