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Assay Detail

CHEMBL914532

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

Functional
Inhibition of human AChE-induced beta amyloid peptide(1-40) aggregation by thioflavin T-based fluorometric assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Acetylcholinesterase (CHEMBL220)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and biological evaluation of dual binding site acetylcholinesterase inhibitors: new disease-modifying agents for Alzheimer's disease.
Muñoz-Ruiz P, Rubio L, García-Palomero E, Dorronsoro I, del Monte-Millán M, Valenzuela R, Usán P, de Austria C, Bartolini M, Andrisano V, Bidon-Chanal A, Orozco M, Luque FJ, Medina M, Martínez A.
J Med Chem (2005) 48 : 7223 -7233
PubMed 16279781 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.25 5.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL225567 1 5.70
CHEMBL225021 1 5.70
CHEMBL225198 1 5.22
CHEMBL223443 1 5.16
CHEMBL345124 PROPIDIUM 1 4.89
CHEMBL225326 1 4.82
CHEMBL95 TACRINE 4.0 1 -
CHEMBL1190 DECAMETHONIUM 4.0 1 -
CHEMBL502 DONEPEZIL 4.0 1 -
CHEMBL60745 EDROPHONIUM BROMIDE 1 -
CHEMBL94 PHYSOSTIGMINE 3.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL225567 IC50 = 2000.0 nM 5.70
CHEMBL225021 IC50 = 2000.0 nM 5.70
CHEMBL225198 IC50 = 6000.0 nM 5.22
CHEMBL223443 IC50 = 7000.0 nM 5.16
CHEMBL345124 PROPIDIUM IC50 = 13000.0 nM 4.89
CHEMBL225326 IC50 = 15000.0 nM 4.82
CHEMBL95 TACRINE IC50 - -
CHEMBL1190 DECAMETHONIUM IC50 - -
CHEMBL502 DONEPEZIL IC50 - -
CHEMBL60745 EDROPHONIUM BROMIDE IC50 - -
CHEMBL94 PHYSOSTIGMINE IC50 - -