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Assay Detail

CHEMBL914529

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

Binding
Inhibition of human brain AchE
10
Total Activities
5
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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 5 10.06 10.70
Ki 5 10.79 10.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL225567 2 10.85
CHEMBL223443 2 10.82
CHEMBL225198 2 10.70
CHEMBL225326 2 10.70
CHEMBL225021 2 9.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL225567 Ki = 0.014 nM 10.85
CHEMBL223443 Ki = 0.015 nM 10.82
CHEMBL225198 IC50 = 0.02 nM 10.70
CHEMBL225326 Ki = 0.02 nM 10.70
CHEMBL225567 IC50 = 0.07 nM 10.15
CHEMBL223443 IC50 = 0.12 nM 9.92
CHEMBL225021 IC50 = 0.13 nM 9.89
CHEMBL225326 IC50 = 0.23 nM 9.64
CHEMBL225198 Ki = 0.009 nM -
CHEMBL225021 Ki = 0.0017 nM -