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Assay Detail

CHEMBL3363249

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

Binding
Inhibition of human recombinant AChE using acetylthiocholine iodide as substrate by spectrophotometric analysis
8
Total Activities
8
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

Tetrahydrobenzo[h][1,6]naphthyridine-6-chlorotacrine hybrids as a new family of anti-Alzheimer agents targeting β-amyloid, tau, and cholinesterase pathologies.
Di Pietro O, Pérez-Areales FJ, Juárez-Jiménez J, Espargaró A, Clos MV, Pérez B, Lavilla R, Sabaté R, Luque FJ, Muñoz-Torrero D.
Eur J Med Chem (2014) 84 : 107 -117
PubMed 25016233 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.92 8.69

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3322231 1 8.69
CHEMBL292314 1 8.23
CHEMBL3322234 1 7.85
CHEMBL3322233 1 7.85
CHEMBL1196204 1 7.71
CHEMBL3122167 1 7.19
CHEMBL1194313 1 -
CHEMBL3322232 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3322231 IC50 = 2.06 nM 8.69
CHEMBL292314 IC50 = 5.9 nM 8.23
CHEMBL3322234 IC50 = 14.2 nM 7.85
CHEMBL3322233 IC50 = 14.2 nM 7.85
CHEMBL1196204 IC50 = 19.3 nM 7.71
CHEMBL3122167 IC50 = 65.0 nM 7.19
CHEMBL1194313 IC50 - -
CHEMBL3322232 IC50 = 0.006 nM -