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Assay Detail

CHEMBL1820356

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

Binding
Inhibition of human serum recombinant AChE using acetylthiocholine iodide as substrate preincubated for 20 mins by Ellman's method
14
Total Activities
14
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

Multi-target strategy to address Alzheimer's disease: design, synthesis and biological evaluation of new tacrine-based dimers.
Rizzo S, Bisi A, Bartolini M, Mancini F, Belluti F, Gobbi S, Andrisano V, Rampa A.
Eur J Med Chem (2011) 46 : 4336 -4343
PubMed 21798635 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 7.41 9.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL32823 1 9.09
CHEMBL1819176 1 8.98
CHEMBL1819177 1 7.92
CHEMBL1819175 1 7.86
CHEMBL1819171 1 7.78
CHEMBL1819173 1 7.55
CHEMBL1819172 1 7.47
CHEMBL1819170 1 7.35
CHEMBL1819169 1 7.16
CHEMBL95 TACRINE 4.0 1 6.60
CHEMBL1819179 1 6.59
CHEMBL1819174 1 6.55
CHEMBL1819178 1 6.51
CHEMBL1819180 1 6.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL32823 IC50 = 0.81 nM 9.09
CHEMBL1819176 IC50 = 1.05 nM 8.98
CHEMBL1819177 IC50 = 12.1 nM 7.92
CHEMBL1819175 IC50 = 13.9 nM 7.86
CHEMBL1819171 IC50 = 16.5 nM 7.78
CHEMBL1819173 IC50 = 28.4 nM 7.55
CHEMBL1819172 IC50 = 34.0 nM 7.47
CHEMBL1819170 IC50 = 44.5 nM 7.35
CHEMBL1819169 IC50 = 68.9 nM 7.16
CHEMBL95 TACRINE IC50 = 250.0 nM 6.60
CHEMBL1819179 IC50 = 258.0 nM 6.59
CHEMBL1819174 IC50 = 283.0 nM 6.55
CHEMBL1819178 IC50 = 310.0 nM 6.51
CHEMBL1819180 IC50 = 455.0 nM 6.34