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Assay Detail

CHEMBL4013232

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

Binding
Inhibition of AChE in human erythrocytes using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured every minute for 10 mins by Ellman's spectrophotometric method
26
Total Activities
26
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

Donepezil-Based Central Acetylcholinesterase Inhibitors by Means of a "Bio-Oxidizable" Prodrug Strategy: Design, Synthesis, and in Vitro Biological Evaluation.
Peauger L, Azzouz R, Gembus V, Ţînţaş ML, Sopková-de Oliveira Santos J, Bohn P, Papamicaël C, Levacher V.
J Med Chem (2017) 60 : 5909 -5926
PubMed 28613859 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 7.43 8.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4071377 1 8.54
CHEMBL4102333 1 8.48
CHEMBL4095535 1 8.24
CHEMBL4081915 1 8.06
CHEMBL4094081 1 7.85
CHEMBL4060011 1 7.75
CHEMBL4066548 1 7.75
CHEMBL4068149 1 7.59
CHEMBL4074062 1 7.56
CHEMBL4094591 1 7.52
CHEMBL4098418 1 7.44
CHEMBL4092048 1 7.39
CHEMBL4084371 1 7.22
CHEMBL4072999 1 7.04
CHEMBL4099873 1 6.58
CHEMBL4061527 1 6.37
CHEMBL4105085 1 6.18
CHEMBL4076930 1 6.17
CHEMBL4064413 1 -
CHEMBL4092123 1 -
CHEMBL4101303 1 -
CHEMBL4072865 1 -
CHEMBL4093567 1 -
CHEMBL4083445 1 -
CHEMBL4099794 1 -
CHEMBL4081776 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4071377 IC50 = 2.92 nM 8.54
CHEMBL4102333 IC50 = 3.27 nM 8.48
CHEMBL4095535 IC50 = 5.8 nM 8.24
CHEMBL4081915 IC50 = 8.8 nM 8.06
CHEMBL4094081 IC50 = 14.0 nM 7.85
CHEMBL4060011 IC50 = 18.0 nM 7.75
CHEMBL4066548 IC50 = 18.0 nM 7.75
CHEMBL4068149 IC50 = 25.6 nM 7.59
CHEMBL4074062 IC50 = 27.7 nM 7.56
CHEMBL4094591 IC50 = 30.0 nM 7.52
CHEMBL4098418 IC50 = 36.5 nM 7.44
CHEMBL4092048 IC50 = 41.0 nM 7.39
CHEMBL4084371 IC50 = 60.0 nM 7.22
CHEMBL4072999 IC50 = 91.0 nM 7.04
CHEMBL4099873 IC50 = 262.0 nM 6.58
CHEMBL4061527 IC50 = 428.0 nM 6.37
CHEMBL4105085 IC50 = 653.0 nM 6.18
CHEMBL4076930 IC50 = 678.0 nM 6.17
CHEMBL4064413 IC50 > 1000.0 nM -
CHEMBL4092123 IC50 > 1000.0 nM -
CHEMBL4101303 IC50 > 1000.0 nM -
CHEMBL4072865 IC50 > 1000.0 nM -
CHEMBL4093567 IC50 > 1000.0 nM -
CHEMBL4083445 IC50 > 1000.0 nM -
CHEMBL4099794 IC50 > 1000.0 nM -
CHEMBL4081776 IC50 > 1000.0 nM -