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Assay Detail

CHEMBL636836

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

Binding
In vitro inhibition of acetylcholinesterase, isolated from rat brain.
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Acetylcholinesterase (CHEMBL3199)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Novel tacrine analogues for potential use against Alzheimer's disease: potent and selective acetylcholinesterase inhibitors and 5-HT uptake inhibitors.
McKenna MT, Proctor GR, Young LC, Harvey AL.
J Med Chem (1997) 40 : 3516 -3523
PubMed 9357518 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 5.39 7.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL330883 1 7.41
CHEMBL118752 1 7.25
CHEMBL95 TACRINE 4.0 1 7.11
CHEMBL431844 1 6.62
CHEMBL60167 1 6.46
CHEMBL119390 1 5.46
CHEMBL118968 1 5.04
CHEMBL119389 1 4.60
CHEMBL89012 1 4.43
CHEMBL118139 1 4.42
CHEMBL118033 1 4.32
CHEMBL115697 1 4.16
CHEMBL119634 1 4.16
CHEMBL119528 1 4.04
CHEMBL325203 1 -
CHEMBL331637 1 -
CHEMBL333011 1 -
CHEMBL332454 1 -
CHEMBL115580 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL330883 IC50 = 39.0 nM 7.41
CHEMBL118752 IC50 = 56.0 nM 7.25
CHEMBL95 TACRINE IC50 = 78.0 nM 7.11
CHEMBL431844 IC50 = 240.0 nM 6.62
CHEMBL60167 IC50 = 350.0 nM 6.46
CHEMBL119390 IC50 = 3500.0 nM 5.46
CHEMBL118968 IC50 = 9100.0 nM 5.04
CHEMBL119389 IC50 = 25000.0 nM 4.60
CHEMBL89012 IC50 = 37400.0 nM 4.43
CHEMBL118139 IC50 = 38200.0 nM 4.42
CHEMBL118033 IC50 = 47500.0 nM 4.32
CHEMBL115697 IC50 = 69400.0 nM 4.16
CHEMBL119634 IC50 = 68800.0 nM 4.16
CHEMBL119528 IC50 = 91000.0 nM 4.04
CHEMBL325203 IC50 = 391100.0 nM -
CHEMBL331637 IC50 = 110000.0 nM -
CHEMBL333011 IC50 = 144100.0 nM -
CHEMBL332454 IC50 = 166100.0 nM -
CHEMBL115580 IC50 = 134000.0 nM -