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Assay Detail

CHEMBL2020730

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

Binding
Inhibition of bovine erythrocytes AChE by Ellman's method
30
Total Activities
30
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Acetylcholinesterase (CHEMBL4768)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

New tacrine-4-oxo-4H-chromene hybrids as multifunctional agents for the treatment of Alzheimer's disease, with cholinergic, antioxidant, and β-amyloid-reducing properties.
Fernández-Bachiller MI, Pérez C, Monjas L, Rademann J, Rodríguez-Franco MI.
J Med Chem (2012) 55 : 1303 -1317
PubMed 22243648 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 7.11 8.30
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2019035 1 8.30
CHEMBL2019032 1 8.30
CHEMBL2019041 1 8.19
CHEMBL2019049 1 8.00
CHEMBL2019053 1 7.76
CHEMBL2019034 1 7.46
CHEMBL2019048 1 7.42
CHEMBL95 TACRINE 4.0 1 7.40
CHEMBL2019038 1 7.30
CHEMBL2019030 1 7.12
CHEMBL2019043 1 7.12
CHEMBL2019051 1 7.12
CHEMBL2019044 1 7.10
CHEMBL2019050 1 7.10
CHEMBL2019040 1 7.07
CHEMBL2019054 1 7.05
CHEMBL2019037 1 7.00
CHEMBL2019027 1 7.00
CHEMBL2019029 1 6.90
CHEMBL2019039 1 6.82
CHEMBL2019031 1 6.82
CHEMBL2019028 1 6.82
CHEMBL2019042 1 6.76
CHEMBL2019046 1 6.60
CHEMBL2019052 1 6.52
CHEMBL2019045 1 6.46
CHEMBL2019047 1 6.30
CHEMBL2019036 1 6.26
CHEMBL2019033 1 6.00
CHEMBL83628 CHROMOCARB 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2019035 IC50 = 5.0 nM 8.30
CHEMBL2019032 IC50 = 5.0 nM 8.30
CHEMBL2019041 IC50 = 6.5 nM 8.19
CHEMBL2019049 IC50 = 10.0 nM 8.00
CHEMBL2019053 IC50 = 17.5 nM 7.76
CHEMBL2019034 IC50 = 35.0 nM 7.46
CHEMBL2019048 IC50 = 38.0 nM 7.42
CHEMBL95 TACRINE IC50 = 40.0 nM 7.40
CHEMBL2019038 IC50 = 50.0 nM 7.30
CHEMBL2019030 IC50 = 75.0 nM 7.12
CHEMBL2019043 IC50 = 75.0 nM 7.12
CHEMBL2019051 IC50 = 75.0 nM 7.12
CHEMBL2019044 IC50 = 80.0 nM 7.10
CHEMBL2019050 IC50 = 80.0 nM 7.10
CHEMBL2019040 IC50 = 85.0 nM 7.07
CHEMBL2019054 IC50 = 90.0 nM 7.05
CHEMBL2019037 IC50 = 100.0 nM 7.00
CHEMBL2019027 IC50 = 100.0 nM 7.00
CHEMBL2019029 IC50 = 125.0 nM 6.90
CHEMBL2019039 IC50 = 150.0 nM 6.82
CHEMBL2019031 IC50 = 150.0 nM 6.82
CHEMBL2019028 IC50 = 150.0 nM 6.82
CHEMBL2019042 IC50 = 175.0 nM 6.76
CHEMBL2019046 IC50 = 250.0 nM 6.60
CHEMBL2019052 IC50 = 300.0 nM 6.52
CHEMBL2019045 IC50 = 350.0 nM 6.46
CHEMBL2019047 IC50 = 500.0 nM 6.30
CHEMBL2019036 IC50 = 550.0 nM 6.26
CHEMBL2019033 IC50 = 1000.0 nM 6.00
CHEMBL83628 CHROMOCARB Inhibition - % -