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Assay Detail

CHEMBL2020733

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

Binding
Inhibition of human serum BChE by Ellman's method
19
Total Activities
19
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

Cholinesterase (CHEMBL1914)
Type SINGLE PROTEIN
Organism Homo sapiens

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 19 8.83 10.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2019034 1 10.42
CHEMBL2019032 1 10.10
CHEMBL2019035 1 10.00
CHEMBL2019037 1 10.00
CHEMBL2019038 1 10.00
CHEMBL2019030 1 9.82
CHEMBL2019047 1 9.10
CHEMBL2019046 1 9.00
CHEMBL2019043 1 8.82
CHEMBL2019044 1 8.82
CHEMBL2019049 1 8.60
CHEMBL2019048 1 8.30
CHEMBL2019040 1 7.82
CHEMBL2019052 1 7.52
CHEMBL95 TACRINE 4.0 1 7.40
CHEMBL2019041 1 7.30
CHEMBL2019053 1 7.02
CHEMBL45 MELATONIN 4.0 1 -
CHEMBL28 APIGENIN 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2019034 IC50 = 0.038 nM 10.42
CHEMBL2019032 IC50 = 0.08 nM 10.10
CHEMBL2019035 IC50 = 0.1 nM 10.00
CHEMBL2019037 IC50 = 0.1 nM 10.00
CHEMBL2019038 IC50 = 0.1 nM 10.00
CHEMBL2019030 IC50 = 0.15 nM 9.82
CHEMBL2019047 IC50 = 0.8 nM 9.10
CHEMBL2019046 IC50 = 1.0 nM 9.00
CHEMBL2019043 IC50 = 1.5 nM 8.82
CHEMBL2019044 IC50 = 1.5 nM 8.82
CHEMBL2019049 IC50 = 2.5 nM 8.60
CHEMBL2019048 IC50 = 5.0 nM 8.30
CHEMBL2019040 IC50 = 15.0 nM 7.82
CHEMBL2019052 IC50 = 30.0 nM 7.52
CHEMBL95 TACRINE IC50 = 40.0 nM 7.40
CHEMBL2019041 IC50 = 50.0 nM 7.30
CHEMBL2019053 IC50 = 95.0 nM 7.02
CHEMBL45 MELATONIN IC50 - -
CHEMBL28 APIGENIN IC50 - -