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Assay Detail

CHEMBL2188841

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

Binding
Inhibition of AChE in Wistar rat brain homogenates using acetylthiocholine iodide and DTNB as substrate after 10 mins by Ellman method
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Acetylcholinesterase (CHEMBL3199)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Combining galantamine and memantine in multitargeted, new chemical entities potentially useful in Alzheimer's disease.
Simoni E, Daniele S, Bottegoni G, Pizzirani D, Trincavelli ML, Goldoni L, Tarozzo G, Reggiani A, Martini C, Piomelli D, Melchiorre C, Rosini M, Cavalli A.
J Med Chem (2012) 55 : 9708 -9721
PubMed 23033965 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 7.63 9.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2178790 1 9.28
CHEMBL2178788 1 8.99
CHEMBL2178784 MEMAGAL 1 8.94
CHEMBL2178789 1 8.88
CHEMBL2178785 1 8.75
CHEMBL2178787 1 8.63
CHEMBL2178783 1 8.37
CHEMBL2178786 1 8.27
CHEMBL2178781 1 7.95
CHEMBL2178779 1 7.25
CHEMBL2178791 1 7.09
CHEMBL2178777 1 6.88
CHEMBL2178778 1 6.78
CHEMBL2178780 1 6.43
CHEMBL2178782 1 6.16
CHEMBL659 GALANTAMINE 4.0 1 5.59
CHEMBL2178776 1 5.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2178790 IC50 = 0.52 nM 9.28
CHEMBL2178788 IC50 = 1.03 nM 8.99
CHEMBL2178784 MEMAGAL IC50 = 1.16 nM 8.94
CHEMBL2178789 IC50 = 1.33 nM 8.88
CHEMBL2178785 IC50 = 1.79 nM 8.75
CHEMBL2178787 IC50 = 2.32 nM 8.63
CHEMBL2178783 IC50 = 4.31 nM 8.37
CHEMBL2178786 IC50 = 5.36 nM 8.27
CHEMBL2178781 IC50 = 11.3 nM 7.95
CHEMBL2178779 IC50 = 55.7 nM 7.25
CHEMBL2178791 IC50 = 80.9 nM 7.09
CHEMBL2178777 IC50 = 131.1 nM 6.88
CHEMBL2178778 IC50 = 167.8 nM 6.78
CHEMBL2178780 IC50 = 369.0 nM 6.43
CHEMBL2178782 IC50 = 695.9 nM 6.16
CHEMBL659 GALANTAMINE IC50 = 2550.0 nM 5.59
CHEMBL2178776 IC50 = 3920.0 nM 5.41