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Assay Detail

CHEMBL2188840

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

Binding
Displacement of [3H]MK-801 from NMDAR in Sprague-Dawley rat cerebral cortex homogenates after 2 hrs by liquid scintillation counting
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Cerebral cortex
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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
Ki 18 5.42 5.94

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL807 MEMANTINE 4.0 1 5.94
CHEMBL2178782 1 5.63
CHEMBL305187 IFENPRODIL 2.0 1 5.51
CHEMBL2178784 MEMAGAL 1 5.34
CHEMBL2178787 1 5.33
CHEMBL2178786 1 5.30
CHEMBL2178778 1 5.27
CHEMBL2178785 1 5.00
CHEMBL2178780 1 -
CHEMBL2178779 1 -
CHEMBL2178777 1 -
CHEMBL2178776 1 -
CHEMBL2178791 1 -
CHEMBL2178790 1 -
CHEMBL2178789 1 -
CHEMBL2178783 1 -
CHEMBL659 GALANTAMINE 4.0 1 -
CHEMBL2178788 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL807 MEMANTINE Ki = 1160.0 nM 5.94
CHEMBL2178782 Ki = 2320.0 nM 5.63
CHEMBL305187 IFENPRODIL Ki = 3080.0 nM 5.51
CHEMBL2178784 MEMAGAL Ki = 4600.0 nM 5.34
CHEMBL2178787 Ki = 4630.0 nM 5.33
CHEMBL2178786 Ki = 4990.0 nM 5.30
CHEMBL2178778 Ki = 5410.0 nM 5.27
CHEMBL2178785 Ki = 10000.0 nM 5.00
CHEMBL2178780 Ki > 10000.0 nM -
CHEMBL2178779 Ki > 10000.0 nM -
CHEMBL2178777 Ki > 10000.0 nM -
CHEMBL2178776 Ki > 10000.0 nM -
CHEMBL2178791 Ki > 10000.0 nM -
CHEMBL2178790 Ki > 10000.0 nM -
CHEMBL2178789 Ki > 10000.0 nM -
CHEMBL2178783 Ki > 10000.0 nM -
CHEMBL659 GALANTAMINE Ki > 10000.0 nM -
CHEMBL2178788 Ki > 10000.0 nM -