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Assay Detail

CHEMBL4307304

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

Binding
Antagonist activity at NMDA receptor in rat CGN cells assessed as increase in intracellular calcium level incubated for 30 mins in presence of Fura-2AM followed by NMDA/glycine stimulation by fluorescence spectrometer analysis
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Glutamate NMDA receptor (CHEMBL1907608)
Type PROTEIN COMPLEX GROUP
Organism Rattus norvegicus

Publication

A novel class of multitarget anti-Alzheimer benzohomoadamantane‒chlorotacrine hybrids modulating cholinesterases and glutamate NMDA receptors.
Pérez-Areales FJ, Turcu AL, Barniol-Xicota M, Pont C, Pivetta D, Espargaró A, Bartolini M, De Simone A, Andrisano V, Pérez B, Sabate R, Sureda FX, Vázquez S, Muñoz-Torrero D.
Eur J Med Chem (2019) 180 : 613 -626
PubMed 31351393 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.59 6.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4558495 1 6.05
CHEMBL4471659 1 5.92
CHEMBL807 MEMANTINE 4.0 1 5.82
CHEMBL3259988 1 5.72
CHEMBL4469343 1 5.48
CHEMBL4591167 1 5.47
CHEMBL4438626 1 5.16
CHEMBL4462369 1 5.08
CHEMBL292314 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4558495 IC50 = 900.0 nM 6.05
CHEMBL4471659 IC50 = 1200.0 nM 5.92
CHEMBL807 MEMANTINE IC50 = 1500.0 nM 5.82
CHEMBL3259988 IC50 = 1900.0 nM 5.72
CHEMBL4469343 IC50 = 3300.0 nM 5.48
CHEMBL4591167 IC50 = 3400.0 nM 5.47
CHEMBL4438626 IC50 = 7000.0 nM 5.16
CHEMBL4462369 IC50 = 8300.0 nM 5.08
CHEMBL292314 IC50 - -