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Receptor Binding Assay from US Patent US11535596: "Analogs of dextromethorphan with balanced receptor activities"
Assay data:15 Active, 15 Activity ≤ 1 µM, 16 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Effects of Test Articles on Cloned Human NR1/GuN2B Ion Channels Expressed in Mammalian Cells from US Patent US11530210: "Substituted heteroaromatic pyrazolo-pyridines and their use as GLUN2B receptor modulators"
Assay data:281 Active, 246 Activity ≤ 1 µM, 291 Tested
Binding affinity to TCP-stimulated NMDA (unknown origin)
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Binding affinity to NMDA receptor (unknown origin)
Assay data:4 Active, 4 Activity ≤ 1 µM, 4 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Selectivity interaction (PRESTO-Tango GPCR-ome screening) EUB0000539a GRIN1
SummaryCompounds, ActiveRelated BioAssays by Target
Inhibition of human GluN1/N2A expressed in HEK293 cells assessed as NMDA/glycine-induced fraction of total transmembrane voltage field at 10 uM preincubated for 20 secs followed by NMDA treatment for 10 secs by patch-clamp method
Assay data:2 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of GluN1/N2A (unknown origin) expressed in human tsA201 cells assessed as glutamate-induced change in voltage at -65 mV holding potential for 30 secs by whole-cell patch-clamp method
Inhibition of eGFP-tagged rat GluN1-1a/GluN2A transfected in human tsA201 cells assessed as glutamate-induced fraction of total transmembrane voltage field at 10 uM by whole-cell patch-clamp method
Assay data:1 Tested
Inhibition of eGFP-tagged rat GluN1-1a/GluN2A transfected in human tsA201 cells assessed as glutamate-induced change in voltage at 10 uM by whole-cell patch-clamp method
Inhibition of eGFP-tagged rat GluN1-1a/GluN2A transfected in human tsA201 cells assessed as inhibition glutamate-induced current measured at -65 mV holding potential applied for 10 secs in presence of Mg2+ by whole-cell patch-clamp method
Inhibition of eGFP-tagged rat GluN1-1a/GluN2A transfected in human tsA201 cells assessed as inhibition glutamate-induced current measured at -65 mV holding potential applied for 10 secs by whole-cell patch-clamp method
Assay data:3 Active, 2 Activity ≤ 1 µM, 4 Tested
Inhibition of eGFP-tagged rat GluN1/GluN2A transfected in human tsA201 cells assessed as weighted time constant for recovery of glycine/NMDA-induced current at 10 uM treated for 40 secs followed by application of +60 mV holding potential for 5 secs measured after 40 secs of compound removal by whole-cell patch-clamp method
Inhibition of eGFP-tagged rat GluN1/GluN2A transfected in human tsA201 cells assessed as recovery of glycine/NMDA-induced current at 10 uM treated for 40 secs followed by application of +60 mV holding potential for 5 secs measured after 40 secs of compound removal by whole-cell patch-clamp method relative to control
Assay data:1 Active, 3 Tested
Inhibition of eGFP-tagged rat GluN1/GluN2A transfected in human tsA201 cells assessed as weighted time constant for blockade of glycine/NMDA-induced current at 10 uM at 1 sec by whole-cell patch-clamp method
Assay data:3 Active, 4 Tested
Inhibition of eGFP-tagged rat GluN1/GluN2A transfected in human tsA201 cells assessed as blockade of glycine/NMDA-induced current at 10 uM treated for 40 secs measured at +60 mV holding potential applied for 5 secs by whole-cell patch-clamp method relative to control
Assay data:3 Tested
Inhibition of eGFP-tagged rat GluN1/GluN2A transfected in human tsA201 cells assessed as blockade of glycine/NMDA-induced current at 10 uM treated for 40 secs measured at -60 mV holding potential after returning from +60 mV application for 5 secs by whole-cell patch-clamp method relative to control
Assay data:4 Tested
Inhibition of NMDA receptor in NMDA-stimulated rat cerebellar granule neurons assessed as measuring intracellular calcium concentration in presence of glycine by Fura2-AM dye based fluorescence assay
Assay data:1 Active, 13 Tested
Binding affinity to NMDAR (unknown origin) assessed as inhibition constant by [3H]MK-801 binding assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Positive allosteric modulator activity at GluN1a/GluN2D (unknown origin) expressed in CHO cells at 30 uM in presence of glutamate by Ca2+ influx assay relative to control
Positive allosteric modulator activity at GluN1a/GluN2C (unknown origin) expressed in CHO cells at 30 uM in presence of glutamate by Ca2+ influx assay relative to control
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