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Inhibition of human Nav1.2 alpha subunit expressed in HEK293 cells co-expressing beta1 subunit at -35 mV holding potential by PatchXpress automated voltage clamp electrophysiology technique
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
SummaryRelated BioAssays by Target
Inhibition of Nav1.2 (unknown origin)
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Selectivity interaction (CEREP panel (GPCRs, ion channels, transporters, kinases)) EUB0000103c SCN2A
Assay data:1 Tested
Selectivity interaction (CEREP Wide Ligand screening panel (ion channels, receptors, enzymes)) EUB0000304b SCN2A
Selectivity interaction (CEREP panel (receptors, ion chanels, radiometric assay)) EUB0000192d SCN2A
Assay data:1 Active, 1 Tested
Inhibition of recombinant human Nav1.2 expressed in HEK293 cells incubated for 3 mins by FRET based membrane potential assay
Assay data:2 Active, 4 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Inhibition of NaV1.2 (unknown origin)
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of human Nav1.2 expressed in CHO cells at -120 mV holding potential by automated patch clamp electrophysiology recording
Inhibition of full length human Nav1.2 expressed in HEK cells by whole cell voltage clamp analysis
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of human Nav1.2 stably expressed in cells with train pulses to -20 mV at 0.1 Hz and holding potential of -95 mV by Qube-automated patch clamp assay
Assay data:1 Active, 3 Tested
Automated patch clamp (Inactivation State Block) from US Patent US10577308: "Sodium channel modulators"
Assay data:28 Active, 8 Activity ≤ 1 µM, 36 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
Automated patch clamp (Tonic Block) from US Patent US10577308: "Sodium channel modulators"
Assay data:14 Active, 1 Activity ≤ 1 µM, 36 Tested
Inhibition Assay from US Patent US9181219: "Compounds of modulating TRPV3 function"
Assay data:20 Active, 13 Activity ≤ 1 µM, 20 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Voltage-Clamp Assay from US Patent US9675591: "Methods for treating seizure disorders and pain"
SummaryCompounds, ActiveRelated BioAssays by Target
Radioligand Binding Assay from US Patent US9694002: "Substituted benzamides and methods of use thereof"
Assay data:572 Active, 5 Activity ≤ 1 nM, 546 Activity ≤ 1 µM, 574 Tested
Na+ channel (site 2) CEREP ligand profiling
NA+/SITE2ATG Eurofins-Panlabs selectivity data (BI)
NA+/SITE2AG Eurofins-Panlabs selectivity data (BI)
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