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Selectivity interaction (CEREP ligand displacement assays (non-kinase proteins)) EUB0001326b SCN5A
Assay data:1 Tested
SummaryRelated BioAssays by Target
Selectivity interaction (Eurofins-Panlabs Screen) EUB0001548a SCN2A
Selectivity interaction (CEREB panel (panel of receptors, transporters, ion channels, and other enzymes)) EUB0001119a SCN2A
Selectivity interaction (Eurofins CEREP Diversity Profile (receptors and ion channels)) EUB0000279b SCN2A
Selectivity interaction (Panel of non-epigenetic targets (kinases, GPCRs, ion channels, and transporters, Eurofins) ) EUB0000271b SCN2A
Selectivity interaction (Panel of kinases, GPCRs, ion channels and transporters (enzymatic assay)) EUB0000223bCl SCN5A
Selectivity interaction (Panel of kinases, GPCRs, ion channels and transporters (enzymatic assay)) EUB0000266bCl SCN5A
Selectivity interaction (CEREP selectivity screen) EUB0000318b SCN1B
Selectivity interaction (SafetyScreen enzymatic and binding assays (Eurofins, panel of GPCRs, transporters, ion channels, nuclear receptors, and other enzymes)) EUB0000050b SCN2A
Selectivity interaction (BET inhibitor selectivity panel (Human Blocker ionworks assay)) EUB0000102c SCN5A
Activity against NA+/SITE2/RA in the Eurofins Panlabs screen (BI) by Radioactive Assay
Activity against NA+/SITE2/R in the Eurofins SafetyScreen44 (CEREP) (BI) by Radioactive Assay (Cerep_169)
Assay data:5 Tested
SafetyScreen: Sodium Ion Channel Site 2 (Non-Selective) Rat Ion Channel [3H] Batrachotoxinin Binding LeadHunter Assay, catalogue number: 169
Assay data:10 Tested
Compounds were solubilised to 10 mM in DMSO and diluted in HBPS to 30 mM. 6-Point concentration-response curves were generated using serial dilutions from the top test concentration. Electrophysiological recordings were made from a Chinese Hamster Ovary cell line stably expressing the full-length ion channel. Single cell ionic currents were measured in whole-cell configuration at room temperature. The internal solution for hNaV1.5 is buffered to pH 7.3, and the external solution is buffered to pH 7.4. The test pulse was applied according to voltage protocol. Compounds were incubated for 2 min to allow stabilization of the parameters. Concentration-response curves were generated by cumulative addition of compound with concentrations low to high. In all cases, steady-state inhibition was achieved before the next concentration of compound was added. To investigate any use-dependence, an 8-pulse voltage protocol is applied at a frequency of 3 Hz. Inhibition is compared at pulse 1 and pulse 8. Any difference in the potency of a compound at P8 versus P1 would be typical of use-dependent block. IC50 values or % inhibition at the top test concentration is obtained. The assay has been performed by Concept Life Sciences Ltd.
Assay data:9 Tested
Binding affinity to Nav1.5 (unknown origin) expressed in HEK293T cells assessed as retention time by cell membrane chromatography analysis
Assay data:20 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of human Nav1.2 expressed in CHO cells by whole-cell patch clamp assay
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Inhibition of human Nav1.6 expressed in HEK293 cells by automated patch-clamp assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of human Nav1.5 channel
Inhibition of human Nav1.5 expressed in HEK293 cells at 10 uM by QPatch voltage clamp assay relative to control
Inhibition of human Nav1.5 expressed in HEK293 cells by QPatch voltage clamp assay
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