Affinity DataIC50: 0.200nMpH: 7.4 T: 2°CAssay Description:Binding of this radioligand was preformed in 5 mL borosilicate glass test tubes at room temperature. Binding was initiated by adding membranes to inc...More data for this Ligand-Target Pair
TargetSodium channel protein type 2 subunit alpha(Homo sapiens (Human))
Xenon Pharmaceuticals
Curated by ChEMBL
Xenon Pharmaceuticals
Curated by ChEMBL
Affinity DataIC50: 0.200nMAssay Description:Inhibition of full length human Nav1.2 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -35 mV by...More data for this Ligand-Target Pair
Affinity DataIC50: 0.200nMpH: 7.2Assay Description:Patch voltage clamp electrophysiology allows for the direct measurement and quantification of block of voltage-gated sodium channels (NaV's), and...More data for this Ligand-Target Pair
TargetSodium channel protein type 9 subunit alpha(Mus musculus)
Xenon Pharmaceuticals
Curated by ChEMBL
Xenon Pharmaceuticals
Curated by ChEMBL
Affinity DataIC50: 0.200nMAssay Description:Inhibition of Nav1.7 channel in mouse CAD cells by whole-cell patch clamp assayMore data for this Ligand-Target Pair
TargetSodium channel protein type 1/10/11/2/3/4/5/8/9 subunit alpha(Homo sapiens (Human))
Genentech
US Patent
Genentech
US Patent
Affinity DataIC50: 0.300nMpH: 7.4 T: 2°CAssay Description:Binding of this radioligand was preformed in 5 mL borosilicate glass test tubes at room temperature. Binding was initiated by adding membranes to inc...More data for this Ligand-Target Pair
Affinity DataIC50: 0.300nMAssay Description:Inhibition of full length human Nav1.7 channel expressed in HEK cells co-expressing human sodium channel subunit beta3 at -150 mV by manual voltage c...More data for this Ligand-Target Pair
Affinity DataIC50: 0.300nMAssay Description:Inhibition of full length human Nav1.7 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -60 mV by...More data for this Ligand-Target Pair
Affinity DataIC50: 0.300nMT: 2°CAssay Description:Patch voltage clamp electrophysiology allows for the direct measurement and quantification of block of voltage-gated sodium channels (NaV's), and all...More data for this Ligand-Target Pair
Affinity DataIC50: 0.300nMpH: 7.4 T: 2°CAssay Description:Preparation of membranes containing recombinantly expressed sodium channels: Frozen recombinant cell pellets were thawed on ice and diluted to 4 time...More data for this Ligand-Target Pair
Affinity DataIC50: 0.300nMAssay Description:The following patch voltage clamp electrophysiology studies were performed on representative compounds of the invention using human embryonic kidney ...More data for this Ligand-Target Pair
Affinity DataIC50: 0.300nMpH: 7.4 T: 2°CAssay Description:Radioligand Binding Studies: Saturation experiments. A representative compound of formula (I) having a methyl group was tritiated. Three tritiums wer...More data for this Ligand-Target Pair
Affinity DataIC50: 0.300nMAssay Description:Inhibition of human Nav1.7 alpha subunit expressed in HEK293 cells co-expressing beta1 subunit at -60 mV holding potential by whole-cell patch voltag...More data for this Ligand-Target Pair
Affinity DataIC50: 0.400nMAssay Description:Inhibition of full length human Nav1.7 channel expressed in HEK cells co-expressing human sodium channel subunit beta3 at -150 mV by manual voltage c...More data for this Ligand-Target Pair
Affinity DataIC50: 0.400nMAssay Description:Inhibition of full length human Nav1.7 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -60 mV by...More data for this Ligand-Target Pair
Affinity DataIC50: 0.400nMT: 2°CAssay Description:Patch voltage clamp electrophysiology allows for the direct measurement and quantification of block of voltage-gated sodium channels (NaV's), and all...More data for this Ligand-Target Pair
Affinity DataIC50: 0.400nMAssay Description:The following patch voltage clamp electrophysiology studies were performed on representative compounds of the invention using human embryonic kidney ...More data for this Ligand-Target Pair
Affinity DataIC50: 0.5nMAssay Description:Inhibition of full length human Nav1.7 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -60 mV by...More data for this Ligand-Target Pair
Affinity DataIC50: 0.600nMAssay Description:Inhibition of human Nav1.7 alpha subunit expressed in HEK293 cells co-expressing beta1 subunit at -60 mV holding potential by whole-cell patch voltag...More data for this Ligand-Target Pair
Affinity DataIC50: 0.700nMAssay Description:Inhibition of human Nav1.7 alpha subunit expressed in HEK293 cells co-expressing beta1 subunit at -60 mV holding potential by whole-cell patch voltag...More data for this Ligand-Target Pair
Affinity DataIC50: 0.800nMpH: 7.4 T: 2°CAssay Description:Radioligand Binding Studies: Saturation experiments. A representative compound of formula (I) having a methyl group was tritiated. Three tritiums wer...More data for this Ligand-Target Pair
TargetSodium channel protein type 1/10/11/2/3/4/5/8/9 subunit alpha(Homo sapiens (Human))
Genentech
US Patent
Genentech
US Patent
Affinity DataIC50: 0.800nMpH: 7.4 T: 2°CAssay Description:Binding of this radioligand was preformed in 5 mL borosilicate glass test tubes at room temperature. Binding was initiated by adding membranes to inc...More data for this Ligand-Target Pair
TargetSodium channel protein type 8 subunit alpha(Homo sapiens (Human))
Xenon Pharmaceuticals
Curated by ChEMBL
Xenon Pharmaceuticals
Curated by ChEMBL
Affinity DataIC50: 0.800nMAssay Description:Inhibition of full length human Nav1.6 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -35 mV by...More data for this Ligand-Target Pair
Affinity DataIC50: 0.900nMpH: 7.2Assay Description:Patch voltage clamp electrophysiology allows for the direct measurement and quantification of block of voltage-gated sodium channels (NaV's), and...More data for this Ligand-Target Pair
Affinity DataIC50: 0.900nMAssay Description:Inhibition of human Nav1.7 expressed in HEK cells assessed as reduction in sodium current at -60 mV holding potential by PatchXpress platform based w...More data for this Ligand-Target Pair
Affinity DataIC50: 0.900nMpH: 7.4 T: 2°CAssay Description:Binding of this radioligand was preformed in 5 mL borosilicate glass test tubes at room temperature. Binding was initiated by adding membranes to inc...More data for this Ligand-Target Pair
Affinity DataIC50: 1nMpH: 7.4 T: 2°CAssay Description:Radioligand Binding Studies: Saturation experiments. A representative compound of formula (I) was tritiated. Three tritiums were incorporated in plac...More data for this Ligand-Target Pair
Affinity DataIC50: 1nMpH: 7.4 T: 2°CAssay Description:Radioligand Binding Studies: Saturation experiments. A representative compound of formula (I) was tritiated. Three tritiums were incorporated in plac...More data for this Ligand-Target Pair
Affinity DataIC50: 1nMpH: 7.4 T: 2°CAssay Description:Radioligand Binding Studies: Saturation experiments. A representative compound of formula (I) was tritiated. Three tritiums were incorporated in plac...More data for this Ligand-Target Pair
Affinity DataIC50: 1nMpH: 7.4 T: 2°CAssay Description:Radioligand Binding Studies: Saturation experiments. A representative compound of formula (I) was tritiated. Three tritiums were incorporated in plac...More data for this Ligand-Target Pair
Affinity DataIC50: 1nMpH: 7.4 T: 2°CAssay Description:Radioligand Binding Studies: Saturation experiments. A representative compound of formula (I) was tritiated. Three tritiums were incorporated in plac...More data for this Ligand-Target Pair
TargetSodium channel protein type 8 subunit alpha(Homo sapiens (Human))
Xenon Pharmaceuticals
Curated by ChEMBL
Xenon Pharmaceuticals
Curated by ChEMBL
Affinity DataIC50: 1nMAssay Description:Sodium currents were measured using the patch clamp technique in the whole-cell configuration using either a PatchXpress automated voltage clamp or m...More data for this Ligand-Target Pair
TargetSodium channel protein type 8 subunit alpha(Homo sapiens (Human))
Xenon Pharmaceuticals
Curated by ChEMBL
Xenon Pharmaceuticals
Curated by ChEMBL
Affinity DataIC50: 1nMAssay Description:Patch voltage clamp electrophysiology allows for the direct measurement and quantification of block of voltage-gated sodium channels (NaV's), and...More data for this Ligand-Target Pair
TargetSodium channel protein type 8 subunit alpha(Homo sapiens (Human))
Xenon Pharmaceuticals
Curated by ChEMBL
Xenon Pharmaceuticals
Curated by ChEMBL
Affinity DataIC50: 1nMAssay Description:This sodium influx assay employs the use of the cell permeable, sodium sensitive dye ANG2 to quantify sodium ion influx through sodium channels which...More data for this Ligand-Target Pair
TargetSodium channel protein type 8 subunit alpha(Homo sapiens (Human))
Xenon Pharmaceuticals
Curated by ChEMBL
Xenon Pharmaceuticals
Curated by ChEMBL
Affinity DataIC50: 1nMAssay Description:Patch voltage clamp electrophysiology allows for the direct measurement and quantification of block of voltage-gated sodium channels (NaV's), and...More data for this Ligand-Target Pair
TargetSodium channel protein type 8 subunit alpha(Homo sapiens (Human))
Xenon Pharmaceuticals
Curated by ChEMBL
Xenon Pharmaceuticals
Curated by ChEMBL
Affinity DataIC50: 1nMAssay Description:Patch voltage clamp electrophysiology allows for the direct measurement and quantification of block of voltage-gated sodium channels (Nay's), and...More data for this Ligand-Target Pair
Affinity DataIC50: 1nMAssay Description:Inhibition of inactivated state of recombinant human NaV1.7 expressed in HEK293 cell membranes coexpressing Nav beta1 subunit assessed as decrease in...More data for this Ligand-Target Pair
TargetSodium channel protein type 8 subunit alpha(Homo sapiens (Human))
Xenon Pharmaceuticals
Curated by ChEMBL
Xenon Pharmaceuticals
Curated by ChEMBL
Affinity DataIC50: 1nMAssay Description:The following patch voltage clamp electrophysiology studies were performed on representative compounds of the invention using human embryonic kidney ...More data for this Ligand-Target Pair
TargetSodium channel protein type 8 subunit alpha(Homo sapiens (Human))
Xenon Pharmaceuticals
Curated by ChEMBL
Xenon Pharmaceuticals
Curated by ChEMBL
Affinity DataIC50: 1nMAssay Description:Patch voltage clamp electrophysiology allows for the direct measurement and quantification of block of voltage-gated sodium channels (Nay's), and...More data for this Ligand-Target Pair
Affinity DataIC50: <1nMpH: 7.2Assay Description:Patch voltage clamp electrophysiology allows for the direct measurement and quantification of block of voltage-gated sodium channels (NaV's), and...More data for this Ligand-Target Pair
Affinity DataIC50: 1nMT: 2°CAssay Description:Patch voltage clamp electrophysiology allows for the direct measurement and quantification of block of voltage-gated sodium channels (NaV's), and all...More data for this Ligand-Target Pair
Affinity DataIC50: <1nMpH: 7.4 T: 2°CAssay Description:Binding of this radioligand was preformed in 5 mL borosilicate glass test tubes at room temperature. Binding was initiated by adding membranes to inc...More data for this Ligand-Target Pair
Affinity DataIC50: 1nMT: 2°CAssay Description:Patch voltage clamp electrophysiology allows for the direct measurement and quantification of block of voltage-gated sodium channels (NaV's), and all...More data for this Ligand-Target Pair
Affinity DataIC50: 1nMpH: 7.4 T: 2°CAssay Description:Radioligand Binding Studies: Saturation experiments. A representative compound of formula (I) was tritiated. Three tritiums were incorporated in plac...More data for this Ligand-Target Pair
Affinity DataIC50: 1.10nMAssay Description:Inhibition of human Nav1.7 expressed in HEK cells assessed as reduction in sodium current at -60 mV holding potential by PatchXpress platform based w...More data for this Ligand-Target Pair
Affinity DataIC50: 1.30nMpH: 7.4 T: 2°CAssay Description:Radioligand Binding Studies: Saturation experiments. A representative compound of formula (I) having a methyl group was tritiated. Three tritiums wer...More data for this Ligand-Target Pair
TargetSodium channel protein type 1/10/11/2/3/4/5/8/9 subunit alpha(Homo sapiens (Human))
Genentech
US Patent
Genentech
US Patent
Affinity DataIC50: 1.30nMpH: 7.4 T: 2°CAssay Description:Binding of this radioligand was preformed in 5 mL borosilicate glass test tubes at room temperature. Binding was initiated by adding membranes to inc...More data for this Ligand-Target Pair
Affinity DataIC50: 1.31nMAssay Description:The following patch voltage clamp electrophysiology studies were performed on representative compounds of the invention using human embryonic kidney ...More data for this Ligand-Target Pair
Affinity DataIC50: 1.31nMT: 2°CAssay Description:Patch voltage clamp electrophysiology allows for the direct measurement and quantification of block of voltage-gated sodium channels (NaV's), and all...More data for this Ligand-Target Pair
Affinity DataIC50: 1.40nMT: 2°CAssay Description:Patch voltage clamp electrophysiology allows for the direct measurement and quantification of block of voltage-gated sodium channels (NaV's), and all...More data for this Ligand-Target Pair
Affinity DataIC50: 1.40nMAssay Description:The following patch voltage clamp electrophysiology studies were performed on representative compounds of the invention using human embryonic kidney ...More data for this Ligand-Target Pair