BDBM145466 US8952169, 245
SMILES CC1(COc2cc(F)c(cc2C2CC2)C(=O)NS(=O)(=O)C2CC2)CCC(F)(F)CC1
InChI Key InChIKey=XUCXIMYTIQZZHZ-UHFFFAOYSA-N
Data 16 IC50
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 16 hits for monomerid = 145466
TargetSodium channel protein type 9 subunit alpha(Homo sapiens (Human))
Xenon Pharmaceuticals
US Patent
Xenon Pharmaceuticals
US Patent
Affinity DataIC50: 4nMpH: 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 9 subunit alpha(Homo sapiens (Human))
Xenon Pharmaceuticals
US Patent
Xenon Pharmaceuticals
US Patent
Affinity DataIC50: 15nMAssay Description:Displacement of [3H]GX-545 from human Nav1.7 alpha subunit expressed in HEK293 cells co-expressing beta1 subunit by liquid scintillation counting ana...More data for this Ligand-Target Pair
TargetSodium channel protein type 9 subunit alpha(Homo sapiens (Human))
Xenon Pharmaceuticals
US Patent
Xenon Pharmaceuticals
US Patent
Affinity DataIC50: 3nMAssay 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: >1.00E+4nMAssay Description:Inhibition of CYP3A4 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of CYP1A2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of CYP2C19 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of CYP2C9 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of CYP2D6 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 2.5nMAssay Description:Inhibition of mouse Nav1.7 at -60 mV holding potential by PatchXpress automated voltage clamp electrophysiology techniqueMore data for this Ligand-Target Pair
Affinity DataIC50: 9nMAssay Description:Inhibition of rat Nav1.7 at -60 mV holding potential by PatchXpress automated voltage clamp electrophysiology techniqueMore data for this Ligand-Target Pair
Affinity DataIC50: 260nMAssay Description:Inhibition of human Nav1.5 alpha subunit expressed in HEK293 cells co-expressing beta1 subunit at -60 mV holding potential by PatchXpress automated v...More data for this Ligand-Target Pair
Affinity DataIC50: 6nMAssay Description:Inhibition of human Nav1.2 alpha subunit expressed in HEK293 cells co-expressing beta1 subunit at -35 mV holding potential by PatchXpress automated v...More data for this Ligand-Target Pair
Affinity DataIC50: 48nMAssay Description:Inhibition of human Nav1.1 alpha subunit expressed in HEK293 cells co-expressing beta1 subunit at -40 mV holding potential by PatchXpress automated v...More data for this Ligand-Target Pair
Affinity DataIC50: 49nMAssay Description:Inhibition of human Nav1.6 alpha subunit expressed in HEK293 cells co-expressing beta1 subunit at -35 mV holding potential by PatchXpress automated v...More data for this Ligand-Target Pair
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of TTX-resistant Nav1.8 in mouse dorsal root ganglion neuron by voltage clamp recordingMore data for this Ligand-Target Pair
TargetSodium channel protein type 9 subunit alpha(Homo sapiens (Human))
Xenon Pharmaceuticals
US Patent
Xenon Pharmaceuticals
US Patent
Affinity DataIC50: 10nMT: 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