BDBM145285 US8952169, 64::US9771376, Example 64
SMILES Fc1cc(OCC23CC4CC(CC(C4)C2)C3)c(cc1C(=O)NS(=O)(=O)N1CCC1)C1CC1
InChI Key InChIKey=PTCBNPULJWGSML-UHFFFAOYSA-N
Data 23 IC50
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 23 hits for monomerid = 145285
TargetSodium channel protein type 9 subunit alpha(Homo sapiens (Human))
Xenon Pharmaceuticals
US Patent
Xenon Pharmaceuticals
US Patent
Affinity DataIC50: 2nMpH: 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: 51nMAssay Description:Inhibition of human Nav1.5/beta1/2 transfected in HEK293-A cells assessed as inhibition of channel current incubated for 5.5 mins by high-throughput ...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: 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
TargetSodium channel protein type 9 subunit alpha(Homo sapiens (Human))
Xenon Pharmaceuticals
US Patent
Xenon Pharmaceuticals
US Patent
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
TargetSodium channel protein type 9 subunit alpha(Homo sapiens (Human))
Xenon Pharmaceuticals
US Patent
Xenon Pharmaceuticals
US Patent
Affinity DataIC50: 0.400nMAssay Description:Inhibition of Nav1.7 (unknown origin) by electrophysiology assayMore data for this Ligand-Target Pair
TargetSodium channel protein type 1 subunit alpha(Homo sapiens (Human))
Siteone Therapeutics
Curated by ChEMBL
Siteone Therapeutics
Curated by ChEMBL
Affinity DataIC50: 11nMAssay Description:Inhibition of human Nav1.1 expressed in HEK293 cells by electrophysiology assayMore data for this Ligand-Target Pair
TargetSodium channel protein type 7 subunit alpha(Homo sapiens (Human))
Siteone Therapeutics
Curated by ChEMBL
Siteone Therapeutics
Curated by ChEMBL
Affinity DataIC50: 0.400nMAssay Description:Inhibition of human Nav1.7 expressed in HEK293 cells by electrophysiology assayMore data for this Ligand-Target Pair
TargetSodium channel protein type 2 subunit alpha(Homo sapiens (Human))
Siteone Therapeutics
Curated by ChEMBL
Siteone Therapeutics
Curated by ChEMBL
Affinity DataIC50: 20nMAssay Description:Inhibition of human Nav1.2 expressed in HEK293 cells by electrophysiology assayMore data for this Ligand-Target Pair
TargetSodium channel protein type 8 subunit alpha(Homo sapiens (Human))
Siteone Therapeutics
Curated by ChEMBL
Siteone Therapeutics
Curated by ChEMBL
Affinity DataIC50: 480nMAssay Description:Inhibition of human Nav1.6 expressed in HEK293 cells by electrophysiology assayMore data for this Ligand-Target Pair
TargetSodium channel protein type 5 subunit alpha(Homo sapiens (Human))
Siteone Therapeutics
Curated by ChEMBL
Siteone Therapeutics
Curated by ChEMBL
Affinity DataIC50: 49nMAssay Description:Inhibition of human Nav1.5 expressed in HEK293 cells by electrophysiology assayMore data for this Ligand-Target Pair
TargetSodium channel protein type 7 subunit alpha(Homo sapiens (Human))
Siteone Therapeutics
Curated by ChEMBL
Siteone Therapeutics
Curated by ChEMBL
Affinity DataIC50: 1.10nMAssay Description:Displacement of [3H]GX-545 Nav1.7 (unknown origin) expressed in HEK cells by liquid scintillation counting based radioligand competition assayMore data for this Ligand-Target Pair
TargetSodium channel protein type 7 subunit alpha(Homo sapiens (Human))
Siteone Therapeutics
Curated by ChEMBL
Siteone Therapeutics
Curated by ChEMBL
Affinity DataIC50: 49nMAssay Description:Inhibition of human Nav1.7 expressed in HEK293 cells incubated for 1 hr in presence of veratridine by sodium influx assayMore data for this Ligand-Target Pair
TargetSodium channel protein type 5 subunit alpha(Homo sapiens (Human))
Siteone Therapeutics
Curated by ChEMBL
Siteone Therapeutics
Curated by ChEMBL
Affinity DataIC50: 870nMAssay Description:Inhibition of human Nav1.5 expressed in HEK293 cells incubated for 1 hr in presence of veratridine and anthropleurin-C by sodium influx assayMore data for this Ligand-Target Pair
TargetSodium channel protein type 7 subunit alpha(Homo sapiens (Human))
Siteone Therapeutics
Curated by ChEMBL
Siteone Therapeutics
Curated by ChEMBL
Affinity DataIC50: 0.400nMAssay Description:Inhibition of full length human Nav1.7 expressed in HEK cells by whole cell voltage clamp analysisMore data for this Ligand-Target Pair
TargetSodium channel protein type 1 subunit alpha(Homo sapiens (Human))
Siteone Therapeutics
Curated by ChEMBL
Siteone Therapeutics
Curated by ChEMBL
Affinity DataIC50: 11nMAssay Description:Inhibition of full length human Nav1.1 expressed in HEK cells by whole cell voltage clamp analysisMore data for this Ligand-Target Pair
TargetSodium channel protein type 2 subunit alpha(Homo sapiens (Human))
Siteone Therapeutics
Curated by ChEMBL
Siteone Therapeutics
Curated by ChEMBL
Affinity DataIC50: 19nMAssay Description:Inhibition of full length human Nav1.2 expressed in HEK cells by whole cell voltage clamp analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 8.5nMAssay Description:Inhibition of full length human Nav1.4 expressed in HEK cells by whole cell voltage clamp analysisMore data for this Ligand-Target Pair
TargetSodium channel protein type 5 subunit alpha(Homo sapiens (Human))
Siteone Therapeutics
Curated by ChEMBL
Siteone Therapeutics
Curated by ChEMBL
Affinity DataIC50: 51nMAssay Description:Inhibition of full length human Nav1.5 expressed in HEK cells by whole cell voltage clamp analysisMore data for this Ligand-Target Pair
TargetSodium channel protein type 8 subunit alpha(Homo sapiens (Human))
Siteone Therapeutics
Curated by ChEMBL
Siteone Therapeutics
Curated by ChEMBL
Affinity DataIC50: 480nMAssay Description:Inhibition of human Nav1.6 expressed in CHO cells by whole cell voltage clamp analysisMore 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: 0.400nMAssay Description:Inhibition of human Nav1.7/beta1/2 transfected in HEK293-A cells assessed as inhibition of channel current incubated for 5.5 mins by high-throughput ...More data for this Ligand-Target Pair
Affinity DataIC50: 11nMAssay Description:Inhibition of human Nav1.1/beta1/2 transfected in HEK293-A cells assessed as inhibition of channel current incubated for 5.5 mins by high-throughput ...More data for this Ligand-Target Pair
TargetSodium channel protein type 5 subunit alpha(Homo sapiens (Human))
Siteone Therapeutics
Curated by ChEMBL
Siteone Therapeutics
Curated by ChEMBL
Affinity DataIC50: 51.5nMT: 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