BDBM268418 N-(7-(adamantan-1-ylmethoxy)-6-ethyl-[1,2,4]triazolo[4,3-a]-pyridin-3-yl)-cyclopropanesulfonamide::US9550775, 1
SMILES O=S(=O)(Nc1nnc2cc(OCC34CC5CC(CC(C5)C3)C4)c(cn12)C1CC1)C1CC1
InChI Key InChIKey=FPERPEQIXLOVIK-UHFFFAOYSA-N
Data 13 IC50
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 13 hits for monomerid = 268418
Affinity DataIC50: 2.92nMpH: 7.2Assay 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: 92nMAssay Description:Inhibition of inactivated state of recombinant human NaV1.6 expressed in HEK293 cell membranes coexpressing Nav beta1 subunit assessed as decrease in...More data for this Ligand-Target Pair
TargetSodium channel protein type 5 subunit alpha(Homo sapiens (Human))
Xenon Pharmaceuticals
Curated by ChEMBL
Xenon Pharmaceuticals
Curated by ChEMBL
Affinity DataIC50: 110nMAssay Description:Inhibition of inactivated state of recombinant human NaV1.5 expressed in HEK293 cell membranes coexpressing Nav beta1 subunit assessed as decrease in...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: 7nMAssay Description:Inhibition of inactivated state of recombinant human NaV1.2 expressed in HEK293 cell membranes coexpressing Nav beta1 subunit assessed as decrease in...More data for this Ligand-Target Pair
TargetSodium channel protein type 1 subunit alpha(Homo sapiens (Human))
Xenon Pharmaceuticals
Curated by ChEMBL
Xenon Pharmaceuticals
Curated by ChEMBL
Affinity DataIC50: 45nMAssay Description:Inhibition of inactivated state of recombinant human NaV1.1 expressed in HEK293 cell membranes coexpressing Nav beta1 subunit assessed as decrease in...More data for this Ligand-Target Pair
Affinity DataIC50: 7nMAssay Description:Inhibition of inactivated state of recombinant wild type human NaV1.7 expressed in HEK293 cell membranes coexpressing Nav beta1 subunit assessed as d...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: 7nMAssay Description:Inhibition of inactivated state of mouse NaV1.7 assessed as decrease in sodium current amplitude at -60 mV holding potential after 20 mins by Qube384...More data for this Ligand-Target Pair
Affinity DataIC50: 10nMAssay Description:Displacement of [3H]GX-545 from recombinant human NaV1.7 expressed in HEK293 cell membranes coexpressing Nav beta1 subunit after 18 hrs by liquid sci...More data for this Ligand-Target Pair
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of CYP3A4 in human liver microsomes using testosterone/midazolam as substrate after 30 mins by LC-MS/MS methodMore data for this Ligand-Target Pair
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of CYP1A2 in human liver microsomes using phenacetin as substrate after 30 mins by LC-MS/MS methodMore data for this Ligand-Target Pair
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of CYP2C9 in human liver microsomes using warfarin as substrate after 30 mins by LC-MS/MS methodMore data for this Ligand-Target Pair
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of CYP2D6 in human liver microsomes using dextromethorphan as substrate after 30 mins by LC-MS/MS methodMore data for this Ligand-Target Pair
Affinity DataIC50: 3nMAssay 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