BDBM50530539 CHEMBL4460028::US11174268, Example 300
SMILES CC1(C)CCN1Cc1cccc(F)c1CNc1cc(F)c(c(F)c1)S(=O)(=O)Nc1cscn1
InChI Key InChIKey=GFSUVQOECDPIQJ-UHFFFAOYSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 29 hits for monomerid = 50530539
TargetSodium channel protein type 5 subunit alpha/subunit beta-1(Homo sapiens (Human))
Xenon Pharmaceuticals
Curated by ChEMBL
Xenon Pharmaceuticals
Curated by ChEMBL
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of recombinant human full length Nav1.5 co-expressed with human SCN1B in HEK293 cells measured after 20 mins at -60 mV holding potential b...More data for this Ligand-Target Pair
TargetSodium channel protein type 1 subunit alpha(Homo sapiens (Human))
Xenon Pharmaceuticals
US Patent
Xenon Pharmaceuticals
US Patent
Affinity DataIC50: 1.00E+4nMAssay 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 1 subunit alpha/subunit beta-1(Homo sapiens (Human))
Xenon Pharmaceuticals
Curated by ChEMBL
Xenon Pharmaceuticals
Curated by ChEMBL
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of recombinant human full length Nav1.1 co-expressed with human SCN1B in HEK293 cells measured after 20 mins at -45 mV holding potential b...More data for this Ligand-Target Pair
Affinity DataIC50: 5.00E+4nMAssay Description:Inhibition of CYP1A2 in human liver microsomes using phenacetin as substrate incubated for 10 mins in presence of NADPH by LC-MS/MS analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 5.00E+4nMAssay Description:Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate incubated for 10 mins in presence of NADPH by LC-MS/MS analysisMore data for this Ligand-Target Pair
TargetSodium channel protein type 5 subunit alpha/subunit beta-1(Homo sapiens (Human))
Xenon Pharmaceuticals
Curated by ChEMBL
Xenon Pharmaceuticals
Curated by ChEMBL
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of recombinant human full length Nav1.5 co-expressed with human SCN1B in HEK293 cells measured after 20 mins at -60 mV holding potential b...More data for this Ligand-Target Pair
Affinity DataIC50: 31nMAssay Description:Inhibition of recombinant human full length Nav1.2 co-expressed with human SCN1B in HEK293 cells measured after 20 mins at -45 mV holding potential b...More data for this Ligand-Target Pair
TargetNuclear receptor subfamily 1 group I member 2(Homo sapiens (Human))
Xenon Pharmaceuticals
Curated by ChEMBL
Xenon Pharmaceuticals
Curated by ChEMBL
Affinity DataEC50: 1.18E+4nMAssay Description:Agonist activity at PXR in human DPX2 cells after 24 hrs by luciferase reporter gene assayMore data for this Ligand-Target Pair
TargetNuclear receptor subfamily 1 group I member 2(Homo sapiens (Human))
Xenon Pharmaceuticals
Curated by ChEMBL
Xenon Pharmaceuticals
Curated by ChEMBL
Affinity DataEC50: 1.18E+4nMAssay Description:Agonist activity at PXR in human DPX2 cells after 24 hrs by luciferase reporter gene assayMore data for this Ligand-Target Pair
Affinity DataIC50: 5.00E+4nMAssay Description:Inhibition of CYP1A2 in human liver microsomes using phenacetin as substrate incubated for 10 mins in presence of NADPH by LC-MS/MS analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 5.00E+4nMAssay Description:Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate incubated for 10 mins in presence of NADPH by LC-MS/MS analysisMore data for this Ligand-Target Pair
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Xenon Pharmaceuticals
Curated by ChEMBL
Xenon Pharmaceuticals
Curated by ChEMBL
Affinity DataIC50: 2.22E+4nMAssay Description:Inhibition of human ERG expressed in HEK293 cells by IonWorks barracuda patch clamp methodMore data for this Ligand-Target Pair
TargetSodium channel protein type 9 subunit alpha/subunit beta-1(Homo sapiens (Human))
Xenon Pharmaceuticals
Curated by ChEMBL
Xenon Pharmaceuticals
Curated by ChEMBL
Affinity DataIC50: 664nMAssay Description:Inhibition of recombinant human full length Nav1.7 co-expressed with human SCN1B in HEK293 cells measured after 20 mins at -60 mV holding potential b...More data for this Ligand-Target Pair
Affinity DataIC50: 2.30E+4nMAssay Description:Inhibition of CYP2C9 in human liver microsomes using diclofenac as substrate incubated for 10 mins in presence of NADPH by LC-MS/MS analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 4.20E+4nMAssay Description:Inhibition of CYP2D6 in human liver microsomes using dextromethorphan as substrate incubated for 10 mins in presence of NADPH by LC-MS/MS analysisMore data for this Ligand-Target Pair
TargetSodium channel protein type 1 subunit alpha/subunit beta-1(Homo sapiens (Human))
Xenon Pharmaceuticals
Curated by ChEMBL
Xenon Pharmaceuticals
Curated by ChEMBL
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of recombinant human full length Nav1.1 co-expressed with human SCN1B in HEK293 cells measured after 20 mins at -45 mV holding potential b...More data for this Ligand-Target Pair
Affinity DataIC50: 2.30E+4nMAssay Description:Inhibition of CYP2C9 in human liver microsomes using diclofenac as substrate incubated for 10 mins in presence of NADPH by LC-MS/MS analysisMore data for this Ligand-Target Pair
TargetSodium channel protein type 8 subunit alpha/subunit beta-1(Homo sapiens (Human))
Xenon Pharmaceuticals
Curated by ChEMBL
Xenon Pharmaceuticals
Curated by ChEMBL
Affinity DataIC50: 60nMAssay Description:Inhibition of recombinant human full length Nav1.6 co-expressed with human SCN1B in HEK293 cells measured after 20 mins at -45 mV holding potential b...More data for this Ligand-Target Pair
Affinity DataIC50: 5.00E+4nMAssay Description:Inhibition of CYP2C19 in human liver microsomes using S-mephenytoin as substrate incubated for 10 mins in presence of NADPH by LC-MS/MS analysisMore data for this Ligand-Target Pair
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Xenon Pharmaceuticals
Curated by ChEMBL
Xenon Pharmaceuticals
Curated by ChEMBL
Affinity DataIC50: 2.22E+4nMAssay Description:Inhibition of human ERG expressed in HEK293 cells by IonWorks barracuda patch clamp methodMore data for this Ligand-Target Pair
TargetSodium channel protein type 9 subunit alpha/subunit beta-1(Homo sapiens (Human))
Xenon Pharmaceuticals
Curated by ChEMBL
Xenon Pharmaceuticals
Curated by ChEMBL
Affinity DataIC50: 664nMAssay Description:Inhibition of recombinant human full length Nav1.7 co-expressed with human SCN1B in HEK293 cells measured after 20 mins at -60 mV holding potential b...More data for this Ligand-Target Pair
Affinity DataIC50: 5.00E+4nMAssay Description:Inhibition of CYP2C19 in human liver microsomes using S-mephenytoin as substrate incubated for 10 mins in presence of NADPH by LC-MS/MS analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 4.20E+4nMAssay Description:Inhibition of CYP2D6 in human liver microsomes using dextromethorphan as substrate incubated for 10 mins in presence of NADPH by LC-MS/MS analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 31nMAssay Description:Inhibition of recombinant human full length Nav1.2 co-expressed with human SCN1B in HEK293 cells measured after 20 mins at -45 mV holding potential b...More data for this Ligand-Target Pair
TargetSodium channel protein type 8 subunit alpha(Homo sapiens (Human))
Xenon Pharmaceuticals
US Patent
Xenon Pharmaceuticals
US Patent
Affinity DataIC50: 346nMAssay 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
US Patent
Xenon Pharmaceuticals
US Patent
Affinity DataIC50: 64nMAssay 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 5 subunit alpha(Homo sapiens (Human))
Xenon Pharmaceuticals
US Patent
Xenon Pharmaceuticals
US Patent
Affinity DataIC50: 3.00E+4nMAssay 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 1 subunit alpha(Homo sapiens (Human))
Xenon Pharmaceuticals
US Patent
Xenon Pharmaceuticals
US Patent
Affinity DataIC50: 1.59E+4nMAssay 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/subunit beta-1(Homo sapiens (Human))
Xenon Pharmaceuticals
Curated by ChEMBL
Xenon Pharmaceuticals
Curated by ChEMBL
Affinity DataIC50: 60nMAssay Description:Inhibition of recombinant human full length Nav1.6 co-expressed with human SCN1B in HEK293 cells measured after 20 mins at -45 mV holding potential b...More data for this Ligand-Target Pair