BDBM268527 N-(6-cyclopropyl-7-((3,5-dichlorophenoxy)methyl)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)methanesulfonamide::US9550775, 106::US9550775, 51

SMILES CS(=O)(=O)Nc1nnc2cc(COc3cc(Cl)cc(Cl)c3)c(cn12)C1CC1

InChI Key InChIKey=DPIPLAYFRAXNRK-UHFFFAOYSA-N

Data  13 IC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
Find this compound or compounds like it in BindingDB:
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Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 13 hits for monomerid = 268527   

TargetSodium channel protein type 9 subunit alpha(Homo sapiens (Human))
Genentech

US Patent
LigandPNGBDBM268527(N-(6-cyclopropyl-7-((3,5-dichlorophenoxy)methyl)-[...)
Affinity DataIC50:  3.15nMpH: 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
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetSodium channel protein type 9 subunit alpha(Homo sapiens (Human))
Genentech

US Patent
LigandPNGBDBM268527(N-(6-cyclopropyl-7-((3,5-dichlorophenoxy)methyl)-[...)
Affinity DataIC50:  3nMpH: 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
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetSodium channel protein type 5 subunit alpha(Homo sapiens (Human))
Xenon Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM268527(N-(6-cyclopropyl-7-((3,5-dichlorophenoxy)methyl)-[...)
Affinity DataIC50:  1.31E+3nMAssay 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
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetCytochrome P450 1A2(Homo sapiens (Human))
Xenon Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM268527(N-(6-cyclopropyl-7-((3,5-dichlorophenoxy)methyl)-[...)
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
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetSodium channel protein type 2 subunit alpha(Homo sapiens (Human))
Xenon Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM268527(N-(6-cyclopropyl-7-((3,5-dichlorophenoxy)methyl)-[...)
Affinity DataIC50:  10nMAssay 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
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetSodium channel protein type 1 subunit alpha(Homo sapiens (Human))
Xenon Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM268527(N-(6-cyclopropyl-7-((3,5-dichlorophenoxy)methyl)-[...)
Affinity DataIC50:  112nMAssay 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
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C9(Homo sapiens (Human))
Xenon Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM268527(N-(6-cyclopropyl-7-((3,5-dichlorophenoxy)methyl)-[...)
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
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetSodium channel protein type 9 subunit alpha(Homo sapiens (Human))
Genentech

US Patent
LigandPNGBDBM268527(N-(6-cyclopropyl-7-((3,5-dichlorophenoxy)methyl)-[...)
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
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetCytochrome P450 2D6(Homo sapiens (Human))
Xenon Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM268527(N-(6-cyclopropyl-7-((3,5-dichlorophenoxy)methyl)-[...)
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
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetSodium channel protein type 9 subunit alpha(Mus musculus)
Xenon Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM268527(N-(6-cyclopropyl-7-((3,5-dichlorophenoxy)methyl)-[...)
Affinity DataIC50:  5nMAssay 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
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetSodium channel protein type 9 subunit alpha(Homo sapiens (Human))
Genentech

US Patent
LigandPNGBDBM268527(N-(6-cyclopropyl-7-((3,5-dichlorophenoxy)methyl)-[...)
Affinity DataIC50:  20nMAssay 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
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetCytochrome P450 3A4(Homo sapiens (Human))
Xenon Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM268527(N-(6-cyclopropyl-7-((3,5-dichlorophenoxy)methyl)-[...)
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
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetSodium channel protein type 9 subunit alpha(Homo sapiens (Human))
Genentech

US Patent
LigandPNGBDBM268527(N-(6-cyclopropyl-7-((3,5-dichlorophenoxy)methyl)-[...)
Affinity DataIC50:  2nMAssay 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
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed