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

  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 23 hits for monomerid = 145285   

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

US Patent
LigandPNGBDBM145285(US8952169, 64 | US9771376, Example 64)
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
In DepthDetails US Patent
LigandPNGBDBM145285(US8952169, 64 | US9771376, Example 64)
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
In DepthDetails PubMed
TargetSodium channel protein type 9 subunit alpha(Homo sapiens (Human))
Xenon Pharmaceuticals

US Patent
LigandPNGBDBM145285(US8952169, 64 | US9771376, Example 64)
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
In DepthDetails US Patent
TargetSodium channel protein type 9 subunit alpha(Homo sapiens (Human))
Xenon Pharmaceuticals

US Patent
LigandPNGBDBM145285(US8952169, 64 | US9771376, Example 64)
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
In DepthDetails US Patent
TargetSodium channel protein type 9 subunit alpha(Homo sapiens (Human))
Xenon Pharmaceuticals

US Patent
LigandPNGBDBM145285(US8952169, 64 | US9771376, Example 64)
Affinity DataIC50:  0.400nMAssay Description:Inhibition of Nav1.7 (unknown origin) by electrophysiology assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium channel protein type 1 subunit alpha(Homo sapiens (Human))
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM145285(US8952169, 64 | US9771376, Example 64)
Affinity DataIC50:  11nMAssay Description:Inhibition of human Nav1.1 expressed in HEK293 cells by electrophysiology assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium channel protein type 7 subunit alpha(Homo sapiens (Human))
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM145285(US8952169, 64 | US9771376, Example 64)
Affinity DataIC50:  0.400nMAssay Description:Inhibition of human Nav1.7 expressed in HEK293 cells by electrophysiology assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium channel protein type 2 subunit alpha(Homo sapiens (Human))
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM145285(US8952169, 64 | US9771376, Example 64)
Affinity DataIC50:  20nMAssay Description:Inhibition of human Nav1.2 expressed in HEK293 cells by electrophysiology assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium channel protein type 8 subunit alpha(Homo sapiens (Human))
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM145285(US8952169, 64 | US9771376, Example 64)
Affinity DataIC50:  480nMAssay Description:Inhibition of human Nav1.6 expressed in HEK293 cells by electrophysiology assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium channel protein type 5 subunit alpha(Homo sapiens (Human))
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM145285(US8952169, 64 | US9771376, Example 64)
Affinity DataIC50:  49nMAssay Description:Inhibition of human Nav1.5 expressed in HEK293 cells by electrophysiology assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium channel protein type 7 subunit alpha(Homo sapiens (Human))
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM145285(US8952169, 64 | US9771376, Example 64)
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
In DepthDetails ArticlePubMed
TargetSodium channel protein type 7 subunit alpha(Homo sapiens (Human))
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM145285(US8952169, 64 | US9771376, Example 64)
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
In DepthDetails ArticlePubMed
TargetSodium channel protein type 5 subunit alpha(Homo sapiens (Human))
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM145285(US8952169, 64 | US9771376, Example 64)
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
In DepthDetails ArticlePubMed
TargetSodium channel protein type 7 subunit alpha(Homo sapiens (Human))
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM145285(US8952169, 64 | US9771376, Example 64)
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
In DepthDetails ArticlePubMed
TargetSodium channel protein type 1 subunit alpha(Homo sapiens (Human))
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM145285(US8952169, 64 | US9771376, Example 64)
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
In DepthDetails ArticlePubMed
TargetSodium channel protein type 2 subunit alpha(Homo sapiens (Human))
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM145285(US8952169, 64 | US9771376, Example 64)
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
In DepthDetails ArticlePubMed
TargetSodium channel protein type 4 subunit alpha(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM145285(US8952169, 64 | US9771376, Example 64)
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
In DepthDetails ArticlePubMed
TargetSodium channel protein type 5 subunit alpha(Homo sapiens (Human))
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM145285(US8952169, 64 | US9771376, Example 64)
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
In DepthDetails ArticlePubMed
TargetSodium channel protein type 8 subunit alpha(Homo sapiens (Human))
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM145285(US8952169, 64 | US9771376, Example 64)
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
In DepthDetails ArticlePubMed
TargetCytochrome P450 3A4(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM145285(US8952169, 64 | US9771376, Example 64)
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of CYP3A4 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium channel subunit beta-2(Homo sapiens)TBA
LigandPNGBDBM145285(US8952169, 64 | US9771376, Example 64)
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
In DepthDetails PubMed
LigandPNGBDBM145285(US8952169, 64 | US9771376, Example 64)
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
In DepthDetails PubMed
TargetSodium channel protein type 5 subunit alpha(Homo sapiens (Human))
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM145285(US8952169, 64 | US9771376, Example 64)
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
In DepthDetails US Patent