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Found 24 of ic50 for monomerid = 145227
TargetSodium channel protein type 9 subunit alpha(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM145227(US8952169, 6 | US9771376, Example 6)
Affinity DataIC50:  3.80nMAssay Description:Inhibition of Nav1.7 (unknown origin) by PatchXpress methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium channel protein type 9 subunit alpha(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM145227(US8952169, 6 | US9771376, Example 6)
Affinity DataIC50:  4nMAssay 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
In DepthDetails ArticlePubMed
TargetSodium channel protein type 9 subunit alpha(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM145227(US8952169, 6 | US9771376, Example 6)
Affinity DataIC50:  5.5nMT: 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
TargetSodium channel protein type 9 subunit alpha(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM145227(US8952169, 6 | US9771376, Example 6)
Affinity DataIC50:  5.5nMAssay 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))
Pfizer

Curated by ChEMBL
LigandPNGBDBM145227(US8952169, 6 | US9771376, Example 6)
Affinity DataIC50:  6nMAssay Description:Inhibition of human Nav1.7 alpha subunit expressed in HEK293 cells co-expressing beta1 subunit at -60 mV holding potential by whole-cell patch voltag...More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetSodium channel protein type 9 subunit alpha(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM145227(US8952169, 6 | US9771376, Example 6)
Affinity DataIC50:  6nMAssay Description:Inhibition of full length human NaV1.7 expressed in HEK293 cells coexpressing Nav beta1 subunit assessed as decrease in sodium current amplitude by P...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium channel protein type 9 subunit alpha(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM145227(US8952169, 6 | US9771376, Example 6)
Affinity DataIC50:  29nMpH: 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
TargetSodium channel protein type 9 subunit alpha(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM145227(US8952169, 6 | US9771376, Example 6)
Affinity DataIC50:  40nMAssay Description:Inhibition of inactivated state of recombinant human NaV1.7 Y1537A mutant expressed in HEK293 cell membranes coexpressing Nav beta1 subunit assessed ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium channel protein type 9 subunit alpha(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM145227(US8952169, 6 | US9771376, Example 6)
Affinity DataIC50:  70nMAssay Description:Displacement of [3H]GX-545 from human Nav1.7 alpha subunit expressed in HEK293 cells co-expressing beta1 subunit by liquid scintillation counting ana...More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetSodium channel protein type 9 subunit alpha(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM145227(US8952169, 6 | US9771376, Example 6)
Affinity DataIC50:  70nMAssay 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
In DepthDetails ArticlePubMed
TargetSodium channel protein type 5 subunit alpha(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM145227(US8952169, 6 | US9771376, Example 6)
Affinity DataIC50:  1.07E+3nMAssay Description:Inhibition of Nav1.5 (unknown origin) by PatchXpress methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium channel protein type 9 subunit alpha(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM145227(US8952169, 6 | US9771376, Example 6)
Affinity DataIC50:  1.37E+3nMAssay Description:Inhibition of inactivated state of recombinant human NaV1.7 R1602A mutant expressed in HEK293 cell membranes coexpressing Nav beta1 subunit assessed ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium channel protein type 5 subunit alpha(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM145227(US8952169, 6 | US9771376, Example 6)
Affinity DataIC50:  1.90E+3nMAssay Description:Inhibition of full length human NaV1.5 expressed in HEK293 cells coexpressing Nav beta1 subunit assessed as decrease in sodium current amplitude by P...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium channel protein type 5 subunit alpha(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM145227(US8952169, 6 | US9771376, Example 6)
Affinity DataIC50:  1.90E+3nMT: 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 5 subunit alpha(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM145227(US8952169, 6 | US9771376, Example 6)
Affinity DataIC50:  1.90E+3nMAssay Description:Inhibition of human Nav1.5 alpha subunit expressed in HEK293 cells co-expressing beta1 subunit at -60 mV holding potential by whole-cell patch voltag...More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetSodium channel protein type 5 subunit alpha(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM145227(US8952169, 6 | US9771376, Example 6)
Affinity DataIC50:  1.91E+3nMAssay 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))
Pfizer

Curated by ChEMBL
LigandPNGBDBM145227(US8952169, 6 | US9771376, Example 6)
Affinity DataIC50:  8.87E+3nMAssay Description:Inhibition of inactivated state of recombinant human NaV1.7 R1605A mutant expressed in HEK293 cell membranes coexpressing Nav beta1 subunit assessed ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 1A2(Homo sapiens (Human))TBA
LigandPNGBDBM145227(US8952169, 6 | US9771376, Example 6)
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of CYP1A2 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetCytochrome P450 2C9(Homo sapiens (Human))TBA
LigandPNGBDBM145227(US8952169, 6 | US9771376, Example 6)
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of CYP2C9 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetCytochrome P450 2D6(Homo sapiens (Human))TBA
LigandPNGBDBM145227(US8952169, 6 | US9771376, Example 6)
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of CYP2D6 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetCytochrome P450 3A4(Homo sapiens (Human))TBA
LigandPNGBDBM145227(US8952169, 6 | US9771376, Example 6)
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of CYP3A4 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails PubMed
LigandPNGBDBM145227(US8952169, 6 | US9771376, Example 6)
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of hERGMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetCytochrome P450 2C19(Homo sapiens (Human))TBA
LigandPNGBDBM145227(US8952169, 6 | US9771376, Example 6)
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of CYP2C19 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetSodium channel protein type 9 subunit alpha(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM145227(US8952169, 6 | US9771376, Example 6)
Affinity DataIC50:  2.74E+4nMAssay Description:Inhibition of inactivated state of recombinant human NaV1.7 R1608A mutant expressed in HEK293 cell membranes coexpressing Nav beta1 subunit assessed ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed