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Report error Found 2794 Enz. Inhib. hit(s) with Target = 'Sodium channel protein type 8 subunit alpha'
TargetSodium channel protein type 8 subunit alpha(Human)
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM50505257(CHEMBL4471012)
Affinity DataKd:  620nMAssay Description:Binding affinity to human recombinant Nav1.6 by radioligand binding assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetSodium channel protein type 8 subunit alpha(Human)
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM76858(US9694002, 580 | US9546164, 580)
Affinity DataKd:  210nMAssay Description:Binding affinity to human recombinant Nav1.6 by radioligand binding assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetSodium channel protein type 8 subunit alpha(Human)
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM50521571(CHEMBL4464990)
Affinity DataKd:  29nMAssay Description:Inhibition of full length human Nav1.6 expressed in CHO cells at -60 mV holding potential by manual patch clamp electrophysiology methodMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetSodium channel protein type 8 subunit alpha(Human)
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM50558815(CHEMBL4742035)
Affinity DataEC50:  72nMAssay Description:Inhibition of human Nav1.6 expressed in HEK293 cells incubated for 30 mins by FLIPRTetra fluorescent membrane potential assayMore data for this Ligand-Target Pair
Ligand InfoKEGGSimilars
In DepthDetails Article
PubMed
TargetSodium channel protein type 8 subunit alpha(Human)
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM50558815(CHEMBL4742035)
Affinity DataEC50:  72.4nMAssay Description:Inhibition of human Nav1.6 expressed in HEK293 cells incubated for 30 mins by FLIPRTetra fluorescent membrane potential assayMore data for this Ligand-Target Pair
Ligand InfoKEGGSimilars
In DepthDetails Article
PubMed
TargetSodium channel protein type 8 subunit alpha(Human)
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM50558815(CHEMBL4742035)
Affinity DataEC50:  72nMAssay Description:Inhibition of human Nav1.6 expressed in HEK293 cells incubated for 30 mins by FLIPRTetra fluorescent membrane potential assayMore data for this Ligand-Target Pair
Ligand InfoKEGGSimilars
In DepthDetails Article
PubMed
TargetSodium channel protein type 8 subunit alpha(Human)
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM50558815(CHEMBL4742035)
Affinity DataEC50:  72.4nMAssay Description:Inhibition of human Nav1.6 expressed in HEK293 cells incubated for 30 mins by FLIPRTetra fluorescent membrane potential assayMore data for this Ligand-Target Pair
Ligand InfoKEGGSimilars
In DepthDetails Article
PubMed
TargetSodium channel protein type 8 subunit alpha(Human)
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM50558815(CHEMBL4742035)
Affinity DataEC50:  6.20nMAssay Description:Inhibition of human Nav1.6 expressed in HEK293 cells assessed as decrease in peak current at pulses to 0 mV by whole cell patch clamp assayMore data for this Ligand-Target Pair
Ligand InfoKEGGSimilars
In DepthDetails Article
PubMed
TargetSodium channel protein type 8 subunit alpha(Human)
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM50558815(CHEMBL4742035)
Affinity DataEC50:  6.30nMAssay Description:Inhibition of human Nav1.6 expressed in HEK293 cells assessed as decrease in peak current at pulses to 0 mV by whole cell patch clamp assayMore data for this Ligand-Target Pair
Ligand InfoKEGGSimilars
In DepthDetails Article
PubMed
TargetSodium channel protein type 8 subunit alpha(Human)
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM50554320(CHEMBL4745065)
Affinity DataKd:  9.01E+4nMAssay Description:Binding affinity to human recombinant Nav1.6 C-terminal domain expressed in Escherichia coli BL21 assessed as dissociation constant by SPR analysisMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetSodium channel protein type 8 subunit alpha(Human)
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM50554321(CHEMBL4792323)
Affinity DataKd:  6.73E+4nMAssay Description:Binding affinity to human recombinant Nav1.6 C-terminal domain expressed in Escherichia coli BL21 assessed as dissociation constant by SPR analysisMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetSodium channel protein type 8 subunit alpha(Human)
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM50554322(CHEMBL4787949)
Affinity DataKd: >2.00E+5nMAssay Description:Binding affinity to human recombinant Nav1.6 C-terminal domain expressed in Escherichia coli BL21 assessed as dissociation constant by SPR analysisMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetSodium channel protein type 8 subunit alpha(Human)
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM50554323(CHEMBL4778774)
Affinity DataKd: >2.00E+5nMAssay Description:Binding affinity to human recombinant Nav1.6 C-terminal domain expressed in Escherichia coli BL21 assessed as dissociation constant by SPR analysisMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetSodium channel protein type 8 subunit alpha(Human)
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM50554324(CHEMBL4784008)
Affinity DataKd: >2.00E+5nMAssay Description:Binding affinity to human recombinant Nav1.6 C-terminal domain expressed in Escherichia coli BL21 assessed as dissociation constant by SPR analysisMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetSodium channel protein type 8 subunit alpha(Human)
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM50554325(CHEMBL4762315)
Affinity DataKd: >2.00E+5nMAssay Description:Binding affinity to human recombinant Nav1.6 C-terminal domain expressed in Escherichia coli BL21 assessed as dissociation constant by SPR analysisMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetSodium channel protein type 8 subunit alpha(Human)
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM50554326(CHEMBL4758370)
Affinity DataKd:  1.64E+4nMAssay Description:Binding affinity to human recombinant Nav1.6 C-terminal domain expressed in Escherichia coli BL21 assessed as dissociation constant by SPR analysisMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetSodium channel protein type 8 subunit alpha(Human)
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM50554328(CHEMBL4746549)
Affinity DataKd: >2.00E+5nMAssay Description:Binding affinity to human recombinant Nav1.6 C-terminal domain expressed in Escherichia coli BL21 assessed as dissociation constant by SPR analysisMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetSodium channel protein type 8 subunit alpha(Mouse)
Uppsala University

Curated by ChEMBL
LigandPNGBDBM50582054(CHEMBL5091679)
Affinity DataEC50:  240nMAssay Description:Modulator activity at mouse Nav1.6 expressed in Xenopus laevis oocytes assessed as elicitation in sodium current measured after 1 to 4 days by two-el...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetSodium channel protein type 8 subunit alpha(Mouse)
Uppsala University

Curated by ChEMBL
LigandPNGBDBM50582055(CHEMBL5083412)
Affinity DataEC50:  1.36E+3nMAssay Description:Modulator activity at mouse Nav1.6 expressed in Xenopus laevis oocytes assessed as elicitation in sodium current measured after 1 to 4 days by two-el...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetSodium channel protein type 8 subunit alpha(Mouse)
Uppsala University

Curated by ChEMBL
LigandPNGBDBM50582056(CHEMBL5091623)
Affinity DataEC50:  93nMAssay Description:Modulator activity at mouse Nav1.6 expressed in Xenopus laevis oocytes assessed as elicitation in sodium current measured after 1 to 4 days by two-el...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetSodium channel protein type 8 subunit alpha(Mouse)
Uppsala University

Curated by ChEMBL
LigandPNGBDBM50582057(CHEMBL5077579)
Affinity DataEC50:  124nMAssay Description:Modulator activity at mouse Nav1.6 expressed in Xenopus laevis oocytes assessed as elicitation in sodium current measured after 1 to 4 days by two-el...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetSodium channel protein type 8 subunit alpha(Mouse)
Uppsala University

Curated by ChEMBL
LigandPNGBDBM50582058(CHEMBL5093878)
Affinity DataEC50:  67nMAssay Description:Modulator activity at mouse Nav1.6 expressed in Xenopus laevis oocytes assessed as elicitation in sodium current measured after 1 to 4 days by two-el...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetSodium channel protein type 8 subunit alpha(Mouse)
Uppsala University

Curated by ChEMBL
LigandPNGBDBM50582059(CHEMBL5082582)
Affinity DataEC50:  36nMAssay Description:Modulator activity at mouse Nav1.6 expressed in Xenopus laevis oocytes assessed as elicitation in sodium current measured after 1 to 4 days by two-el...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetSodium channel protein type 8 subunit alpha(Mouse)
Uppsala University

Curated by ChEMBL
LigandPNGBDBM50582060(CHEMBL5084333)
Affinity DataEC50:  148nMAssay Description:Modulator activity at mouse Nav1.6 expressed in Xenopus laevis oocytes assessed as elicitation in sodium current measured after 1 to 4 days by two-el...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetSodium channel protein type 8 subunit alpha(Human)
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM50240277(CHEMBL4061793)
Affinity DataIC50: 0.0600nMAssay Description:Inhibition of human Nav1.6 alpha expressed in HEK293 cells incubated for 5 mins with 6 consecutive train pulses to -10 mV at 0.1 Hz and holding poten...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetSodium channel protein type 8 subunit alpha(Human)
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM50240278(CHEMBL4062780)
Affinity DataIC50: 0.0900nMAssay Description:Inhibition of human Nav1.6 alpha expressed in HEK293 cells incubated for 5 mins with 6 consecutive train pulses to -10 mV at 0.1 Hz and holding poten...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetSodium channel protein type 8 subunit alpha(Human)
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM630994(US11802122, Example 73A | US11802122, Example 73B ...)
Affinity DataIC50: 0.200nMAssay Description:The following buffers were used for the Qube recordings: External buffer for NaV1.8 Qube recording: 150 NaCl, 2 CaCl2, 5 KCl, 1 Mg Cl2, 10 HEPES, 12 ...More data for this Ligand-Target Pair
In DepthDetails
US Patent

TargetSodium channel protein type 8 subunit alpha(Human)
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM630994(US11802122, Example 73A | US11802122, Example 73B ...)
Affinity DataIC50: 0.200nMAssay Description:The following buffers were used for the Qube recordings: External buffer for NaV1.8 Qube recording: 150 NaCl, 2 CaCl2, 5 KCl, 1 Mg Cl2, 10 HEPES, 12 ...More data for this Ligand-Target Pair
In DepthDetails
US Patent

TargetSodium channel protein type 8 subunit alpha(Human)
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM621932(US20230312528, Example 73A | (S)-N-((R or S)-(3- c...)
Affinity DataIC50: 0.200nMAssay Description:Compounds were tested on human NaV1.8 and NaV1.5 channels stably expressed in human embryo kidney (HEK) 293 cells. Sodium current measurements on Qub...More data for this Ligand-Target Pair
In DepthDetails
US Patent

TargetSodium channel protein type 8 subunit alpha(Human)
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM621933(US20230312528, Example 73B | (S)-N-((R or S)-(3- c...)
Affinity DataIC50: 0.200nMAssay Description:Compounds were tested on human NaV1.8 and NaV1.5 channels stably expressed in human embryo kidney (HEK) 293 cells. Sodium current measurements on Qub...More data for this Ligand-Target Pair
In DepthDetails
US Patent

TargetSodium channel protein type 8 subunit alpha(Human)
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM621910(US20230312528, Example 62A | US11802122, Example 6...)
Affinity DataIC50: 0.400nMAssay Description:The following buffers were used for the Qube recordings: External buffer for NaV1.8 Qube recording: 150 NaCl, 2 CaCl2, 5 KCl, 1 Mg Cl2, 10 HEPES, 12 ...More data for this Ligand-Target Pair
In DepthDetails
US Patent

TargetSodium channel protein type 8 subunit alpha(Human)
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM621911(US20230312528, Example 62B | (S)-N-((R or S)-(3- c...)
Affinity DataIC50: 0.400nMAssay Description:Compounds were tested on human NaV1.8 and NaV1.5 channels stably expressed in human embryo kidney (HEK) 293 cells. Sodium current measurements on Qub...More data for this Ligand-Target Pair
In DepthDetails
US Patent

TargetSodium channel protein type 8 subunit alpha(Human)
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM630957(US11802122, Example 17A | (S)-N-((R or S)-(4- chlo...)
Affinity DataIC50: 0.600nMAssay Description:The following buffers were used for the Qube recordings: External buffer for NaV1.8 Qube recording: 150 NaCl, 2 CaCl2, 5 KCl, 1 Mg Cl2, 10 HEPES, 12 ...More data for this Ligand-Target Pair
In DepthDetails
US Patent

TargetSodium channel protein type 8 subunit alpha(Human)
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM621824(US20230312528, Example 17A | (S)-N-((R or S)-(4- c...)
Affinity DataIC50: 0.600nMAssay Description:Compounds were tested on human NaV1.8 and NaV1.5 channels stably expressed in human embryo kidney (HEK) 293 cells. Sodium current measurements on Qub...More data for this Ligand-Target Pair
In DepthDetails
US Patent

TargetSodium channel protein type 8 subunit alpha(Human)
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM621909(US20230312528, Example 61 | US11802122, Example 61...)
Affinity DataIC50: 0.700nMAssay Description:The following buffers were used for the Qube recordings: External buffer for NaV1.8 Qube recording: 150 NaCl, 2 CaCl2, 5 KCl, 1 Mg Cl2, 10 HEPES, 12 ...More data for this Ligand-Target Pair
In DepthDetails
US Patent

TargetSodium channel protein type 8 subunit alpha(Human)
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM621909(US20230312528, Example 61 | US11802122, Example 61...)
Affinity DataIC50: 0.700nMAssay Description:Compounds were tested on human NaV1.8 and NaV1.5 channels stably expressed in human embryo kidney (HEK) 293 cells. Sodium current measurements on Qub...More data for this Ligand-Target Pair
In DepthDetails
US Patent

TargetSodium channel protein type 8 subunit alpha(Human)
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM50118514(US9481677, 38 | CHEMBL3617063)
Affinity DataIC50: 0.800nMAssay Description:Inhibition of full length human Nav1.6 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -35 mV by...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetSodium channel protein type 8 subunit alpha(Human)
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM374028(US10246453, Example 295 | (S)-4-((1-benzylpyrrolid...)
Affinity DataIC50: 1nMAssay Description:Patch voltage clamp electrophysiology allows for the direct measurement and quantification of block of voltage-gated sodium channels (Nay's), and...More data for this Ligand-Target Pair
In DepthDetails
US Patent

TargetSodium channel protein type 8 subunit alpha(Human)
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM374028(US10246453, Example 295 | (S)-4-((1-benzylpyrrolid...)
Affinity DataIC50: 1nMAssay 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 8 subunit alpha(Human)
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM374028(US10246453, Example 295 | (S)-4-((1-benzylpyrrolid...)
Affinity DataIC50: 1nMAssay Description:Patch voltage clamp electrophysiology allows for the direct measurement and quantification of block of voltage-gated sodium channels (Nay's), and...More data for this Ligand-Target Pair
In DepthDetails
US Patent

TargetSodium channel protein type 8 subunit alpha(Human)
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM526220(4-((2-(azetidin-1-ylmethyl)benzyl)amino)-3-chloro-...)
Affinity DataIC50: 1nMAssay 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
In DepthDetails
US Patent

TargetSodium channel protein type 8 subunit alpha(Human)
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM526223(4-((2-(azetidin-1-ylmethyl)benzyl)amino)-2,6-diflu...)
Affinity DataIC50: 1nMAssay 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
In DepthDetails
US Patent

TargetSodium channel protein type 8 subunit alpha(Human)
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM526223(4-((2-(azetidin-1-ylmethyl)benzyl)amino)-2,6-diflu...)
Affinity DataIC50: 1nMAssay 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
In DepthDetails
US Patent

TargetSodium channel protein type 8 subunit alpha(Human)
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM374028(US10246453, Example 295 | (S)-4-((1-benzylpyrrolid...)
Affinity DataIC50: 1nMAssay Description:Sodium currents were measured using the patch clamp technique in the whole-cell configuration using either a PatchXpress automated voltage clamp or m...More data for this Ligand-Target Pair
In DepthDetails
US Patent

TargetSodium channel protein type 8 subunit alpha(Human)
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM161329(US9163042, 1a | US9051270, 114 | US10087143, Compo...)
Affinity DataIC50: 1nMAssay Description:1) Pre-spotted compounds (in neat DMSO) into compound plates. Vehicle control (neat DMSO), the positive control (20 mM DMSO stock tetracaine, 125 ...More data for this Ligand-Target Pair
In DepthDetails
US Patent

TargetSodium channel protein type 8 subunit alpha(Human)
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM621746(US11802122, Example 7A | US20230312522, Compound 1...)
Affinity DataIC50: 1.10nMAssay Description:The following buffers were used for the Qube recordings: External buffer for NaV1.8 Qube recording: 150 NaCl, 2 CaCl2, 5 KCl, 1 Mg Cl2, 10 HEPES, 12 ...More data for this Ligand-Target Pair
In DepthDetails
US Patent

TargetSodium channel protein type 8 subunit alpha(Human)
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM630941(US11802122, Example 13A | (4S)-N-[((R or S)-5- chl...)
Affinity DataIC50: 1.10nMAssay Description:The following buffers were used for the Qube recordings: External buffer for NaV1.8 Qube recording: 150 NaCl, 2 CaCl2, 5 KCl, 1 Mg Cl2, 10 HEPES, 12 ...More data for this Ligand-Target Pair
In DepthDetails
US Patent

TargetSodium channel protein type 8 subunit alpha(Human)
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM630953(US11802122, Example 16A | US11802122, Example 16B ...)
Affinity DataIC50: 1.10nMAssay Description:The following buffers were used for the Qube recordings: External buffer for NaV1.8 Qube recording: 150 NaCl, 2 CaCl2, 5 KCl, 1 Mg Cl2, 10 HEPES, 12 ...More data for this Ligand-Target Pair
In DepthDetails
US Patent

TargetSodium channel protein type 8 subunit alpha(Human)
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM190233(US9174999, Table 1, Compound 1)
Affinity DataIC50: 1.10nMAssay Description:Inhibition of human Nav1.6 expressed in HEK293 cells by electrophysiology assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetSodium channel protein type 8 subunit alpha(Human)
Siteone Therapeutics

Curated by ChEMBL
LigandPNGBDBM621868(US20230312528, Example 38 | US11802122, Example 38...)
Affinity DataIC50: 1.10nMAssay Description:The following buffers were used for the Qube recordings: External buffer for NaV1.8 Qube recording: 150 NaCl, 2 CaCl2, 5 KCl, 1 Mg Cl2, 10 HEPES, 12 ...More data for this Ligand-Target Pair
In DepthDetails
US Patent

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