Target family: Voltage-gated sodium channels (Na<sub>V</sub>) (type: vgic)
Target: Na<sub>v</sub>1.7

Ligand: XEN907 (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.5 pIC50
Reference (Journal): Discovery of XEN907, a spirooxindole blocker of NaV1.7 for the treatment of pain.
Published in: Bioorg Med Chem Lett

Ligand: vixotrigine (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.210000038146973 pIC50
Reference (Journal): Characterization of Vixotrigine, a Broad-Spectrum Voltage-Gated Sodium Channel Blocker.
Published in: Mol Pharmacol

Ligand: veratridine (Natural product)
Interaction type: Activator
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: tetrodotoxin (Natural product)
Interaction type: Channel blocker
Action: Pore blocker
Ligand approved: no
Primary target: no
Median affinity: 8.399999618530273 pIC50
Reference (Journal): A novel tetrodotoxin-sensitive, voltage-gated sodium channel expressed in rat and human dorsal root ganglia.
Published in: J Biol Chem

Ligand: tetrodotoxin (Natural product)
Interaction type: Channel blocker
Action: Pore blocker
Ligand approved: no
Primary target: no
Median affinity: 7.599999904632568 pIC50
Reference (Journal): Structure and functional expression of a new member of the tetrodotoxin-sensitive voltage-activated sodium channel family from human neuroendocrine cells.
Published in: EMBO J

Ligand: saxitoxin (Natural product)
Interaction type: Channel blocker
Action: Pore blocker
Ligand approved: no
Primary target: no
Median affinity: 6.199999809265137 pIC50
Reference (Journal): Marked difference in saxitoxin and tetrodotoxin affinity for the human nociceptive voltage-gated sodium channel (Nav1.7) [corrected].
Published in: Proc Natl Acad Sci USA

Ligand: pyrrolopyrimidine 48 [PMID: 22318156] (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7 pIC50
Reference (Journal): Discovery and hit-to-lead optimization of pyrrolopyrimidines as potent, state-dependent Na(v)1.7 antagonists.
Published in: Bioorg Med Chem Lett

Ligand: PF‐06526290 (Synthetic organic)
Interaction type: Gating inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.569999694824219 pEC50
Reference (Journal): PF-06526290 can both enhance and inhibit conduction through voltage-gated sodium channels.
Published in: Br J Pharmacol

Ligand: PF-05089771 (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Lidocaine Binding Enhances Inhibition of Nav1.7 Channels by the Sulfonamide PF-05089771.
Published in: Mol Pharmacol

Ligand: N-Me-aminopyrimidinone 9 (Synthetic organic)
Interaction type: Gating inhibitor
Action: Inhibition
Ligand approved: no
Median affinity: 7.1 pIC50
Reference (Journal): Discovery and optimization of aminopyrimidinones as potent and state-dependent Nav1.7 antagonists.
Published in: Bioorg Med Chem Lett

Ligand: lidocaine (Synthetic organic)
Interaction type: Channel blocker
Action: Pore blocker
Ligand approved: yes
Approval source: FDA (1948)
Primary target: no
Median affinity: 3.299999952316284 pIC50
Reference (Journal): Differential modulation of Nav1.7 and Nav1.8 peripheral nerve sodium channels by the local anesthetic lidocaine.
Published in: Br J Pharmacol

Ligand: lacosamide (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: yes
Approval source: EMA and FDA (2008)
Primary target: yes
Median affinity: 3.700000047683716 pIC50
Reference (Journal): Differential block of sensory neuronal voltage-gated sodium channels by lacosamide [(2R)-2-(acetylamino)-N-benzyl-3-methoxypropanamide], lidocaine, and carbamazepine.
Published in: J Pharmacol Exp Ther

Ligand: GNE-616 (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.480000019073486 pKd
Reference (Journal): Structure- and Ligand-Based Discovery of Chromane Arylsulfonamide Na<sub>v</sub>1.7 Inhibitors for the Treatment of Chronic Pain.
Published in: J Med Chem

Ligand: GNE-616 (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.100000381469727 pKi
Reference (Journal): Structure- and Ligand-Based Discovery of Chromane Arylsulfonamide Na<sub>v</sub>1.7 Inhibitors for the Treatment of Chronic Pain.
Published in: J Med Chem

Ligand: GNE-616 (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.420000076293945 pKd
Reference (Journal): Structure- and Ligand-Based Discovery of Chromane Arylsulfonamide Na<sub>v</sub>1.7 Inhibitors for the Treatment of Chronic Pain.
Published in: J Med Chem

Ligand: GNE-131 (Synthetic organic)
Interaction type: Inhibitor
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 8 pIC50
Reference (Journal): Design of Conformationally Constrained Acyl Sulfonamide Isosteres: Identification of N-([1,2,4]Triazolo[4,3- a]pyridin-3-yl)methane-sulfonamides as Potent and Selective hNa<sub>V</sub>1.7 Inhibitors for the Treatment of Pain.
Published in: J Med Chem

Ligand: GNE-131 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.520000457763672 pIC50
Reference (Journal): Design of Conformationally Constrained Acyl Sulfonamide Isosteres: Identification of N-([1,2,4]Triazolo[4,3- a]pyridin-3-yl)methane-sulfonamides as Potent and Selective hNa<sub>V</sub>1.7 Inhibitors for the Treatment of Pain.
Published in: J Med Chem

Ligand: funapide (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.269999980926514 pIC50
Reference (Journal): Challenges and Opportunities for Therapeutics Targeting the Voltage-Gated Sodium Channel Isoform Na<sub>V</sub>1.7.
Published in: J Med Chem

Ligand: DS-1971a (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.579999923706055 pIC50
Reference (Journal): Discovery of DS-1971a, a Potent, Selective Na<sub>V</sub>1.7 Inhibitor.
Published in: J Med Chem

Ligand: DS-1971a (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.610000133514404 pIC50
Reference (Journal): Discovery of DS-1971a, a Potent, Selective Na<sub>V</sub>1.7 Inhibitor.
Published in: J Med Chem

Ligand: Cd2+ (Inorganic)
Interaction type: Channel blocker
Action: Pore blocker
Primary target: no
Median affinity: 3 pIC50
Reference (Journal): Structure and functional expression of a new member of the tetrodotoxin-sensitive voltage-activated sodium channel family from human neuroendocrine cells.
Published in: EMBO J

Ligand: batrachotoxin (Natural product)
Interaction type: Activator
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: AM-6120 (Peptide)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.100000381469727 pIC50
Reference (Journal): Discovery of Tarantula Venom-Derived Na<sub>V</sub>1.7-Inhibitory JzTx-V Peptide 5-Br-Trp24 Analogue AM-6120 with Systemic Block of Histamine-Induced Pruritis.
Published in: J Med Chem

Ligand: AM-6120 (Peptide)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.270000457763672 pIC50
Reference (Journal): Discovery of Tarantula Venom-Derived Na<sub>V</sub>1.7-Inhibitory JzTx-V Peptide 5-Br-Trp24 Analogue AM-6120 with Systemic Block of Histamine-Induced Pruritis.
Published in: J Med Chem

Ligand: ABBV-318 (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.550000190734863 pIC50
Reference (Journal): Discovery of (R)-(3-fluoropyrrolidin-1-yl)(6-((5-(trifluoromethyl)pyridin-2-yl)oxy)quinolin-2-yl)methanone (ABBV-318) and analogs as small molecule Na<sub>v</sub>1.7/ Nav1.8 blockers for the treatment of pain.
Published in: Bioorg Med Chem