Target family: Voltage-gated sodium channels (Na<sub>V</sub>) (type: vgic)
Target: Na<sub>v</sub>1.4

Ligand: AFT-II (Peptide)
Interaction type: Gating inhibitor
Action: Slows inactivation
Ligand approved: no
Primary target: no
Median affinity: 7.5 pEC50
Reference (Journal): Binding specificity of sea anemone toxins to Nav 1.1-1.6 sodium channels: unexpected contributions from differences in the IV/S3-S4 outer loop.
Published in: J Biol Chem

Ligand: AM-6120 (Peptide)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.980000019073486 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: ATX-II (Peptide)
Interaction type: Gating inhibitor
Action: Slows inactivation
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Binding specificity of sea anemone toxins to Nav 1.1-1.6 sodium channels: unexpected contributions from differences in the IV/S3-S4 outer loop.
Published in: J Biol Chem

Ligand: ATX-II (Peptide)
Interaction type: Gating inhibitor
Action: Slows inactivation
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Sea anemone toxin (ATX II) modulation of heart and skeletal muscle sodium channel alpha-subunits expressed in tsA201 cells.
Published in: J Membr Biol

Ligand: batrachotoxin (Natural product)
Interaction type: Activator
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Point mutations in segment I-S6 render voltage-gated Na+ channels resistant to batrachotoxin.
Published in: Proc Natl Acad Sci USA

Ligand: Bc-III (Peptide)
Interaction type: Gating inhibitor
Action: Slows inactivation
Ligand approved: no
Primary target: no
Median affinity: 6.099999904632568 pEC50
Reference (Journal): Binding specificity of sea anemone toxins to Nav 1.1-1.6 sodium channels: unexpected contributions from differences in the IV/S3-S4 outer loop.
Published in: J Biol Chem

Ligand: β-scorpion toxin TiTXγ (Peptide)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Median affinity:  -
Reference (Journal): Effects of Tityus serrulatus scorpion toxin gamma on voltage-gated Na+ channels.
Published in: Circ Res

Ligand: GNE-616 (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6 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: grayanotoxin III (Natural product)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Median affinity:  -
Reference (Journal): Novel site on sodium channel alpha-subunit responsible for the differential sensitivity of grayanotoxin in skeletal and cardiac muscle.
Published in: Mol Pharmacol

Ligand: lidocaine (Synthetic organic)
Interaction type: Channel blocker
Action: Pore blocker
Ligand approved: yes
Approval source: FDA (1948)
Primary target: no
Median affinity: 2.700000047683716 pIC50
Reference (Journal): Intrinsic lidocaine affinity for Na channels expressed in Xenopus oocytes depends on alpha (hH1 vs. rSkM1) and beta 1 subunits.
Published in: Cardiovasc Res

Ligand: mexiletine (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1985)
Primary target: yes
Median affinity: 3.4000000953674316 pIC50
Reference (Journal): Mexiletine block of wild-type and inactivation-deficient human skeletal muscle hNav1.4 Na+ channels.
Published in: J Physiol (Lond.)

Ligand: μ-conotoxin GIIIA (Peptide)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Distinction among neuronal subtypes of voltage-activated sodium channels by mu-conotoxin PIIIA.
Published in: J Neurosci

Ligand: μ-conotoxin GIIIA (Peptide)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Chimeric study of sodium channels from rat skeletal and cardiac muscle.
Published in: FEBS Lett

Ligand: μ-conotoxin GIIIA (Peptide)
Interaction type: Channel blocker
Action: Pore blocker
Ligand approved: no
Primary target: no
Median affinity: 5.900000095367432 pIC50
Reference (Journal): Functional expression and properties of the human skeletal muscle sodium channel.
Published in: Pflugers Arch

Ligand: μ-conotoxin PIIIA (Peptide)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Median affinity: 7.4 pIC50
Reference (Journal): Distinction among neuronal subtypes of voltage-activated sodium channels by mu-conotoxin PIIIA.
Published in: J Neurosci

Ligand: saxitoxin (Natural product)
Interaction type: Channel blocker
Action: Pore blocker
Ligand approved: no
Primary target: no
Median affinity: 8.399999618530273 pIC50
Reference (Journal): Specific neosaxitoxin interactions with the Na+ channel outer vestibule determined by mutant cycle analysis.
Published in: Biophys J

Ligand: tetrodotoxin (Natural product)
Interaction type: Channel blocker
Action: Pore blocker
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pIC50
Reference (Journal): Primary structure and functional expression of a mammalian skeletal muscle sodium channel.
Published in: Neuron

Ligand: tetrodotoxin (Natural product)
Interaction type: Channel blocker
Action: Pore blocker
Ligand approved: no
Primary target: no
Median affinity: 7.599999904632568 pIC50
Reference (Journal): Functional expression and properties of the human skeletal muscle sodium channel.
Published in: Pflugers Arch

Ligand: veratridine (Natural product)
Interaction type: Activator
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Point mutations in segment I-S6 render voltage-gated Na+ channels resistant to batrachotoxin.
Published in: Proc Natl Acad Sci USA