dwb2023/gtopdb-target-family-interaction-detail huggingface dataset:
Target family: Voltage-gated potassium channels (K<sub>v</sub>) (type: vgic)
Target: K<SUB>v</SUB>4.1

Ligand: HmTx1 (Peptide)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 6.5 pIC50
Reference (Journal): Novel tarantula toxins for subtypes of voltage-dependent potassium channels in the Kv2 and Kv4 subfamilies.
Published in: Mol Pharmacol

Ligand: fampridine (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (2010), EMA (2011)
Primary target: yes
Median affinity: 2 pIC50
Reference (Journal): Gene structures and expression profiles of three human KCND (Kv4) potassium channels mediating A-type currents I(TO) and I(SA).
Published in: Genomics

Ligand: fampridine (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (2010), EMA (2011)
Median affinity: 2 pIC50
Reference (Journal): Elimination of fast inactivation in Kv4 A-type potassium channels by an auxiliary subunit domain.
Published in: Proc Natl Acad Sci USA
Target family: Voltage-gated potassium channels (K<sub>v</sub>) (type: vgic)
Target: K<SUB>v</SUB>3.4

Ligand: thiopental (Synthetic organic)
Interaction type: Gating inhibitor
Action: None
Ligand approved: yes
Approval source: FDA (approval date not specified)
Median affinity: 4 pIC50
Reference (Journal): Inhibitory effect of thiopental on ultra-rapid delayed rectifier K+ current in H9c2 cells.
Published in: J Pharmacol Sci

Ligand: tetraethylammonium (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 3.5 pIC50
Reference (Journal): Characterization of a Shaw-related potassium channel family in rat brain.
Published in: EMBO J

Ligand: tetraethylammonium (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 3.5 pIC50
Reference (Journal): Cloning and functional expression of a TEA-sensitive A-type potassium channel from rat brain.
Published in: FEBS Lett

Ligand: sea anemone toxin BDS-I (Peptide)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 7.300000190734863 pIC50
Reference (Journal): Sea anemone peptides with a specific blocking activity against the fast inactivating potassium channel Kv3.4.
Published in: J Biol Chem
Target family: Voltage-gated potassium channels (K<sub>v</sub>) (type: vgic)
Target: K<SUB>v</SUB>1.1

Ligand: resiniferatoxin (Natural product)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 5.099999904632568 pIC50
Reference (Journal): Pharmacological characterization of five cloned voltage-gated K+ channels, types Kv1.1, 1.2, 1.3, 1.5, and 3.1, stably expressed in mammalian cell lines.
Published in: Mol Pharmacol

Ligand: ShK Toxin (Peptide)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 10.800000190734863 pIC50
Reference (Journal): Pharmacological characterization of five cloned voltage-gated K+ channels, types Kv1.1, 1.2, 1.3, 1.5, and 3.1, stably expressed in mammalian cell lines.
Published in: Mol Pharmacol

Ligand: tetraethylammonium (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 3.5 pKd
Reference (Journal): Pharmacological characterization of five cloned voltage-gated K+ channels, types Kv1.1, 1.2, 1.3, 1.5, and 3.1, stably expressed in mammalian cell lines.
Published in: Mol Pharmacol
Target family: Voltage-gated potassium channels (K<sub>v</sub>) (type: vgic)
Target: K<SUB>v</SUB>11.1

Ligand: A-935142 (Synthetic organic)
Interaction type: Activator
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Electrophysiologic characterization of a novel hERG channel activator.
Published in: Biochem Pharmacol
Target family: Voltage-gated potassium channels (K<sub>v</sub>) (type: vgic)
Target: K<SUB>v</SUB>3.2

Ligand: ShK Toxin (Peptide)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 9.5 pIC50
Reference (Journal): Stichodactyla helianthus peptide, a pharmacological tool for studying Kv3.2 channels.
Published in: Mol Pharmacol

Ligand: tetraethylammonium (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 4.199999809265137 pIC50
Reference (Journal): Gating, modulation and subunit composition of voltage-gated K(+) channels in dendritic inhibitory interneurones of rat hippocampus.
Published in: J Physiol (Lond.)

Ligand: verapamil (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (1981)
Median affinity: 4.9 pEC50
Reference (Journal): Sensitivity of native and cloned hippocampal delayed-rectifier potassium channels to verapamil.
Published in: Neuropharmacology
Target family: Voltage-gated potassium channels (K<sub>v</sub>) (type: vgic)
Target: K<SUB>v</SUB>3.3

Ligand: fampridine (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (2010), EMA (2011)
Median affinity: 2.9 pIC50
Reference (Journal): Cloning of ShIII (Shaw-like) cDNAs encoding a novel high-voltage-activating, TEA-sensitive, type-A K+ channel.
Published in: Proc Biol Sci

Ligand: tetraethylammonium (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 3.9000000953674316 pIC50
Reference (Journal): Cloning of ShIII (Shaw-like) cDNAs encoding a novel high-voltage-activating, TEA-sensitive, type-A K+ channel.
Published in: Proc Biol Sci
Target family: Voltage-gated potassium channels (K<sub>v</sub>) (type: vgic)
Target: K<SUB>v</SUB>3.4

Ligand: DABCO (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 3.2 pIC50
Reference (Journal): 1,4-Diazabicyclo[2.2.2]octane derivatives: a novel class of voltage-gated potassium channel blockers.
Published in: Mol Pharmacol

Ligand: DABCO-C16 (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 6.2 pIC50
Reference (Journal): 1,4-Diazabicyclo[2.2.2]octane derivatives: a novel class of voltage-gated potassium channel blockers.
Published in: Mol Pharmacol
Target family: Voltage-gated potassium channels (K<sub>v</sub>) (type: vgic)
Target: K<SUB>v</SUB>11.2

Ligand: BeKm-1 (Peptide)
Interaction type: Gating inhibitor
Action: None
Ligand approved: no
Median affinity: 8.1 pKd
Reference (Journal): Identification of two nervous system-specific members of the erg potassium channel gene family.
Published in: J Neurosci

Ligand: E4031 (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 6.9 pKd
Reference (Journal): Identification of two nervous system-specific members of the erg potassium channel gene family.
Published in: J Neurosci

Ligand: ErgTx-1 (Peptide)
Interaction type: Gating inhibitor
Action: None
Ligand approved: no
Median affinity: 8.5 pKd
Reference (Journal): Identification of two nervous system-specific members of the erg potassium channel gene family.
Published in: J Neurosci

Ligand: ErgTx-1 (Peptide)
Interaction type: Gating inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.699999809265137 pKd
Reference (Journal): Incorporation of [18O]water into 4-hydroxybenzoic acid in the reaction of 4-chlorobenzoate dehalogenase from pseudomonas spec. CBS 3.
Published in: Biochem Biophys Res Commun

Ligand: γ-KTx1.7 (Peptide)
Interaction type: Gating inhibitor
Action: None
Ligand approved: no
Primary target: no
Median affinity: 8.800000190734863 pKd
Reference (Journal): Two novel ergtoxins, blockers of K+-channels, purified from the Mexican scorpion Centruroides elegans elegans.
Published in: Neurochem Res

Ligand: NS1643 (Synthetic organic)
Interaction type: Activator
Action: None
Ligand approved: no
Median affinity: 4.9 pEC50
Reference (Journal): Activation of ERG2 potassium channels by the diphenylurea NS1643.
Published in: Neuropharmacology
Target family: Voltage-gated potassium channels (K<sub>v</sub>) (type: vgic)
Target: K<SUB>v</SUB>11.3

Ligand: BeKm-1 (Peptide)
Interaction type: Channel blocker
Action: Pore blocker
Ligand approved: no
Primary target: no
Median affinity: 7.900000095367432 pKd
Reference (Journal): Toxins interacting with ether-à-go-go-related gene voltage-dependent potassium channels.
Published in: Toxicon

Ligand: E4031 (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 6.7 pKd
Reference (Journal): Identification of two nervous system-specific members of the erg potassium channel gene family.
Published in: J Neurosci

Ligand: ErgTx-1 (Peptide)
Interaction type: Channel blocker
Action: Pore blocker
Ligand approved: no
Primary target: no
Median affinity: 8.399999618530273 pKd
Reference (Journal): Toxins interacting with ether-à-go-go-related gene voltage-dependent potassium channels.
Published in: Toxicon

Ligand: NS1643 (Synthetic organic)
Interaction type: Activator
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Effects of the small molecule HERG activator NS1643 on Kv11.3 channels.
Published in: PLoS ONE
Target family: Voltage-gated potassium channels (K<sub>v</sub>) (type: vgic)
Target: K<SUB>v</SUB>12.1

Ligand: Ba2+ (Inorganic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 3.7 pIC50
Reference (Journal): Distribution and functional properties of human KCNH8 (Elk1) potassium channels.
Published in: Am J Physiol, Cell Physiol

Ligand: Cd2+ (Inorganic)
Interaction type: Gating inhibitor
Action: None
Primary target: no
Median affinity:  -
Reference (Journal): Divalent cations slow activation of EAG family K+ channels through direct binding to S4.
Published in: Biophys J

Ligand: Zn2+ (Inorganic)
Interaction type: Gating inhibitor
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Divalent cations slow activation of EAG family K+ channels through direct binding to S4.
Published in: Biophys J
Target family: Voltage-gated potassium channels (K<sub>v</sub>) (type: vgic)
Target: K<SUB>v</SUB>12.2

Ligand: Cs+ (Inorganic)
Interaction type: Channel blocker
Action: Pore blocker
Ligand approved: no
Primary target: no
Median affinity: 1.2000000476837158 pKd
Reference (Journal): The functional properties of the human ether-à-go-go-like (HELK2) K+ channel.
Published in: Eur J Neurosci

Ligand: CX4 (Synthetic organic)
Interaction type: Gating inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5 pIC50
Reference (Journal): Deletion of the potassium channel Kv12.2 causes hippocampal hyperexcitability and epilepsy.
Published in: Nat Neurosci
Target family: Voltage-gated potassium channels (K<sub>v</sub>) (type: vgic)
Target: K<SUB>v</SUB>1.4

Ligand: CP-339818 (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 6.5 pIC50
Reference (Journal): Novel nonpeptide agents potently block the C-type inactivated conformation of Kv1.3 and suppress T cell activation.
Published in: Mol Pharmacol

Ligand: fampridine (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (2010), EMA (2011)
Primary target: no
Median affinity: 1.899999976158142 pIC50
Reference (Journal): Molecular basis of functional diversity of voltage-gated potassium channels in mammalian brain.
Published in: EMBO J

Ligand: nicardipine (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (1988)
Median affinity: 6.1 pIC50
Reference (Journal): Dihydropyridine Ca2+ channel antagonists and agonists block Kv4.2, Kv4.3 and Kv1.4 K+ channels expressed in HEK293 cells.
Published in: Br J Pharmacol

Ligand: quinidine (Natural product)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (1950)
Median affinity: 3.7 pIC50
Reference (Journal): Antiarrhythmic and bradycardic drugs inhibit currents of cloned K+ channels, KV1.2 and KV1.4.
Published in: Eur J Pharmacol
Target family: Voltage-gated potassium channels (K<sub>v</sub>) (type: vgic)
Target: K<SUB>v</SUB>1.6

Ligand: α-dendrotoxin (Peptide)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 7.699999809265137 pIC50
Reference (Journal): Cloning and expression of a human voltage-gated potassium channel. A novel member of the RCK potassium channel family.
Published in: EMBO J

Ligand: charybdotoxin (Peptide)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 9 pIC50
Reference (Journal): Cloning and expression of a human voltage-gated potassium channel. A novel member of the RCK potassium channel family.
Published in: EMBO J

Ligand: conopeptide Y-PI1 (Peptide)
Interaction type: Channel blocker
Action: Pore blocker
Ligand approved: no
Primary target: no
Median affinity: 6.800000190734863 pIC50
Reference (Journal): Tyrosine-rich conopeptides affect voltage-gated K+ channels.
Published in: J Biol Chem

Ligand: hongotoxin-1 (Peptide)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 11 pKd
Reference (Journal): Subunit composition of brain voltage-gated potassium channels determined by hongotoxin-1, a novel peptide derived from Centruroides limbatus venom.
Published in: J Biol Chem

Ligand: mast cell degranulating peptide (Peptide)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 8 pIC50
Reference (Journal): Cloning and expression of a human voltage-gated potassium channel. A novel member of the RCK potassium channel family.
Published in: EMBO J

Ligand: ShK Toxin (Peptide)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 9.8 pIC50
Reference (Journal): ShK-Dap22, a potent Kv1.3-specific immunosuppressive polypeptide.
Published in: J Biol Chem

Ligand: [125I]α-DTX (Peptide)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 10.4 pKd
Reference (Journal): Characterization of a novel radiolabeled peptide selective for a subpopulation of voltage-gated potassium channels in mammalian brain.
Published in: J Biol Chem

Ligand: [125I]BgK (W5Y / Y26F) (Peptide)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 11.4 pKd
Reference (Journal): Characterization of a novel radiolabeled peptide selective for a subpopulation of voltage-gated potassium channels in mammalian brain.
Published in: J Biol Chem

Ligand: tetraethylammonium (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 2.200000047683716 pIC50
Reference (Journal): Cloning and expression of a human voltage-gated potassium channel. A novel member of the RCK potassium channel family.
Published in: EMBO J
Target family: Voltage-gated potassium channels (K<sub>v</sub>) (type: vgic)
Target: K<SUB>v</SUB>1.8

Ligand: Ba2+ (Inorganic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 2.3 pIC50
Reference (Journal): KCNA10: a novel ion channel functionally related to both voltage-gated potassium and CNG cation channels.
Published in: Am J Physiol Renal Physiol

Ligand: charybdotoxin (Peptide)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 7 pIC50
Reference (Journal): KCNA10: a novel ion channel functionally related to both voltage-gated potassium and CNG cation channels.
Published in: Am J Physiol Renal Physiol

Ligand: fampridine (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (2010), EMA (2011)
Primary target: yes
Median affinity: 2.799999952316284 pIC50
Reference (Journal): KCNA10: a novel ion channel functionally related to both voltage-gated potassium and CNG cation channels.
Published in: Am J Physiol Renal Physiol

Ligand: ketoconazole (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (1981), EMA (2014)
Median affinity: 6.3 pIC50
Reference (Journal): KCNA10: a novel ion channel functionally related to both voltage-gated potassium and CNG cation channels.
Published in: Am J Physiol Renal Physiol

Ligand: pimozide (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (1984)
Median affinity: 6.5 pIC50
Reference (Journal): KCNA10: a novel ion channel functionally related to both voltage-gated potassium and CNG cation channels.
Published in: Am J Physiol Renal Physiol

Ligand: tetraethylammonium (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 1.3 pIC50
Reference (Journal): KCNA10: a novel ion channel functionally related to both voltage-gated potassium and CNG cation channels.
Published in: Am J Physiol Renal Physiol

Ligand: verapamil (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (1981)
Median affinity: 4.3 pIC50
Reference (Journal): KCNA10: a novel ion channel functionally related to both voltage-gated potassium and CNG cation channels.
Published in: Am J Physiol Renal Physiol
Target family: Voltage-gated potassium channels (K<sub>v</sub>) (type: vgic)
Target: K<SUB>v</SUB>2.1

Ligand: 3-bicyclo[2.2.1]hept-2-yl-benzene-1,2-diol (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 6 pIC50
Reference (Journal): Novel neuroprotective K+ channel inhibitor identified by high-throughput screening in yeast.
Published in: Mol Pharmacol

Ligand: Ba2+ (Inorganic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 1.5 pKd
Reference (Journal): Barium blockade of a clonal potassium channel and its regulation by a critical pore residue.
Published in: Mol Pharmacol

Ligand: Ba2+ (Inorganic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 4.9 pKd
Reference (Journal): Barium blockade of a clonal potassium channel and its regulation by a critical pore residue.
Published in: Mol Pharmacol

Ligand: DABCO-C16 (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 5.7 pIC50
Reference (Journal): 1,4-Diazabicyclo[2.2.2]octane derivatives: a novel class of voltage-gated potassium channel blockers.
Published in: Mol Pharmacol

Ligand: fampridine (Synthetic organic)
Interaction type: Channel blocker
Action: Pore blocker
Ligand approved: yes
Approval source: FDA (2010), EMA (2011)
Primary target: no
Median affinity: 3.299999952316284 pIC50
Reference (Journal): Gating-dependent mechanism of 4-aminopyridine block in two related potassium channels.
Published in: J Gen Physiol

Ligand: GxTx-1E (Peptide)
Interaction type: Gating inhibitor
Action: None
Ligand approved: no
Primary target: no
Median affinity: 2 pIC50
Reference (Journal): Blockers of the delayed-rectifier potassium current in pancreatic beta-cells enhance glucose-dependent insulin secretion.
Published in: Diabetes
Target family: Voltage-gated proton channel  (H<sub>v</sub>1) (type: vgic)
Target: H<sub>v</sub>1

Ligand: Cd2+ (Inorganic)
Interaction type: Channel blocker
Action: None
Median affinity: 5 pIC50

Ligand: Zn2+ (Inorganic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity:  pIC50
Target family: Voltage-gated sodium channels (Na<sub>V</sub>) (type: vgic)
Target: Na<sub>v</sub>1.5

Ligand: GS-458967 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.889999866485596 pIC50
Reference (Journal): Discovery of triazolopyridine GS-458967, a late sodium current inhibitor (Late INai) of the cardiac NaV 1.5 channel with improved efficacy and potency relative to ranolazine.
Published in: Bioorg Med Chem Lett

Ligand: aconitine (Natural product)
Interaction type: Activator
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Comparison of aconitine-modified human heart (hH1) and rat skeletal (mu1) muscle Na+ channels: an important role for external Na+ ions.
Published in: J Physiol (Lond.)
Target family: Voltage-gated sodium channels (Na<sub>V</sub>) (type: vgic)
Target: Na<sub>v</sub>1.3

Ligand: AFT-II (Peptide)
Interaction type: Gating inhibitor
Action: Slows inactivation
Ligand approved: no
Primary target: no
Median affinity: 6.300000190734863 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: 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: batrachotoxin (Natural product)
Interaction type: Activator
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: Bc-III (Peptide)
Interaction type: Gating inhibitor
Action: Slows inactivation
Ligand approved: no
Primary target: no
Median affinity: 5.800000190734863 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: 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: lacosamide (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: yes
Approval source: EMA and FDA (2008)
Primary target: no
Median affinity: 3.4000000953674316 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: PF‐06526290 (Synthetic organic)
Interaction type: Gating inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.960000038146973 pEC50
Reference (Journal): PF-06526290 can both enhance and inhibit conduction through voltage-gated sodium channels.
Published in: Br J Pharmacol

Ligand: saxitoxin (Natural product)
Interaction type: Channel blocker
Action: Pore blocker
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): Cloning, distribution and functional analysis of the type III sodium channel from human brain.
Published in: Eur J Neurosci

Ligand: veratridine (Natural product)
Interaction type: Activator
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Target family: Voltage-gated sodium channels (Na<sub>V</sub>) (type: vgic)
Target: Na<sub>v</sub>1.9

Ligand: tetrodotoxin (Natural product)
Interaction type: Channel blocker
Action: Pore blocker
Ligand approved: no
Primary target: no
Median affinity: 4.400000095367432 pIC50
Reference (Journal): A novel persistent tetrodotoxin-resistant sodium current in SNS-null and wild-type small primary sensory neurons.
Published in: J Neurosci