Target family: Voltage-gated potassium channels (K<sub>v</sub>) (type: vgic)
Target: K<SUB>v</SUB>4.3

Ligand: sibutramine (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (1997)
Median affinity: 4.7 pIC50
Reference (Journal): Open channel block of A-type, kv4.3, and delayed rectifier K+ channels, Kv1.3 and Kv3.1, by sibutramine.
Published in: J Pharmacol Exp Ther

Ligand: riluzole (Synthetic organic)
Interaction type: Gating inhibitor
Action: None
Ligand approved: yes
Approval source: FDA (1995), EMA (1996)
Median affinity: 3.9 pIC50
Reference (Journal): Interaction of riluzole with the closed inactivated state of Kv4.3 channels.
Published in: J Pharmacol Exp Ther

Ligand: phrixotoxin 2 (Peptide)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 7 pIC50
Reference (Journal): W-7 modulates Kv4.3: pore block and Ca2+-calmodulin inhibition.
Published in: Am J Physiol Heart Circ Physiol

Ligand: phrixotoxin 2 (Peptide)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 7 pIC50
Reference (Journal): Pharmacological and molecular evidence for the involvement of Kv4.3 in ultra-fast activating K+ currents in murine portal vein myocytes.
Published in: Br J Pharmacol

Ligand: phrixotoxin 2 (Peptide)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Nicotine is a potent blocker of the cardiac A-type K(+) channels. Effects on cloned Kv4.3 channels and native transient outward current.
Published in: Circulation

Ligand: phrixotoxin 1 (Peptide)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Nicotine is a potent blocker of the cardiac A-type K(+) channels. Effects on cloned Kv4.3 channels and native transient outward current.
Published in: Circulation

Ligand: nicotine (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (1984)
Median affinity: 7.4 pIC50
Reference (Journal): Nicotine is a potent blocker of the cardiac A-type K(+) channels. Effects on cloned Kv4.3 channels and native transient outward current.
Published in: Circulation

Ligand: fampridine (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (2010), EMA (2011)
Median affinity: 2.4 pIC50
Reference (Journal): Pharmacological and molecular evidence for the involvement of Kv4.3 in ultra-fast activating K+ currents in murine portal vein myocytes.
Published in: Br J Pharmacol

Ligand: bupivacaine (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (1972), EMA (2020)
Median affinity: 4 pIC50
Reference (Journal): W-7 modulates Kv4.3: pore block and Ca2+-calmodulin inhibition.
Published in: Am J Physiol Heart Circ Physiol

Ligand: bupivacaine (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (1972), EMA (2020)
Median affinity: 4.5 pIC50
Reference (Journal): Pharmacological and molecular evidence for the involvement of Kv4.3 in ultra-fast activating K+ currents in murine portal vein myocytes.
Published in: Br J Pharmacol