Target family: Voltage-gated potassium channels (K<sub>v</sub>) (type: vgic)
Target: K<SUB>v</SUB>1.5

Ligand: bupivacaine (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (1972), EMA (2020)
Median affinity: 5.4 pKd
Reference (Journal): Molecular determinants of stereoselective bupivacaine block of hKv1.5 channels.
Published in: Circ Res

Ligand: clofilium (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 6.9 pIC50
Reference (Journal): Mechanism of clofilium block of the human Kv1.5 delayed rectifier potassium channel.
Published in: Mol Pharmacol

Ligand: diltiazem (Synthetic organic)
Interaction type: Channel blocker
Action: Pore blocker
Ligand approved: yes
Approval source: FDA (1982)
Primary target: no
Median affinity: 3.9000000953674316 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

Ligand: DPO-1 (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 7.300000190734863 pIC50
Reference (Journal): Discovery of triarylethanolamine inhibitors of the Kv1.5 potassium channel.
Published in: Bioorg Med Chem Lett

Ligand: dronedarone (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA and EMA (2009)
Primary target: no
Median affinity: 5.630000114440918 pIC50
Reference (Journal): Discovery of 1-aryloxyethyl piperazine derivatives as Kv1.5 potassium channel inhibitors (part I).
Published in: Eur J Med Chem

Ligand: fampridine (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (2010), EMA (2011)
Primary target: no
Median affinity: 4.300000190734863 pIC50
Reference (Journal): Identity of a novel delayed rectifier current from human heart with a cloned K+ channel current.
Published in: Circ Res

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: 3.5999999046325684 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

Ligand: flecainide (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (1985)
Median affinity: 4 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

Ligand: nifedipine (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (1981)
Median affinity: 4.1 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

Ligand: propafenone (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (1989)
Primary target: no
Median affinity: 4.400000095367432 pIC50
Reference (Journal): Effects of propafenone and 5-hydroxy-propafenone on hKv1.5 channels.
Published in: Br J Pharmacol

Ligand: quinidine (Natural product)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (1950)
Median affinity: 5.2 pKd
Reference (Journal): Time-, voltage-, and state-dependent block by quinidine of a cloned human cardiac potassium channel.
Published in: Mol Pharmacol

Ligand: resiniferatoxin (Natural product)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 4.6 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

Ligand: S9947 (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 6.4 pIC50
Reference (Journal): Electrophysiological and antiarrhythmic effects of the novel I(Kur) channel blockers, S9947 and S20951, on left vs. right pig atrium in vivo in comparison with the I(Kr) blockers dofetilide, azimilide, d,l-sotalol and ibutilide.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: S9947 (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 6.4 pIC50
Reference (Journal): Characterization of a novel Kv1.5 channel blocker in Xenopus oocytes, CHO cells, human and rat cardiomyocytes.
Published in: Naunyn Schmiedebergs Arch Pharmacol