Target family: Voltage-gated potassium channels (K<sub>v</sub>) (type: vgic)
Target: K<SUB>v</SUB>10.1

Ligand: astemizole (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Median affinity: 6.7 pIC50
Reference (Journal): Mechanism of block of hEag1 K+ channels by imipramine and astemizole.
Published in: J Gen Physiol

Ligand: calmodulin (Peptide)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 7.2 pIC50
Reference (Journal): Elevation of intracellular calcium by muscarinic receptor activation induces a block of voltage-activated rat ether-à-go-go channels in a stably transfected cell line.
Published in: Proc Natl Acad Sci USA

Ligand: clofilium (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 6.6 pIC50
Reference (Journal): Inhibition of hEAG1 and hERG1 potassium channels by clofilium and its tertiary analogue LY97241.
Published in: Br J Pharmacol

Ligand: dofetilide (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (1999)
Median affinity: 7.5 pIC50
Reference (Journal): Different relevance of inactivation and F468 residue in the mechanisms of hEag1 channel blockage by astemizole, imipramine and dofetilide.
Published in: FEBS Lett

Ligand: E4031 (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 6.4 pIC50
Reference (Journal): Inhibition of hEAG1 and hERG1 potassium channels by clofilium and its tertiary analogue LY97241.
Published in: Br J Pharmacol

Ligand: haloperidol (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (1967)
Median affinity: 6.2 pIC50
Reference (Journal): Inhibition of hEAG1 and hERG1 potassium channels by clofilium and its tertiary analogue LY97241.
Published in: Br J Pharmacol

Ligand: ICA-105574 (Synthetic organic)
Interaction type: Gating inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.900000095367432 pIC50
Reference (Journal): ICA-105574 interacts with a common binding site to elicit opposite effects on inactivation gating of EAG and ERG potassium channels.
Published in: Mol Pharmacol

Ligand: imipramine (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (1959)
Median affinity: 5.7 pIC50
Reference (Journal): Mechanism of block of hEag1 K+ channels by imipramine and astemizole.
Published in: J Gen Physiol

Ligand: LY97241 (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 8.3 pIC50
Reference (Journal): Inhibition of hEAG1 and hERG1 potassium channels by clofilium and its tertiary analogue LY97241.
Published in: Br J Pharmacol

Ligand: MK-499 (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 6 pIC50
Reference (Journal): Different relevance of inactivation and F468 residue in the mechanisms of hEag1 channel blockage by astemizole, imipramine and dofetilide.
Published in: FEBS Lett

Ligand: MK-499 (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 6 pIC50
Reference (Journal): Molecular determinants for high-affinity block of human EAG potassium channels by antiarrhythmic agents.
Published in: Mol Pharmacol

Ligand: quinidine (Natural product)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (1950)
Median affinity: 5.8 pIC50
Reference (Journal): Functional distinction of human EAG1 and EAG2 potassium channels.
Published in: FEBS Lett

Ligand: terfenadine (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA
Median affinity: 7.8 pIC50
Reference (Journal): Molecular determinants for high-affinity block of human EAG potassium channels by antiarrhythmic agents.
Published in: Mol Pharmacol