Target family: Voltage-gated potassium channels (K<sub>v</sub>) (type: vgic)
Target: K<SUB>v</SUB>11.1

Ligand: APETx-1 (Peptide)
Interaction type: Gating inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.5 pIC50
Reference (Journal): APETx1, a new toxin from the sea anemone Anthopleura elegantissima, blocks voltage-gated human ether-a-go-go-related gene potassium channels.
Published in: Mol Pharmacol

Ligand: APETx-1 (Peptide)
Interaction type: Gating inhibitor
Action: None
Ligand approved: no
Median affinity: 7.4 pKd
Reference (Journal): APETx1 from sea anemone Anthopleura elegantissima is a gating modifier peptide toxin of the human ether-a-go-go- related potassium channel.
Published in: Mol Pharmacol

Ligand: astemizole (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Primary target: no
Median affinity: 9 pIC50
Reference (Journal): Block of HERG potassium channels by the antihistamine astemizole and its metabolites desmethylastemizole and norastemizole.
Published in: J Cardiovasc Electrophysiol

Ligand: AZD3778 (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 4.800000190734863 pIC50
Reference (Journal): The discovery of CCR3/H1 dual antagonists with reduced hERG risk.
Published in: Bioorg Med Chem Lett

Ligand: BeKm-1 (Peptide)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 7.699999809265137 pKd
Reference (Journal): Species diversity and peptide toxins blocking selectivity of ether-a-go-go-related gene subfamily K+ channels in the central nervous system.
Published in: Mol Pharmacol

Ligand: BeKm-1 (Peptide)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 8.199999809265137 pKd
Reference (Journal): Unique interaction of scorpion toxins with the hERG channel.
Published in: J Mol Recognit

Ligand: cisapride (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (1993)
Primary target: no
Median affinity: 7.400000095367432 pIC50
Reference (Journal): A mechanism for the proarrhythmic effects of cisapride (Propulsid): high affinity blockade of the human cardiac potassium channel HERG.
Published in: FEBS Lett

Ligand: disopyramide (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1977)
Primary target: no
Median affinity: 4.039999961853027 pIC50
Reference (Journal): Prediction of hERG potassium channel affinity by traditional and hologram qSAR methods.
Published in: Bioorg Med Chem Lett

Ligand: dofetilide (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1999)
Primary target: yes
Median affinity: 8.1899995803833 pKi
Reference (Journal): Fluorescently labeled analogues of dofetilide as high-affinity fluorescence polarization ligands for the human ether-a-go-go-related gene (hERG) channel.
Published in: J Med Chem

Ligand: E4031 (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 7 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
Primary target: no
Median affinity: 8.100000381469727 pIC50
Reference (Journal): Properties of HERG channels stably expressed in HEK 293 cells studied at physiological temperature.
Published in: Biophys J

Ligand: ErgTx-1 (Peptide)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 8.199999809265137 pKd
Reference (Journal): Species diversity and peptide toxins blocking selectivity of ether-a-go-go-related gene subfamily K+ channels in the central nervous system.
Published in: Mol Pharmacol

Ligand: ErgTx-1 (Peptide)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pKd
Reference (Journal): Species diversity and peptide toxins blocking selectivity of ether-a-go-go-related gene subfamily K+ channels in the central nervous system.
Published in: Mol Pharmacol

Ligand: γ-KTx1.7 (Peptide)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 7.900000095367432 pKd
Reference (Journal): Two novel ergtoxins, blockers of K+-channels, purified from the Mexican scorpion Centruroides elegans elegans.
Published in: Neurochem Res

Ligand: ginsenoside Rg3 (Natural product)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 6.400000095367432 pEC50
Reference (Journal): Ginsenoside Rg(3) decelerates hERG K(+) channel deactivation through Ser631 residue interaction.
Published in: Eur J Pharmacol

Ligand: halofantrine (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1992)
Primary target: no
Median affinity: 7.400000095367432 pIC50
Reference (Journal): Candidate selection and preclinical evaluation of N-tert-butyl isoquine (GSK369796), an affordable and effective 4-aminoquinoline antimalarial for the 21st century.
Published in: J Med Chem

Ligand: ibutilide (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (1995)
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Structural determinants of HERG channel block by clofilium and ibutilide.
Published in: Mol Pharmacol

Ligand: ibutilide (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (1995)
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Prediction of hERG potassium channel affinity by traditional and hologram qSAR methods.
Published in: Bioorg Med Chem Lett

Ligand: ICA-105574 (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 6.300000190734863 pEC50
Reference (Journal): Pharmacological removal of human ether-à-go-go-related gene potassium channel inactivation by 3-nitro-N-(4-phenoxyphenyl) benzamide (ICA-105574).
Published in: Mol Pharmacol

Ligand: KB-130015 (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 4.900000095367432 pEC50
Reference (Journal): The amiodarone derivative KB130015 activates hERG1 potassium channels via a novel mechanism.
Published in: Eur J Pharmacol

Ligand: LUF7244 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity: 5.409999847412109 pIC50
Reference (Journal): Allosteric Modulation of Kv11.1 (hERG) Channels Protects Against Drug-Induced Ventricular Arrhythmias.
Published in: Circ Arrhythm Electrophysiol

Ligand: MK-7145 (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 4.659999847412109 pIC50
Reference (Journal): Discovery of MK-7145, an Oral Small Molecule ROMK Inhibitor for the Treatment of Hypertension and Heart Failure.
Published in: ACS Med Chem Lett

Ligand: nemiralisib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.5 pIC50
Reference (Journal): Optimization of Novel Indazoles as Highly Potent and Selective Inhibitors of Phosphoinositide 3-Kinase δ for the Treatment of Respiratory Disease.
Published in: J Med Chem

Ligand: NS1643 (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 5 pEC50
Reference (Journal): Mechanism of action of a novel human ether-a-go-go-related gene channel activator.
Published in: Mol Pharmacol

Ligand: NS1643 (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 5 pEC50
Reference (Journal): Activation of human ether-a-go-go-related gene potassium channels by the diphenylurea 1,3-bis-(2-hydroxy-5-trifluoromethyl-phenyl)-urea (NS1643).
Published in: Mol Pharmacol

Ligand: NS3623 (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 4.099999904632568 pEC50
Reference (Journal): Biophysical characterization of the new human ether-a-go-go-related gene channel opener NS3623 [N-(4-bromo-2-(1H-tetrazol-5-yl)-phenyl)-N'-(3'-trifluoromethylphenyl)urea].
Published in: Mol Pharmacol

Ligand: PD-118057 (Synthetic organic)
Interaction type: Activator
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Novel potent human ether-a-go-go-related gene (hERG) potassium channel enhancers and their in vitro antiarrhythmic activity.
Published in: Mol Pharmacol

Ligand: PD-307243 (Synthetic organic)
Interaction type: Activator
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): 2-[2-(3,4-dichloro-phenyl)-2,3-dihydro-1H-isoindol-5-ylamino]-nicotinic acid (PD-307243) causes instantaneous current through human ether-a-go-go-related gene potassium channels.
Published in: Mol Pharmacol

Ligand: PF-04885614 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.739999771118164 pIC50
Reference (Journal): Discovery and optimisation of potent and highly subtype selective Nav1.8 inhibitors with reduced cardiovascular liabilities
Published in: Med. Chem. Commun

Ligand: riluzole (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1995), EMA (1996)
Primary target: no
Median affinity: 4.300000190734863 pIC50
Reference (Journal): Naphtho[1,2-d]thiazol-2-ylamine (SKA-31), a new activator of KCa2 and KCa3.1 potassium channels, potentiates the endothelium-derived hyperpolarizing factor response and lowers blood pressure.
Published in: Mol Pharmacol

Ligand: rottlerin (Natural product)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 6.5 pEC50
Reference (Journal): Mallotoxin is a novel human ether-a-go-go-related gene (hERG) potassium channel activator.
Published in: J Pharmacol Exp Ther

Ligand: RPR260243 (Synthetic organic)
Interaction type: Activator
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Discovery of a small molecule activator of the human ether-a-go-go-related gene (HERG) cardiac K+ channel.
Published in: Mol Pharmacol

Ligand: terfenadine (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA
Primary target: no
Median affinity: 7.300000190734863 pIC50
Reference (Journal): A mechanism for the proarrhythmic effects of cisapride (Propulsid): high affinity blockade of the human cardiac potassium channel HERG.
Published in: FEBS Lett

Ligand: VU0405601 (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Identification and characterization of a compound that protects cardiac tissue from human Ether-à-go-go-related gene (hERG)-related drug-induced arrhythmias.
Published in: J Biol Chem

Ligand: zorifertinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 4.880000114440918 pIC50
Reference (Journal): Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor.
Published in: J Med Chem