Target family: Voltage-gated potassium channels (K<sub>v</sub>) (type: vgic)
Target: K<SUB>v</SUB>7.2

Ligand: flupirtine (Synthetic organic)
Interaction type: Activator
Action: None
Ligand approved: no
Median affinity: 5 pEC50
Reference (Journal): M channels containing KCNQ2 subunits modulate norepinephrine, aspartate, and GABA release from hippocampal nerve terminals.
Published in: J Neurosci

Ligand: ICA-27243 (Synthetic organic)
Interaction type: Activator
Action: None
Ligand approved: no
Primary target: no
Median affinity: 6.300000190734863 pEC50
Reference (Journal): The KCNQ2/3 selective channel opener ICA-27243 binds to a novel voltage-sensor domain site.
Published in: Neurosci Lett

Ligand: L735821 (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 5.8 pIC50
Reference (Journal): The KCNQ2 potassium channel: splice variants, functional and developmental expression. Brain localization and comparison with KCNQ3.
Published in: FEBS Lett

Ligand: linopirdine (Synthetic organic)
Interaction type: Inhibitor
Action: None
Ligand approved: no
Primary target: no
Median affinity: 5.300000190734863 pIC50
Reference (Journal): KCNQ2 and KCNQ3 potassium channel subunits: molecular correlates of the M-channel.
Published in: Science

Ligand: PIP2 (Metabolite)
Interaction type: Activator
Action: None
Ligand approved: no
Median affinity: 3.7 pEC50
Reference (Journal): Regulation of Kv7 (KCNQ) K+ channel open probability by phosphatidylinositol 4,5-bisphosphate.
Published in: J Neurosci

Ligand: QO-58 (Synthetic organic)
Interaction type: Activator
Action: None
Ligand approved: no
Primary target: no
Median affinity: 6.300000190734863 pEC50
Reference (Journal): Modulation of K(v)7 potassium channels by a novel opener pyrazolo[1,5-a]pyrimidin-7(4H)-one compound QO-58.
Published in: Br J Pharmacol

Ligand: retigabine (Synthetic organic)
Interaction type: Allosteric modulator
Action: Activation
Ligand approved: yes
Approval source: FDA and EMA (2011)
Primary target: yes
Median affinity: 5.599999904632568 pEC50
Reference (Journal): Activation of expressed KCNQ potassium currents and native neuronal M-type potassium currents by the anti-convulsant drug retigabine.
Published in: J Neurosci

Ligand: retigabine (Synthetic organic)
Interaction type: Allosteric modulator
Action: Activation
Ligand approved: yes
Approval source: FDA and EMA (2011)
Primary target: yes
Median affinity: 5.599999904632568 pEC50
Reference (Journal): Molecular basis for ligand activation of the human KCNQ2 channel.
Published in: Cell Res

Ligand: (S)-N-[1-(3-morpholin-4-yl-phenyl)-ethyl]-3-phenyl-acrylamide (Synthetic organic)
Interaction type: Activator
Action: None
Ligand approved: no
Median affinity: 5.5 pEC50
Reference (Journal): (S)-N-[1-(3-morpholin-4-ylphenyl)ethyl]- 3-phenylacrylamide: an orally bioavailable KCNQ2 opener with significant activity in a cortical spreading depression model of migraine.
Published in: J Med Chem

Ligand: (S)-N-[1-(3-morpholin-4-yl-phenyl)-ethyl]-3-phenyl-acrylamide (Synthetic organic)
Interaction type: Activator
Action: None
Ligand approved: no
Median affinity: 5.5 pEC50
Reference (Journal): The acrylamide (S)-1 differentially affects Kv7 (KCNQ) potassium channels.
Published in: Neuropharmacology

Ligand: tetraethylammonium (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Retigabine, a novel anti-convulsant, enhances activation of KCNQ2/Q3 potassium channels.
Published in: Mol Pharmacol

Ligand: tetraethylammonium (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Differential tetraethylammonium sensitivity of KCNQ1-4 potassium channels.
Published in: Br J Pharmacol

Ligand: XE991 (Synthetic organic)
Interaction type: Inhibitor
Action: None
Ligand approved: no
Primary target: no
Median affinity: 6.150000095367432 pIC50
Reference (Journal): KCNQ2 and KCNQ3 potassium channel subunits: molecular correlates of the M-channel.
Published in: Science

Ligand: zinc pyrithione (Synthetic organic)
Interaction type: Activator
Action: None
Ligand approved: no
Median affinity: 5.8 pEC50
Reference (Journal): Zinc pyrithione-mediated activation of voltage-gated KCNQ potassium channels rescues epileptogenic mutants.
Published in: Nat Chem Biol

Ligand: ztz240 (Synthetic organic)
Interaction type: Activator
Action: None
Ligand approved: no
Primary target: no
Median affinity: 6.699999809265137 pEC50
Reference (Journal): Isoform-specific prolongation of Kv7 (KCNQ) potassium channel opening mediated by new molecular determinants for drug-channel interactions.
Published in: J Biol Chem