Target family: Calcium- and sodium-activated potassium channels (K<sub>Ca</sub>, K<sub>Na</sub>) (type: vgic)
Target: K<sub>Ca</sub>2.2

Ligand: zoxazolamine (Synthetic organic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 3.200000047683716 pEC50
Reference (Journal): Modulation of recombinant small-conductance Ca(2+)-activated K(+) channels by the muscle relaxant chlorzoxazone and structurally related compounds.
Published in: J Pharmacol Exp Ther

Ligand: zoxazolamine (Synthetic organic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 3.200000047683716 pEC50
Reference (Journal): Pharmacological activation of cloned intermediate- and small-conductance Ca(2+)-activated K(+) channels.
Published in: Am J Physiol, Cell Physiol

Ligand: UCL1848 (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.600000381469727 pIC50
Reference (Journal): Calcium-activated potassium channels sustain calcium signaling in T lymphocytes. Selective blockers and manipulated channel expression levels.
Published in: J Biol Chem

Ligand: UCL1848 (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): The SK3 subunit of small conductance Ca2+-activated K+ channels interacts with both SK1 and SK2 subunits in a heterologous expression system.
Published in: J Biol Chem

Ligand: UCL1684 (Synthetic organic)
Interaction type: Inhibitor
Action: None
Ligand approved: no
Primary target: no
Median affinity: 9.600000381469727 pIC50
Reference (Journal): Small conductance calcium-activated potassium channels: from structure to function.
Published in: Prog Neurobiol

Ligand: UCL1684 (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.399999618530273 pIC50
Reference (Journal): Pharmacological characterization of small-conductance Ca(2+)-activated K(+) channels stably expressed in HEK 293 cells.
Published in: Br J Pharmacol

Ligand: UCL1684 (Synthetic organic)
Interaction type: Inhibitor
Action: None
Ligand approved: no
Primary target: no
Median affinity: 9.600000381469727 pIC50
Reference (Journal): Calcium-activated potassium channels sustain calcium signaling in T lymphocytes. Selective blockers and manipulated channel expression levels.
Published in: J Biol Chem

Ligand: tubocurarine (Natural product)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1945)
Primary target: no
Median affinity:  pIC50
Reference (Journal): Pharmacological characterization of small-conductance Ca(2+)-activated K(+) channels stably expressed in HEK 293 cells.
Published in: Br J Pharmacol

Ligand: tubocurarine (Natural product)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1945)
Primary target: no
Median affinity:  pIC50
Reference (Journal): Small-conductance, calcium-activated potassium channels from mammalian brain.
Published in: Science

Ligand: tubocurarine (Natural product)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1945)
Primary target: no
Median affinity: 5.699999809265137 pIC50
Reference (Journal): SK2 encodes the apamin-sensitive Ca(2+)-activated K(+) channels in the human leukemic T cell line, Jurkat.
Published in: FEBS Lett

Ligand: tubocurarine (Natural product)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1945)
Primary target: no
Median affinity:  pIC50
Reference (Journal): Determinants of apamin and d-tubocurarine block in SK potassium channels.
Published in: J Biol Chem

Ligand: tetraethylammonium (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 2.700000047683716 pIC50
Reference (Journal): Small conductance calcium-activated potassium channels: from structure to function.
Published in: Prog Neurobiol

Ligand: tamapin (Peptide)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 10.600000381469727 pIC50
Reference (Journal): Tamapin, a venom peptide from the Indian red scorpion (Mesobuthus tamulus) that targets small conductance Ca2+-activated K+ channels and afterhyperpolarization currents in central neurons.
Published in: J Biol Chem

Ligand: SKA-31 (Synthetic organic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.699999809265137 pEC50
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: riluzole (Synthetic organic)
Interaction type: Activator
Action: Agonist
Ligand approved: yes
Approval source: FDA (1995), EMA (1996)
Primary target: no
Median affinity: 4.889999866485596 pEC50
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: RA-2 (Synthetic organic)
Interaction type: Gating inhibitor
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.699999809265137 pIC50
Reference (Journal): A novel pan-negative-gating modulator of KCa2/3 channels, fluoro-di-benzoate, RA-2, inhibits endothelium-derived hyperpolarization-type relaxation in coronary artery and produces bradycardia in vivo.
Published in: Mol Pharmacol

Ligand: P05 (Peptide)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.699999809265137 pIC50
Reference (Journal): Design and characterization of a highly selective peptide inhibitor of the small conductance calcium-activated K+ channel, SkCa2.
Published in: J Biol Chem

Ligand: NS8593 (Synthetic organic)
Interaction type: Gating inhibitor
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.199999809265137 pIC50
Reference (Journal): Inhibitory gating modulation of small conductance Ca2+-activated K+ channels by the synthetic compound (R)-N-(benzimidazol-2-yl)-1,2,3,4-tetrahydro-1-naphtylamine (NS8593) reduces afterhyperpolarizing current in hippocampal CA1 neurons.
Published in: Mol Pharmacol

Ligand: NS309 (Synthetic organic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.199999809265137 pEC50
Reference (Journal): Specific enhancement of SK channel activity selectively potentiates the afterhyperpolarizing current I(AHP) and modulates the firing properties of hippocampal pyramidal neurons.
Published in: J Biol Chem

Ligand: NS309 (Synthetic organic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.199999809265137 pEC50
Reference (Journal): Activation of human IK and SK Ca2+ -activated K+ channels by NS309 (6,7-dichloro-1H-indole-2,3-dione 3-oxime).
Published in: Biochim Biophys Acta

Ligand: NS309 (Synthetic organic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.199999809265137 pEC50
Reference (Journal): Small conductance calcium-activated potassium channels: from structure to function.
Published in: Prog Neurobiol

Ligand: NS13001 (Synthetic organic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.739999771118164 pEC50
Reference (Journal): Selective positive modulator of calcium-activated potassium channels exerts beneficial effects in a mouse model of spinocerebellar ataxia type 2.
Published in: Chem Biol

Ligand: leiurotoxin I (Peptide)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): SK2 encodes the apamin-sensitive Ca(2+)-activated K(+) channels in the human leukemic T cell line, Jurkat.
Published in: FEBS Lett

Ligand: leiurotoxin I (Peptide)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Design and characterization of a highly selective peptide inhibitor of the small conductance calcium-activated K+ channel, SkCa2.
Published in: J Biol Chem

Ligand: leiurotoxin I (Peptide)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.5 pIC50
Reference (Journal): Pharmacological characterization of small-conductance Ca(2+)-activated K(+) channels stably expressed in HEK 293 cells.
Published in: Br J Pharmacol

Ligand: Lei-Dab7 (Peptide)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pIC50
Reference (Journal): Design and characterization of a highly selective peptide inhibitor of the small conductance calcium-activated K+ channel, SkCa2.
Published in: J Biol Chem

Ligand: EBIO (Synthetic organic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 3 pEC50
Reference (Journal): Modulation of recombinant small-conductance Ca(2+)-activated K(+) channels by the muscle relaxant chlorzoxazone and structurally related compounds.
Published in: J Pharmacol Exp Ther

Ligand: EBIO (Synthetic organic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 3 pEC50
Reference (Journal): Control of electrical activity in central neurons by modulating the gating of small conductance Ca2+-activated K+ channels.
Published in: J Biol Chem

Ligand: EBIO (Synthetic organic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 3.299999952316284 pEC50
Reference (Journal): Small conductance calcium-activated potassium channels: from structure to function.
Published in: Prog Neurobiol

Ligand: EBIO (Synthetic organic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 3.299999952316284 pEC50
Reference (Journal): Specific enhancement of SK channel activity selectively potentiates the afterhyperpolarizing current I(AHP) and modulates the firing properties of hippocampal pyramidal neurons.
Published in: J Biol Chem

Ligand: dequalinium (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Block of rat brain recombinant SK channels by tricyclic antidepressants and related compounds.
Published in: Eur J Pharmacol

Ligand: dequalinium (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Pharmacological characterization of small-conductance Ca(2+)-activated K(+) channels stably expressed in HEK 293 cells.
Published in: Br J Pharmacol

Ligand: DC-EBIO (Synthetic organic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 4.599999904632568 pEC50
Reference (Journal): Specific enhancement of SK channel activity selectively potentiates the afterhyperpolarizing current I(AHP) and modulates the firing properties of hippocampal pyramidal neurons.
Published in: J Biol Chem

Ligand: CyPPA (Synthetic organic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 4.900000095367432 pEC50
Reference (Journal): Selective positive modulation of the SK3 and SK2 subtypes of small conductance Ca2+-activated K+ channels.
Published in: Br J Pharmacol

Ligand: chlorzoxazone (Synthetic organic)
Interaction type: Activator
Action: None
Ligand approved: yes
Approval source: FDA (1958)
Primary target: no
Median affinity:  pEC50
Reference (Journal): Modulation of recombinant small-conductance Ca(2+)-activated K(+) channels by the muscle relaxant chlorzoxazone and structurally related compounds.
Published in: J Pharmacol Exp Ther