Target family: Calcium- and sodium-activated potassium channels (K<sub>Ca</sub>, K<sub>Na</sub>) (type: vgic)
Target: K<sub>Ca</sub>3.1

Ligand: TRAM-34 (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity:  pKd
Reference (Journal): Blockade of the intermediate-conductance calcium-activated potassium channel as a new therapeutic strategy for restenosis.
Published in: Circulation

Ligand: TRAM-34 (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity:  pKd
Reference (Journal): Design of a potent and selective inhibitor of the intermediate-conductance Ca2+-activated K+ channel, IKCa1: a potential immunosuppressant.
Published in: Proc Natl Acad Sci USA

Ligand: SKA-31 (Synthetic organic)
Interaction type: Activator
Action: None
Ligand approved: no
Primary target: no
Median affinity: 6.599999904632568 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: SKA-121 (Synthetic organic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.960000038146973 pEC50
Reference (Journal): New positive Ca2+-activated K+ channel gating modulators with selectivity for KCa3.1.
Published in: Mol Pharmacol

Ligand: SKA-111 (Synthetic organic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.949999809265137 pEC50
Reference (Journal): New positive Ca2+-activated K+ channel gating modulators with selectivity for KCa3.1.
Published in: Mol Pharmacol

Ligand: senicapoc (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.960000038146973 pIC50
Reference (Journal): ICA-17043, a novel Gardos channel blocker, prevents sickled red blood cell dehydration in vitro and in vivo in SAD mice.
Published in: Blood

Ligand: riluzole (Synthetic organic)
Interaction type: Activator
Action: None
Ligand approved: yes
Approval source: FDA (1995), EMA (1996)
Primary target: no
Median affinity: 5.699999809265137 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: NS6180 (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9 pIC50
Reference (Journal): NS6180, a new K(Ca) 3.1 channel inhibitor prevents T-cell activation and inflammation in a rat model of inflammatory bowel disease.
Published in: Br J Pharmacol

Ligand: NS309 (Synthetic organic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8 pEC50
Reference (Journal): Small conductance calcium-activated potassium channels: from structure to function.
Published in: Prog Neurobiol

Ligand: NS309 (Synthetic organic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8 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: nitrendipine (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: yes
Primary target: no
Median affinity: 7.599999904632568 pIC50
Reference (Journal): Characterization of the cloned human intermediate-conductance Ca2+-activated K+ channel.
Published in: Am J Physiol

Ligand: nitrendipine (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: yes
Primary target: no
Median affinity: 6.099999904632568 pKd
Reference (Journal): Design of a potent and selective inhibitor of the intermediate-conductance Ca2+-activated K+ channel, IKCa1: a potential immunosuppressant.
Published in: Proc Natl Acad Sci USA

Ligand: maurotoxin (Peptide)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Median affinity: 9 pIC50
Reference (Journal): Maurotoxin: a potent inhibitor of intermediate conductance Ca2+-activated potassium channels.
Published in: Mol Pharmacol

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

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

Ligand: DC-EBIO (Synthetic organic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Median affinity: 6.1 pEC50
Reference (Journal): Benzimidazolone activators of chloride secretion: potential therapeutics for cystic fibrosis and chronic obstructive pulmonary disease.
Published in: J Pharmacol Exp Ther

Ligand: compound rac-16 [PMID: 15603962] (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): IKCa-channel blockers. Part 2: discovery of cyclohexadienes.
Published in: Bioorg Med Chem Lett

Ligand: compound rac-16 [PMID: 15603962] (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Selective intermediate-/small-conductance calcium-activated potassium channel (KCNN4) blockers are potent and effective therapeutics in experimental brain oedema and traumatic brain injury caused by acute subdural haematoma.
Published in: Eur J Neurosci

Ligand: clotrimazole (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1975)
Primary target: no
Median affinity:  pKd
Reference (Journal): Human calcium-activated potassium channel gene KCNN4 maps to chromosome 19q13.2 in the region deleted in diamond-blackfan anemia.
Published in: Genomics

Ligand: clotrimazole (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1975)
Primary target: no
Median affinity:  pKd
Reference (Journal): A human intermediate conductance calcium-activated potassium channel.
Published in: Proc Natl Acad Sci USA

Ligand: clotrimazole (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1975)
Primary target: no
Median affinity:  pKd
Reference (Journal): A novel gene, hKCa4, encodes the calcium-activated potassium channel in human T lymphocytes.
Published in: J Biol Chem

Ligand: clotrimazole (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1975)
Primary target: no
Median affinity:  pKd
Reference (Journal): Design of a potent and selective inhibitor of the intermediate-conductance Ca2+-activated K+ channel, IKCa1: a potential immunosuppressant.
Published in: Proc Natl Acad Sci USA

Ligand: chlorzoxazone (Synthetic organic)
Interaction type: Activator
Action: Agonist
Ligand approved: yes
Approval source: FDA (1958)
Primary target: no
Median affinity: 4 pEC50
Reference (Journal): Pharmacological activation of cloned intermediate- and small-conductance Ca(2+)-activated K(+) channels.
Published in: Am J Physiol, Cell Physiol

Ligand: charybdotoxin-GLU32 analog (Peptide)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.5 pKd
Reference (Journal): Structure-guided transformation of charybdotoxin yields an analog that selectively targets Ca(2+)-activated over voltage-gated K(+) channels.
Published in: J Biol Chem

Ligand: charybdotoxin (Peptide)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Characterization of the cloned human intermediate-conductance Ca2+-activated K+ channel.
Published in: Am J Physiol

Ligand: charybdotoxin (Peptide)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): hSK4, a member of a novel subfamily of calcium-activated potassium channels.
Published in: Proc Natl Acad Sci USA

Ligand: charybdotoxin (Peptide)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.5 pKd
Reference (Journal): Up-regulation of the IKCa1 potassium channel during T-cell activation. Molecular mechanism and functional consequences.
Published in: J Biol Chem

Ligand: Ca2+ (Inorganic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): hSK4, a member of a novel subfamily of calcium-activated potassium channels.
Published in: Proc Natl Acad Sci USA

Ligand: Ca2+ (Inorganic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Pharmacological activation of cloned intermediate- and small-conductance Ca(2+)-activated K(+) channels.
Published in: Am J Physiol, Cell Physiol

Ligand: Ca2+ (Inorganic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): A human intermediate conductance calcium-activated potassium channel.
Published in: Proc Natl Acad Sci USA

Ligand: Ca2+ (Inorganic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Calcium-activated potassium channels in resting and activated human T lymphocytes. Expression levels, calcium dependence, ion selectivity, and pharmacology.
Published in: J Gen Physiol

Ligand: Ca2+ (Inorganic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): A novel gene, hKCa4, encodes the calcium-activated potassium channel in human T lymphocytes.
Published in: J Biol Chem

Ligand: ASP-0819 (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 7.03000020980835 pEC50
Reference (Patent): Benzothiophene compound