Target family: GABA<sub>A</sub> receptors (type: lgic)
Target: GABA<sub>A</sub> receptor &alpha;6 subunit

Ligand: 5α-pregnan-3α-ol-20-one (Metabolite)
Interaction type: Allosteric modulator
Action: Potentiation
Ligand approved: yes
Approval source: FDA (2019)
Primary target: no
Median affinity:  -

Ligand: amiloride (Synthetic organic)
Interaction type: Allosteric modulator
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1981)
Primary target: no
Median affinity:  -
Reference (Journal): International Union of Basic and Clinical Pharmacology. CVI: GABA<sub>A</sub> Receptor Subtype- and Function-selective Ligands: Key Issues in Translation to Humans.
Published in: Pharmacol Rev

Ligand: bicuculline (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: bretazenil (Synthetic organic)
Interaction type: Allosteric modulator
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): The point mutation gamma 2F77I changes the potency and efficacy of benzodiazepine site ligands in different GABAA receptor subtypes.
Published in: Eur J Pharmacol

Ligand: cenobamate (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: yes
Approval source: FDA (2019), EMA (2021)
Primary target: no
Median affinity: 4.239999771118164 pEC50
Reference (Journal): Positive allosteric modulation of GABA<sub>A</sub> receptors by a novel antiepileptic drug cenobamate.
Published in: Eur J Pharmacol

Ligand: CGS8216 (Synthetic organic)
Interaction type: Agonist
Action: Inverse agonist
Ligand approved: no
Primary target: no
Median affinity: 7.769999980926514 pKi

Ligand: flumazenil (Synthetic organic)
Interaction type: Allosteric modulator
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1991)
Primary target: no
Median affinity: 6.829999923706055 pKi
Reference (Journal): International Union of Basic and Clinical Pharmacology. CVI: GABA<sub>A</sub> Receptor Subtype- and Function-selective Ligands: Key Issues in Translation to Humans.
Published in: Pharmacol Rev

Ligand: furosemide (Synthetic organic)
Interaction type: Allosteric modulator
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1966)
Primary target: no
Median affinity:  -
Reference (Journal): International Union of Basic and Clinical Pharmacology. CVI: GABA<sub>A</sub> Receptor Subtype- and Function-selective Ligands: Key Issues in Translation to Humans.
Published in: Pharmacol Rev

Ligand: gabazine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: gaboxadol (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: isoguvacine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: isonipecotic acid (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: LAU159 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): &alpha; 6-Containing GABA<sub>A</sub> Receptors: Functional Roles and Therapeutic Potentials.
Published in: Pharmacol Rev

Ligand: LAU159 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): International Union of Basic and Clinical Pharmacology. CVI: GABA<sub>A</sub> Receptor Subtype- and Function-selective Ligands: Key Issues in Translation to Humans.
Published in: Pharmacol Rev

Ligand: LAU463 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): International Union of Basic and Clinical Pharmacology. CVI: GABA<sub>A</sub> Receptor Subtype- and Function-selective Ligands: Key Issues in Translation to Humans.
Published in: Pharmacol Rev

Ligand: LAU463 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): &alpha; 6-Containing GABA<sub>A</sub> Receptors: Functional Roles and Therapeutic Potentials.
Published in: Pharmacol Rev

Ligand: muscimol (Natural product)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: picrotoxin (Natural product)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: piperidine-4-sulphonic acid (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: PZ-II-029 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): International Union of Basic and Clinical Pharmacology. CVI: GABA<sub>A</sub> Receptor Subtype- and Function-selective Ligands: Key Issues in Translation to Humans.
Published in: Pharmacol Rev

Ligand: PZ-II-029 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): &alpha; 6-Containing GABA<sub>A</sub> Receptors: Functional Roles and Therapeutic Potentials.
Published in: Pharmacol Rev

Ligand: Ro15-4513 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: [11C]flumazenil (Synthetic organic)
Interaction type: Allosteric modulator
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: [18F]fluoroethylflumazenil (Synthetic organic)
Interaction type: Allosteric modulator
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: [35S]TBPS (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -