Target family: GABA<sub>A</sub> receptors (type: lgic)
Target: GABA<sub>A</sub> receptor &alpha;4 subunit

Ligand: Zn2+ (Inorganic)
Interaction type: Allosteric modulator
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: tetrahydrodeoxycorticosterone (Metabolite)
Interaction type: Allosteric modulator
Action: Potentiation
Ligand approved: no
Primary target: no
Median affinity:  -

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

Ligand: [3H]Ro154513 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: [3H]muscimol (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: [3H]gabazine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: [3H]CGS8216 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Mixed
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:  -

Ligand: [18F]fluoroethylflumazenil (Synthetic organic)
Interaction type: Allosteric modulator
Action: None
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: Ro15-4513 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Full agonist
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: picrotoxin (Natural product)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -

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

Ligand: flumazenil (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: yes
Approval source: FDA (1991)
Primary target: no
Median affinity: 7.03000020980835 pKi
Reference (Journal): Four amino acid exchanges convert a diazepam-insensitive, inverse agonist-preferring GABAA receptor into a diazepam-preferring GABAA receptor.
Published in: J Med Chem

Ligand: cenobamate (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: yes
Approval source: FDA (2019), EMA (2021)
Primary target: no
Median affinity: 4.380000114440918 pEC50
Reference (Journal): Positive allosteric modulation of GABA<sub>A</sub> receptors by a novel antiepileptic drug cenobamate.
Published in: Eur J Pharmacol

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

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:  -