Target family: GABA<sub>A</sub> receptors (type: lgic)
Target: GABA<sub>A</sub> receptor &alpha;5 subunit

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: None
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: RY024 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Inverse 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: RO4938581 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Inverse 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: Ro19-4603 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Inverse agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: Ro15-4513 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Inverse 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: ONO-8590580 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity: 8.100000381469727 pKi
Reference (Journal): ONO-8590580, a Novel GABA<sub>A</sub><i>α</i>5 Negative Allosteric Modulator Enhances Long-Term Potentiation and Improves Cognitive Deficits in Preclinical Models.
Published in: J Pharmacol Exp Ther

Ligand: ocinaplon (Synthetic organic)
Interaction type: Allosteric modulator
Action: Partial agonist
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: MRK016 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Inverse 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: L838417 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Partial 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: L655708 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Inverse 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: isonipecotic acid (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: 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: flunitrazepam (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: yes
Primary target: yes
Median affinity: 8.260000228881836 pKi
Reference (Journal): Cloning of cDNAs encoding the human gamma-aminobutyric acid type A receptor alpha 6 subunit and characterization of the pharmacology of alpha 6-containing receptors.
Published in: Mol Pharmacol

Ligand: flumazenil (Synthetic organic)
Interaction type: Allosteric modulator
Action: None
Ligand approved: yes
Approval source: FDA (1991)
Primary target: yes
Median affinity: 9.220000267028809 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: DMCM (Synthetic organic)
Interaction type: Allosteric modulator
Action: Inverse 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: compound 20 [PMID: 35584373] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity: 8.390000343322754 pKd
Reference (Journal): Multiparameter Optimization of Naphthyridine Derivatives as Selective α5-GABA<sub>A</sub> Receptor Negative Allosteric Modulators.
Published in: J Med Chem

Ligand: CGS8216 (Synthetic organic)
Interaction type: Agonist
Action: Inverse agonist
Ligand approved: no
Primary target: no
Median affinity: 9.600000381469727 pKi
Reference (Journal): Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach.
Published in: J Med Chem

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

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

Ligand: basmisanil (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity: 8.329999923706055 pKi
Reference (Patent): Isoxazolo-pyridine derivatives

Ligand: alprazolam (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: yes
Approval source: FDA (1981)
Primary target: no
Median affinity: 8 pEC50
Reference (Journal): Synthesis and biological evaluation of 7,8,9,10-tetrahydroimidazo[1,2-c]pyrido[3,4-e]pyrimdin-5(6H)-ones as functionally selective ligands of the benzodiazepine receptor site on the GABA(A) receptor.
Published in: J Med Chem

Ligand: α5IA (Synthetic organic)
Interaction type: Allosteric modulator
Action: Inverse 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: α3IA (Synthetic organic)
Interaction type: Allosteric modulator
Action: Inverse 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: 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:  -