Target family: GABA<sub>A</sub> receptors (type: lgic)
Target: GABA<sub>A</sub> receptor &alpha;1 subunit

Ligand: zolpidem (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: yes
Approval source: FDA (1992)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Expression and pharmacology of human GABAA receptors containing gamma 3 subunits.
Published in: Eur J Pharmacol

Ligand: zolpidem (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: yes
Approval source: FDA (1992)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Affinity of various ligands for GABAA receptors containing alpha 4 beta 3 gamma 2, alpha 4 gamma 2, or alpha 1 beta 3 gamma 2 subunits.
Published in: Eur J Pharmacol

Ligand: zolpidem (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: yes
Approval source: FDA (1992)
Primary target: yes
Median affinity:  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: Zn2+ (Inorganic)
Interaction type: Allosteric modulator
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: ZK93426 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: ZK93423 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 9 pKi
Reference (Journal): Synthesis and evaluation of analogues of the partial agonist 6-(propyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (6-PBC) and the full agonist 6-(benzyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (Zk 93423) at wild type and recombinant GABAA receptors.
Published in: J Med Chem

Ligand: triazolam (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: yes
Approval source: FDA (1982)
Primary target: yes
Median affinity: 9 pKd
Reference (Journal): Selective influence on contextual memory: physiochemical properties associated with selectivity of benzodiazepine ligands at GABAA receptors containing the alpha5 subunit.
Published in: J Med Chem

Ligand: triazolam (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: yes
Approval source: FDA (1982)
Primary target: yes
Median affinity: 9.100000381469727 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: TPA023 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: TP003 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Antagonist
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]zolpidem (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
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: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -

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

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: yes
Median affinity:  -

Ligand: ocinaplon (Synthetic organic)
Interaction type: Allosteric modulator
Action: Full 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:  -

Ligand: L838417 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Antagonist
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: 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: indiplon (Synthetic organic)
Interaction type: Allosteric modulator
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: ganaxolone (Synthetic organic)
Interaction type: Allosteric modulator
Action: Potentiation
Ligand approved: yes
Approval source: FDA (2022)
Primary target: no
Median affinity: 6.590000152587891 pEC50
Reference (Journal): Synthesis and in vitro activity of 3 beta-substituted-3 alpha-hydroxypregnan-20-ones: allosteric modulators of the GABAA receptor.
Published in: J Med Chem

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: 8.279999732971191 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: Antagonist
Ligand approved: yes
Approval source: FDA (1991)
Primary target: yes
Median affinity: 9.100000381469727 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: diazepam (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: yes
Approval source: FDA (1986)
Primary target: yes
Median affinity: 7.789999961853027 pKi
Reference (Journal): Type I and type II GABAA-benzodiazepine receptors produced in transfected cells.
Published in: Science

Ligand: clonazepam (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: yes
Approval source: FDA (1975)
Primary target: yes
Median affinity: 8.899999618530273 pKi
Reference (Journal): Type I and type II GABAA-benzodiazepine receptors produced in transfected cells.
Published in: Science

Ligand: CGS8216 (Synthetic organic)
Interaction type: Agonist
Action: Inverse agonist
Ligand approved: no
Primary target: no
Median affinity: 10.300000190734863 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: alprazolam (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: yes
Approval source: FDA (1981)
Primary target: no
Median affinity: 7.429999828338623 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:  -