DGIdb - GABRA3 Gene Record

GABRA3 2556 Druggable Genome

Alternate Names:

2556
GAMMA-AMINOBUTYRIC ACID TYPE A RECEPTOR ALPHA3 SUBUNIT
GABRA3
305660
4077
ENSG00000011677
OTTHUMG00000024183
P34903
GBRA3_HUMAN
Gamma-aminobutyric acid receptor subunit alpha-3
GABA(A) receptor subunit alpha-3
GAMMA-AMINOBUTYRIC-ACID RECEPTOR ALPHA-3 SUBUNIT PRECURSOR (GABA(A) RECEPTOR). [SOURCE:UNIPROT/SWISSPROT;ACC:P34903]
GABA(A) receptor alpha-3
T62292
gamma-aminobutyric acid type A receptor subunit alpha3

Gene Info:

Target Class	Receptors
Target Subclass	TC:1.A.9
Transmembrane Helix Count	4
Target Subclass	Ligand_gated_ion_channels
Target Subclass	Channels
Target Main Class	Receptors
Target Subclass	cys-loop
Interpro Acc	IPR006201
Interpro Name	Neurotransmitter-gated ion-channel ligand-binding
Interpro Short Name	Neur_channel
Interpro Short Name	Neur_chan_lig-bd
Uniprot Status	Swiss-Prot
Interpro Acc	IPR006202
Human Readable Name	ION CHANNEL
Uniprot Evidence	2: Evidence at transcript level
Human Readable Name	DRUGGABLE GENOME
Interpro Type	Domain
Interpro Type	Family
Interpro Name	Neurotransmitter-gated ion-channel
Gene Biotype	PROTEIN_CODING

(6 More Sources)

Gene Categories: Category Details

ION CHANNEL
DRUGGABLE GENOME

Publications:

Rho et al., 1997, Barbiturate-like actions of the propanediol dicarbamates felbamate and meprobamate., J. Pharmacol. Exp. Ther.
Gonzalez et al., 2009, Carisoprodol-mediated modulation of GABAA receptors: in vitro and in vivo studies., J. Pharmacol. Exp. Ther.
Mehta et al., 1999, An update on GABAA receptors., Brain Res. Brain Res. Rev.
Yamakura et al., 2001, Anesthetics and ion channels: molecular models and sites of action., Annu. Rev. Pharmacol. Toxicol.
Iorio et al., 1984, Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites., Life Sci.
Wamsley et al., 1985, Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain., Pharmacol. Biochem. Behav.
Nutt et al., 2010, Searching for perfect sleep: the continuing evolution of GABAA receptor modulators as hypnotics., J. Psychopharmacol. (Oxford)
Hanson et al., 2008, Structural requirements for eszopiclone and zolpidem binding to the gamma-aminobutyric acid type-A (GABAA) receptor are different., J. Med. Chem.
Mandrioli et al., 2008, Benzodiazepine metabolism: an analytical perspective., Curr. Drug Metab.
Walash et al., 1994, A selective fluorimetric method for the determination of some 1,4-benzodiazepine drugs containing a hydroxyl group at C-3., J Pharm Biomed Anal
Möhler et al., 2002, A new benzodiazepine pharmacology., J. Pharmacol. Exp. Ther.
Riss et al., 2008, Benzodiazepines in epilepsy: pharmacology and pharmacokinetics., Acta Neurol. Scand.
Smith et al., 2001, Effect of alpha subunit on allosteric modulation of ion channel function in stably expressed human recombinant gamma-aminobutyric acid(A) receptors determined using (36)Cl ion flux., Mol. Pharmacol.
Pritchett et al., 1990, Gamma-aminobutyric acidA receptor alpha 5-subunit creates novel type II benzodiazepine receptor pharmacology., J. Neurochem.
Crestani F et al., 2000, Mechanism of action of the hypnotic zolpidem in vivo., Br J Pharmacol
Vlainić et al., 2009, Effects of acute and repeated zolpidem treatment on pentylenetetrazole-induced seizure threshold and on locomotor activity: comparison with diazepam., Neuropharmacology
Tan KR et al., 2011, Hooked on benzodiazepines: GABAA receptor subtypes and addiction., Trends Neurosci
Derry et al., 2004, Identification of a residue in the gamma-aminobutyric acid type A receptor alpha subunit that differentially affects diazepam-sensitive and -insensitive benzodiazepine site binding., J. Neurochem.
Schove et al., 1994, Molecular determinants of recognition and activation at the cerebellar benzodiazepine receptor site., Bioorg. Med. Chem.
You et al., 2010, Benzodiazepine modulation of the rat GABAA receptor α4β3γ2L subtype expressed in Xenopus oocytes., Neuropharmacology
Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
Billard et al., 1988, Selective affinity of the benzodiazepines quazepam and 2-oxo-quazepam for BZ1 binding site and demonstration of 3H-2-oxo-quazepam as a BZ1 selective radioligand., Life Sci.
Meldrum et al., 1986, Benzodiazepine receptors and their relationship to the treatment of epilepsy., Epilepsia
Zhou D et al., 2012, A clinical study to assess CYP1A2 and CYP3A4 induction by AZD7325, a selective GABA(A) receptor modulator - an in vitro and in vivo comparison., Br J Clin Pharmacol
Chen X et al., 2014, The central nervous system effects of the partial GABA-Aα2,3 -selective receptor modulator AZD7325 in comparison with lorazepam in healthy males., Br J Clin Pharmacol
Nakatsuka et al., 1985, Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity., Life Sci.
Braestrup et al., 1978, Pharmacological characterization of benzodiazepine receptors in the brain., Eur. J. Pharmacol.
Miller et al., 1987, Benzodiazepine receptor binding of triazolobenzodiazepines in vivo: increased receptor number with low-dose alprazolam., J. Neurochem.
Husain SS et al., 2006, Synthesis of trifluoromethylaryl diazirine and benzophenone derivatives of etomidate that are potent general anesthetics and effective photolabels for probing sites on ligand-gated ion channels., J Med Chem
Lahti et al., 1983, Pharmacological profile of the antidepressant adinazolam, a triazolobenzodiazepine., Neuropharmacology
Sethy et al., 1984, Determination of biological activity of adinazolam and its metabolites., J. Pharm. Pharmacol.
Ramerstorfer et al., 2010, The point mutation gamma 2F77I changes the potency and efficacy of benzodiazepine site ligands in different GABAA receptor subtypes., Eur. J. Pharmacol.
Giersch et al., 2010, Atypical behavioural effects of lorazepam: clues to the design of novel therapies?, Pharmacol. Ther.
Olsen et al., 2011, GABA(A) receptors as molecular targets of general anesthetics: identification of binding sites provides clues to allosteric modulation., Can J Anaesth

AZD7325 GABRA3

Interaction Score: 1.22

Interaction Types & Directionality:

positive modulator (activating)

allosteric modulator

Interaction Info:

Direct Interaction yes

Mechanism of Interaction GABA receptor alpha-3 subunit positive allosteric modulator

PMIDs:
22122233 24802722

Sources:
ChemblInteractions
CHEMBL381625 GABRA3

Interaction Score: 0.81

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
ZOPICLONE GABRA3

Interaction Score: 0.81

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
20303942 19942638 18973287

Sources:
TdgClinicalTrial TEND
ZOLPIDEM GABRA3

Interaction Score: 0.63

Interaction Types & Directionality:

agonist (activating)

allosteric modulator

Interaction Info:

Trial Name OX-22, zolpidem sublingual,Edluar, Sublinox

Novel drug target Established target

PMIDs:
11306694 2157817 11090095 19345234 21353710

Sources:
TdgClinicalTrial TEND
FLUNITRAZEPAM GABRA3

Interaction Score: 0.51

Interaction Types & Directionality:

allosteric modulator

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
20638393 17016423 17139284

Sources:
TdgClinicalTrial TEND
AZD6280 GABRA3

Interaction Score: 0.41

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA receptor alpha-3 subunit positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
MEPHOBARBITAL GABRA3

Interaction Score: 0.34

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
21194017 10209232 11264449

Sources:
TdgClinicalTrial TEND
BUTETHAL GABRA3

Interaction Score: 0.33

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
10209232 11264449

Sources:
TdgClinicalTrial TEND
SECOBARBITAL GABRA3

Interaction Score: 0.33

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
10209232 11264449

Sources:
TdgClinicalTrial TEND
HEXOBARBITAL GABRA3

Interaction Score: 0.33

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
10209232 11264449

Sources:
TdgClinicalTrial TEND
THIOPENTAL GABRA3

Interaction Score: 0.3

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
10209232 11264449

Sources:
TdgClinicalTrial TEND
MEPROBAMATE GABRA3

Interaction Score: 0.23

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel agonist

Direct Interaction yes

Trial Name -

PMIDs:
9067327 19244096

Sources:
TdgClinicalTrial ChemblInteractions TEND
TALBUTAL GABRA3

Interaction Score: 0.2

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Trial Name -

PMIDs:
10209232 11264449

Sources:
TdgClinicalTrial ChemblInteractions TEND
BUTALBITAL GABRA3

Interaction Score: 0.2

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

Novel drug target Established target

Trial Name -

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

PMIDs:
10209232 11264449

Sources:
TdgClinicalTrial ChemblInteractions TEND
QUAZEPAM GABRA3

Interaction Score: 0.2

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Trial Name -

PMIDs:
2892106 3017690

Sources:
TdgClinicalTrial ChemblInteractions TEND
METHARBITAL GABRA3

Interaction Score: 0.2

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

Novel drug target Established target

Trial Name -

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

PMIDs:
10209232 11264449

Sources:
TdgClinicalTrial ChemblInteractions TEND
HALAZEPAM GABRA3

Interaction Score: 0.2

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

Direct Interaction yes

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Trial Name -

PMIDs:
6738302 2867566

Sources:
TdgClinicalTrial ChemblInteractions TEND
PENTOBARBITAL GABRA3

Interaction Score: 0.2

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

Direct Interaction yes

PMIDs:
10209232 11264449

Sources:
TdgClinicalTrial ChemblInteractions TEND
ADINAZOLAM GABRA3

Interaction Score: 0.19

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
6320036 6148400

Sources:
TdgClinicalTrial TEND
TEMAZEPAM GABRA3

Interaction Score: 0.18

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Trial Name -

PMIDs:
20138190 18384456

Sources:
TdgClinicalTrial ChemblInteractions TEND
ESZOPICLONE GABRA3

Interaction Score: 0.18

Interaction Types & Directionality:

positive modulator (activating)

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name Lunesta

Direct Interaction yes

PMIDs:
19942638 18973287

Sources:
TdgClinicalTrial ChemblInteractions
ESTAZOLAM GABRA3

Interaction Score: 0.18

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Trial Name -

PMIDs:
639854 2889803

Sources:
TdgClinicalTrial ChemblInteractions TEND
FLUMAZENIL GABRA3

Interaction Score: 0.17

Interaction Types & Directionality:

allosteric modulator

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel allosteric antagonist

Direct Interaction yes

Trial Name -

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions TEND TTD
BUTABARBITAL GABRA3

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial TEND
DIAZEPAM GABRA3

Interaction Score: 0.16

Interaction Types & Directionality:

positive modulator (activating)

allosteric modulator

potentiator

Interaction Info:

Trial Name diazepam rectal gel

Novel drug target Established target

Trial Name NRL-01

PMIDs:
15009644 11752090 18384456

Sources:
TdgClinicalTrial ChemblInteractions TEND
OXAZEPAM GABRA3

Interaction Score: 0.16

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

Direct Interaction yes

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Trial Name -

PMIDs:
11752090 18384456

Sources:
TdgClinicalTrial ChemblInteractions TEND
NITRAZEPAM GABRA3

Interaction Score: 0.15

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11752090 18384456

Sources:
TdgClinicalTrial TEND
FLURAZEPAM GABRA3

Interaction Score: 0.15

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11752090 18384456

Sources:
TdgClinicalTrial TEND
PRAZEPAM GABRA3

Interaction Score: 0.15

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

Novel drug target Established target

Trial Name -

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

PMIDs:
7773620

Sources:
TdgClinicalTrial ChemblInteractions TEND
ETOMIDATE GABRA3

Interaction Score: 0.14

Interaction Types & Directionality:

n/a

Interaction Info:

Direct Interaction yes

Mechanism of Interaction GABA-A receptor; anion channel positive modulator

PMIDs:
16884293

Sources:
DTC ChemblInteractions
FLUDIAZEPAM GABRA3

Interaction Score: 0.14

Interaction Types & Directionality:

potentiator

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
2857046

Sources:
TdgClinicalTrial TEND
CINOLAZEPAM GABRA3

Interaction Score: 0.14

Interaction Types & Directionality:

potentiator

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
7849137

Sources:
TdgClinicalTrial TEND
CLOTIAZEPAM GABRA3

Interaction Score: 0.14

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
18855614

Sources:
TdgClinicalTrial TEND
TRIAZOLAM GABRA3

Interaction Score: 0.14

Interaction Types & Directionality:

positive modulator (activating)

allosteric modulator

potentiator

Interaction Info:

Trial Name ARX-03, sufentanil + triazolam NanoTab

Novel drug target Established target

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

PMIDs:
11752090 18384456

Sources:
TdgClinicalTrial ChemblInteractions TEND
PRIMIDONE GABRA3

Interaction Score: 0.13

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

PMIDs:
10209232 11264449

Sources:
TdgClinicalTrial ChemblInteractions TEND
ADIPIPLON GABRA3

Interaction Score: 0.13

Interaction Types & Directionality:

partial agonist (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; benzodiazepine site partial agonist

Direct Interaction yes

Trial Name NG2-73

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions TTD
GABOXADOL GABRA3

Interaction Score: 0.13

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name gaboxadol

Mechanism of Interaction GABA-A receptor; agonist GABA site agonist

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions
BROMAZEPAM GABRA3

Interaction Score: 0.12

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
18384456

Sources:
TdgClinicalTrial TEND
CHLORDIAZEPOXIDE GABRA3

Interaction Score: 0.12

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Trial Name -

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions TEND
CLOBAZAM GABRA3

Interaction Score: 0.12

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Trial Name Clobazam

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions TEND
LORAZEPAM GABRA3

Interaction Score: 0.11

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Trial Name -

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions TEND
CLONAZEPAM GABRA3

Interaction Score: 0.11

Interaction Types & Directionality:

positive modulator (activating)

allosteric modulator

Interaction Info:

Trial Name JZP-8

Novel drug target Established target

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions TEND
AZIETOMIDATE GABRA3

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16884293

Sources:
DTC
LOREDIPLON GABRA3

Interaction Score: 0.09

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; benzodiazepine site positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
GANAXOLONE GABRA3

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name Ganaxolone

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
RESEQUINIL GABRA3

Interaction Score: 0.09

Interaction Types & Directionality:

inverse agonist (inhibitory)

Interaction Info:

Mechanism of Interaction GABA-A receptor; benzodiazepine site inverse agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
MIDAZOLAM GABRA3

Interaction Score: 0.09

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11752090 18384456

Sources:
TdgClinicalTrial TEND
CLORAZEPIC ACID GABRA3

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial TEND
ALPRAZOLAM GABRA3

Interaction Score: 0.08

Interaction Types & Directionality:

positive modulator (activating)

allosteric modulator

Interaction Info:

Trial Name alprazolam,Xanax, Xanax XR

Novel drug target Established target

Trial Name AZ-002, Staccato alprazolam

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions TEND
BUTABARBITAL SODIUM GABRA3

Interaction Score: 0.05

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
SECOBARBITAL SODIUM GABRA3

Interaction Score: 0.05

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
CLORAZEPATE DIPOTASSIUM GABRA3

Interaction Score: 0.05

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ETHCHLORVYNOL GABRA3

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
METHYPRYLON GABRA3

Interaction Score: 0.05

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
TRICLOFOS SODIUM GABRA3

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

Direct Interaction yes

Mechanism of Interaction GABA-A receptor; anion channel positive modulator

PMIDs:
None found

Sources:
ChemblInteractions
PENTOBARBITAL SODIUM GABRA3

Interaction Score: 0.05

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

PMIDs:
None found

Sources:
ChemblInteractions
ETAZOLATE GABRA3

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name EHT 0202

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
PF-06372865 GABRA3

Interaction Score: 0.05

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction GABA-A receptor; anion channel agonist

PMIDs:
None found

Sources:
ChemblInteractions
CHLORDIAZEPOXIDE HYDROCHLORIDE GABRA3

Interaction Score: 0.05

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
METHOHEXITAL SODIUM GABRA3

Interaction Score: 0.05

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
GLUTETHIMIDE GABRA3

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
THIOPENTAL SODIUM GABRA3

Interaction Score: 0.05

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
THIAMYLAL SODIUM GABRA3

Interaction Score: 0.05

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
MIDAZOLAM HYDROCHLORIDE GABRA3

Interaction Score: 0.05

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
REMIMAZOLAM GABRA3

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name CNS-7056

PMIDs:
None found

Sources:
TdgClinicalTrial
OCINAPLON GABRA3

Interaction Score: 0.05

Interaction Types & Directionality:

allosteric modulator

Interaction Info:

Novel drug target Established target

Trial Name ocinaplon

PMIDs:
None found

Sources:
TdgClinicalTrial
PHENOBARBITAL GABRA3

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial TEND
METHOXYFLURANE GABRA3

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ACAMPROSATE CALCIUM GABRA3

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
HALOTHANE GABRA3

Interaction Score: 0.03

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ISOFLURANE GABRA3

Interaction Score: 0.03

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
PROPOFOL GABRA3

Interaction Score: 0.03

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
DESFLURANE GABRA3

Interaction Score: 0.03

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ENFLURANE GABRA3

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

Direct Interaction yes

Mechanism of Interaction GABA-A receptor; anion channel positive modulator

PMIDs:
None found

Sources:
ChemblInteractions
SEVOFLURANE GABRA3

Interaction Score: 0.02

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
TOPIRAMATE GABRA3

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Ensembl: ENSG00000011677
- Version: 101_38
Alternate Names:

GABRA3 Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
HopkinsGroom: P34903
- Version: 11-September-2012
Alternate Names:

ENSG00000011677 Ensembl Gene Id

2556 Entrez Gene Id

GAMMA-AMINOBUTYRIC ACID RECEPTOR SUBUNIT ALPHA-3 Uniprot Protein Name

Gene Info:

Interpro Acc IPR006201

Interpro Name Neurotransmitter-gated ion-channel ligand-binding

Interpro Short Name Neur_channel

Gene Categories:

ION CHANNEL, DRUGGABLE GENOME

Publications:
TEND: P34903
- Version: 01-August-2011
Alternate Names:

ENSG00000011677 Ensembl Gene Id

GABRA3 Gene Symbol

P34903 Uniprot Accession

Gene Info:

Transmembrane Helix Count 4

Target Subclass Ligand_gated_ion_channels

Target Subclass Channels

Publications:
RussLampel: ENSG00000011677
- Version: 26-July-2011
Alternate Names:

GABRA3 Display Id

GAMMA-AMINOBUTYRIC-ACID RECEPTOR ALPHA-3 SUBUNIT PRECURSOR (GABA(A) RECEPTOR). [SOURCE:UNIPROT/SWISSPROT;ACC:P34903] Description

ENSG00000011677 Ensembl Gene Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:
TdgClinicalTrial: P34903
- Version: January-2014
Alternate Names:

GABRA3 Gene Symbol

Gene Info:

Target Class Receptors

Target Subclass TC:1.A.9

Publications:

DTC: GABRA3

Version: 02-September-2020

Alternate Names:

Gene Info:

Publications:

Husain SS et al., 2006, Synthesis of trifluoromethylaryl diazirine and benzophenone derivatives of etomidate that are potent general anesthetics and effective photolabels for probing sites on ligand-gated ion channels., J Med Chem

ChemblInteractions: GABRA3
- Version: chembl_23
Alternate Names:

GABRA3 GENE_SYMBOL

Gamma-aminobutyric acid receptor subunit alpha-3 UNIPROT

GABA(A) receptor subunit alpha-3 UNIPROT

Gene Info:

Publications:
HingoraniCasas: ENSG00000011677
- Version: 31-May-2017
Alternate Names:

ENSG00000011677 Gene Symbol

GABRA3 Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
TTD: GABA(A) receptor alpha-3
- Version: 2020.06.01
Alternate Names:

GABRA3 TTD Gene Abbreviation

T62292 TTD Target ID

Gene Info:

Publications:
Pharos: GABRA3
- Version: 01-February-2022
Alternate Names:

Gamma-aminobutyric acid receptor subunit alpha-3 Gene Name

P34903 UniProt ID

Gene Info:

Gene Categories:

ION CHANNEL

Publications:

Direct Interaction	yes
Mechanism of Interaction	GABA receptor alpha-3 subunit positive allosteric modulator

Trial Name	OX-22, zolpidem sublingual,Edluar, Sublinox
Novel drug target	Established target

Mechanism of Interaction	GABA-A receptor; anion channel agonist
Direct Interaction	yes
Trial Name	-

Mechanism of Interaction	GABA-A receptor; anion channel positive allosteric modulator
Direct Interaction	yes
Trial Name	-

Mechanism of Interaction	GABA-A receptor; anion channel allosteric antagonist
Direct Interaction	yes
Trial Name	-

Trial Name	diazepam rectal gel
Novel drug target	Established target
Trial Name	NRL-01

Trial Name	ARX-03, sufentanil + triazolam NanoTab
Novel drug target	Established target
Mechanism of Interaction	GABA-A receptor; anion channel positive allosteric modulator

Mechanism of Interaction	GABA-A receptor; benzodiazepine site partial agonist
Direct Interaction	yes
Trial Name	NG2-73

Trial Name	JZP-8
Novel drug target	Established target
Mechanism of Interaction	GABA-A receptor; anion channel positive allosteric modulator

Mechanism of Interaction	GABA-A receptor; benzodiazepine site positive allosteric modulator
Direct Interaction	yes

positive modulator (activating)
potentiator

positive modulator (activating)
potentiator

positive modulator (activating)
potentiator

positive modulator (activating)
potentiator

Mechanism of Interaction	GABA-A receptor; benzodiazepine site inverse agonist
Direct Interaction	yes

Trial Name	alprazolam,Xanax, Xanax XR
Novel drug target	Established target
Trial Name	AZ-002, Staccato alprazolam

ENSG00000011677	Ensembl Gene Id
2556	Entrez Gene Id
GAMMA-AMINOBUTYRIC ACID RECEPTOR SUBUNIT ALPHA-3	Uniprot Protein Name

GABRA3	Display Id
GAMMA-AMINOBUTYRIC-ACID RECEPTOR ALPHA-3 SUBUNIT PRECURSOR (GABA(A) RECEPTOR). [SOURCE:UNIPROT/SWISSPROT;ACC:P34903]	Description
ENSG00000011677	Ensembl Gene Id

GABRA3	GENE_SYMBOL
Gamma-aminobutyric acid receptor subunit alpha-3	UNIPROT
GABA(A) receptor subunit alpha-3	UNIPROT

Gamma-aminobutyric acid receptor subunit alpha-3	Gene Name
P34903	UniProt ID

GABRA3 Gene Record

GABRA3 2556 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: positive modulator (activating) allosteric modulator

Interaction Info: Direct Interaction yes Mechanism of Interaction GABA receptor alpha-3 subunit positive allosteric modulator

PMIDs: 22122233 24802722

Sources: ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: potentiator

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 20303942 19942638 18973287

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: agonist (activating) allosteric modulator

Interaction Info: Trial Name OX-22, zolpidem sublingual,Edluar, Sublinox Novel drug target Established target

PMIDs: 11306694 2157817 11090095 19345234 21353710

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: allosteric modulator potentiator

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 20638393 17016423 17139284

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: positive modulator (activating)

Interaction Info: Mechanism of Interaction GABA receptor alpha-3 subunit positive allosteric modulator Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: potentiator

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 21194017 10209232 11264449

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: potentiator

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 10209232 11264449

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: potentiator

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 10209232 11264449

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: potentiator

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 10209232 11264449

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: potentiator

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 10209232 11264449

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: agonist (activating)

Interaction Info: Mechanism of Interaction GABA-A receptor; anion channel agonist Direct Interaction yes Trial Name -

PMIDs: 9067327 19244096

Sources: TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality: positive modulator (activating) potentiator

Interaction Info: Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator Direct Interaction yes Trial Name -

PMIDs: 10209232 11264449

Sources: TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality: positive modulator (activating) potentiator

Interaction Info: Novel drug target Established target Trial Name - Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

PMIDs: 10209232 11264449

Sources: TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality: positive modulator (activating) potentiator

Interaction Info: Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator Direct Interaction yes Trial Name -

PMIDs: 2892106 3017690

Sources: TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality: positive modulator (activating) potentiator

Interaction Info: Novel drug target Established target Trial Name - Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

PMIDs: 10209232 11264449

Sources: TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality: positive modulator (activating) potentiator

Interaction Info: Direct Interaction yes Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator Trial Name -

PMIDs: 6738302 2867566

Sources: TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality: positive modulator (activating) potentiator

Interaction Info: Trial Name - Novel drug target Established target Direct Interaction yes

PMIDs: 10209232 11264449

Sources: TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality: potentiator

Interaction Info: Trial Name - Novel drug target Established target

Interaction Types & Directionality:

positive modulator (activating)

allosteric modulator

Interaction Info:

Direct Interaction yes

Mechanism of Interaction GABA receptor alpha-3 subunit positive allosteric modulator

PMIDs:
22122233 24802722

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
20303942 19942638 18973287

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

agonist (activating)

allosteric modulator

Interaction Info:

Trial Name OX-22, zolpidem sublingual,Edluar, Sublinox

Novel drug target Established target

PMIDs:
11306694 2157817 11090095 19345234 21353710

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

allosteric modulator

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
20638393 17016423 17139284

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA receptor alpha-3 subunit positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
21194017 10209232 11264449

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
10209232 11264449

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
10209232 11264449

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
10209232 11264449

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
10209232 11264449

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel agonist

Direct Interaction yes

Trial Name -

PMIDs:
9067327 19244096

Sources:
TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Trial Name -

PMIDs:
10209232 11264449

Sources:
TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

Novel drug target Established target

Trial Name -

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

PMIDs:
10209232 11264449

Sources:
TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Trial Name -

PMIDs:
2892106 3017690

Sources:
TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

Novel drug target Established target

Trial Name -

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

PMIDs:
10209232 11264449

Sources:
TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

Direct Interaction yes

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Trial Name -

PMIDs:
6738302 2867566

Sources:
TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

Direct Interaction yes

PMIDs:
10209232 11264449

Sources:
TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
6320036 6148400

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Trial Name -

PMIDs:
20138190 18384456

Sources:
TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality:

positive modulator (activating)

agonist (activating)