DGIdb - GABRE Gene Record

GABRE 2564 Druggable Genome

Alternate Names:

2564
GAMMA-AMINOBUTYRIC ACID TYPE A RECEPTOR EPSILON SUBUNIT
GABRE
300093
4085
ENSG00000102287
OTTHUMG00000024176
P78334
GAMMA-AMINOBUTYRIC ACID RECEPTOR SUBUNIT EPSILON
GBRE_HUMAN
GABA(A) receptor subunit epsilon
GAMMA-AMINOBUTYRIC-ACID RECEPTOR EPSILON SUBUNIT PRECURSOR (GABA(A) RECEPTOR). [SOURCE:UNIPROT/SWISSPROT;ACC:P78334]
gamma-aminobutyric acid type A receptor subunit epsilon

Gene Info:

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

(5 More Sources)

Gene Categories: Category Details

ION CHANNEL
DRUGGABLE GENOME

Publications:

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
Nakatsuka et al., 1985, Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity., Life Sci.
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.
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
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
Giersch et al., 2010, Atypical behavioural effects of lorazepam: clues to the design of novel therapies?, Pharmacol. Ther.
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.
Mandrioli et al., 2008, Benzodiazepine metabolism: an analytical perspective., Curr. Drug Metab.
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.
Schove et al., 1994, Molecular determinants of recognition and activation at the cerebellar benzodiazepine receptor site., Bioorg. Med. Chem.

HALAZEPAM GABRE

Interaction Score: 0.26

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
QUAZEPAM GABRE

Interaction Score: 0.26

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:
2892106 3017690

Sources:
TdgClinicalTrial ChemblInteractions TEND
ADINAZOLAM GABRE

Interaction Score: 0.24

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
6320036 6148400

Sources:
TdgClinicalTrial TEND
TEMAZEPAM GABRE

Interaction Score: 0.23

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
ESTAZOLAM GABRE

Interaction Score: 0.22

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:
639854 2889803

Sources:
TdgClinicalTrial ChemblInteractions TEND
OXAZEPAM GABRE

Interaction Score: 0.2

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:
11752090 18384456

Sources:
TdgClinicalTrial ChemblInteractions TEND
FLURAZEPAM GABRE

Interaction Score: 0.2

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11752090 18384456

Sources:
TdgClinicalTrial TEND
NITRAZEPAM GABRE

Interaction Score: 0.2

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11752090 18384456

Sources:
TdgClinicalTrial TEND
PRAZEPAM GABRE

Interaction Score: 0.19

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:
7773620

Sources:
TdgClinicalTrial ChemblInteractions TEND
ETOMIDATE GABRE

Interaction Score: 0.18

Interaction Types & Directionality:

n/a

Interaction Info:

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

Direct Interaction yes

PMIDs:
16884293

Sources:
DTC ChemblInteractions
CLOTIAZEPAM GABRE

Interaction Score: 0.18

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
18855614

Sources:
TdgClinicalTrial TEND
CINOLAZEPAM GABRE

Interaction Score: 0.18

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
7849137

Sources:
TdgClinicalTrial TEND
FLUDIAZEPAM GABRE

Interaction Score: 0.18

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
2857046

Sources:
TdgClinicalTrial TEND
DIAZEPAM GABRE

Interaction Score: 0.17

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 diazepam rectal gel

PMIDs:
11752090 18384456

Sources:
TdgClinicalTrial ChemblInteractions TEND
TRIAZOLAM GABRE

Interaction Score: 0.17

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

Trial Name ARX-03, sufentanil + triazolam NanoTab

Novel drug target Established target

Direct Interaction yes

PMIDs:
11752090 18384456

Sources:
TdgClinicalTrial ChemblInteractions TEND
CLOBAZAM GABRE

Interaction Score: 0.15

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Trial Name Clobazam

Novel drug target Established target

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

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions TEND
BROMAZEPAM GABRE

Interaction Score: 0.15

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
18384456

Sources:
TdgClinicalTrial TEND
CHLORDIAZEPOXIDE GABRE

Interaction Score: 0.15

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

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

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions TEND
LORAZEPAM GABRE

Interaction Score: 0.14

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 GABRE

Interaction Score: 0.13

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Direct Interaction yes

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

Trial Name JZP-8

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions TEND
AZIETOMIDATE GABRE

Interaction Score: 0.13

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16884293

Sources:
DTC
MIDAZOLAM GABRE

Interaction Score: 0.11

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11752090 18384456

Sources:
TdgClinicalTrial TEND
CLORAZEPIC ACID GABRE

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial TEND
ALPRAZOLAM GABRE

Interaction Score: 0.1

Interaction Types & Directionality:

positive modulator (activating)

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
GABOXADOL GABRE

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name gaboxadol

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
CLORAZEPATE DIPOTASSIUM GABRE

Interaction Score: 0.06

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 GABRE

Interaction Score: 0.06

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
PF-06372865 GABRE

Interaction Score: 0.06

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
BUTABARBITAL SODIUM GABRE

Interaction Score: 0.06

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
CHLORDIAZEPOXIDE HYDROCHLORIDE GABRE

Interaction Score: 0.06

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
TRICLOFOS SODIUM GABRE

Interaction Score: 0.06

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 GABRE

Interaction Score: 0.06

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
PENTOBARBITAL SODIUM GABRE

Interaction Score: 0.06

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
ETAZOLATE GABRE

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name EHT 0202

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
METHOHEXITAL SODIUM GABRE

Interaction Score: 0.06

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 GABRE

Interaction Score: 0.06

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
THIAMYLAL SODIUM GABRE

Interaction Score: 0.06

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
THIOPENTAL SODIUM GABRE

Interaction Score: 0.06

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 GABRE

Interaction Score: 0.06

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
MIDAZOLAM HYDROCHLORIDE GABRE

Interaction Score: 0.06

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 GABRE

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name CNS-7056

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
ESZOPICLONE GABRE

Interaction Score: 0.06

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
OCINAPLON GABRE

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name ocinaplon

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
MEPROBAMATE GABRE

Interaction Score: 0.06

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction GABA-A receptor; anion channel agonist

PMIDs:
None found

Sources:
ChemblInteractions
ADIPIPLON GABRE

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name NG2-73

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
FLUMAZENIL GABRE

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

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

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
BUTALBITAL GABRE

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
METHARBITAL GABRE

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
PENTOBARBITAL GABRE

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
TALBUTAL GABRE

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
METHOXYFLURANE GABRE

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
ACAMPROSATE CALCIUM GABRE

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
ISOFLURANE GABRE

Interaction Score: 0.04

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
HALOTHANE GABRE

Interaction Score: 0.04

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 GABRE

Interaction Score: 0.04

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 GABRE

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 GABRE

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
PRIMIDONE GABRE

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
SEVOFLURANE GABRE

Interaction Score: 0.03

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
TOPIRAMATE GABRE

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

Ensembl: ENSG00000102287
- Version: 101_38
Alternate Names:

GABRE Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
TEND: P78334
- Version: 01-August-2011
Alternate Names:

ENSG00000102287 Ensembl Gene Id

P78334 Uniprot Accession

GABRE Gene Symbol

Gene Info:

Target Main Class Receptors

Transmembrane Helix Count 4

Target Subclass Channels

Publications:
RussLampel: ENSG00000102287
- Version: 26-July-2011
Alternate Names:

GABRE Display Id

GAMMA-AMINOBUTYRIC-ACID RECEPTOR EPSILON SUBUNIT PRECURSOR (GABA(A) RECEPTOR). [SOURCE:UNIPROT/SWISSPROT;ACC:P78334] Description

ENSG00000102287 Ensembl Gene Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:
TdgClinicalTrial: P78334
- Version: January-2014
Alternate Names:

GABRE Gene Symbol

Gene Info:

Target Class Receptors

Target Subclass TC:1.A.9

Publications:
HopkinsGroom: P78334
- Version: 11-September-2012
Alternate Names:

GAMMA-AMINOBUTYRIC ACID RECEPTOR SUBUNIT EPSILON Uniprot Protein Name

GBRE_HUMAN Uniprot Id

ENSG00000102287 Ensembl Gene Id

Gene Info:

Interpro Acc IPR006202

Interpro Type Family

Interpro Type Domain

Gene Categories:

ION CHANNEL, DRUGGABLE GENOME

Publications:

DTC: GABRE

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

HingoraniCasas: ENSG00000102287
- Version: 31-May-2017
Alternate Names:

ENSG00000102287 Gene Symbol

GABRE Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
ChemblInteractions: GABRE
- Version: chembl_23
Alternate Names:

GABRE GENE_SYMBOL

Gamma-aminobutyric acid receptor subunit epsilon UNIPROT

GABA(A) receptor subunit epsilon UNIPROT

Gene Info:

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

Gamma-aminobutyric acid receptor subunit epsilon Gene Name

P78334 UniProt ID

Gene Info:

Gene Categories:

ION CHANNEL

Publications:

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

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

Trial Name	ARX-03, sufentanil + triazolam NanoTab
Novel drug target	Established target
Direct Interaction	yes

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

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

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

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

ENSG00000102287	Ensembl Gene Id
P78334	Uniprot Accession
GABRE	Gene Symbol

GABRE	Display Id
GAMMA-AMINOBUTYRIC-ACID RECEPTOR EPSILON SUBUNIT PRECURSOR (GABA(A) RECEPTOR). [SOURCE:UNIPROT/SWISSPROT;ACC:P78334]	Description
ENSG00000102287	Ensembl Gene Id

GAMMA-AMINOBUTYRIC ACID RECEPTOR SUBUNIT EPSILON	Uniprot Protein Name
GBRE_HUMAN	Uniprot Id
ENSG00000102287	Ensembl Gene Id

positive modulator (activating)
potentiator

positive modulator (activating)
potentiator

positive modulator (activating)
potentiator

positive modulator (activating)
potentiator

GABRE	GENE_SYMBOL
Gamma-aminobutyric acid receptor subunit epsilon	UNIPROT
GABA(A) receptor subunit epsilon	UNIPROT

Gamma-aminobutyric acid receptor subunit epsilon	Gene Name
P78334	UniProt ID

GABRE Gene Record

GABRE 2564 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

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

PMIDs: 2892106 3017690

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) potentiator

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

PMIDs: 639854 2889803

Sources: TdgClinicalTrial ChemblInteractions TEND

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: 11752090 18384456

Sources: TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality: potentiator

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 11752090 18384456

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: potentiator

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 11752090 18384456

Sources: TdgClinicalTrial TEND

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: 7773620

Sources: TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality: n/a

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

PMIDs: 16884293

Sources: DTC ChemblInteractions

Interaction Types & Directionality: potentiator

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 18855614

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: potentiator

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 7849137

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: potentiator

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 2857046

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 diazepam rectal gel

PMIDs: 11752090 18384456

Sources: TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality: positive modulator (activating) potentiator

Interaction Info: Trial Name ARX-03, sufentanil + triazolam NanoTab Novel drug target Established target Direct Interaction yes

PMIDs: 11752090 18384456

Sources: TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality: positive modulator (activating)

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

PMIDs: None found

Sources: TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality: potentiator

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 18384456

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: positive modulator (activating)

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

PMIDs: None found

Sources: TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality: positive modulator (activating)

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

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:

Direct Interaction yes

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

Trial Name -

PMIDs:
2892106 3017690

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)

potentiator

Interaction Info:

Novel drug target Established target

Trial Name -

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

PMIDs:
639854 2889803

Sources:
TdgClinicalTrial ChemblInteractions TEND

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:
11752090 18384456

Sources:
TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11752090 18384456

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11752090 18384456

Sources:
TdgClinicalTrial TEND

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:
7773620

Sources:
TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality:

n/a

Interaction Info:

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

Direct Interaction yes

PMIDs:
16884293

Sources:
DTC ChemblInteractions

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
18855614

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
7849137

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
2857046

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 diazepam rectal gel

PMIDs:
11752090 18384456

Sources:
TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

Trial Name ARX-03, sufentanil + triazolam NanoTab

Novel drug target Established target

Direct Interaction yes

PMIDs:
11752090 18384456

Sources:
TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Trial Name Clobazam

Novel drug target Established target

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

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
18384456

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

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

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions TEND

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

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Direct Interaction yes

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

Trial Name JZP-8

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions TEND