DGIdb - GABRA4 Gene Record

GABRA4 2557 Druggable Genome

Alternate Names:

2557
GAMMA-AMINOBUTYRIC ACID TYPE A RECEPTOR ALPHA4 SUBUNIT
GABRA4
137141
4078
ENSG00000109158
OTTHUMG00000099431
P48169
GABRB2
GBRA4_HUMAN
GAMMA-AMINOBUTYRIC-ACID RECEPTOR ALPHA-4 SUBUNIT PRECURSOR (GABA(A) RECEPTOR). [SOURCE:UNIPROT/SWISSPROT;ACC:P48169]
GABA(A) receptor subunit alpha-4
Gamma-aminobutyric acid receptor subunit alpha-4
gamma-aminobutyric acid type A receptor subunit alpha4

Gene Info:

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

(5 More Sources)

Gene Categories: Category Details

ION CHANNEL
DRUGGABLE GENOME

Publications:

Giersch et al., 2010, Atypical behavioural effects of lorazepam: clues to the design of novel therapies?, Pharmacol. Ther.
Riss et al., 2008, Benzodiazepines in epilepsy: pharmacology and pharmacokinetics., Acta Neurol. Scand.
Möhler et al., 2002, A new benzodiazepine pharmacology., J. Pharmacol. Exp. Ther.
Mehta et al., 1999, An update on GABAA receptors., Brain Res. Brain Res. Rev.
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
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.
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
Oblak et al., 2011, Reduced GABAA receptors and benzodiazepine binding sites in the posterior cingulate cortex and fusiform gyrus in autism., Brain Res.
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
Skilbeck et al., 2008, Antipsychotic drug administration differentially affects [3H]muscimol and [3H]flunitrazepam GABA(A) receptor binding sites., Prog. Neuropsychopharmacol. Biol. Psychiatry
You et al., 2010, Benzodiazepine modulation of the rat GABAA receptor α4β3γ2L subtype expressed in Xenopus oocytes., Neuropharmacology

FLUNITRAZEPAM GABRA4

Interaction Score: 0.82

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
20858465 17016423 17139284 17976880 20638393

Sources:
TdgClinicalTrial TEND
MEPHOBARBITAL GABRA4

Interaction Score: 0.31

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
21194017 10209232

Sources:
TdgClinicalTrial TEND
SECOBARBITAL GABRA4

Interaction Score: 0.28

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
10209232

Sources:
TdgClinicalTrial TEND
BUTETHAL GABRA4

Interaction Score: 0.28

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
10209232

Sources:
TdgClinicalTrial TEND
HEXOBARBITAL GABRA4

Interaction Score: 0.28

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
10209232

Sources:
TdgClinicalTrial TEND
MEPROBAMATE GABRA4

Interaction Score: 0.26

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction GABA-A receptor; anion channel agonist

Trial Name -

PMIDs:
9067327 19244096

Sources:
TdgClinicalTrial ChemblInteractions TEND
THIOPENTAL GABRA4

Interaction Score: 0.26

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
10209232

Sources:
TdgClinicalTrial TEND
TEMAZEPAM GABRA4

Interaction Score: 0.21

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
BUTABARBITAL GABRA4

Interaction Score: 0.19

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial TEND
BUTALBITAL GABRA4

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:
10209232

Sources:
TdgClinicalTrial ChemblInteractions TEND
TALBUTAL GABRA4

Interaction Score: 0.19

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

Sources:
TdgClinicalTrial ChemblInteractions TEND
PENTOBARBITAL GABRA4

Interaction Score: 0.19

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

Sources:
TdgClinicalTrial ChemblInteractions TEND
METHARBITAL GABRA4

Interaction Score: 0.19

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

Sources:
TdgClinicalTrial ChemblInteractions TEND
OXAZEPAM GABRA4

Interaction Score: 0.18

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
NITRAZEPAM GABRA4

Interaction Score: 0.18

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11752090 18384456

Sources:
TdgClinicalTrial TEND
FLURAZEPAM GABRA4

Interaction Score: 0.18

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11752090 18384456

Sources:
TdgClinicalTrial TEND
ETOMIDATE GABRA4

Interaction Score: 0.17

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
TRIAZOLAM GABRA4

Interaction Score: 0.16

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 ARX-03, sufentanil + triazolam NanoTab

PMIDs:
11752090 18384456

Sources:
TdgClinicalTrial ChemblInteractions TEND
GABOXADOL GABRA4

Interaction Score: 0.14

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 GABRA4

Interaction Score: 0.13

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
18384456

Sources:
TdgClinicalTrial TEND
CLOBAZAM GABRA4

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 Clobazam

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions TEND
CHLORDIAZEPOXIDE GABRA4

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 -

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions TEND
LORAZEPAM GABRA4

Interaction Score: 0.13

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
CLONAZEPAM GABRA4

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 JZP-8

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions TEND
PRIMIDONE GABRA4

Interaction Score: 0.12

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

Novel drug target Established target

Trial Name -

Direct Interaction yes

PMIDs:
10209232

Sources:
TdgClinicalTrial ChemblInteractions TEND
AZIETOMIDATE GABRA4

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16884293

Sources:
DTC
LOREDIPLON GABRA4

Interaction Score: 0.1

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
RESEQUINIL GABRA4

Interaction Score: 0.1

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
GANAXOLONE GABRA4

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name Ganaxolone

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
MIDAZOLAM GABRA4

Interaction Score: 0.1

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11752090 18384456

Sources:
TdgClinicalTrial TEND
ADIPIPLON GABRA4

Interaction Score: 0.1

Interaction Types & Directionality:

partial agonist (activating)

Interaction Info:

Direct Interaction yes

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

Trial Name NG2-73

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions
CLORAZEPIC ACID GABRA4

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial TEND
ALPRAZOLAM GABRA4

Interaction Score: 0.09

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
SECOBARBITAL SODIUM GABRA4

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 GABRA4

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
METHOHEXITAL SODIUM GABRA4

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
BUTABARBITAL SODIUM GABRA4

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 GABRA4

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
TRICLOFOS SODIUM GABRA4

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
CLORAZEPATE DIPOTASSIUM GABRA4

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
METHYPRYLON GABRA4

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
PENTOBARBITAL SODIUM GABRA4

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
CHLORDIAZEPOXIDE HYDROCHLORIDE GABRA4

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 GABRA4

Interaction Score: 0.06

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
MIDAZOLAM HYDROCHLORIDE GABRA4

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
THIAMYLAL SODIUM GABRA4

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 GABRA4

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
ESZOPICLONE GABRA4

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 GABRA4

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 GABRA4

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name ocinaplon

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
PHENOBARBITAL GABRA4

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial TEND
FLUMAZENIL GABRA4

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

Direct Interaction yes

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

PMIDs:
None found

Sources:
ChemblInteractions
QUAZEPAM GABRA4

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
HALAZEPAM GABRA4

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 GABRA4

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
PRAZEPAM GABRA4

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
ESTAZOLAM GABRA4

Interaction Score: 0.04

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
ACAMPROSATE CALCIUM GABRA4

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
HALOTHANE GABRA4

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 GABRA4

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 GABRA4

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
DIAZEPAM GABRA4

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 GABRA4

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 GABRA4

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
SEVOFLURANE GABRA4

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
TOPIRAMATE GABRA4

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: ENSG00000109158
- Version: 101_38
Alternate Names:

GABRA4 Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
TdgClinicalTrial: P48169
- Version: January-2014
Alternate Names:

GABRA4 Gene Symbol

GABRB2 Gene Symbol

Gene Info:

Target Class Receptors

Target Subclass TC:1.A.9

Publications:
HopkinsGroom: P48169
- Version: 11-September-2012
Alternate Names:

GAMMA-AMINOBUTYRIC ACID RECEPTOR SUBUNIT ALPHA-4 Uniprot Protein Name

GABRA4 Uniprot Gene Name

GBRA4_HUMAN Uniprot Id

Gene Info:

Interpro Short Name Neur_chan_lig-bd

Uniprot Evidence 1: Evidence at protein level

Interpro Type Family

Gene Categories:

ION CHANNEL, DRUGGABLE GENOME

Publications:
TEND: P48169
- Version: 01-August-2011
Alternate Names:

GBRA4_HUMAN Uniprot Id

2557 Entrez Gene Id

P48169 Uniprot Accession

Gene Info:

Target Main Class Receptors

Target Subclass Ligand_gated_ion_channels

Target Subclass Channels

Publications:
RussLampel: ENSG00000109158
- Version: 26-July-2011
Alternate Names:

GAMMA-AMINOBUTYRIC-ACID RECEPTOR ALPHA-4 SUBUNIT PRECURSOR (GABA(A) RECEPTOR). [SOURCE:UNIPROT/SWISSPROT;ACC:P48169] Description

GABRA4 Display Id

ENSG00000109158 Ensembl Gene Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:

DTC: GABRA4

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: GABRA4
- Version: chembl_23
Alternate Names:

GABRA4 GENE_SYMBOL

Gamma-aminobutyric acid receptor subunit alpha-4 UNIPROT

GABA(A) receptor subunit alpha-4 UNIPROT

Gene Info:

Publications:
HingoraniCasas: ENSG00000109158
- Version: 31-May-2017
Alternate Names:

ENSG00000109158 Gene Symbol

GABRA4 Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
Pharos: GABRA4
- Version: 01-February-2022
Alternate Names:

Gamma-aminobutyric acid receptor subunit alpha-4 Gene Name

P48169 UniProt ID

Gene Info:

Gene Categories:

ION CHANNEL

Publications:

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

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

Trial Name	-
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

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

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

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

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

GAMMA-AMINOBUTYRIC ACID RECEPTOR SUBUNIT ALPHA-4	Uniprot Protein Name
GABRA4	Uniprot Gene Name
GBRA4_HUMAN	Uniprot Id

GAMMA-AMINOBUTYRIC-ACID RECEPTOR ALPHA-4 SUBUNIT PRECURSOR (GABA(A) RECEPTOR). [SOURCE:UNIPROT/SWISSPROT;ACC:P48169]	Description
GABRA4	Display Id
ENSG00000109158	Ensembl Gene Id

positive modulator (activating)
potentiator

positive modulator (activating)
potentiator

positive modulator (activating)
potentiator

positive modulator (activating)
potentiator

GABRA4	GENE_SYMBOL
Gamma-aminobutyric acid receptor subunit alpha-4	UNIPROT
GABA(A) receptor subunit alpha-4	UNIPROT

Gamma-aminobutyric acid receptor subunit alpha-4	Gene Name
P48169	UniProt ID

GABRA4 Gene Record

GABRA4 2557 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: agonist (activating)

Interaction Info: Novel drug target Established target Trial Name -

PMIDs: 20858465 17016423 17139284 17976880 20638393

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: potentiator

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 21194017 10209232

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: potentiator

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 10209232

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: potentiator

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 10209232

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: potentiator

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 10209232

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: agonist (activating)

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

PMIDs: 9067327 19244096

Sources: TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality: potentiator

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 10209232

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: n/a

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: None found

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: 10209232

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

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

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

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: 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: positive modulator (activating) potentiator

Interaction Info: Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator Direct Interaction yes Trial Name ARX-03, sufentanil + triazolam NanoTab

PMIDs: 11752090 18384456

Sources: TdgClinicalTrial ChemblInteractions TEND

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

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
20858465 17016423 17139284 17976880 20638393

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
21194017 10209232

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
10209232

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
10209232

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
10209232

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction GABA-A receptor; anion channel agonist

Trial Name -

PMIDs:
9067327 19244096

Sources:
TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
10209232

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:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
None found

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:
10209232

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

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

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

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:

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:

positive modulator (activating)

potentiator

Interaction Info:

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

Direct Interaction yes

Trial Name ARX-03, sufentanil + triazolam NanoTab

PMIDs:
11752090 18384456

Sources:
TdgClinicalTrial ChemblInteractions TEND

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

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
18384456

Sources:
TdgClinicalTrial TEND