DGIdb - GABRB3 Gene Record

GABRB3 2562 Druggable Genome

Alternate Names:

2562
GAMMA-AMINOBUTYRIC ACID TYPE A RECEPTOR BETA3 SUBUNIT
GABRB3
ECA5
EIEE43
137192
4083
ENSG00000166206
OTTHUMG00000129231
P28472
GAMMA-AMINOBUTYRIC-ACID RECEPTOR BETA-3 SUBUNIT PRECURSOR (GABA(A) RECEPTOR). [SOURCE:UNIPROT/SWISSPROT;ACC:P28472]
GBRB3_HUMAN
GABA(A) receptor subunit beta-3
Gamma-aminobutyric acid receptor subunit beta-3
gamma-aminobutyric acid type A receptor subunit beta3
DEE43

Gene Info:

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

(5 More Sources)

Gene Categories: Category Details

ION CHANNEL
DRUGGABLE GENOME

Publications:

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.
Franks, 2006, Molecular targets underlying general anaesthesia., Br. J. Pharmacol.
Mandrioli et al., 2008, Benzodiazepine metabolism: an analytical perspective., Curr. Drug Metab.
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
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.
Giersch et al., 2010, Atypical behavioural effects of lorazepam: clues to the design of novel therapies?, Pharmacol. Ther.
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.
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
Schove et al., 1994, Molecular determinants of recognition and activation at the cerebellar benzodiazepine receptor site., Bioorg. Med. Chem.
Nakatsuka et al., 1985, Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity., Life Sci.
Knust H et al., 2009, The discovery and unique pharmacological profile of RO4938581 and RO4882224 as potent and selective GABAA alpha5 inverse agonists for the treatment of cognitive dysfunction., Bioorg Med Chem Lett
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.

FOSPROPOFOL GABRB3

Interaction Score: 0.75

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name fospropofol disodium, GPI-15715,Lusedra, Aquavan

Novel drug target Established target

PMIDs:
16402123

Sources:
TdgClinicalTrial TEND
CHEMBL1077391 GABRB3

Interaction Score: 0.66

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19762240

Sources:
DTC
HALAZEPAM GABRB3

Interaction Score: 0.25

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:
6738302 2867566

Sources:
TdgClinicalTrial ChemblInteractions TEND
QUAZEPAM GABRB3

Interaction Score: 0.25

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
ADINAZOLAM GABRB3

Interaction Score: 0.23

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
6320036 6148400

Sources:
TdgClinicalTrial TEND
TEMAZEPAM GABRB3

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 GABRB3

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 GABRB3

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:
11752090 18384456

Sources:
TdgClinicalTrial ChemblInteractions TEND
FLURAZEPAM GABRB3

Interaction Score: 0.19

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11752090 18384456

Sources:
TdgClinicalTrial TEND
NITRAZEPAM GABRB3

Interaction Score: 0.19

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11752090 18384456

Sources:
TdgClinicalTrial TEND
PRAZEPAM GABRB3

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:
7773620

Sources:
TdgClinicalTrial ChemblInteractions TEND
FLUDIAZEPAM GABRB3

Interaction Score: 0.18

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
2857046

Sources:
TdgClinicalTrial TEND
ETOMIDATE GABRB3

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
CINOLAZEPAM GABRB3

Interaction Score: 0.18

Interaction Types & Directionality:

potentiator

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
7849137

Sources:
TdgClinicalTrial TEND
CLOTIAZEPAM GABRB3

Interaction Score: 0.18

Interaction Types & Directionality:

potentiator

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
18855614

Sources:
TdgClinicalTrial TEND
DIAZEPAM GABRB3

Interaction Score: 0.17

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

Trial Name diazepam rectal gel

Novel drug target Established target

Trial Name NRL-01

PMIDs:
11752090 18384456

Sources:
TdgClinicalTrial ChemblInteractions TEND
TRIAZOLAM GABRB3

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
GABOXADOL GABRB3

Interaction Score: 0.15

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name gaboxadol

Novel drug target Established target

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

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions
BROMAZEPAM GABRB3

Interaction Score: 0.14

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
18384456

Sources:
TdgClinicalTrial TEND
CLOBAZAM GABRB3

Interaction Score: 0.14

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Novel drug target Established target

Trial Name Clobazam

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

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions TEND
CHLORDIAZEPOXIDE GABRB3

Interaction Score: 0.14

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
PROPOFOL GABRB3

Interaction Score: 0.14

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

Trial Name propofol lingual spray

Novel drug target Established target

Trial Name propofol,Diprivan

PMIDs:
16402123

Sources:
TdgClinicalTrial ChemblInteractions TEND
LORAZEPAM GABRB3

Interaction Score: 0.14

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 GABRB3

Interaction Score: 0.13

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
AZIETOMIDATE GABRB3

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16884293

Sources:
DTC
MIDAZOLAM GABRB3

Interaction Score: 0.11

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11752090 18384456

Sources:
TdgClinicalTrial TEND
ALPRAZOLAM GABRB3

Interaction Score: 0.1

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

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

Direct Interaction yes

Trial Name AZ-002, Staccato alprazolam

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions TEND
CLORAZEPIC ACID GABRB3

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial TEND
METHOHEXITAL SODIUM GABRB3

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
TRICLOFOS SODIUM GABRB3

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
ETAZOLATE GABRB3

Interaction Score: 0.06

Interaction Types & Directionality:

positive modulator (activating)

allosteric modulator

Interaction Info:

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

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
METHYPRYLON GABRB3

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 GABRB3

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 GABRB3

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 GABRB3

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 GABRB3

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 GABRB3

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
ETHCHLORVYNOL GABRB3

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 GABRB3

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
MIDAZOLAM HYDROCHLORIDE GABRB3

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
THIAMYLAL SODIUM GABRB3

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 GABRB3

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
GLUTETHIMIDE GABRB3

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
ESZOPICLONE GABRB3

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 GABRB3

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
MEPROBAMATE GABRB3

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
OCINAPLON GABRB3

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name ocinaplon

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
FLUMAZENIL GABRB3

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
ADIPIPLON GABRB3

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
TALBUTAL GABRB3

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 GABRB3

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
BUTALBITAL GABRB3

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
METHARBITAL GABRB3

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 GABRB3

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 GABRB3

Interaction Score: 0.04

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
ISOFLURANE GABRB3

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 GABRB3

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
DESFLURANE GABRB3

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
PRIMIDONE GABRB3

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 GABRB3

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 GABRB3

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 GABRB3

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: ENSG00000166206
- Version: 101_38
Alternate Names:

GABRB3 Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
RussLampel: ENSG00000166206
- Version: 26-July-2011
Alternate Names:

GABRB3 Display Id

GAMMA-AMINOBUTYRIC-ACID RECEPTOR BETA-3 SUBUNIT PRECURSOR (GABA(A) RECEPTOR). [SOURCE:UNIPROT/SWISSPROT;ACC:P28472] Description

ENSG00000166206 Ensembl Gene Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:
HopkinsGroom: P28472
- Version: 11-September-2012
Alternate Names:

GBRB3_HUMAN Uniprot Id

ENSG00000166206 Ensembl Gene Id

P28472 Uniprot Accession

Gene Info:

Interpro Acc IPR006201

Interpro Short Name Neur_chan_lig-bd

Uniprot Status Swiss-Prot

Gene Categories:

ION CHANNEL, DRUGGABLE GENOME

Publications:
TdgClinicalTrial: P28472
- Version: January-2014
Alternate Names:

GABRB3 Gene Symbol

Gene Info:

Target Class Receptors

Target Subclass TC:1.A.9

Publications:
TEND: P28472
- Version: 01-August-2011
Alternate Names:

2562 Entrez Gene Id

ENSG00000166206 Ensembl Gene Id

P28472 Uniprot Accession

Gene Info:

Target Subclass Ligand_gated_ion_channels

Transmembrane Helix Count 4

Target Subclass Channels

Publications:

DTC: GABRB3

Version: 02-September-2020

Alternate Names:

Gene Info:

Publications:

Knust H et al., 2009, The discovery and unique pharmacological profile of RO4938581 and RO4882224 as potent and selective GABAA alpha5 inverse agonists for the treatment of cognitive dysfunction., Bioorg Med Chem Lett

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: GABRB3
- Version: chembl_23
Alternate Names:

GABRB3 GENE_SYMBOL

Gamma-aminobutyric acid receptor subunit beta-3 UNIPROT

GABA(A) receptor subunit beta-3 UNIPROT

Gene Info:

Publications:
HingoraniCasas: ENSG00000166206
- Version: 31-May-2017
Alternate Names:

ENSG00000166206 Gene Symbol

GABRB3 Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
Pharos: GABRB3
- Version: 01-February-2022
Alternate Names:

Gamma-aminobutyric acid receptor subunit beta-3 Gene Name

P28472 UniProt ID

Gene Info:

Gene Categories:

ION CHANNEL

Publications:

Trial Name	fospropofol disodium, GPI-15715,Lusedra, Aquavan
Novel drug target	Established target

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

Trial Name	gaboxadol
Novel drug target	Established target
Mechanism of Interaction	GABA-A receptor; agonist GABA site agonist

Trial Name	propofol lingual spray
Novel drug target	Established target
Trial Name	propofol,Diprivan

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

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

GABRB3	Display Id
GAMMA-AMINOBUTYRIC-ACID RECEPTOR BETA-3 SUBUNIT PRECURSOR (GABA(A) RECEPTOR). [SOURCE:UNIPROT/SWISSPROT;ACC:P28472]	Description
ENSG00000166206	Ensembl Gene Id

positive modulator (activating)
potentiator

positive modulator (activating)
potentiator

positive modulator (activating)
potentiator

positive modulator (activating)
potentiator

GBRB3_HUMAN	Uniprot Id
ENSG00000166206	Ensembl Gene Id
P28472	Uniprot Accession

2562	Entrez Gene Id
ENSG00000166206	Ensembl Gene Id
P28472	Uniprot Accession

GABRB3	GENE_SYMBOL
Gamma-aminobutyric acid receptor subunit beta-3	UNIPROT
GABA(A) receptor subunit beta-3	UNIPROT

Gamma-aminobutyric acid receptor subunit beta-3	Gene Name
P28472	UniProt ID

GABRB3 Gene Record

GABRB3 2562 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: potentiator

Interaction Info: Trial Name fospropofol disodium, GPI-15715,Lusedra, Aquavan Novel drug target Established target

PMIDs: 16402123

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 19762240

Sources: DTC

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: 6738302 2867566

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

PMIDs: 7773620

Sources: TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality: potentiator

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 2857046

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: potentiator

Interaction Info: Novel drug target Established target Trial Name -

PMIDs: 7849137

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: potentiator

Interaction Info: Novel drug target Established target Trial Name -

PMIDs: 18855614

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: positive modulator (activating) potentiator

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

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: agonist (activating)

Interaction Info: Trial Name gaboxadol Novel drug target Established target 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

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name fospropofol disodium, GPI-15715,Lusedra, Aquavan

Novel drug target Established target

PMIDs:
16402123

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

n/a

PMIDs:
19762240

Sources:
DTC

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:
6738302 2867566

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:

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:

Novel drug target Established target

Trial Name -

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:

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

Direct Interaction yes

Trial Name -

PMIDs:
7773620

Sources:
TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
2857046

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:

potentiator

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
7849137

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

potentiator

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
18855614

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

Trial Name diazepam rectal gel

Novel drug target Established target

Trial Name NRL-01

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:

agonist (activating)

Interaction Info:

Trial Name gaboxadol

Novel drug target Established target

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

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Novel drug target Established target

Trial Name Clobazam

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

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality:

positive modulator (activating)