DGIdb - GABRB1 Gene Record

GABRB1 2560 Druggable Genome

Alternate Names:

2560
GAMMA-AMINOBUTYRIC ACID TYPE A RECEPTOR BETA1 SUBUNIT
GABRB1
EIEE45
137190
4081
ENSG00000163288
OTTHUMG00000044269
P18505
GBRB1_HUMAN
P18507
GABRG2
GABA(A) receptor subunit beta-1
Gamma-aminobutyric acid receptor subunit beta-1
GAMMA-AMINOBUTYRIC-ACID RECEPTOR BETA-1 SUBUNIT PRECURSOR (GABA(A) RECEPTOR). [SOURCE:UNIPROT/SWISSPROT;ACC:P18505]
gamma-aminobutyric acid type A receptor subunit beta1
DEE45

Gene Info:

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

(6 More Sources)

Gene Categories: Category Details

ION CHANNEL
DRUGGABLE GENOME

Publications:

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.
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
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.
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.
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
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.
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.
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
Giersch et al., 2010, Atypical behavioural effects of lorazepam: clues to the design of novel therapies?, Pharmacol. Ther.
Anzini M et al., 2011, New insight into the central benzodiazepine receptor-ligand interactions: design, synthesis, biological evaluation, and molecular modeling of 3-substituted 6-phenyl-4H-imidazo[1,5-a][1,4]benzodiazepines and related compounds., J Med Chem

CHEMBL2170369 GABRB1

Interaction Score: 0.49

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21751815

Sources:
DTC
ZOLPIDEM TARTRATE GABRB1

Interaction Score: 0.33

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA A receptor alpha-1/beta-1/gamma-2 positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ZALEPLON GABRB1

Interaction Score: 0.25

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA A receptor alpha-1/beta-1/gamma-2 positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
QUAZEPAM GABRB1

Interaction Score: 0.25

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

Direct Interaction yes

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

Novel drug target Established target

PMIDs:
2892106 3017690

Sources:
TdgClinicalTrial ChemblInteractions TEND
HALAZEPAM GABRB1

Interaction Score: 0.25

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:
6738302 2867566

Sources:
TdgClinicalTrial ChemblInteractions TEND
ADINAZOLAM GABRB1

Interaction Score: 0.23

Interaction Types & Directionality:

potentiator

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
6320036 6148400

Sources:
TdgClinicalTrial TEND
TEMAZEPAM GABRB1

Interaction Score: 0.22

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:
20138190 18384456

Sources:
TdgClinicalTrial ChemblInteractions TEND
ESTAZOLAM GABRB1

Interaction Score: 0.21

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 GABRB1

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 GABRB1

Interaction Score: 0.19

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11752090 18384456

Sources:
TdgClinicalTrial TEND
NITRAZEPAM GABRB1

Interaction Score: 0.19

Interaction Types & Directionality:

potentiator

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
18384456 11752090

Sources:
TdgClinicalTrial TEND
PRAZEPAM GABRB1

Interaction Score: 0.18

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

Novel drug target Established target

Trial Name -

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

PMIDs:
7773620

Sources:
TdgClinicalTrial ChemblInteractions TEND
ETOMIDATE GABRB1

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
CLOTIAZEPAM GABRB1

Interaction Score: 0.17

Interaction Types & Directionality:

potentiator

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
18855614

Sources:
TdgClinicalTrial TEND
CINOLAZEPAM GABRB1

Interaction Score: 0.17

Interaction Types & Directionality:

potentiator

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
7849137

Sources:
TdgClinicalTrial TEND
FLUDIAZEPAM GABRB1

Interaction Score: 0.17

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
2857046

Sources:
TdgClinicalTrial TEND
DIAZEPAM GABRB1

Interaction Score: 0.16

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

Direct Interaction yes

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

Trial Name diazepam rectal gel

PMIDs:
11752090 18384456

Sources:
TdgClinicalTrial ChemblInteractions TEND
TRIAZOLAM GABRB1

Interaction Score: 0.16

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

Direct Interaction yes

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

Trial Name ARX-03, sufentanil + triazolam NanoTab

PMIDs:
11752090 18384456

Sources:
TdgClinicalTrial ChemblInteractions TEND
GABOXADOL GABRB1

Interaction Score: 0.15

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

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

Direct Interaction yes

Trial Name gaboxadol

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions
BROMAZEPAM GABRB1

Interaction Score: 0.14

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
18384456

Sources:
TdgClinicalTrial TEND
CHLORDIAZEPOXIDE GABRB1

Interaction Score: 0.14

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Novel drug target Established target

Trial Name -

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

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions TEND
CLOBAZAM GABRB1

Interaction Score: 0.14

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
LORAZEPAM GABRB1

Interaction Score: 0.13

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Novel drug target Established target

Trial Name -

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

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions TEND
CLONAZEPAM GABRB1

Interaction Score: 0.13

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Trial Name JZP-8

Novel drug target Established target

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

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions TEND
AZIETOMIDATE GABRB1

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16884293

Sources:
DTC
MIDAZOLAM GABRB1

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 GABRB1

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 GABRB1

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
PF-06372865 GABRB1

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
CLORAZEPATE DIPOTASSIUM GABRB1

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 GABRB1

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
SECOBARBITAL SODIUM GABRB1

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 GABRB1

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 GABRB1

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 GABRB1

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 GABRB1

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 GABRB1

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
BUTABARBITAL SODIUM GABRB1

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 GABRB1

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 GABRB1

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 GABRB1

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 GABRB1

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
THIOPENTAL SODIUM GABRB1

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 GABRB1

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
MEPROBAMATE GABRB1

Interaction Score: 0.05

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
OCINAPLON GABRB1

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name ocinaplon

PMIDs:
None found

Sources:
TdgClinicalTrial
REMIMAZOLAM GABRB1

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
ADIPIPLON GABRB1

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 GABRB1

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
METHARBITAL GABRB1

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
TALBUTAL GABRB1

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 GABRB1

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 GABRB1

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 GABRB1

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

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

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ACAMPROSATE CALCIUM GABRB1

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 GABRB1

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
ISOFLURANE GABRB1

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
PROPOFOL GABRB1

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
DESFLURANE GABRB1

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 GABRB1

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 GABRB1

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 GABRB1

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 GABRB1

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: ENSG00000163288
- Version: 101_38
Alternate Names:

GABRB1 Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
RussLampel: ENSG00000163288
- Version: 26-July-2011
Alternate Names:

GABRB1 Display Id

ENSG00000163288 Ensembl Gene Id

GAMMA-AMINOBUTYRIC-ACID RECEPTOR BETA-1 SUBUNIT PRECURSOR (GABA(A) RECEPTOR). [SOURCE:UNIPROT/SWISSPROT;ACC:P18505] Description

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:
TdgClinicalTrial: P18505
- Version: January-2014
Alternate Names:

GABRB1 Gene Symbol

Gene Info:

Target Class Receptors

Target Subclass TC:1.A.9

Publications:
TEND: P18505
- Version: 01-August-2011
Alternate Names:

2560 Entrez Gene Id

GABRB1 Gene Symbol

ENSG00000163288 Ensembl Gene Id

Gene Info:

Target Subclass Channels

Target Subclass cys-loop

Transmembrane Helix Count 4

Publications:
HopkinsGroom: P18505
- Version: 11-September-2012
Alternate Names:

GAMMA-AMINOBUTYRIC ACID RECEPTOR SUBUNIT BETA-1 Uniprot Protein Name

2560 Entrez Gene Id

P18505 Uniprot Accession

Gene Info:

Human Readable Name DRUGGABLE GENOME

Uniprot Status Swiss-Prot

Interpro Type Domain

Gene Categories:

ION CHANNEL, DRUGGABLE GENOME

Publications:
TdgClinicalTrial: P18507
- Version: January-2014
Alternate Names:

GABRG2 Gene Symbol

GABRB1 Gene Symbol

Gene Info:

Target Class Receptors

Target Subclass TC:1.A.9

Publications:

DTC: GABRB1

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

Anzini M et al., 2011, New insight into the central benzodiazepine receptor-ligand interactions: design, synthesis, biological evaluation, and molecular modeling of 3-substituted 6-phenyl-4H-imidazo[1,5-a][1,4]benzodiazepines and related compounds., J Med Chem

HingoraniCasas: ENSG00000163288
- Version: 31-May-2017
Alternate Names:

ENSG00000163288 Gene Symbol

GABRB1 Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
ChemblInteractions: GABRB1
- Version: chembl_23
Alternate Names:

GABRB1 GENE_SYMBOL

Gamma-aminobutyric acid receptor subunit beta-1 UNIPROT

GABA(A) receptor subunit beta-1 UNIPROT

Gene Info:

Publications:
Pharos: GABRB1
- Version: 01-February-2022
Alternate Names:

Gamma-aminobutyric acid receptor subunit beta-1 Gene Name

P18505 UniProt ID

Gene Info:

Gene Categories:

ION CHANNEL

Publications:

Mechanism of Interaction	GABA A receptor alpha-1/beta-1/gamma-2 positive allosteric modulator
Direct Interaction	yes

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

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

Mechanism of Interaction	GABA-A receptor; agonist GABA site agonist
Direct Interaction	yes
Trial Name	gaboxadol

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

Trial Name	JZP-8
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

GABRB1	Display Id
ENSG00000163288	Ensembl Gene Id
GAMMA-AMINOBUTYRIC-ACID RECEPTOR BETA-1 SUBUNIT PRECURSOR (GABA(A) RECEPTOR). [SOURCE:UNIPROT/SWISSPROT;ACC:P18505]	Description

positive modulator (activating)
potentiator

positive modulator (activating)
potentiator

positive modulator (activating)
potentiator

positive modulator (activating)
potentiator

2560	Entrez Gene Id
GABRB1	Gene Symbol
ENSG00000163288	Ensembl Gene Id

GAMMA-AMINOBUTYRIC ACID RECEPTOR SUBUNIT BETA-1	Uniprot Protein Name
2560	Entrez Gene Id
P18505	Uniprot Accession

GABRB1	GENE_SYMBOL
Gamma-aminobutyric acid receptor subunit beta-1	UNIPROT
GABA(A) receptor subunit beta-1	UNIPROT

Gamma-aminobutyric acid receptor subunit beta-1	Gene Name
P18505	UniProt ID

GABRB1 Gene Record

GABRB1 2560 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 21751815

Sources: DTC

Interaction Types & Directionality: positive modulator (activating)

Interaction Info: Mechanism of Interaction GABA A receptor alpha-1/beta-1/gamma-2 positive allosteric modulator Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: positive modulator (activating)

Interaction Info: Mechanism of Interaction GABA A receptor alpha-1/beta-1/gamma-2 positive allosteric modulator Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: positive modulator (activating) potentiator

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

PMIDs: 2892106 3017690

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: 6738302 2867566

Sources: TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality: potentiator

Interaction Info: Novel drug target Established target Trial Name -

PMIDs: 6320036 6148400

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: 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: Novel drug target Established target Trial Name -

PMIDs: 18384456 11752090

Sources: TdgClinicalTrial 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: 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: Novel drug target Established target Trial Name -

PMIDs: 18855614

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: potentiator

Interaction Info: Novel drug target Established target Trial Name -

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

PMIDs: 11752090 18384456

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 ARX-03, sufentanil + triazolam NanoTab

PMIDs: 11752090 18384456

Sources: TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality: agonist (activating)

Interaction Info: Mechanism of Interaction GABA-A receptor; agonist GABA site agonist Direct Interaction yes Trial Name gaboxadol

Interaction Types & Directionality:

n/a

PMIDs:
21751815

Sources:
DTC

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA A receptor alpha-1/beta-1/gamma-2 positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA A receptor alpha-1/beta-1/gamma-2 positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

Direct Interaction yes

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

Novel drug target Established target

PMIDs:
2892106 3017690

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:
6738302 2867566

Sources:
TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality:

potentiator

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
6320036 6148400

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:
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:

Novel drug target Established target

Trial Name -

PMIDs:
18384456 11752090

Sources:
TdgClinicalTrial 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:
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:

Novel drug target Established target

Trial Name -

PMIDs:
18855614

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

potentiator

Interaction Info:

Novel drug target Established target

Trial Name -

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:

Direct Interaction yes

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

Trial Name diazepam rectal gel

PMIDs:
11752090 18384456

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 ARX-03, sufentanil + triazolam NanoTab

PMIDs:
11752090 18384456

Sources:
TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

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

Direct Interaction yes

Trial Name gaboxadol

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)