DGIdb - GABRG2 Gene Record

GABRG2 2566 Druggable Genome

Alternate Names:

2566
GAMMA-AMINOBUTYRIC ACID TYPE A RECEPTOR GAMMA2 SUBUNIT
GABRG2
CAE2
ECA2
GEFSP3
137164
4087
ENSG00000113327
OTTHUMG00000130350
P18507
GBRG2_HUMAN
Gamma-aminobutyric acid receptor subunit gamma-2
GABA(A) receptor subunit gamma-2
GAMMA-AMINOBUTYRIC-ACID RECEPTOR GAMMA-2 SUBUNIT PRECURSOR (GABA(A) RECEPTOR). [SOURCE:UNIPROT/SWISSPROT;ACC:P18507]
GABA(A) receptor gamma-2
T08910
gamma-aminobutyric acid type A receptor subunit gamma2
DEE74
EIEE74
FEB8

Gene Info:

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

(5 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.
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
Riss et al., 2008, Benzodiazepines in epilepsy: pharmacology and pharmacokinetics., Acta Neurol. Scand.
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
Möhler et al., 2002, A new benzodiazepine pharmacology., J. Pharmacol. Exp. Ther.
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
Padgett et al., 2008, The F-loop of the GABA A receptor gamma2 subunit contributes to benzodiazepine modulation., J. Biol. Chem.
Wingrove et al., 2002, Mechanism of alpha-subunit selectivity of benzodiazepine pharmacology at gamma-aminobutyric acid type A receptors., Eur. J. Pharmacol.
Whitwam et al., 1995, Pharmacology of flumazenil., Acta Anaesthesiol Scand Suppl
Husain SS et al., 2010, p-Trifluoromethyldiazirinyl-etomidate: a potent photoreactive general anesthetic derivative of etomidate that is selective for ligand-gated cationic ion channels., J Med Chem
Baburin et al., 2008, Estimating the efficiency of benzodiazepines on GABA(A) receptors comprising gamma1 or gamma2 subunits., Br. J. Pharmacol.
Mandrioli et al., 2008, Benzodiazepine metabolism: an analytical perspective., Curr. Drug Metab.
Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
Schove et al., 1994, Molecular determinants of recognition and activation at the cerebellar benzodiazepine receptor site., Bioorg. Med. Chem.
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.
Nakatsuka et al., 1985, Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity., Life Sci.
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.
Giersch et al., 2010, Atypical behavioural effects of lorazepam: clues to the design of novel therapies?, Pharmacol. Ther.
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
Petersen JG et al., 2014, Synthesis and pharmacological evaluation of 6-aminonicotinic acid analogues as novel GABA(A) receptor agonists., Eur J Med Chem

CHEMBL1077391 GABRG2

Interaction Score: 0.62

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19762240

Sources:
DTC
ISONIPECOTIC ACID GABRG2

Interaction Score: 0.47

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25038482

Sources:
DTC
CHEMBL2170369 GABRG2

Interaction Score: 0.47

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21751815

Sources:
DTC
ZOLPIDEM TARTRATE GABRG2

Interaction Score: 0.31

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Direct Interaction yes

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

PMIDs:
None found

Sources:
ChemblInteractions
CHEMBL1518572 GABRG2

Interaction Score: 0.23

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
ZALEPLON GABRG2

Interaction Score: 0.23

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
CLOTIAZEPAM GABRG2

Interaction Score: 0.22

Interaction Types & Directionality:

potentiator

Interaction Info:

PMIDs:
18604239 18855614 10592235

Sources:
TEND
ETOMIDATE GABRG2

Interaction Score: 0.22

Interaction Types & Directionality:

n/a

Interaction Info:

Direct Interaction yes

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

PMIDs:
16884293 20704351

Sources:
DTC ChemblInteractions
FLUMAZENIL GABRG2

Interaction Score: 0.2

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

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

Direct Interaction yes

PMIDs:
17974564 11864636 8693922

Sources:
ChemblInteractions
THIOCOLCHICOSIDE GABRG2

Interaction Score: 0.19

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
BREXANOLONE GABRG2

Interaction Score: 0.19

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
QUAZEPAM GABRG2

Interaction Score: 0.19

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

Direct Interaction yes

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

PMIDs:
2892106 3017690

Sources:
ChemblInteractions TEND
HALAZEPAM GABRG2

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

PMIDs:
6738302 2867566

Sources:
ChemblInteractions TEND
TEMAZEPAM GABRG2

Interaction Score: 0.17

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

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

Direct Interaction yes

PMIDs:
20138190 18384456

Sources:
ChemblInteractions TEND
ADINAZOLAM GABRG2

Interaction Score: 0.17

Interaction Types & Directionality:

potentiator

Interaction Info:

PMIDs:
6320036 6148400

Sources:
TEND
ESTAZOLAM GABRG2

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

PMIDs:
639854 2889803

Sources:
ChemblInteractions TEND
OXAZEPAM GABRG2

Interaction Score: 0.14

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

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

Direct Interaction yes

PMIDs:
11752090 18384456

Sources:
ChemblInteractions TEND
NITRAZEPAM GABRG2

Interaction Score: 0.13

Interaction Types & Directionality:

potentiator

Interaction Info:

PMIDs:
11752090 18384456

Sources:
TEND
FLURAZEPAM GABRG2

Interaction Score: 0.13

Interaction Types & Directionality:

potentiator

Interaction Info:

PMIDs:
11752090 18384456

Sources:
TEND
PRAZEPAM GABRG2

Interaction Score: 0.13

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

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

Direct Interaction yes

PMIDs:
7773620

Sources:
ChemblInteractions TEND
TRIAZOLAM GABRG2

Interaction Score: 0.12

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

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

Direct Interaction yes

PMIDs:
11752090 18384456

Sources:
ChemblInteractions TEND
DIAZEPAM GABRG2

Interaction Score: 0.12

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

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

Direct Interaction yes

PMIDs:
11752090 18384456

Sources:
ChemblInteractions TEND
AZIETOMIDATE GABRG2

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16884293

Sources:
DTC
CINOLAZEPAM GABRG2

Interaction Score: 0.11

Interaction Types & Directionality:

potentiator

Interaction Info:

PMIDs:
7849137

Sources:
TEND
FLUDIAZEPAM GABRG2

Interaction Score: 0.11

Interaction Types & Directionality:

potentiator

Interaction Info:

PMIDs:
2857046

Sources:
TEND
RESEQUINIL GABRG2

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
LOREDIPLON GABRG2

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
CHLORDIAZEPOXIDE GABRG2

Interaction Score: 0.09

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 TEND
CLOBAZAM GABRG2

Interaction Score: 0.09

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 TEND
BROMAZEPAM GABRG2

Interaction Score: 0.09

Interaction Types & Directionality:

potentiator

Interaction Info:

PMIDs:
18384456

Sources:
TEND
LORAZEPAM GABRG2

Interaction Score: 0.09

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 TEND
CLONAZEPAM GABRG2

Interaction Score: 0.08

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 TEND
MIDAZOLAM GABRG2

Interaction Score: 0.08

Interaction Types & Directionality:

potentiator

Interaction Info:

PMIDs:
11752090 18384456

Sources:
TEND
ALPRAZOLAM GABRG2

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 TEND
CHLORDIAZEPOXIDE HYDROCHLORIDE GABRG2

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
METHOHEXITAL SODIUM GABRG2

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 GABRG2

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 GABRG2

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 GABRG2

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
TRICLOFOS SODIUM GABRG2

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 GABRG2

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 GABRG2

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 GABRG2

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
SECOBARBITAL SODIUM GABRG2

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 GABRG2

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 GABRG2

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 GABRG2

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
THIOPENTAL SODIUM GABRG2

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
MEPROBAMATE GABRG2

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
ESZOPICLONE GABRG2

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
ADIPIPLON GABRG2

Interaction Score: 0.05

Interaction Types & Directionality:

partial agonist (activating)

Interaction Info:

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

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
CLORAZEPIC ACID GABRG2

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TEND
BUTALBITAL GABRG2

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 GABRG2

Interaction Score: 0.05

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

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

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
METHARBITAL GABRG2

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
PENTOBARBITAL GABRG2

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
METHOXYFLURANE GABRG2

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 GABRG2

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

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

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ISOFLURANE GABRG2

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
HALOTHANE GABRG2

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 GABRG2

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 GABRG2

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
ENFLURANE GABRG2

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
PRIMIDONE GABRG2

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
SEVOFLURANE GABRG2

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 GABRG2

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: ENSG00000113327
- Version: 101_38
Alternate Names:

GABRG2 Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
HopkinsGroom: P18507
- Version: 11-September-2012
Alternate Names:

ENSG00000113327 Ensembl Gene Id

GABRG2 Uniprot Gene Name

2566 Entrez Gene Id

Gene Info:

Interpro Short Name Neur_chan_lig-bd

Interpro Type Domain

Interpro Short Name Neur_channel

Gene Categories:

ION CHANNEL, DRUGGABLE GENOME

Publications:
RussLampel: ENSG00000113327
- Version: 26-July-2011
Alternate Names:

GAMMA-AMINOBUTYRIC-ACID RECEPTOR GAMMA-2 SUBUNIT PRECURSOR (GABA(A) RECEPTOR). [SOURCE:UNIPROT/SWISSPROT;ACC:P18507] Description

GABRG2 Display Id

ENSG00000113327 Ensembl Gene Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:
TEND: P18507
- Version: 01-August-2011
Alternate Names:

ENSG00000113327 Ensembl Gene Id

2566 Entrez Gene Id

GBRG2_HUMAN Uniprot Id

Gene Info:

Target Subclass Channels

Target Subclass Ligand_gated_ion_channels

Target Subclass cys-loop

Publications:

DTC: GABRG2

Version: 02-September-2020

Alternate Names:

Gene Info:

Publications:

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

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: GABRG2
- Version: chembl_23
Alternate Names:

GABRG2 GENE_SYMBOL

Gamma-aminobutyric acid receptor subunit gamma-2 UNIPROT

GABA(A) receptor subunit gamma-2 UNIPROT

Gene Info:

Publications:
HingoraniCasas: ENSG00000113327
- Version: 31-May-2017
Alternate Names:

ENSG00000113327 Gene Symbol

GABRG2 Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
TTD: GABA(A) receptor gamma-2
- Version: 2020.06.01
Alternate Names:

GABRG2 TTD Gene Abbreviation

T08910 TTD Target ID

Gene Info:

Publications:
Pharos: GABRG2
- Version: 01-February-2022
Alternate Names:

Gamma-aminobutyric acid receptor subunit gamma-2 Gene Name

P18507 UniProt ID

Gene Info:

Gene Categories:

ION CHANNEL

Publications:

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

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

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

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

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

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

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

ENSG00000113327	Ensembl Gene Id
GABRG2	Uniprot Gene Name
2566	Entrez Gene Id

GAMMA-AMINOBUTYRIC-ACID RECEPTOR GAMMA-2 SUBUNIT PRECURSOR (GABA(A) RECEPTOR). [SOURCE:UNIPROT/SWISSPROT;ACC:P18507]	Description
GABRG2	Display Id
ENSG00000113327	Ensembl Gene Id

GABRG2	GENE_SYMBOL
Gamma-aminobutyric acid receptor subunit gamma-2	UNIPROT
GABA(A) receptor subunit gamma-2	UNIPROT

positive modulator (activating)
potentiator

positive modulator (activating)
potentiator

positive modulator (activating)
potentiator

positive modulator (activating)
potentiator

Gamma-aminobutyric acid receptor subunit gamma-2	Gene Name
P18507	UniProt ID

GABRG2 Gene Record

GABRG2 2566 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 19762240

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 25038482

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 21751815

Sources: DTC

Interaction Types & Directionality: positive modulator (activating)

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

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

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: potentiator

Interaction Info:

PMIDs: 18604239 18855614 10592235

Sources: TEND

Interaction Types & Directionality: n/a

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

PMIDs: 16884293 20704351

Sources: DTC ChemblInteractions

Interaction Types & Directionality: antagonist (inhibitory)

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

PMIDs: 17974564 11864636 8693922

Sources: ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: positive modulator (activating) potentiator

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

PMIDs: 2892106 3017690

Sources: 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

PMIDs: 6738302 2867566

Sources: 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

PMIDs: 20138190 18384456

Sources: ChemblInteractions TEND

Interaction Types & Directionality: potentiator

Interaction Info:

PMIDs: 6320036 6148400

Sources: TEND

Interaction Types & Directionality: positive modulator (activating) potentiator

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

PMIDs: 639854 2889803

Sources: 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

PMIDs: 11752090 18384456

Sources: ChemblInteractions TEND

Interaction Types & Directionality: potentiator

Interaction Info:

PMIDs: 11752090 18384456

Sources: TEND

Interaction Types & Directionality: potentiator

Interaction Info:

Interaction Types & Directionality:

n/a

PMIDs:
19762240

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
25038482

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
21751815

Sources:
DTC

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Direct Interaction yes

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

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

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:

potentiator

PMIDs:
18604239 18855614 10592235

Sources:
TEND

Interaction Types & Directionality:

n/a

Interaction Info:

Direct Interaction yes

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

PMIDs:
16884293 20704351

Sources:
DTC ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

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

Direct Interaction yes

PMIDs:
17974564 11864636 8693922

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

Direct Interaction yes

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

PMIDs:
2892106 3017690

Sources:
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

PMIDs:
6738302 2867566

Sources:
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

PMIDs:
20138190 18384456

Sources:
ChemblInteractions TEND

Interaction Types & Directionality:

potentiator

PMIDs:
6320036 6148400

Sources:
TEND

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

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

Direct Interaction yes

PMIDs:
639854 2889803

Sources:
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

PMIDs:
11752090 18384456

Sources:
ChemblInteractions TEND

Interaction Types & Directionality:

potentiator

PMIDs:
11752090 18384456

Sources:
TEND

Interaction Types & Directionality:

potentiator

PMIDs:
11752090 18384456

Sources:
TEND

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

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

Direct Interaction yes

PMIDs:
7773620

Sources:
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

PMIDs:
11752090 18384456

Sources:
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

PMIDs:
11752090 18384456

Sources:
ChemblInteractions TEND

Interaction Types & Directionality:

n/a

PMIDs:
16884293