DGIdb - GABRP Gene Record

GABRP 2568 Druggable Genome

Alternate Names:

2568
GAMMA-AMINOBUTYRIC ACID TYPE A RECEPTOR PI SUBUNIT
GABRP
602729
4089
ENSG00000094755
OTTHUMG00000130443
O00591
GBRP_HUMAN
Gamma-aminobutyric acid receptor subunit pi
GABA(A) receptor subunit pi
GAMMA-AMINOBUTYRIC-ACID RECEPTOR PI SUBUNIT PRECURSOR (GABA(A) RECEPTOR). [SOURCE:UNIPROT/SWISSPROT;ACC:O00591]
PA28503
gamma-aminobutyric acid type A receptor subunit pi

Gene Info:

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

(7 More Sources)

Gene Categories: Category Details

ION CHANNEL
DRUGGABLE GENOME

Publications:

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.
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
Mandrioli et al., 2008, Benzodiazepine metabolism: an analytical perspective., Curr. Drug Metab.
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.
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
Schove et al., 1994, Molecular determinants of recognition and activation at the cerebellar benzodiazepine receptor site., Bioorg. Med. Chem.
Walash et al., 1994, A selective fluorimetric method for the determination of some 1,4-benzodiazepine drugs containing a hydroxyl group at C-3., J Pharm Biomed Anal
Giersch et al., 2010, Atypical behavioural effects of lorazepam: clues to the design of novel therapies?, Pharmacol. Ther.
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.
Pu M et al., 2013, Influence of genetic polymorphisms in the glutamatergic and GABAergic systems and their interactions with environmental stressors on antidepressant response., Pharmacogenomics
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.

HALAZEPAM GABRP

Interaction Score: 0.26

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
QUAZEPAM GABRP

Interaction Score: 0.26

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

Direct Interaction yes

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

Trial Name -

PMIDs:
2892106 3017690

Sources:
TdgClinicalTrial ChemblInteractions TEND
ADINAZOLAM GABRP

Interaction Score: 0.24

Interaction Types & Directionality:

potentiator

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
6320036 6148400

Sources:
TdgClinicalTrial TEND
TEMAZEPAM GABRP

Interaction Score: 0.23

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 GABRP

Interaction Score: 0.22

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:
639854 2889803

Sources:
TdgClinicalTrial ChemblInteractions TEND
OXAZEPAM GABRP

Interaction Score: 0.2

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 GABRP

Interaction Score: 0.2

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11752090 18384456

Sources:
TdgClinicalTrial TEND
NITRAZEPAM GABRP

Interaction Score: 0.2

Interaction Types & Directionality:

potentiator

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
11752090 18384456

Sources:
TdgClinicalTrial TEND
PRAZEPAM GABRP

Interaction Score: 0.19

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

Novel drug target Established target

Trial Name -

Direct Interaction yes

PMIDs:
7773620

Sources:
TdgClinicalTrial ChemblInteractions TEND
FLUDIAZEPAM GABRP

Interaction Score: 0.18

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
2857046

Sources:
TdgClinicalTrial TEND
ETOMIDATE GABRP

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 GABRP

Interaction Score: 0.18

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
7849137

Sources:
TdgClinicalTrial TEND
CLOTIAZEPAM GABRP

Interaction Score: 0.18

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
18855614

Sources:
TdgClinicalTrial TEND
TRIAZOLAM GABRP

Interaction Score: 0.17

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

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

Direct Interaction yes

Trial Name ARX-03, sufentanil + triazolam NanoTab

PMIDs:
11752090 18384456

Sources:
TdgClinicalTrial ChemblInteractions TEND
DIAZEPAM GABRP

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
BROMAZEPAM GABRP

Interaction Score: 0.15

Interaction Types & Directionality:

potentiator

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
18384456

Sources:
TdgClinicalTrial TEND
CLOBAZAM GABRP

Interaction Score: 0.15

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Trial Name Clobazam

Novel drug target Established target

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

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions TEND
CHLORDIAZEPOXIDE GABRP

Interaction Score: 0.15

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

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

Direct Interaction yes

Trial Name -

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions TEND
LORAZEPAM GABRP

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
VENLAFAXINE GABRP

Interaction Score: 0.14

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23394390

Sources:
PharmGKB
CLONAZEPAM GABRP

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 GABRP

Interaction Score: 0.13

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16884293

Sources:
DTC
MIDAZOLAM GABRP

Interaction Score: 0.11

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11752090 18384456

Sources:
TdgClinicalTrial TEND
ALPRAZOLAM GABRP

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 alprazolam,Xanax, Xanax XR

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions TEND
CLORAZEPIC ACID GABRP

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
None found

Sources:
TdgClinicalTrial TEND
GABOXADOL GABRP

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name gaboxadol

PMIDs:
None found

Sources:
TdgClinicalTrial
TRICLOFOS SODIUM GABRP

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
SECOBARBITAL SODIUM GABRP

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 GABRP

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
CLORAZEPATE DIPOTASSIUM GABRP

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 GABRP

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 GABRP

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 GABRP

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 GABRP

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 GABRP

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 GABRP

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
MIDAZOLAM HYDROCHLORIDE GABRP

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 GABRP

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 GABRP

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 GABRP

Interaction Score: 0.06

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

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

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
OCINAPLON GABRP

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name ocinaplon

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
REMIMAZOLAM GABRP

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 GABRP

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
ESZOPICLONE GABRP

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
FLUMAZENIL GABRP

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

Direct Interaction yes

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

PMIDs:
None found

Sources:
ChemblInteractions
ADIPIPLON GABRP

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name NG2-73

PMIDs:
None found

Sources:
TdgClinicalTrial
METHARBITAL GABRP

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 GABRP

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 GABRP

Interaction Score: 0.05

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Direct Interaction yes

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

PMIDs:
None found

Sources:
ChemblInteractions
TALBUTAL GABRP

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 GABRP

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 GABRP

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 GABRP

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 GABRP

Interaction Score: 0.04

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

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

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
PROPOFOL GABRP

Interaction Score: 0.04

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

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

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
DESFLURANE GABRP

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 GABRP

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 GABRP

Interaction Score: 0.03

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

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

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
SEVOFLURANE GABRP

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 GABRP

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

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

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Ensembl: ENSG00000094755
- Version: 101_38
Alternate Names:

GABRP Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
TEND: O00591
- Version: 01-August-2011
Alternate Names:

O00591 Uniprot Accession

GBRP_HUMAN Uniprot Id

GABRP Gene Symbol

Gene Info:

Target Main Class Receptors

Target Subclass Channels

Target Subclass cys-loop

Publications:
RussLampel: ENSG00000094755
- Version: 26-July-2011
Alternate Names:

GABRP Display Id

GAMMA-AMINOBUTYRIC-ACID RECEPTOR PI SUBUNIT PRECURSOR (GABA(A) RECEPTOR). [SOURCE:UNIPROT/SWISSPROT;ACC:O00591] Description

ENSG00000094755 Ensembl Gene Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:
TdgClinicalTrial: O00591
- Version: January-2014
Alternate Names:

GABRP Gene Symbol

Gene Info:

Target Class Receptors

Target Subclass TC:1.A.9

Publications:
HopkinsGroom: O00591
- Version: 11-September-2012
Alternate Names:

GAMMA-AMINOBUTYRIC ACID RECEPTOR SUBUNIT PI Uniprot Protein Name

ENSG00000094755 Ensembl Gene Id

2568 Entrez Gene Id

Gene Info:

Interpro Name Neurotransmitter-gated ion-channel ligand-binding

Interpro Acc IPR006201

Interpro Acc IPR006202

Gene Categories:

ION CHANNEL, DRUGGABLE GENOME

Publications:

PharmGKB: GABRP

Version: 18-August-2020

Alternate Names:

PA28503 PharmGKB ID

Gene Info:

Publications:

Pu M et al., 2013, Influence of genetic polymorphisms in the glutamatergic and GABAergic systems and their interactions with environmental stressors on antidepressant response., Pharmacogenomics

DTC: GABRP

Version: 02-September-2020

Alternate Names:

Gene Info:

Publications:

Husain SS et al., 2006, Synthesis of trifluoromethylaryl diazirine and benzophenone derivatives of etomidate that are potent general anesthetics and effective photolabels for probing sites on ligand-gated ion channels., J Med Chem

ChemblInteractions: GABRP
- Version: chembl_23
Alternate Names:

GABRP GENE_SYMBOL

Gamma-aminobutyric acid receptor subunit pi UNIPROT

GABA(A) receptor subunit pi UNIPROT

Gene Info:

Publications:
HingoraniCasas: ENSG00000094755
- Version: 31-May-2017
Alternate Names:

ENSG00000094755 Gene Symbol

GABRP Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
IDG: GABRP
- Version: 15-July-2019
Alternate Names:

GABRP Gene Symbol

Gene Info:

Gene Categories:

ION CHANNEL

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

Gamma-aminobutyric acid receptor subunit pi Gene Name

O00591 UniProt ID

Gene Info:

Gene Categories:

ION CHANNEL

Publications:

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

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

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

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

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

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

GABRP	Display Id
GAMMA-AMINOBUTYRIC-ACID RECEPTOR PI SUBUNIT PRECURSOR (GABA(A) RECEPTOR). [SOURCE:UNIPROT/SWISSPROT;ACC:O00591]	Description
ENSG00000094755	Ensembl Gene Id

GAMMA-AMINOBUTYRIC ACID RECEPTOR SUBUNIT PI	Uniprot Protein Name
ENSG00000094755	Ensembl Gene Id
2568	Entrez Gene Id

GABRP	GENE_SYMBOL
Gamma-aminobutyric acid receptor subunit pi	UNIPROT
GABA(A) receptor subunit pi	UNIPROT

Gamma-aminobutyric acid receptor subunit pi	Gene Name
O00591	UniProt ID

positive modulator (activating)
potentiator

positive modulator (activating)
potentiator

positive modulator (activating)
potentiator

positive modulator (activating)
potentiator

GABRP Gene Record

GABRP 2568 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

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: positive modulator (activating) potentiator

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

PMIDs: 2892106 3017690

Sources: TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality: potentiator

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

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: 11752090 18384456

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: positive modulator (activating) potentiator

Interaction Info: Novel drug target Established target Trial Name - Direct Interaction yes

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: Trial Name - Novel drug target Established target

PMIDs: 7849137

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: potentiator

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 18855614

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 ARX-03, sufentanil + triazolam NanoTab

PMIDs: 11752090 18384456

Sources: TdgClinicalTrial ChemblInteractions 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: potentiator

Interaction Info: Novel drug target Established target Trial Name -

PMIDs: 18384456

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: positive modulator (activating)

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

PMIDs: None found

Sources: TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality: positive modulator (activating)

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

PMIDs: None found

Sources: TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality: positive modulator (activating)

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

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:

positive modulator (activating)

potentiator

Interaction Info:

Direct Interaction yes

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

Trial Name -

PMIDs:
2892106 3017690

Sources:
TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality:

potentiator

Interaction Info:

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:

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

Direct Interaction yes

Trial Name -

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:
11752090 18384456

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

Novel drug target Established target

Trial Name -

Direct Interaction yes

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:

Trial Name -

Novel drug target Established target

PMIDs:
7849137

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
18855614

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 ARX-03, sufentanil + triazolam NanoTab

PMIDs:
11752090 18384456

Sources:
TdgClinicalTrial ChemblInteractions 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:

potentiator

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
18384456

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Trial Name Clobazam

Novel drug target Established target

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

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

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

Direct Interaction yes

Trial Name -

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Direct Interaction yes

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

Trial Name -

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality:

n/a

PMIDs:
23394390

Sources:
PharmGKB

Interaction Types & Directionality:

positive modulator (activating)