DGIdb - GABRA5 Gene Record

GABRA5 2558 Druggable Genome

Alternate Names:

2558
GAMMA-AMINOBUTYRIC ACID TYPE A RECEPTOR ALPHA5 SUBUNIT
GABRA5
137142
4079
ENSG00000186297
OTTHUMG00000171824
GABA(A) receptor subunit alpha-5
Gamma-aminobutyric acid receptor subunit alpha-5
P31644
GBRA5_HUMAN
GAMMA-AMINOBUTYRIC-ACID RECEPTOR ALPHA-5 SUBUNIT PRECURSOR (GABA(A) RECEPTOR). [SOURCE:UNIPROT/SWISSPROT;ACC:P31644]
408
NP_000801
NM_000810
GABA<sub>A</sub> receptor α5 subunit
GABA(A) receptor alpha-5
T26368
gamma-aminobutyric acid type A receptor subunit alpha5
DEE79
EIEE79

Gene Info:

Interpro Type	Domain
Human Readable Name	DRUGGABLE GENOME
Interpro Acc	IPR006201
Uniprot Evidence	1: Evidence at protein level
Interpro Acc	IPR006202
Interpro Short Name	Neur_channel
Uniprot Status	Swiss-Prot
Interpro Type	Family
Human Readable Name	ION CHANNEL
Interpro Name	Neurotransmitter-gated ion-channel ligand-binding
Interpro Name	Neurotransmitter-gated ion-channel
Interpro Short Name	Neur_chan_lig-bd
GuideToPharmacology Gene Category Name	GABA<sub>A</sub> receptors
GuideToPharmacology Gene Category ID	72
Target Main Class	Receptors
Target Subclass	Ligand_gated_ion_channels
Target Subclass	Channels
Transmembrane Helix Count	4
Target Subclass	cys-loop
Target Class	Receptors
Target Subclass	TC:1.A.9
Gene Biotype	PROTEIN_CODING

(8 More Sources)

Gene Categories: Category Details

TRANSPORTER
ION CHANNEL
DRUGGABLE GENOME

Publications:

Mehta et al., 1999, An update on GABAA receptors., Brain Res. Brain Res. Rev.
Yamakura et al., 2001, Anesthetics and ion channels: molecular models and sites of action., Annu. Rev. Pharmacol. Toxicol.
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
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
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.
Clément et al., 2009, Pharmacological alterations of anxious behaviour in mice depending on both strain and the behavioural situation., PLoS ONE
Schove et al., 1994, Molecular determinants of recognition and activation at the cerebellar benzodiazepine receptor site., Bioorg. Med. Chem.
Mandrioli et al., 2008, Benzodiazepine metabolism: an analytical perspective., Curr. Drug Metab.
Giersch et al., 2010, Atypical behavioural effects of lorazepam: clues to the design of novel therapies?, Pharmacol. Ther.
Husain SS et al., 2006, Synthesis of trifluoromethylaryl diazirine and benzophenone derivatives of etomidate that are potent general anesthetics and effective photolabels for probing sites on ligand-gated ion channels., J Med Chem
Oblak et al., 2011, Reduced GABAA receptors and benzodiazepine binding sites in the posterior cingulate cortex and fusiform gyrus in autism., Brain Res.
Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
You et al., 2010, Benzodiazepine modulation of the rat GABAA receptor α4β3γ2L subtype expressed in Xenopus oocytes., Neuropharmacology
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
Rho et al., 1997, Barbiturate-like actions of the propanediol dicarbamates felbamate and meprobamate., J. Pharmacol. Exp. Ther.
Gonzalez et al., 2009, Carisoprodol-mediated modulation of GABAA receptors: in vitro and in vivo studies., J. Pharmacol. Exp. Ther.
Derry et al., 2004, Identification of a residue in the gamma-aminobutyric acid type A receptor alpha subunit that differentially affects diazepam-sensitive and -insensitive benzodiazepine site binding., J. Neurochem.
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.
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.
Olsen et al., 2011, GABA(A) receptors as molecular targets of general anesthetics: identification of binding sites provides clues to allosteric modulation., Can J Anaesth
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.
Ramerstorfer et al., 2010, The point mutation gamma 2F77I changes the potency and efficacy of benzodiazepine site ligands in different GABAA receptor subtypes., Eur. J. Pharmacol.
Nutt et al., 2010, Searching for perfect sleep: the continuing evolution of GABAA receptor modulators as hypnotics., J. Psychopharmacol. (Oxford)
Skerritt et al., 1983, Enhancement of GABA binding by benzodiazepines and related anxiolytics., Eur. J. Pharmacol.
Hanson et al., 2008, Structural requirements for eszopiclone and zolpidem binding to the gamma-aminobutyric acid type-A (GABAA) receptor are different., J. Med. Chem.

BASMISANIL GABRA5

Interaction Score: 1.59

Interaction Types & Directionality:

allosteric modulator

Interaction Info:

Details of the Assay for Interaction Binding affinity determined in a radioligand displacement assay: test compound competition for [3H]flumazenil at α5β3γ2 GABAA channels transiently expressed in HEK293 cells.

Specific Action of the Ligand Negative

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology TTD

ZOPICLONE GABRA5

Interaction Score: 0.96

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
20303942 19942638 6135616 18973287

Sources:
TdgClinicalTrial TEND
FLUNITRAZEPAM GABRA5

Interaction Score: 0.62

Interaction Types & Directionality:

allosteric modulator

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

Specific Binding Site for Interaction benzodiazepine site

PMIDs:
20858465 17016423 17139284 20638393

Sources:
TdgClinicalTrial TEND GuideToPharmacology
CHEMBL1077391 GABRA5

Interaction Score: 0.53

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19762240

Sources:
DTC
MEPHOBARBITAL GABRA5

Interaction Score: 0.33

Interaction Types & Directionality:

potentiator

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
21194017 10209232 11264449

Sources:
TdgClinicalTrial TEND
HEXOBARBITAL GABRA5

Interaction Score: 0.32

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
10209232 11264449

Sources:
TdgClinicalTrial TEND
SECOBARBITAL GABRA5

Interaction Score: 0.32

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
10209232 11264449

Sources:
TdgClinicalTrial TEND
BUTETHAL GABRA5

Interaction Score: 0.32

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
10209232 11264449

Sources:
TdgClinicalTrial TEND
THIOPENTAL GABRA5

Interaction Score: 0.29

Interaction Types & Directionality:

potentiator

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
10209232 11264449

Sources:
TdgClinicalTrial TEND
FLUMAZENIL GABRA5

Interaction Score: 0.25

Interaction Types & Directionality:

allosteric modulator

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

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

PMIDs:
19907641

Sources:
TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology TTD
MEPROBAMATE GABRA5

Interaction Score: 0.22

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name -

Mechanism of Interaction GABA-A receptor; anion channel agonist

PMIDs:
9067327 19244096

Sources:
TdgClinicalTrial ChemblInteractions TEND
MK-0777 GABRA5

Interaction Score: 0.2

Interaction Types & Directionality:

allosteric modulator

Interaction Info:

Specific Binding Site for Interaction benzodiazepine site

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
HALAZEPAM GABRA5

Interaction Score: 0.2

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:
6738302 2867566

Sources:
TdgClinicalTrial ChemblInteractions TEND
TALBUTAL GABRA5

Interaction Score: 0.2

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

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

PMIDs:
10209232 11264449

Sources:
TdgClinicalTrial ChemblInteractions TEND
QUAZEPAM GABRA5

Interaction Score: 0.2

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:
2892106 3017690

Sources:
TdgClinicalTrial ChemblInteractions TEND
METHARBITAL GABRA5

Interaction Score: 0.2

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

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

PMIDs:
10209232 11264449

Sources:
TdgClinicalTrial ChemblInteractions TEND
PENTOBARBITAL GABRA5

Interaction Score: 0.2

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

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

Direct Interaction yes

Trial Name -

PMIDs:
10209232 11264449

Sources:
TdgClinicalTrial ChemblInteractions TEND
BUTALBITAL GABRA5

Interaction Score: 0.2

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

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

PMIDs:
10209232 11264449

Sources:
TdgClinicalTrial ChemblInteractions TEND
ADINAZOLAM GABRA5

Interaction Score: 0.19

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
6320036 6148400

Sources:
TdgClinicalTrial TEND
TEMAZEPAM GABRA5

Interaction Score: 0.18

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:
20138190 18384456

Sources:
TdgClinicalTrial ChemblInteractions TEND
ESZOPICLONE GABRA5

Interaction Score: 0.18

Interaction Types & Directionality:

positive modulator (activating)

agonist (activating)

Interaction Info:

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

Direct Interaction yes

Trial Name Lunesta

PMIDs:
19942638 18973287

Sources:
TdgClinicalTrial ChemblInteractions
ESTAZOLAM GABRA5

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 -

PMIDs:
639854 2889803

Sources:
TdgClinicalTrial ChemblInteractions TEND
DIAZEPAM GABRA5

Interaction Score: 0.16

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

Trial Name diazepam rectal gel

Novel drug target Established target

Trial Name NRL-01

PMIDs:
15009644 11752090 18384456

Sources:
TdgClinicalTrial ChemblInteractions TEND
TRIAZOLAM GABRA5

Interaction Score: 0.16

Interaction Types & Directionality:

positive modulator (activating)

allosteric modulator

potentiator

Interaction Info:

Novel drug target Established target

Trial Name ARX-03, sufentanil + triazolam NanoTab

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

PMIDs:
11752090 18384456

Sources:
TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology
BUTABARBITAL GABRA5

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
None found

Sources:
TdgClinicalTrial TEND
OXAZEPAM GABRA5

Interaction Score: 0.15

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
NITRAZEPAM GABRA5

Interaction Score: 0.15

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11752090 18384456

Sources:
TdgClinicalTrial TEND
FLURAZEPAM GABRA5

Interaction Score: 0.15

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11752090 18384456

Sources:
TdgClinicalTrial TEND
GABOXADOL GABRA5

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 GuideToPharmacology
PRAZEPAM GABRA5

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

Trial Name -

PMIDs:
7773620

Sources:
TdgClinicalTrial ChemblInteractions TEND
FLUDIAZEPAM GABRA5

Interaction Score: 0.14

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
2857046

Sources:
TdgClinicalTrial TEND
ETOMIDATE GABRA5

Interaction Score: 0.14

Interaction Types & Directionality:

n/a

Interaction Info:

Direct Interaction yes

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

PMIDs:
16884293

Sources:
DTC ChemblInteractions
CLOTIAZEPAM GABRA5

Interaction Score: 0.14

Interaction Types & Directionality:

potentiator

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
18855614

Sources:
TdgClinicalTrial TEND
CINOLAZEPAM GABRA5

Interaction Score: 0.14

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
7849137

Sources:
TdgClinicalTrial TEND
BRETAZENIL GABRA5

Interaction Score: 0.13

Interaction Types & Directionality:

allosteric modulator

Interaction Info:

Specific Binding Site for Interaction benzodiazepine site

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
PRIMIDONE GABRA5

Interaction Score: 0.12

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

Novel drug target Established target

Trial Name -

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

PMIDs:
10209232 11264449

Sources:
TdgClinicalTrial ChemblInteractions TEND
CLOBAZAM GABRA5

Interaction Score: 0.11

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

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

Direct Interaction yes

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions TEND
BICUCULLINE GABRA5

Interaction Score: 0.11

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Binding Site for Interaction GABA site

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
BROMAZEPAM GABRA5

Interaction Score: 0.11

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
18384456

Sources:
TdgClinicalTrial TEND
CHLORDIAZEPOXIDE GABRA5

Interaction Score: 0.11

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
ALPRAZOLAM GABRA5

Interaction Score: 0.11

Interaction Types & Directionality:

positive modulator (activating)

allosteric modulator

Interaction Info:

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

Direct Interaction yes

Trial Name AZ-002, Staccato alprazolam

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology
CLONAZEPAM GABRA5

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 JZP-8

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions TEND
LORAZEPAM GABRA5

Interaction Score: 0.1

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

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

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions TEND
AZIETOMIDATE GABRA5

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16884293

Sources:
DTC
GABAZINE GABRA5

Interaction Score: 0.09

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Binding Site for Interaction GABA site

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
LOREDIPLON GABRA5

Interaction Score: 0.09

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Direct Interaction yes

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

PMIDs:
None found

Sources:
ChemblInteractions
MUSCIMOL GABRA5

Interaction Score: 0.09

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Binding Site for Interaction GABA site

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
RESEQUINIL GABRA5

Interaction Score: 0.09

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
ISOGUVACINE GABRA5

Interaction Score: 0.09

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Binding Site for Interaction GABA site

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
OCINAPLON GABRA5

Interaction Score: 0.09

Interaction Types & Directionality:

allosteric modulator

Interaction Info:

Trial Name ocinaplon

Novel drug target Established target

Specific Binding Site for Interaction benzodiazepine site

PMIDs:
None found

Sources:
TdgClinicalTrial GuideToPharmacology
GANAXOLONE GABRA5

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name Ganaxolone

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
MIDAZOLAM GABRA5

Interaction Score: 0.09

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11752090 18384456

Sources:
TdgClinicalTrial TEND
ADIPIPLON GABRA5

Interaction Score: 0.08

Interaction Types & Directionality:

partial agonist (activating)

Interaction Info:

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

Direct Interaction yes

Trial Name NG2-73

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions
CLORAZEPIC ACID GABRA5

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial TEND
METHOHEXITAL SODIUM GABRA5

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
SECOBARBITAL SODIUM GABRA5

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
CLORAZEPATE DIPOTASSIUM GABRA5

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 SODIUM GABRA5

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
PF-06372865 GABRA5

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
METHYPRYLON GABRA5

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
BUTABARBITAL SODIUM GABRA5

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
TRICLOFOS SODIUM GABRA5

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
ETHCHLORVYNOL GABRA5

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

Direct Interaction yes

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

PMIDs:
None found

Sources:
ChemblInteractions
CHLORDIAZEPOXIDE HYDROCHLORIDE GABRA5

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
MIDAZOLAM HYDROCHLORIDE GABRA5

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
GLUTETHIMIDE GABRA5

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
THIAMYLAL SODIUM GABRA5

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
THIOPENTAL SODIUM GABRA5

Interaction Score: 0.05

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

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

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
REMIMAZOLAM GABRA5

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name CNS-7056

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
PHENOBARBITAL GABRA5

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
None found

Sources:
TdgClinicalTrial TEND
METHOXYFLURANE GABRA5

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
PICROTOXIN GABRA5

Interaction Score: 0.03

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand None

PMIDs:
None found

Sources:
GuideToPharmacology
ACAMPROSATE CALCIUM GABRA5

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
ISOFLURANE GABRA5

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
PROPOFOL GABRA5

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 GABRA5

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 GABRA5

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 GABRA5

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

Direct Interaction yes

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

PMIDs:
None found

Sources:
ChemblInteractions
SEVOFLURANE GABRA5

Interaction Score: 0.02

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 GABRA5

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: ENSG00000186297
- Version: 101_38
Alternate Names:

GABRA5 Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
HopkinsGroom: P31644
- Version: 11-September-2012
Alternate Names:

ENSG00000186297 Ensembl Gene Id

GAMMA-AMINOBUTYRIC ACID RECEPTOR SUBUNIT ALPHA-5 Uniprot Protein Name

GBRA5_HUMAN Uniprot Id

Gene Info:

Interpro Type Domain

Human Readable Name DRUGGABLE GENOME

Interpro Acc IPR006201

Gene Categories:

ION CHANNEL, DRUGGABLE GENOME

Publications:
TdgClinicalTrial: P31644
- Version: January-2014
Alternate Names:

GABRA5 Gene Symbol

Gene Info:

Target Class Receptors

Target Subclass TC:1.A.9

Publications:
TEND: P31644
- Version: 01-August-2011
Alternate Names:

2558 Entrez Gene Id

ENSG00000186297 Ensembl Gene Id

GBRA5_HUMAN Uniprot Id

Gene Info:

Target Main Class Receptors

Target Subclass Ligand_gated_ion_channels

Target Subclass Channels

Publications:
RussLampel: ENSG00000186297
- Version: 26-July-2011
Alternate Names:

GABRA5 Display Id

GAMMA-AMINOBUTYRIC-ACID RECEPTOR ALPHA-5 SUBUNIT PRECURSOR (GABA(A) RECEPTOR). [SOURCE:UNIPROT/SWISSPROT;ACC:P31644] Description

ENSG00000186297 Ensembl Gene Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:
GuideToPharmacology: 2558
- Version: 29-September-2020
Alternate Names:

4079 HUGO Gene ID

4079 HUGO Gene Symbol

gamma-aminobutyric acid type A receptor subunit alpha5 HUGO Gene Name

Gene Info:

GuideToPharmacology Gene Category Name GABAA receptors

GuideToPharmacology Gene Category ID 72

Gene Categories:

ION CHANNEL

Publications:

DTC: GABRA5

Version: 02-September-2020

Alternate Names:

Gene Info:

Publications:

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

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

HingoraniCasas: ENSG00000186297
- Version: 31-May-2017
Alternate Names:

ENSG00000186297 Gene Symbol

GABRA5 Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
ChemblInteractions: GABRA5
- Version: chembl_23
Alternate Names:

GABRA5 GENE_SYMBOL

Gamma-aminobutyric acid receptor subunit alpha-5 UNIPROT

GABA(A) receptor subunit alpha-5 UNIPROT

Gene Info:

Publications:
TTD: GABA(A) receptor alpha-5
- Version: 2020.06.01
Alternate Names:

GABRA5 TTD Gene Abbreviation

T26368 TTD Target ID

Gene Info:

Publications:
Pharos: GABRA5
- Version: 01-May-2021
Alternate Names:

Gamma-aminobutyric acid receptor subunit alpha-5 Gene Name

P31644 UniProt ID

Gene Info:

Gene Categories:

ION CHANNEL

Publications:
GO: GABRA5
- Version: 01-May-2021
Alternate Names:

Gene Info:

Gene Categories:

TRANSPORTER

Publications:

Details of the Assay for Interaction	Binding affinity determined in a radioligand displacement assay: test compound competition for [<sup>3</sup>H]flumazenil at α5β3γ2 GABA<sub>A</sub> channels transiently expressed in HEK293 cells.
Specific Action of the Ligand	Negative
Endogenous Drug?	False

Trial Name	-
Novel drug target	Established target
Specific Binding Site for Interaction	benzodiazepine site

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

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

Specific Binding Site for Interaction	GABA site
Specific Action of the Ligand	Antagonist
Endogenous Drug?	False

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

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

Trial Name	ocinaplon
Novel drug target	Established target
Specific Binding Site for Interaction	benzodiazepine site

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

allosteric modulator
antagonist (inhibitory)

positive modulator (activating)
potentiator

positive modulator (activating)
potentiator

positive modulator (activating)
potentiator

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

Direct Interaction?	False
Endogenous Drug?	False
Specific Action of the Ligand	None

ENSG00000186297	Ensembl Gene Id
GAMMA-AMINOBUTYRIC ACID RECEPTOR SUBUNIT ALPHA-5	Uniprot Protein Name
GBRA5_HUMAN	Uniprot Id

2558	Entrez Gene Id
ENSG00000186297	Ensembl Gene Id
GBRA5_HUMAN	Uniprot Id

GABRA5	Display Id
GAMMA-AMINOBUTYRIC-ACID RECEPTOR ALPHA-5 SUBUNIT PRECURSOR (GABA(A) RECEPTOR). [SOURCE:UNIPROT/SWISSPROT;ACC:P31644]	Description
ENSG00000186297	Ensembl Gene Id

4079	HUGO Gene ID
4079	HUGO Gene Symbol
gamma-aminobutyric acid type A receptor subunit alpha5	HUGO Gene Name

GABRA5	GENE_SYMBOL
Gamma-aminobutyric acid receptor subunit alpha-5	UNIPROT
GABA(A) receptor subunit alpha-5	UNIPROT

Gamma-aminobutyric acid receptor subunit alpha-5	Gene Name
P31644	UniProt ID

GABRA5 Gene Record

GABRA5 2558 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: allosteric modulator

PMIDs: None found

Sources: GuideToPharmacology TTD

Interaction Types & Directionality: potentiator

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 20303942 19942638 6135616 18973287

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: allosteric modulator potentiator

Interaction Info: Trial Name - Novel drug target Established target Specific Binding Site for Interaction benzodiazepine site

PMIDs: 20858465 17016423 17139284 20638393

Sources: TdgClinicalTrial TEND GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 19762240

Sources: DTC

Interaction Types & Directionality: potentiator

Interaction Info: Novel drug target Established target Trial Name -

PMIDs: 21194017 10209232 11264449

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: potentiator

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 10209232 11264449

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: potentiator

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 10209232 11264449

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: potentiator

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 10209232 11264449

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: potentiator

Interaction Info: Novel drug target Established target Trial Name -

PMIDs: 10209232 11264449

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: allosteric modulator antagonist (inhibitory)

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

PMIDs: 19907641

Sources: TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology TTD

Interaction Types & Directionality: agonist (activating)

Interaction Info: Novel drug target Established target Trial Name - Mechanism of Interaction GABA-A receptor; anion channel agonist

PMIDs: 9067327 19244096

Sources: TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality: allosteric modulator

Interaction Info: Specific Binding Site for Interaction benzodiazepine site Specific Action of the Ligand Antagonist Endogenous Drug? False

PMIDs: None found

Sources: GuideToPharmacology

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: 6738302 2867566

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: 10209232 11264449

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: 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: 10209232 11264449

Sources: TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality: positive modulator (activating) potentiator

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

PMIDs: 10209232 11264449

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: 10209232 11264449

Sources: TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality: potentiator

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 6320036 6148400

Interaction Types & Directionality:

allosteric modulator

PMIDs:
None found

Sources:
GuideToPharmacology TTD

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
20303942 19942638 6135616 18973287

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

allosteric modulator

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

Specific Binding Site for Interaction benzodiazepine site

PMIDs:
20858465 17016423 17139284 20638393

Sources:
TdgClinicalTrial TEND GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
19762240

Sources:
DTC

Interaction Types & Directionality:

potentiator

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
21194017 10209232 11264449

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
10209232 11264449

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
10209232 11264449

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
10209232 11264449

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

potentiator

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
10209232 11264449

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

allosteric modulator

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

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

PMIDs:
19907641

Sources:
TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology TTD

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name -

Mechanism of Interaction GABA-A receptor; anion channel agonist

PMIDs:
9067327 19244096

Sources:
TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality:

allosteric modulator

Interaction Info:

Specific Binding Site for Interaction benzodiazepine site

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

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:
6738302 2867566

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:
10209232 11264449

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:
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:
10209232 11264449

Sources:
TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

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

Direct Interaction yes

Trial Name -

PMIDs:
10209232 11264449

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:
10209232 11264449

Sources:
TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
6320036 6148400

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

Direct Interaction yes

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

Trial Name -

PMIDs:
20138190 18384456

Sources:
TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality:

positive modulator (activating)

agonist (activating)

Interaction Info:

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

Direct Interaction yes

Trial Name Lunesta