DGIdb - GABRA1 Gene Record

GABRA1 2554 Druggable Genome

Alternate Names:

2554
GAMMA-AMINOBUTYRIC ACID TYPE A RECEPTOR ALPHA1 SUBUNIT
GABRA1
ECA4
EIEE19
EJM
EJM5
137160
4075
ENSG00000022355
OTTHUMG00000163586
GABA(A) receptor subunit alpha-1
Gamma-aminobutyric acid receptor subunit alpha-1
P14867
GBRA1_HUMAN
404
NP_000797
NM_000806
GAMMA-AMINOBUTYRIC-ACID RECEPTOR ALPHA-1 SUBUNIT PRECURSOR (GABA(A) RECEPTOR). [SOURCE:UNIPROT/SWISSPROT;ACC:P14867]
GABA<sub>A</sub> receptor α1 subunit
GABRD
PA28489
GABA(A) receptor alpha-1
T51487
gamma-aminobutyric acid type A receptor subunit alpha1
DEE19

Gene Info:

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

(8 More Sources)

Gene Categories: Category Details

ION CHANNEL
DRUGGABLE GENOME

Publications:

Möhler et al., 2002, A new benzodiazepine pharmacology., J. Pharmacol. Exp. Ther.
Riss et al., 2008, Benzodiazepines in epilepsy: pharmacology and pharmacokinetics., Acta Neurol. Scand.
Zhu S et al., 2018, Structure of a human synaptic GABA<sub>A</sub> receptor., Nature
Sigel E et al., 2012, Structure, function, and modulation of GABA(A) receptors., J Biol Chem
Yamakura et al., 2001, Anesthetics and ion channels: molecular models and sites of action., Annu. Rev. Pharmacol. Toxicol.
Feigenspan et al., 2004, Electrophysiological properties of mouse horizontal cell GABAA receptors., J. Neurophysiol.
Davies et al., 2001, Pressure-sensitive and -insensitive coupling in gamma-aminobutyric acid(A) receptors., Psychopharmacology (Berl.)
Whiting, 2003, The GABAA receptor gene family: new opportunities for drug development., Curr Opin Drug Discov Devel
Mehta et al., 1999, An update on GABAA receptors., Brain Res. Brain Res. Rev.
Rahman et al., 2006, GABA-site antagonism and pentobarbital actions do not depend on the alpha-subunit type in the recombinant rat GABA receptor., Acta Physiol (Oxf)
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Krasowski et al., 1999, General anaesthetic actions on ligand-gated ion channels., Cell. Mol. Life Sci.
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
Steinbach et al., 2001, Modulation of GABA(A) receptor channel gating by pentobarbital., J. Physiol. (Lond.)
Koltchine et al., 1996, Chimeric GABAA/glycine receptors: expression and barbiturate pharmacology., Neuropharmacology
Verster et al., 2004, Clinical pharmacology, clinical efficacy, and behavioral toxicity of alprazolam: a review of the literature., CNS Drug Rev
McCracken et al., 2010, A transmembrane amino acid in the GABAA receptor β2 subunit critical for the actions of alcohols and anesthetics., J. Pharmacol. Exp. Ther.
Seo et al., 2010, Genetic reduction of GABA(A) receptor gamma2 subunit expression potentiates the immobilizing action of isoflurane., Neurosci. Lett.
Braga et al., 2009, Topiramate reduces excitability in the basolateral amygdala by selectively inhibiting GluK1 (GluR5) kainate receptors on interneurons and positively modulating GABAA receptors on principal neurons., J. Pharmacol. Exp. Ther.
Nowakowska et al., 2009, Memory improving and antidepressant effects of topiramate in rats., Arzneimittelforschung
Garnett WR, 2000, Clinical pharmacology of topiramate: a review., Epilepsia
Chung JY et al., 2014, Efficacy of zonisamide in migraineurs with nonresponse to topiramate., Biomed Res Int
de Fiebre et al., 1992, Classical genetic analyses of responses to sedative-hypnotic drugs in crosses derived from long-sleep and short-sleep mice., Alcohol. Clin. Exp. Res.
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.
Amin et al., 1997, Two tyrosine residues on the alpha subunit are crucial for benzodiazepine binding and allosteric modulation of gamma-aminobutyric acidA receptors., Mol. Pharmacol.
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
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.
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.
Greenblatt et al., 2001, Divergence of volatile anesthetic effects in inhibitory neurotransmitter receptors., Anesthesiology
Franks, 2006, Molecular targets underlying general anaesthesia., Br. J. Pharmacol.
Grasshoff et al., 2006, Effects of isoflurane and enflurane on GABAA and glycine receptors contribute equally to depressant actions on spinal ventral horn neurones in rats., Br J Anaesth
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
Roden et al., 2010, Altered GABA(A) receptor subunit expression and pharmacology in human Angelman syndrome cortex., Neurosci. Lett.
Nutt et al., 2010, Searching for perfect sleep: the continuing evolution of GABAA receptor modulators as hypnotics., J. Psychopharmacol. (Oxford)
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.
Wadworth AN et al., 1993, Zopiclone. A review of its pharmacological properties and therapeutic efficacy as an hypnotic., Drugs Aging
Dixon CL et al., 2015, Zolpidem and eszopiclone prime α1β2γ2 GABAA receptors for longer duration of activity., Br J Pharmacol
Döble A et al., 1995, The mechanism of action of zopiclone., Eur Psychiatry
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
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
Martin et al., 2009, Etomidate targets alpha5 gamma-aminobutyric acid subtype A receptors to regulate synaptic plasticity and memory blockade., Anesthesiology
Desai et al., 2009, Gamma-amino butyric acid type A receptor mutations at beta2N265 alter etomidate efficacy while preserving basal and agonist-dependent activity., Anesthesiology
Pritchett et al., 1990, Gamma-aminobutyric acidA receptor alpha 5-subunit creates novel type II benzodiazepine receptor pharmacology., J. Neurochem.
Smith et al., 2001, Effect of alpha subunit on allosteric modulation of ion channel function in stably expressed human recombinant gamma-aminobutyric acid(A) receptors determined using (36)Cl ion flux., Mol. Pharmacol.
Vlainić et al., 2009, Effects of acute and repeated zolpidem treatment on pentylenetetrazole-induced seizure threshold and on locomotor activity: comparison with diazepam., Neuropharmacology
Tan KR et al., 2011, Hooked on benzodiazepines: GABAA receptor subtypes and addiction., Trends Neurosci
Sramka M et al., 1975, Surgical complication of posterior hypothalamotomy., Confin Neurol
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
Nakatsuka et al., 1985, Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity., Life Sci.
Franks NP et al., 1994, Molecular and cellular mechanisms of general anaesthesia., Nature
Qi ZH et al., 2007, Protein kinase C epsilon regulates gamma-aminobutyrate type A receptor sensitivity to ethanol and benzodiazepines through phosphorylation of gamma2 subunits., J Biol 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.
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.
Terzano et al., 2003, New drugs for insomnia: comparative tolerability of zopiclone, zolpidem and zaleplon., Drug Saf
Sanger et al., 1999, Discriminative stimulus effects of drugs acting at GABA(A) receptors: differential profiles and receptor selectivity., Pharmacol. Biochem. Behav.
Patat et al., 2001, Pharmacodynamic profile of Zaleplon, a new non-benzodiazepine hypnotic agent., Hum Psychopharmacol
Barbera et al., 2005, Benefit-risk assessment of zaleplon in the treatment of insomnia., Drug Saf
Agmo et al., 1998, Interactions between dopamine and GABA in the control of ambulatory activity and neophobia in the mouse., Pharmacol. Biochem. Behav.
Grech et al., 1993, Pentobarbital-like discriminative stimulus effects of direct GABA agonists in rats., Psychopharmacology (Berl.)
Fadda et al., 1985, Suppression by progabide of ethanol withdrawal syndrome in rats., Eur. J. 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.
Sanger, 2004, The pharmacology and mechanisms of action of new generation, non-benzodiazepine hypnotic agents., CNS Drugs
Skerritt et al., 1983, Enhancement of GABA binding by benzodiazepines and related anxiolytics., Eur. J. Pharmacol.
Zhou BT et al., 2012, Effects of SCN1A and GABA receptor genetic polymorphisms on carbamazepine tolerability and efficacy in Chinese patients with partial seizures: 2-year longitudinal clinical follow-up., CNS Neurosci Ther
Grasshoff et al., 2008, Depression of spinal network activity by thiopental: shift from phasic to tonic GABA(A) receptor-mediated inhibition., Neuropharmacology
Sugimura et al., 2002, Effects of GABAergic agents on anesthesia induced by halothane, isoflurane, and thiamylal in mice., Pharmacol. Biochem. Behav.
Moody et al., 1988, The imidazobenzodiazepine Ro 15-4513 antagonizes methoxyflurane anesthesia., Life Sci.
Moody et al., 1988, Modulation of the benzodiazepine/gamma-aminobutyric acid receptor chloride channel complex by inhalation anesthetics., J. Neurochem.
Krasowski et al., 2000, The actions of ether, alcohol and alkane general anaesthetics on GABAA and glycine receptors and the effects of TM2 and TM3 mutations., Br. J. Pharmacol.
Stewart DS et al., 2011, p-(4-Azipentyl)propofol: a potent photoreactive general anesthetic derivative of propofol., J 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.
Giersch et al., 2010, Atypical behavioural effects of lorazepam: clues to the design of novel therapies?, Pharmacol. Ther.
Hedera P et al., 2013, Pharmacotherapy of essential tremor., J Cent Nerv Syst Dis
Cutrer et al., Attenuation by butalbital of capsaicin-induced c-fos-like immunoreactivity in trigeminal nucleus caudalis., Headache
Nishikawa K et al., 2002, Volatile anesthetic actions on the GABAA receptors: contrasting effects of alpha 1(S270) and beta 2(N265) point mutations., Neuropharmacology
Nishikawa K et al., 2003, The actions of sevoflurane and desflurane on the gamma-aminobutyric acid receptor type A: effects of TM2 mutations in the alpha and beta subunits., Anesthesiology
Richter et al., 2010, Intrinsic activation of GABA(A) receptors suppresses epileptiform activity in the cerebral cortex of immature mice., Epilepsia
Law et al., 2008, Gaba receptor insecticide non-competitive antagonists may bind at allosteric modulator sites., Int. J. Neurosci.
Macdonald et al., 1986, Anticonvulsant drugs: mechanisms of action., Adv Neurol
Peters et al., 1988, Modulation of the GABAA receptor by depressant barbiturates and pregnane steroids., Br. J. Pharmacol.
Miller et al., 1988, Acute barbiturate administration increases benzodiazepine receptor binding in vivo., Psychopharmacology (Berl.)
Kirkness et al., 1986, The gamma-aminobutyrate/benzodiazepine receptor from pig brain. Purification and characterization of the receptor complex from cerebral cortex and cerebellum., Biochem. J.
Zaugg J et al., 2011, Identification and characterization of GABA(A) receptor modulatory diterpenes from Biota orientalis that decrease locomotor activity in mice., J Nat Prod
Podhorna et al., 2000, Behavioural effects of a benzodiazepine receptor partial agonist, Ro 19-8022, in the social conflict test in mice., Behav Pharmacol
Tanaka et al., 2008, Comparison of short- and long-acting benzodiazepine-receptor agonists with different receptor selectivity on motor coordination and muscle relaxation following thiopental-induced anesthesia in mice., J. Pharmacol. Sci.
Smeyatsky et al., 1992, The treatment of sleep disorders., S. Afr. Med. J.
Skerritt et al., 1983, Interactions of some anaesthetic, convulsant, and anticonvulsant drugs at GABA-benzodiazepine receptor-ionophore complexes in rat brain synaptosomal membranes., Neurochem. Res.
Tomlin et al., 1999, Preparation of barbiturate optical isomers and their effects on GABA(A) receptors., Anesthesiology
Earl et al., 2011, Inhibition of recombinant L-type voltage-gated calcium channels by positive allosteric modulators of GABAA receptors., J. Pharmacol. Exp. Ther.
Davies, 2003, The role of GABAA receptors in mediating the effects of alcohol in the central nervous system., J Psychiatry Neurosci
Santhakumar et al., 2007, Ethanol acts directly on extrasynaptic subtypes of GABAA receptors to increase tonic inhibition., Alcohol
Petersen JG et al., 2014, Synthesis and pharmacological evaluation of 6-aminonicotinic acid analogues as novel GABA(A) receptor agonists., Eur J Med Chem
Carta et al., 2006, The muscle relaxant thiocolchicoside is an antagonist of GABAA receptor function in the central nervous system., Neuropharmacology
Mascia et al., 2007, Thiocolchicoside inhibits the activity of various subtypes of recombinant GABA(A) receptors expressed in Xenopus laevis oocytes., Eur. J. Pharmacol.
Keppel Hesselink JM, 2017, Phenytoin: a step by step insight into its multiple mechanisms of action-80 years of mechanistic studies in neuropharmacology., J Neurol
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

METHOHEXITAL GABRA1

Interaction Score: 4.6

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
9014160 17016423 17139284 11752352

Sources:
TdgClinicalTrial TEND TTD
AMOBARBITAL GABRA1

Interaction Score: 3.95

Interaction Types & Directionality:

potentiator

Interaction Info:

PMIDs:
14579514 10209232 11264449 11752352 10487207

Sources:
TTD
BARBITAL GABRA1

Interaction Score: 3.29

Interaction Types & Directionality:

potentiator

Interaction Info:

PMIDs:
14579514 10209232 11264449 10487207

Sources:
TTD
INDIPLON GABRA1

Interaction Score: 2.63

Interaction Types & Directionality:

positive modulator (activating)

allosteric modulator

Interaction Info:

Mechanism of Interaction GABA receptor alpha-1 subunit positive allosteric modulator

Direct Interaction yes

Trial Name Indiplon

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions GuideToPharmacology TTD
PROGABIDE GABRA1

Interaction Score: 2.3

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
9443561 7831422 17016423 17139284 2985405

Sources:
TdgClinicalTrial TEND
THIAMYLAL GABRA1

Interaction Score: 1.64

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
18619475 11264449 14579514 10209232 10487207 11900777 17016423 17139284

Sources:
TdgClinicalTrial TEND
ZALEPLON GABRA1

Interaction Score: 1.64

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

Direct Interaction yes

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

Trial Name AZ-007, Staccato zaleplon

PMIDs:
12608888 10515302 12404558 15783240 17016423 17139284

Sources:
TdgClinicalTrial ChemblInteractions TEND TTD
ZOPICLONE GABRA1

Interaction Score: 0.92

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
20303942 15291009 19942638 6135616 18973287

Sources:
TdgClinicalTrial TEND
SECOBARBITAL GABRA1

Interaction Score: 0.85

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
2850060 11264449 2906155 3006661 14579514 10209232 11752352 10487207 17016423 17139284

Sources:
TdgClinicalTrial TEND TTD

ZOLPIDEM GABRA1

Interaction Score: 0.8

Interaction Types & Directionality:

agonist (activating)

allosteric modulator

potentiator

Interaction Info:

Details of the Assay for Interaction Assay using recombinant GABAA channels with subunit composition; α1β3γ2.

Specific Action of the Ligand Positive

Endogenous Drug? False

PMIDs:
2157817 17016423 17139284 11306694 19345234 21353710 1093783

Sources:
TdgClinicalTrial TEND GuideToPharmacology TTD

HEXOBARBITAL GABRA1

Interaction Score: 0.72

Interaction Types & Directionality:

potentiator

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
11264449 14579514 10209232 11752352 10487207 10360871 17016423 17139284

Sources:
TdgClinicalTrial TEND TTD
ISOPIMARIC ACID GABRA1

Interaction Score: 0.66

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21793559

Sources:
DTC
BUTETHAL GABRA1

Interaction Score: 0.66

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11264449 14579514 10209232 11752352 10487207 17016423 17139284

Sources:
TdgClinicalTrial TEND TTD
SANDARACOPIMARIC ACID GABRA1

Interaction Score: 0.66

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21793559

Sources:
DTC
MEPHOBARBITAL GABRA1

Interaction Score: 0.66

Interaction Types & Directionality:

potentiator

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
14579514 10209232 11752352 21194017 11264449 10487207 20692323 17016423 17139284

Sources:
TdgClinicalTrial TEND TTD
PENTOBARBITAL GABRA1

Interaction Score: 0.49

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:
11264449 15240758 11605100 14579514 10209232 16866778 11752352 10487207 17016423 17139284 11744750

Sources:
TdgClinicalTrial ChemblInteractions TEND TTD
ETOMIDATE GABRA1

Interaction Score: 0.43

Interaction Types & Directionality:

positive modulator (activating)

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name -

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

PMIDs:
16884293 20704351 19809285 17016423 17139284 11752352 19741491

Sources:
DTC TdgClinicalTrial ChemblInteractions TEND
THIOPENTAL GABRA1

Interaction Score: 0.42

Interaction Types & Directionality:

potentiator

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
14579514 10209232 18619475 11264449 10487207

Sources:
TdgClinicalTrial TEND
THIOCOLCHICOSIDE GABRA1

Interaction Score: 0.39

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
16806306 17234181

Sources:
TTD
BUTALBITAL GABRA1

Interaction Score: 0.39

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:
11279945 11264449 14579514 10209232 11752352 10487207 17016423 17139284

Sources:
TdgClinicalTrial ChemblInteractions TEND TTD
CHEMBL2170369 GABRA1

Interaction Score: 0.33

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21751815

Sources:
DTC
ISONIPECOTIC ACID GABRA1

Interaction Score: 0.33

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25038482

Sources:
DTC
METHARBITAL GABRA1

Interaction Score: 0.33

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:
11264449 14579514 10209232 11752352 10487207 17016423 17139284

Sources:
TdgClinicalTrial ChemblInteractions TEND
BUTABARBITAL GABRA1

Interaction Score: 0.33

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
10209232 11264449

Sources:
TdgClinicalTrial TEND TTD
QUAZEPAM GABRA1

Interaction Score: 0.33

Interaction Types & Directionality:

ligand

positive modulator (activating)

potentiator

Interaction Info:

Direct Interaction yes

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

Trial Name -

PMIDs:
2892106 11752352 17016423 17139284 3017690 29950725 23038269

Sources:
TdgClinicalTrial ChemblInteractions TEND
TALBUTAL GABRA1

Interaction Score: 0.33

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:
11264449 14579514 10209232 11752352 10487207 17016423 17139284

Sources:
TdgClinicalTrial ChemblInteractions TEND
HALAZEPAM GABRA1

Interaction Score: 0.33

Interaction Types & Directionality:

ligand

positive modulator (activating)

potentiator

Interaction Info:

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

Direct Interaction yes

Trial Name -

PMIDs:
11752352 17016423 17139284 6738302 2867566 29950725 23038269

Sources:
TdgClinicalTrial ChemblInteractions TEND
METHYPRYLON GABRA1

Interaction Score: 0.33

Interaction Types & Directionality:

positive modulator (activating)

agonist (activating)

Interaction Info:

Direct Interaction yes

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

Trial Name -

PMIDs:
17016423 17139284 11752352 1352660

Sources:
TdgClinicalTrial ChemblInteractions TEND TTD
NITRAZEPAM GABRA1

Interaction Score: 0.31

Interaction Types & Directionality:

ligand

positive modulator (activating)

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
10877119 11752090 11752352 18603831 18384456 29950725 23038269

Sources:
TdgClinicalTrial TEND TTD
BICUCULLINE GABRA1

Interaction Score: 0.28

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Binding Site for Interaction GABA site

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
17875639

Sources:
DTC GuideToPharmacology
PRAZEPAM GABRA1

Interaction Score: 0.27

Interaction Types & Directionality:

ligand

positive modulator (activating)

potentiator

Interaction Info:

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

Direct Interaction yes

Trial Name -

PMIDs:
11752352 17016423 17139284 9145922 29950725 23038269

Sources:
TdgClinicalTrial ChemblInteractions TEND
PICROTOXIN GABRA1

Interaction Score: 0.26

Interaction Types & Directionality:

antagonist (inhibitory)

blocker (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand None

PMIDs:
11752352 17016423 17139284 20491873 18446586

Sources:
TdgClinicalTrial TEND GuideToPharmacology TTD
ESZOPICLONE GABRA1

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 Lunesta

PMIDs:
19942638 18973287 8241608 25817320 19698408

Sources:
TdgClinicalTrial ChemblInteractions
MEPROBAMATE GABRA1

Interaction Score: 0.26

Interaction Types & Directionality:

positive modulator (activating)

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction GABA-A receptor; anion channel agonist

Trial Name -

PMIDs:
9067327 19244096 11752352

Sources:
TdgClinicalTrial ChemblInteractions TEND TTD
PRIMIDONE GABRA1

Interaction Score: 0.25

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

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

Direct Interaction yes

Trial Name -

PMIDs:
11264449 14579514 10209232 11752352 10487207 17016423 17139284 24385718

Sources:
TdgClinicalTrial ChemblInteractions TEND TTD

FLUMAZENIL GABRA1

Interaction Score: 0.24

Interaction Types & Directionality:

positive modulator (activating)

allosteric modulator

antagonist (inhibitory)

Interaction Info:

Specific Binding Site for Interaction benzodiazepine site

Details of the Assay for Interaction Affinity measured using α1β3γ2 receptors.

Specific Action of the Ligand Antagonist

PMIDs:
11864636 17016423 8693922

Sources:
TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology

METHOXYFLURANE GABRA1

Interaction Score: 0.24

Interaction Types & Directionality:

positive modulator (activating)

agonist (activating)

Interaction Info:

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

Direct Interaction yes

PMIDs:
2845216 2459308 10683198 11752352 17016423 17139284

Sources:
ChemblInteractions TTD
CLOTIAZEPAM GABRA1

Interaction Score: 0.23

Interaction Types & Directionality:

ligand

positive modulator (activating)

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
18604239 18855614 29950725 23038269

Sources:
TdgClinicalTrial TEND
ADINAZOLAM GABRA1

Interaction Score: 0.23

Interaction Types & Directionality:

ligand

positive modulator (activating)

potentiator

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
6320036 6148400 29950725 23038269

Sources:
TdgClinicalTrial TEND
CLONAZEPAM GABRA1

Interaction Score: 0.23

Interaction Types & Directionality:

ligand

positive modulator (activating)

allosteric modulator

Interaction Info:

Trial Name JZP-8

Novel drug target Established target

Details of the Assay for Interaction Assay using recombinant GABAA channels with subunit composition; α1β1γ2.

PMIDs:
11752090 18384456 29950725 23038269

Sources:
TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology

FLUNITRAZEPAM GABRA1

Interaction Score: 0.22

Interaction Types & Directionality:

ligand

positive modulator (activating)

allosteric modulator

Interaction Info:

Specific Binding Site for Interaction benzodiazepine site

Details of the Assay for Interaction Assay using recombinant GABAA channels with subunit composition; α1β3γ2.

Specific Action of the Ligand Positive

PMIDs:
29950725 23038269

Sources:
GuideToPharmacology

ZOLPIDEM TARTRATE GABRA1

Interaction Score: 0.22

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
CLOBAZAM GABRA1

Interaction Score: 0.22

Interaction Types & Directionality:

ligand

positive modulator (activating)

Interaction Info:

Novel drug target Established target

Trial Name Clobazam

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

PMIDs:
11752090 18384456 29950725 23038269

Sources:
TdgClinicalTrial ChemblInteractions TEND
TEMAZEPAM GABRA1

Interaction Score: 0.21

Interaction Types & Directionality:

ligand

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:
20138190 18384456 29950725 23038269

Sources:
TdgClinicalTrial ChemblInteractions TEND
ESTAZOLAM GABRA1

Interaction Score: 0.2

Interaction Types & Directionality:

ligand

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:
639854 2889803 29950725 23038269

Sources:
TdgClinicalTrial ChemblInteractions TEND
DIAZEPAM GABRA1

Interaction Score: 0.2

Interaction Types & Directionality:

ligand

positive modulator (activating)

allosteric modulator

potentiator

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Positive

PMIDs:
15009644 11752090 18384456 29950725 23038269

Sources:
TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology
CINOLAZEPAM GABRA1

Interaction Score: 0.19

Interaction Types & Directionality:

ligand

positive modulator (activating)

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
9145922 29950725 23038269

Sources:
TdgClinicalTrial TEND
FLURAZEPAM GABRA1

Interaction Score: 0.19

Interaction Types & Directionality:

ligand

positive modulator (activating)

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11752090 18384456 29950725 23038269

Sources:
TdgClinicalTrial TEND
CHLORDIAZEPOXIDE GABRA1

Interaction Score: 0.19

Interaction Types & Directionality:

ligand

positive modulator (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

Direct Interaction yes

PMIDs:
6135616 29950725 23038269

Sources:
TdgClinicalTrial ChemblInteractions TEND
OXAZEPAM GABRA1

Interaction Score: 0.18

Interaction Types & Directionality:

ligand

positive modulator (activating)

potentiator

Interaction Info:

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

Direct Interaction yes

Trial Name -

PMIDs:
11752090 18384456 29950725 23038269

Sources:
TdgClinicalTrial ChemblInteractions TEND
TRIAZOLAM GABRA1

Interaction Score: 0.18

Interaction Types & Directionality:

ligand

positive modulator (activating)

allosteric modulator

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 29950725 23038269

Sources:
TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology
ALPRAZOLAM GABRA1

Interaction Score: 0.18

Interaction Types & Directionality:

ligand

positive modulator (activating)

allosteric modulator

Interaction Info:

Direct Interaction yes

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

Specific Binding Site for Interaction benzodiazepine site

PMIDs:
14978513 18384456 29950725 23038269

Sources:
TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology
LORAZEPAM GABRA1

Interaction Score: 0.17

Interaction Types & Directionality:

ligand

positive modulator (activating)

Interaction Info:

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

Direct Interaction yes

Trial Name -

PMIDs:
18384456 29950725 23038269

Sources:
TdgClinicalTrial ChemblInteractions TEND
MK-0777 GABRA1

Interaction Score: 0.16

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
CHEMBL1518572 GABRA1

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
PHENOBARBITAL GABRA1

Interaction Score: 0.16

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11264449 14579514 2871724 10209232 10487207 17016423 17139284

Sources:
TdgClinicalTrial TEND
ISOFLURANE GABRA1

Interaction Score: 0.16

Interaction Types & Directionality:

positive modulator (activating)

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

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

PMIDs:
20826568 17016423 17139284 20097266

Sources:
TdgClinicalTrial ChemblInteractions TEND
BROMAZEPAM GABRA1

Interaction Score: 0.16

Interaction Types & Directionality:

ligand

positive modulator (activating)

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
18384456 29950725 23038269

Sources:
TdgClinicalTrial TEND
MUSCIMOL GABRA1

Interaction Score: 0.15

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Full agonist

PMIDs:
22029276

Sources:
GuideToPharmacology
TOPIRAMATE GABRA1

Interaction Score: 0.14

Interaction Types & Directionality:

positive modulator (activating)

agonist (activating)

Interaction Info:

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

Direct Interaction yes

Trial Name topiramate controlled release,Trokesa

PMIDs:
19417176 19998575 17016423 17139284 10768303 25101297

Sources:
TdgClinicalTrial ChemblInteractions TEND
BREXANOLONE GABRA1

Interaction Score: 0.13

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

PMIDs:
None found

Sources:
TTD
CLORAZEPIC ACID GABRA1

Interaction Score: 0.13

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11752090 18384456

Sources:
TdgClinicalTrial TEND
ENFLURANE GABRA1

Interaction Score: 0.13

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 modulator

PMIDs:
11465594 16402123 16973644

Sources:
TdgClinicalTrial ChemblInteractions TEND
GABOXADOL GABRA1

Interaction Score: 0.12

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

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

Direct Interaction yes

Specific Binding Site for Interaction GABA site

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions GuideToPharmacology
ETHCHLORVYNOL GABRA1

Interaction Score: 0.12

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

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

Direct Interaction yes

PMIDs:
1585214

Sources:
ChemblInteractions TTD
SEVOFLURANE GABRA1

Interaction Score: 0.12

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 -

PMIDs:
17016423 17139284 7509043

Sources:
TdgClinicalTrial ChemblInteractions TEND
FLUDIAZEPAM GABRA1

Interaction Score: 0.12

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
2857046

Sources:
TdgClinicalTrial TEND
BRETAZENIL GABRA1

Interaction Score: 0.11

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
DESFLURANE GABRA1

Interaction Score: 0.11

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:
11752090 18384456

Sources:
TdgClinicalTrial ChemblInteractions TEND
MIDAZOLAM GABRA1

Interaction Score: 0.11

Interaction Types & Directionality:

ligand

positive modulator (activating)

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11752090 18384456 29950725 23038269

Sources:
TdgClinicalTrial TEND
HALOTHANE GABRA1

Interaction Score: 0.11

Interaction Types & Directionality:

positive modulator (activating)

other/unknown

Interaction Info:

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

Direct Interaction yes

PMIDs:
17016423 17139284 11897112 12960553

Sources:
ChemblInteractions
AZIETOMIDATE GABRA1

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16884293

Sources:
DTC
GLUTETHIMIDE GABRA1

Interaction Score: 0.08

Interaction Types & Directionality:

positive modulator (activating)

agonist (activating)

Interaction Info:

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

Direct Interaction yes

PMIDs:
6318143

Sources:
ChemblInteractions
GANAXOLONE GABRA1

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name Ganaxolone

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
RESEQUINIL GABRA1

Interaction Score: 0.07

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
OCINAPLON GABRA1

Interaction Score: 0.07

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
LOREDIPLON GABRA1

Interaction Score: 0.07

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
GABAZINE GABRA1

Interaction Score: 0.07

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
ISOGUVACINE GABRA1

Interaction Score: 0.07

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
ADIPIPLON GABRA1

Interaction Score: 0.07

Interaction Types & Directionality:

partial agonist (activating)

Interaction Info:

Trial Name NG2-73

Novel drug target Established target

Direct Interaction yes

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions
ALCOHOL GABRA1

Interaction Score: 0.05

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
21262851 12921221 11752352 17591544 17016423 17139284

Sources:
TTD
TRICLOFOS SODIUM GABRA1

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
CLORAZEPATE DIPOTASSIUM GABRA1

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
METHOHEXITAL SODIUM GABRA1

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
PENTOBARBITAL SODIUM GABRA1

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
BUTABARBITAL SODIUM GABRA1

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
SECOBARBITAL SODIUM GABRA1

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
PF-06372865 GABRA1

Interaction Score: 0.04

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
CHLORDIAZEPOXIDE HYDROCHLORIDE GABRA1

Interaction Score: 0.04

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Direct Interaction yes

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

PMIDs:
None found

Sources:
ChemblInteractions
THIOPENTAL SODIUM GABRA1

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
MIDAZOLAM HYDROCHLORIDE GABRA1

Interaction Score: 0.04

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Direct Interaction yes

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

PMIDs:
None found

Sources:
ChemblInteractions
THIAMYLAL SODIUM GABRA1

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
REMIMAZOLAM GABRA1

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
PHENYTOIN GABRA1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
28349209

Sources:
PharmGKB
CARBAMAZEPINE GABRA1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22591328

Sources:
PharmGKB
ACAMPROSATE CALCIUM GABRA1

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
PROPOFOL GABRA1

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

Ensembl: ENSG00000022355
- Version: 101_38
Alternate Names:

GABRA1 Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
RussLampel: ENSG00000022355
- Version: 26-July-2011
Alternate Names:

GAMMA-AMINOBUTYRIC-ACID RECEPTOR ALPHA-1 SUBUNIT PRECURSOR (GABA(A) RECEPTOR). [SOURCE:UNIPROT/SWISSPROT;ACC:P14867] Description

GABRA1 Display Id

ENSG00000022355 Ensembl Gene Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:
TEND: P14867
- Version: 01-August-2011
Alternate Names:

2554 Entrez Gene Id

GBRA1_HUMAN Uniprot Id

ENSG00000022355 Ensembl Gene Id

Gene Info:

Target Subclass Channels

Target Subclass Ligand_gated_ion_channels

Target Subclass cys-loop

Publications:
HopkinsGroom: P14867
- Version: 11-September-2012
Alternate Names:

ENSG00000022355 Ensembl Gene Id

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

2554 Entrez Gene Id

Gene Info:

Human Readable Name ION CHANNEL

Interpro Short Name Neur_chan_lig-bd

Human Readable Name DRUGGABLE GENOME

Gene Categories:

ION CHANNEL, DRUGGABLE GENOME

Publications:
TdgClinicalTrial: P14867
- Version: January-2014
Alternate Names:

GABRA1 Gene Symbol

GABRD Gene Symbol

Gene Info:

Target Class Receptors

Target Subclass TC:1.A.9

Publications:
GuideToPharmacology: 2554
- Version: 29-September-2020
Alternate Names:

4075 HUGO Gene ID

4075 HUGO Gene Symbol

gamma-aminobutyric acid type A receptor subunit alpha1 HUGO Gene Name

Gene Info:

GuideToPharmacology Gene Category Name GABAA receptors

GuideToPharmacology Gene Category ID 72

Gene Categories:

ION CHANNEL

Publications:

PharmGKB: GABRA1

Version: 18-August-2020

Alternate Names:

PA28489 PharmGKB ID

Gene Info:

Publications:

Zhou BT et al., 2012, Effects of SCN1A and GABA receptor genetic polymorphisms on carbamazepine tolerability and efficacy in Chinese patients with partial seizures: 2-year longitudinal clinical follow-up., CNS Neurosci Ther

DTC: GABRA1

Version: 02-September-2020

Alternate Names:

Gene Info:

Publications:

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

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

Zaugg J et al., 2011, Identification and characterization of GABA(A) receptor modulatory diterpenes from Biota orientalis that decrease locomotor activity in mice., J Nat Prod

HingoraniCasas: ENSG00000022355
- Version: 31-May-2017
Alternate Names:

ENSG00000022355 Gene Symbol

GABRA1 Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
ChemblInteractions: GABRA1
- Version: chembl_23
Alternate Names:

GABRA1 GENE_SYMBOL

Gamma-aminobutyric acid receptor subunit alpha-1 UNIPROT

GABA(A) receptor subunit alpha-1 UNIPROT

Gene Info:

Publications:
TTD: GABA(A) receptor alpha-1
- Version: 2020.06.01
Alternate Names:

GABRA1 TTD Gene Abbreviation

T51487 TTD Target ID

Gene Info:

Publications:
Pharos: GABRA1
- Version: 01-May-2021
Alternate Names:

Gamma-aminobutyric acid receptor subunit alpha-1 Gene Name

P14867 UniProt ID

Gene Info:

Gene Categories:

ION CHANNEL

Publications:

Mechanism of Interaction	GABA receptor alpha-1 subunit positive allosteric modulator
Direct Interaction	yes
Trial Name	Indiplon

Direct Interaction	yes
Mechanism of Interaction	GABA A receptor alpha-1/beta-1/gamma-2 positive allosteric modulator
Trial Name	AZ-007, Staccato zaleplon

Details of the Assay for Interaction	Assay using recombinant GABA<sub>A</sub> channels with subunit composition; α1β3γ2.
Specific Action of the Ligand	Positive
Endogenous Drug?	False

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

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

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

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

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

Specific Binding Site for Interaction	benzodiazepine site
Details of the Assay for Interaction	Affinity measured using α1β3γ2 receptors.
Specific Action of the Ligand	Antagonist

Trial Name	JZP-8
Novel drug target	Established target
Details of the Assay for Interaction	Assay using recombinant GABA<sub>A</sub> channels with subunit composition; α1β1γ2.

Mechanism of Interaction	GABA-A receptor; agonist GABA site agonist
Direct Interaction	yes
Specific Binding Site for Interaction	GABA site

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

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

Trial Name	NG2-73
Novel drug target	Established target
Direct Interaction	yes

GAMMA-AMINOBUTYRIC-ACID RECEPTOR ALPHA-1 SUBUNIT PRECURSOR (GABA(A) RECEPTOR). [SOURCE:UNIPROT/SWISSPROT;ACC:P14867]	Description
GABRA1	Display Id
ENSG00000022355	Ensembl Gene Id

2554	Entrez Gene Id
GBRA1_HUMAN	Uniprot Id
ENSG00000022355	Ensembl Gene Id

4075	HUGO Gene ID
4075	HUGO Gene Symbol
gamma-aminobutyric acid type A receptor subunit alpha1	HUGO Gene Name

GABRA1	GENE_SYMBOL
Gamma-aminobutyric acid receptor subunit alpha-1	UNIPROT
GABA(A) receptor subunit alpha-1	UNIPROT

Gamma-aminobutyric acid receptor subunit alpha-1	Gene Name
P14867	UniProt ID

GABRA1 Gene Record

GABRA1 2554 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 9014160 17016423 17139284 11752352

Sources: TdgClinicalTrial TEND TTD

Interaction Types & Directionality: potentiator

Interaction Info:

PMIDs: 14579514 10209232 11264449 11752352 10487207

Sources: TTD

Interaction Types & Directionality: potentiator

Interaction Info:

PMIDs: 14579514 10209232 11264449 10487207

Sources: TTD

Interaction Types & Directionality: positive modulator (activating) allosteric modulator

Interaction Info: Mechanism of Interaction GABA receptor alpha-1 subunit positive allosteric modulator Direct Interaction yes Trial Name Indiplon

PMIDs: None found

Sources: TdgClinicalTrial ChemblInteractions GuideToPharmacology TTD

Interaction Types & Directionality: agonist (activating)

Interaction Info: Novel drug target Established target Trial Name -

PMIDs: 9443561 7831422 17016423 17139284 2985405

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: agonist (activating)

Interaction Info: Novel drug target Established target Trial Name -

PMIDs: 18619475 11264449 14579514 10209232 10487207 11900777 17016423 17139284

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: positive modulator (activating) potentiator

Interaction Info: Direct Interaction yes Mechanism of Interaction GABA A receptor alpha-1/beta-1/gamma-2 positive allosteric modulator Trial Name AZ-007, Staccato zaleplon

PMIDs: 12608888 10515302 12404558 15783240 17016423 17139284

Sources: TdgClinicalTrial ChemblInteractions TEND TTD

Interaction Types & Directionality: potentiator

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 20303942 15291009 19942638 6135616 18973287

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: potentiator

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 2850060 11264449 2906155 3006661 14579514 10209232 11752352 10487207 17016423 17139284

Sources: TdgClinicalTrial TEND TTD

Interaction Types & Directionality: agonist (activating) allosteric modulator potentiator

Interaction Info: Details of the Assay for Interaction Assay using recombinant GABA<sub>A</sub> channels with subunit composition; &alpha;1&beta;3&gamma;2. Specific Action of the Ligand Positive Endogenous Drug? False

PMIDs: 2157817 17016423 17139284 11306694 19345234 21353710 1093783

Sources: TdgClinicalTrial TEND GuideToPharmacology TTD

Interaction Types & Directionality: potentiator

Interaction Info: Novel drug target Established target Trial Name -

PMIDs: 11264449 14579514 10209232 11752352 10487207 10360871 17016423 17139284

Sources: TdgClinicalTrial TEND TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 21793559

Sources: DTC

Interaction Types & Directionality: potentiator

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 11264449 14579514 10209232 11752352 10487207 17016423 17139284

Sources: TdgClinicalTrial TEND TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 21793559

Sources: DTC

Interaction Types & Directionality: potentiator

Interaction Info: Novel drug target Established target Trial Name -

PMIDs: 14579514 10209232 11752352 21194017 11264449 10487207 20692323 17016423 17139284

Sources: TdgClinicalTrial TEND TTD

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: 11264449 15240758 11605100 14579514 10209232 16866778 11752352 10487207 17016423 17139284 11744750

Sources: TdgClinicalTrial ChemblInteractions TEND TTD

Interaction Types & Directionality: positive modulator (activating) agonist (activating)

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

PMIDs: 16884293 20704351 19809285 17016423 17139284 11752352 19741491

Sources: DTC TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality: potentiator

Interaction Info: Novel drug target Established target Trial Name -

PMIDs: 14579514 10209232 18619475 11264449 10487207

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info:

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
9014160 17016423 17139284 11752352

Sources:
TdgClinicalTrial TEND TTD

Interaction Types & Directionality:

potentiator

PMIDs:
14579514 10209232 11264449 11752352 10487207

Sources:
TTD

Interaction Types & Directionality:

potentiator

PMIDs:
14579514 10209232 11264449 10487207

Sources:
TTD

Interaction Types & Directionality:

positive modulator (activating)

allosteric modulator

Interaction Info:

Mechanism of Interaction GABA receptor alpha-1 subunit positive allosteric modulator

Direct Interaction yes

Trial Name Indiplon

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions GuideToPharmacology TTD

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
9443561 7831422 17016423 17139284 2985405

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
18619475 11264449 14579514 10209232 10487207 11900777 17016423 17139284

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

Direct Interaction yes

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

Trial Name AZ-007, Staccato zaleplon

PMIDs:
12608888 10515302 12404558 15783240 17016423 17139284

Sources:
TdgClinicalTrial ChemblInteractions TEND TTD

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
20303942 15291009 19942638 6135616 18973287

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
2850060 11264449 2906155 3006661 14579514 10209232 11752352 10487207 17016423 17139284

Sources:
TdgClinicalTrial TEND TTD

Interaction Types & Directionality:

agonist (activating)

allosteric modulator

potentiator

Interaction Info:

Details of the Assay for Interaction Assay using recombinant GABA<sub>A</sub> channels with subunit composition; α1β3γ2.

Specific Action of the Ligand Positive

Endogenous Drug? False

PMIDs:
2157817 17016423 17139284 11306694 19345234 21353710 1093783

Sources:
TdgClinicalTrial TEND GuideToPharmacology TTD

Interaction Types & Directionality:

potentiator

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
11264449 14579514 10209232 11752352 10487207 10360871 17016423 17139284

Sources:
TdgClinicalTrial TEND TTD

Interaction Types & Directionality:

n/a

PMIDs:
21793559

Sources:
DTC

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11264449 14579514 10209232 11752352 10487207 17016423 17139284

Sources:
TdgClinicalTrial TEND TTD

Interaction Types & Directionality:

n/a

PMIDs:
21793559

Sources:
DTC

Interaction Types & Directionality:

potentiator

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
14579514 10209232 11752352 21194017 11264449 10487207 20692323 17016423 17139284

Sources:
TdgClinicalTrial TEND TTD

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:
11264449 15240758 11605100 14579514 10209232 16866778 11752352 10487207 17016423 17139284 11744750

Sources:
TdgClinicalTrial ChemblInteractions TEND TTD

Interaction Types & Directionality:

positive modulator (activating)

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name -

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

PMIDs:
16884293 20704351 19809285 17016423 17139284 11752352 19741491

Sources:
DTC TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality:

potentiator

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
14579514 10209232 18619475 11264449 10487207

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

antagonist (inhibitory)

PMIDs:
16806306 17234181

Sources:
TTD

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:
11279945 11264449 14579514 10209232 11752352 10487207 17016423 17139284

Sources:
TdgClinicalTrial ChemblInteractions TEND TTD

Interaction Types & Directionality:

n/a

PMIDs:
21751815

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
25038482