Page last updated: 2024-08-05 15:01:01

GABA agonist

A drug that binds to and activates gamma-aminobutyric acid receptors.

ChEBI ID: 51373

Members (8)

MemberDefinitionClass
alprazolamA member of the class of triazolobenzodiazepines that is 4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine carrying methyl, phenyl and chloro substituents at positions 1, 6 and 8 respectively. Alprazolam is only found in individuals that have taken this drug.alprazolam
baclofenA monocarboxylic acid that is butanoic acid substituted by an amino group at position 4 and a 4-chlorophenyl group at position 3. It acts as a central nervous system depressant, GABA agonist and muscle relaxant.baclofen zwitterion; baclofen
ethylenediamineAn alkane-alpha,omega-diamine in which the alkane is ethane.ethylenediamine
methaqualoneA member of the class of quinazolines that is quinazolin-4-one substituted at positions 2 and 3 by methyl and o-tolyl groups respectively. A depressant that increases the activity of the GABA receptors in the brain and nervous system, it is used as a sedative and hypnotic medication. It became popular as a recreational drug and club drug in the late 1960s and 1970s.methaqualone
methylimidazoleacetic acidA monocarboxylic acid that is acetic acid in which one of the methyl hydrogens has been replaced by a 1-methyl-1H-imidazol-4-yl group.1-methyl-4-imidazoleacetic acid
muscimolA member of the class of isoxazoles that is 1,2-oxazol-3(2H)-one substituted by an aminomethyl group at position 5. It has been isolated from mushrooms of the genus Amanita.muscimol
tramiprosateAn amino sulfonic acid that is the 3-amino derivative of propanesulfonic acid.3-aminopropanesulfonic acid zwitterion; 3-aminopropanesulfonic acid
zolpidemAn imidazo[1,2-a]pyridine compound having a 4-tolyl group at the 2-position, an N,N-dimethylcarbamoylmethyl group at the 3-position and a methyl substituent at the 6-position.zolpidem

Research

Studies (14,722)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-19903,595 (24.42)18.7374
1990's3,568 (24.24)18.2507
2000's3,543 (24.07)29.6817
2010's3,233 (21.96)24.3611
2020's783 (5.32)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials1,436 (8.75%)5.53%
Reviews959 (5.84%)6.00%
Case Studies1,528 (9.31%)4.05%
Observational39 (0.24%)0.25%
Other12,446 (75.85%)84.16%

Protein Targets (116)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency23.735812
67.9K proteinVaccinia virusPotency3.162311
activating transcription factor 6Homo sapiens (human)Potency0.000211
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency39.810711
AR proteinHomo sapiens (human)Potency17.375569
aryl hydrocarbon receptorHomo sapiens (human)Potency27.293824
arylsulfatase AHomo sapiens (human)Potency2.393411
ATAD5 protein, partialHomo sapiens (human)Potency6.510411
Ataxin-2Homo sapiens (human)Potency13.333212
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency0.756912
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency15.667523
Bloom syndrome protein isoform 1Homo sapiens (human)Potency0.199522
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency27.005012
Chain A, HADH2 proteinHomo sapiens (human)Potency31.622811
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency47.393612
Chain B, HADH2 proteinHomo sapiens (human)Potency31.622811
cytochrome P450 2C19 precursorHomo sapiens (human)Potency39.810711
cytochrome P450 2D6Homo sapiens (human)Potency19.497111
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency12.575224
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency17.376811
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency13.734012
D(1A) dopamine receptorHomo sapiens (human)Potency0.580411
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency89.125111
estrogen nuclear receptor alphaHomo sapiens (human)Potency13.1348814
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency10.464467
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency79.432811
GABA theta subunitRattus norvegicus (Norway rat)Potency12.575212
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency12.575212
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency12.575212
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency12.575212
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency12.575212
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency12.575212
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency12.575212
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency12.575212
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency12.575212
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency12.575212
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency12.575212
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency12.575212
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency12.575212
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency12.575212
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency12.575212
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency12.575212
GLI family zinc finger 3Homo sapiens (human)Potency3.998324
GLS proteinHomo sapiens (human)Potency22.387211
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency17.645233
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency39.810711
lamin isoform A-delta10Homo sapiens (human)Potency3.065414
lethal(3)malignant brain tumor-like protein 1 isoform IHomo sapiens (human)Potency44.668411
LuciferasePhotinus pyralis (common eastern firefly)Potency27.540411
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency28.183811
NFKB1 protein, partialHomo sapiens (human)Potency5.623422
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency53.080411
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency2.253612
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency18.589933
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency40.533411
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency26.832511
phosphopantetheinyl transferaseBacillus subtilisPotency44.668411
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency0.089111
pregnane X nuclear receptorHomo sapiens (human)Potency18.917822
RAR-related orphan receptor gammaMus musculus (house mouse)Potency11.962022
regulator of G-protein signaling 4Homo sapiens (human)Potency0.106211
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency20.425033
TDP1 proteinHomo sapiens (human)Potency27.578126
thioredoxin reductaseRattus norvegicus (Norway rat)Potency8.421612
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency47.438124
thyroid stimulating hormone receptorHomo sapiens (human)Potency31.622822
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency21.130011

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 1BOryctolagus cuniculus (rabbit)IC50100.000011
Amyloid-beta precursor proteinHomo sapiens (human)IC50100.000011
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50133.000011
Bile salt export pumpHomo sapiens (human)IC50133.000011
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50133.000011
Cholecystokinin receptor type ACavia porcellus (domestic guinea pig)IC5064.000011
Cholecystokinin receptor type ARattus norvegicus (Norway rat)IC5064.000011
D-amino-acid oxidaseSus scrofa (pig)IC50100.000022
GABA theta subunitRattus norvegicus (Norway rat)IC500.010169
GABA theta subunitRattus norvegicus (Norway rat)Ki0.020134
Gamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)IC500.016011
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)IC500.010169
Gamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)Ki1.29421441
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Ki0.74501314
Gamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)IC500.016011
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)IC500.010169
Gamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)Ki1.39151239
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Ki0.3452910
Gamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)IC500.016011
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)IC500.010169
Gamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)Ki1.43181441
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Ki0.266089
Gamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)IC500.016011
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)IC500.010169
Gamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)Ki2.1843431
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Ki0.020134
Gamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)IC500.016011
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)IC500.010169
Gamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)Ki3.31701138
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Ki2.873667
Gamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)IC500.016011
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)IC500.010169
Gamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)Ki2.8739734
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Ki3.606789
Gamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)IC500.016011
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)IC500.010169
Gamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)Ki0.023333
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Ki0.020134
Gamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)IC500.016011
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)IC500.010169
Gamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)Ki1.86711138
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Ki1.81402526
Gamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)IC500.016011
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)IC500.010169
Gamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)Ki2.88983232
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Ki1.685956
Gamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)IC500.016011
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)IC500.010169
Gamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)Ki0.008522
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Ki0.020134
Gamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)IC500.016011
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)IC500.010169
Gamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)Ki0.008522
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Ki0.020134
Gamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)IC500.016011
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)IC500.0097710
Gamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)Ki0.008522
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Ki0.020134
Gamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)IC500.016011
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)IC500.010169
Gamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)Ki2.36904269
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Ki2.04282728
Gamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)IC500.016011
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)IC500.010169
Gamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)Ki0.008522
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Ki0.020134
Gamma-aminobutyric acid receptor subunit piHomo sapiens (human)IC500.016011
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)IC500.010169
Gamma-aminobutyric acid receptor subunit piHomo sapiens (human)Ki0.008522
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Ki0.020134
Gamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)IC500.016011
Gamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)Ki0.008522
Gamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)IC500.050011
Gamma-aminobutyric acid type B receptor subunit 1Rattus norvegicus (Norway rat)IC500.276246
Gamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)Ki6.000011
Gamma-aminobutyric acid type B receptor subunit 2Homo sapiens (human)IC500.050011
Gamma-aminobutyric acid type B receptor subunit 2Rattus norvegicus (Norway rat)IC500.276246
Gamma-aminobutyric acid type B receptor subunit 2Homo sapiens (human)Ki6.000011
Gamma-aminobutyric acid type B receptor subunit 2Rattus norvegicus (Norway rat)Ki0.220011
Glutamate receptor 1Rattus norvegicus (Norway rat)IC5010.000011
Glutamate receptor 2Rattus norvegicus (Norway rat)IC5010.000011
Glutamate receptor 3Rattus norvegicus (Norway rat)IC5010.000011
Glutamate receptor 4Rattus norvegicus (Norway rat)IC5010.000011
Glutaminyl-peptide cyclotransferaseMus musculus (house mouse)Ki22,000.000011
Multidrug resistance-associated protein 4Homo sapiens (human)IC50133.000011
Neuronal acetylcholine receptor subunit alpha-7Rattus norvegicus (Norway rat)Ki10.000011
Protein farnesyltransferase subunit betaHomo sapiens (human)IC5015,500.000011
Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alphaHomo sapiens (human)IC5015,500.000011
Proton-coupled amino acid transporter 1Homo sapiens (human)Ki7,100.000011
Sodium- and chloride-dependent betaine transporterRattus norvegicus (Norway rat)IC500.003211
Sodium- and chloride-dependent GABA transporter 1Rattus norvegicus (Norway rat)IC500.003211
Sodium- and chloride-dependent GABA transporter 2Rattus norvegicus (Norway rat)IC500.003211
Sodium- and chloride-dependent GABA transporter 3Rattus norvegicus (Norway rat)IC500.003211
Sphingosine-1-phosphate lyase 1Mus musculus (house mouse)Ki0.765011
Translocator proteinRattus norvegicus (Norway rat)IC504.700011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
AlbuminHomo sapiens (human)Kd63.000011
Bromodomain-containing protein 4Homo sapiens (human)Kd2.460011
Gamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)EC503.313369
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)EC50100.000011
Gamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)EC503.695558
Gamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)EC504.416747
Gamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)EC5027.000011
Gamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)EC5010.003323
Gamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)EC5027.000011
Gamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)EC5027.000011
Gamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)EC502.1371915
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)EC50100.000011
Gamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)EC5027.000011
Gamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)EC500.3612814
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)EC50100.000011
Gamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)EC501.080646
Gamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)Kd2.300011
Gamma-aminobutyric acid receptor subunit rho-2Homo sapiens (human)Kd1.400011
Gamma-aminobutyric acid type B receptor subunit 1Homo sapiens (human)EC501.700011
Gamma-aminobutyric acid type B receptor subunit 2Homo sapiens (human)EC501.700011
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)EC500.191011