GABA agonist

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

ChEBI ID: 51373

Members (8)

Member	Definition	Class
alprazolam	A 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
baclofen	A 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
ethylenediamine	An alkane-alpha,omega-diamine in which the alkane is ethane.	ethylenediamine
methaqualone	A 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methylimidazoleacetic acid	A monocarboxylic acid that is acetic acid in which one of the methyl hydrogens has been replaced by a 1-methyl-1H-imidazol-4-yl group.	1-methyl-4-imidazoleacetic acid
muscimol	A 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
tramiprosate	An amino sulfonic acid that is the 3-amino derivative of propanesulfonic acid.	3-aminopropanesulfonic acid zwitterion; 3-aminopropanesulfonic acid
zolpidem	An 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)

Timeframe	Studies, Drugs with This Role(%)	All Drugs %
pre-1990	3,595 (24.42)	18.7374
1990's	3,568 (24.24)	18.2507
2000's	3,543 (24.07)	29.6817
2010's	3,233 (21.96)	24.3611
2020's	783 (5.32)	2.80

Study Types

Publication Type	Studies, Drugs with this Role (%)	All Drugs (%)
Trials	1,436 (8.75%)	5.53%
Reviews	959 (5.84%)	6.00%
Case Studies	1,528 (9.31%)	4.05%
Observational	39 (0.24%)	0.25%
Other	12,446 (75.85%)	84.16%

Protein Targets (116)

Potency Measurements

Protein	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Drugs
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1	Homo sapiens (human)	Potency	23.7358	1	2
67.9K protein	Vaccinia virus	Potency	3.1623	1	1
activating transcription factor 6	Homo sapiens (human)	Potency	0.0002	1	1
aldehyde dehydrogenase 1 family, member A1	Homo sapiens (human)	Potency	39.8107	1	1
AR protein	Homo sapiens (human)	Potency	17.3755	6	9
aryl hydrocarbon receptor	Homo sapiens (human)	Potency	27.2938	2	4
arylsulfatase A	Homo sapiens (human)	Potency	2.3934	1	1
ATAD5 protein, partial	Homo sapiens (human)	Potency	6.5104	1	1
Ataxin-2	Homo sapiens (human)	Potency	13.3332	1	2
ATP-dependent phosphofructokinase	Trypanosoma brucei brucei TREU927	Potency	0.7569	1	2
ATPase family AAA domain-containing protein 5	Homo sapiens (human)	Potency	15.6675	2	3
Bloom syndrome protein isoform 1	Homo sapiens (human)	Potency	0.1995	2	2
Chain A, 2-oxoglutarate Oxygenase	Homo sapiens (human)	Potency	27.0050	1	2
Chain A, HADH2 protein	Homo sapiens (human)	Potency	31.6228	1	1
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE	Homo sapiens (human)	Potency	47.3936	1	2
Chain B, HADH2 protein	Homo sapiens (human)	Potency	31.6228	1	1
cytochrome P450 2C19 precursor	Homo sapiens (human)	Potency	39.8107	1	1
cytochrome P450 2D6	Homo sapiens (human)	Potency	19.4971	1	1
cytochrome P450 3A4 isoform 1	Homo sapiens (human)	Potency	12.5752	2	4
cytochrome P450 family 3 subfamily A polypeptide 4	Homo sapiens (human)	Potency	17.3768	1	1
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a	Homo sapiens (human)	Potency	13.7340	1	2
D(1A) dopamine receptor	Homo sapiens (human)	Potency	0.5804	1	1
DNA polymerase iota isoform a (long)	Homo sapiens (human)	Potency	89.1251	1	1
estrogen nuclear receptor alpha	Homo sapiens (human)	Potency	13.1348	8	14
estrogen-related nuclear receptor alpha	Homo sapiens (human)	Potency	10.4644	6	7
euchromatic histone-lysine N-methyltransferase 2	Homo sapiens (human)	Potency	79.4328	1	1
GABA theta subunit	Rattus norvegicus (Norway rat)	Potency	12.5752	1	2
Gamma-aminobutyric acid receptor subunit alpha-1	Rattus norvegicus (Norway rat)	Potency	12.5752	1	2
Gamma-aminobutyric acid receptor subunit alpha-2	Rattus norvegicus (Norway rat)	Potency	12.5752	1	2
Gamma-aminobutyric acid receptor subunit alpha-3	Rattus norvegicus (Norway rat)	Potency	12.5752	1	2
Gamma-aminobutyric acid receptor subunit alpha-4	Rattus norvegicus (Norway rat)	Potency	12.5752	1	2
Gamma-aminobutyric acid receptor subunit alpha-5	Rattus norvegicus (Norway rat)	Potency	12.5752	1	2
Gamma-aminobutyric acid receptor subunit alpha-6	Rattus norvegicus (Norway rat)	Potency	12.5752	1	2
Gamma-aminobutyric acid receptor subunit beta-1	Rattus norvegicus (Norway rat)	Potency	12.5752	1	2
Gamma-aminobutyric acid receptor subunit beta-2	Rattus norvegicus (Norway rat)	Potency	12.5752	1	2
Gamma-aminobutyric acid receptor subunit beta-3	Rattus norvegicus (Norway rat)	Potency	12.5752	1	2
Gamma-aminobutyric acid receptor subunit delta	Rattus norvegicus (Norway rat)	Potency	12.5752	1	2
Gamma-aminobutyric acid receptor subunit epsilon	Rattus norvegicus (Norway rat)	Potency	12.5752	1	2
Gamma-aminobutyric acid receptor subunit gamma-1	Rattus norvegicus (Norway rat)	Potency	12.5752	1	2
Gamma-aminobutyric acid receptor subunit gamma-2	Rattus norvegicus (Norway rat)	Potency	12.5752	1	2
Gamma-aminobutyric acid receptor subunit gamma-3	Rattus norvegicus (Norway rat)	Potency	12.5752	1	2
Gamma-aminobutyric acid receptor subunit pi	Rattus norvegicus (Norway rat)	Potency	12.5752	1	2
GLI family zinc finger 3	Homo sapiens (human)	Potency	3.9983	2	4
GLS protein	Homo sapiens (human)	Potency	22.3872	1	1
glucocorticoid receptor [Homo sapiens]	Homo sapiens (human)	Potency	17.6452	3	3
histone acetyltransferase KAT2A isoform 1	Homo sapiens (human)	Potency	39.8107	1	1
lamin isoform A-delta10	Homo sapiens (human)	Potency	3.0654	1	4
lethal(3)malignant brain tumor-like protein 1 isoform I	Homo sapiens (human)	Potency	44.6684	1	1
Luciferase	Photinus pyralis (common eastern firefly)	Potency	27.5404	1	1
muscarinic acetylcholine receptor M1	Rattus norvegicus (Norway rat)	Potency	28.1838	1	1
NFKB1 protein, partial	Homo sapiens (human)	Potency	5.6234	2	2
nuclear factor erythroid 2-related factor 2 isoform 1	Homo sapiens (human)	Potency	53.0804	1	1
nuclear receptor ROR-gamma isoform 1	Mus musculus (house mouse)	Potency	2.2536	1	2
nuclear receptor subfamily 1, group I, member 3	Homo sapiens (human)	Potency	18.5899	3	3
peripheral myelin protein 22	Rattus norvegicus (Norway rat)	Potency	40.5334	1	1
peroxisome proliferator activated receptor gamma	Homo sapiens (human)	Potency	26.8325	1	1
phosphopantetheinyl transferase	Bacillus subtilis	Potency	44.6684	1	1
potassium voltage-gated channel subfamily H member 2 isoform d	Homo sapiens (human)	Potency	0.0891	1	1
pregnane X nuclear receptor	Homo sapiens (human)	Potency	18.9178	2	2
RAR-related orphan receptor gamma	Mus musculus (house mouse)	Potency	11.9620	2	2
regulator of G-protein signaling 4	Homo sapiens (human)	Potency	0.1062	1	1
retinoic acid nuclear receptor alpha variant 1	Homo sapiens (human)	Potency	20.4250	3	3
TDP1 protein	Homo sapiens (human)	Potency	27.5781	2	6
thioredoxin reductase	Rattus norvegicus (Norway rat)	Potency	8.4216	1	2
thyroid hormone receptor beta isoform 2	Rattus norvegicus (Norway rat)	Potency	47.4381	2	4
thyroid stimulating hormone receptor	Homo sapiens (human)	Potency	31.6228	2	2
vitamin D (1,25- dihydroxyvitamin D3) receptor	Homo sapiens (human)	Potency	21.1300	1	1

Inhibition Measurements

Protein	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Drugs
5-hydroxytryptamine receptor 1B	Oryctolagus cuniculus (rabbit)	IC50	100.0000	1	1
Amyloid-beta precursor protein	Homo sapiens (human)	IC50	100.0000	1	1
ATP-binding cassette sub-family C member 3	Homo sapiens (human)	IC50	133.0000	1	1
Bile salt export pump	Homo sapiens (human)	IC50	133.0000	1	1
Canalicular multispecific organic anion transporter 1	Homo sapiens (human)	IC50	133.0000	1	1
Cholecystokinin receptor type A	Cavia porcellus (domestic guinea pig)	IC50	64.0000	1	1
Cholecystokinin receptor type A	Rattus norvegicus (Norway rat)	IC50	64.0000	1	1
D-amino-acid oxidase	Sus scrofa (pig)	IC50	100.0000	2	2
GABA theta subunit	Rattus norvegicus (Norway rat)	IC50	0.0101	6	9
GABA theta subunit	Rattus norvegicus (Norway rat)	Ki	0.0201	3	4
Gamma-aminobutyric acid receptor subunit alpha-1	Homo sapiens (human)	IC50	0.0160	1	1
Gamma-aminobutyric acid receptor subunit alpha-1	Rattus norvegicus (Norway rat)	IC50	0.0101	6	9
Gamma-aminobutyric acid receptor subunit alpha-1	Homo sapiens (human)	Ki	1.2942	14	41
Gamma-aminobutyric acid receptor subunit alpha-1	Rattus norvegicus (Norway rat)	Ki	0.7450	13	14
Gamma-aminobutyric acid receptor subunit alpha-2	Homo sapiens (human)	IC50	0.0160	1	1
Gamma-aminobutyric acid receptor subunit alpha-2	Rattus norvegicus (Norway rat)	IC50	0.0101	6	9
Gamma-aminobutyric acid receptor subunit alpha-2	Homo sapiens (human)	Ki	1.3915	12	39
Gamma-aminobutyric acid receptor subunit alpha-2	Rattus norvegicus (Norway rat)	Ki	0.3452	9	10
Gamma-aminobutyric acid receptor subunit alpha-3	Homo sapiens (human)	IC50	0.0160	1	1
Gamma-aminobutyric acid receptor subunit alpha-3	Rattus norvegicus (Norway rat)	IC50	0.0101	6	9
Gamma-aminobutyric acid receptor subunit alpha-3	Homo sapiens (human)	Ki	1.4318	14	41
Gamma-aminobutyric acid receptor subunit alpha-3	Rattus norvegicus (Norway rat)	Ki	0.2660	8	9
Gamma-aminobutyric acid receptor subunit alpha-4	Homo sapiens (human)	IC50	0.0160	1	1
Gamma-aminobutyric acid receptor subunit alpha-4	Rattus norvegicus (Norway rat)	IC50	0.0101	6	9
Gamma-aminobutyric acid receptor subunit alpha-4	Homo sapiens (human)	Ki	2.1843	4	31
Gamma-aminobutyric acid receptor subunit alpha-4	Rattus norvegicus (Norway rat)	Ki	0.0201	3	4
Gamma-aminobutyric acid receptor subunit alpha-5	Homo sapiens (human)	IC50	0.0160	1	1
Gamma-aminobutyric acid receptor subunit alpha-5	Rattus norvegicus (Norway rat)	IC50	0.0101	6	9
Gamma-aminobutyric acid receptor subunit alpha-5	Homo sapiens (human)	Ki	3.3170	11	38
Gamma-aminobutyric acid receptor subunit alpha-5	Rattus norvegicus (Norway rat)	Ki	2.8736	6	7
Gamma-aminobutyric acid receptor subunit alpha-6	Homo sapiens (human)	IC50	0.0160	1	1
Gamma-aminobutyric acid receptor subunit alpha-6	Rattus norvegicus (Norway rat)	IC50	0.0101	6	9
Gamma-aminobutyric acid receptor subunit alpha-6	Homo sapiens (human)	Ki	2.8739	7	34
Gamma-aminobutyric acid receptor subunit alpha-6	Rattus norvegicus (Norway rat)	Ki	3.6067	8	9
Gamma-aminobutyric acid receptor subunit beta-1	Homo sapiens (human)	IC50	0.0160	1	1
Gamma-aminobutyric acid receptor subunit beta-1	Rattus norvegicus (Norway rat)	IC50	0.0101	6	9
Gamma-aminobutyric acid receptor subunit beta-1	Homo sapiens (human)	Ki	0.0233	3	3
Gamma-aminobutyric acid receptor subunit beta-1	Rattus norvegicus (Norway rat)	Ki	0.0201	3	4
Gamma-aminobutyric acid receptor subunit beta-2	Homo sapiens (human)	IC50	0.0160	1	1
Gamma-aminobutyric acid receptor subunit beta-2	Rattus norvegicus (Norway rat)	IC50	0.0101	6	9
Gamma-aminobutyric acid receptor subunit beta-2	Homo sapiens (human)	Ki	1.8671	11	38
Gamma-aminobutyric acid receptor subunit beta-2	Rattus norvegicus (Norway rat)	Ki	1.8140	25	26
Gamma-aminobutyric acid receptor subunit beta-3	Homo sapiens (human)	IC50	0.0160	1	1
Gamma-aminobutyric acid receptor subunit beta-3	Rattus norvegicus (Norway rat)	IC50	0.0101	6	9
Gamma-aminobutyric acid receptor subunit beta-3	Homo sapiens (human)	Ki	2.8898	32	32
Gamma-aminobutyric acid receptor subunit beta-3	Rattus norvegicus (Norway rat)	Ki	1.6859	5	6
Gamma-aminobutyric acid receptor subunit delta	Homo sapiens (human)	IC50	0.0160	1	1
Gamma-aminobutyric acid receptor subunit delta	Rattus norvegicus (Norway rat)	IC50	0.0101	6	9
Gamma-aminobutyric acid receptor subunit delta	Homo sapiens (human)	Ki	0.0085	2	2
Gamma-aminobutyric acid receptor subunit delta	Rattus norvegicus (Norway rat)	Ki	0.0201	3	4
Gamma-aminobutyric acid receptor subunit epsilon	Homo sapiens (human)	IC50	0.0160	1	1
Gamma-aminobutyric acid receptor subunit epsilon	Rattus norvegicus (Norway rat)	IC50	0.0101	6	9
Gamma-aminobutyric acid receptor subunit epsilon	Homo sapiens (human)	Ki	0.0085	2	2
Gamma-aminobutyric acid receptor subunit epsilon	Rattus norvegicus (Norway rat)	Ki	0.0201	3	4
Gamma-aminobutyric acid receptor subunit gamma-1	Homo sapiens (human)	IC50	0.0160	1	1
Gamma-aminobutyric acid receptor subunit gamma-1	Rattus norvegicus (Norway rat)	IC50	0.0097	7	10
Gamma-aminobutyric acid receptor subunit gamma-1	Homo sapiens (human)	Ki	0.0085	2	2
Gamma-aminobutyric acid receptor subunit gamma-1	Rattus norvegicus (Norway rat)	Ki	0.0201	3	4
Gamma-aminobutyric acid receptor subunit gamma-2	Homo sapiens (human)	IC50	0.0160	1	1
Gamma-aminobutyric acid receptor subunit gamma-2	Rattus norvegicus (Norway rat)	IC50	0.0101	6	9
Gamma-aminobutyric acid receptor subunit gamma-2	Homo sapiens (human)	Ki	2.3690	42	69
Gamma-aminobutyric acid receptor subunit gamma-2	Rattus norvegicus (Norway rat)	Ki	2.0428	27	28
Gamma-aminobutyric acid receptor subunit gamma-3	Homo sapiens (human)	IC50	0.0160	1	1
Gamma-aminobutyric acid receptor subunit gamma-3	Rattus norvegicus (Norway rat)	IC50	0.0101	6	9
Gamma-aminobutyric acid receptor subunit gamma-3	Homo sapiens (human)	Ki	0.0085	2	2
Gamma-aminobutyric acid receptor subunit gamma-3	Rattus norvegicus (Norway rat)	Ki	0.0201	3	4
Gamma-aminobutyric acid receptor subunit pi	Homo sapiens (human)	IC50	0.0160	1	1
Gamma-aminobutyric acid receptor subunit pi	Rattus norvegicus (Norway rat)	IC50	0.0101	6	9
Gamma-aminobutyric acid receptor subunit pi	Homo sapiens (human)	Ki	0.0085	2	2
Gamma-aminobutyric acid receptor subunit pi	Rattus norvegicus (Norway rat)	Ki	0.0201	3	4
Gamma-aminobutyric acid receptor subunit theta	Homo sapiens (human)	IC50	0.0160	1	1
Gamma-aminobutyric acid receptor subunit theta	Homo sapiens (human)	Ki	0.0085	2	2
Gamma-aminobutyric acid type B receptor subunit 1	Homo sapiens (human)	IC50	0.0500	1	1
Gamma-aminobutyric acid type B receptor subunit 1	Rattus norvegicus (Norway rat)	IC50	0.2762	4	6
Gamma-aminobutyric acid type B receptor subunit 1	Homo sapiens (human)	Ki	6.0000	1	1
Gamma-aminobutyric acid type B receptor subunit 2	Homo sapiens (human)	IC50	0.0500	1	1
Gamma-aminobutyric acid type B receptor subunit 2	Rattus norvegicus (Norway rat)	IC50	0.2762	4	6
Gamma-aminobutyric acid type B receptor subunit 2	Homo sapiens (human)	Ki	6.0000	1	1
Gamma-aminobutyric acid type B receptor subunit 2	Rattus norvegicus (Norway rat)	Ki	0.2200	1	1
Glutamate receptor 1	Rattus norvegicus (Norway rat)	IC50	10.0000	1	1
Glutamate receptor 2	Rattus norvegicus (Norway rat)	IC50	10.0000	1	1
Glutamate receptor 3	Rattus norvegicus (Norway rat)	IC50	10.0000	1	1
Glutamate receptor 4	Rattus norvegicus (Norway rat)	IC50	10.0000	1	1
Glutaminyl-peptide cyclotransferase	Mus musculus (house mouse)	Ki	22,000.0000	1	1
Multidrug resistance-associated protein 4	Homo sapiens (human)	IC50	133.0000	1	1
Neuronal acetylcholine receptor subunit alpha-7	Rattus norvegicus (Norway rat)	Ki	10.0000	1	1
Protein farnesyltransferase subunit beta	Homo sapiens (human)	IC50	15,500.0000	1	1
Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha	Homo sapiens (human)	IC50	15,500.0000	1	1
Proton-coupled amino acid transporter 1	Homo sapiens (human)	Ki	7,100.0000	1	1
Sodium- and chloride-dependent betaine transporter	Rattus norvegicus (Norway rat)	IC50	0.0032	1	1
Sodium- and chloride-dependent GABA transporter 1	Rattus norvegicus (Norway rat)	IC50	0.0032	1	1
Sodium- and chloride-dependent GABA transporter 2	Rattus norvegicus (Norway rat)	IC50	0.0032	1	1
Sodium- and chloride-dependent GABA transporter 3	Rattus norvegicus (Norway rat)	IC50	0.0032	1	1
Sphingosine-1-phosphate lyase 1	Mus musculus (house mouse)	Ki	0.7650	1	1
Translocator protein	Rattus norvegicus (Norway rat)	IC50	4.7000	1	1

Activation Measurements

Protein	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Drugs
Albumin	Homo sapiens (human)	Kd	63.0000	1	1
Bromodomain-containing protein 4	Homo sapiens (human)	Kd	2.4600	1	1
Gamma-aminobutyric acid receptor subunit alpha-1	Homo sapiens (human)	EC50	3.3133	6	9
Gamma-aminobutyric acid receptor subunit alpha-1	Rattus norvegicus (Norway rat)	EC50	100.0000	1	1
Gamma-aminobutyric acid receptor subunit alpha-2	Homo sapiens (human)	EC50	3.6955	5	8
Gamma-aminobutyric acid receptor subunit alpha-3	Homo sapiens (human)	EC50	4.4167	4	7
Gamma-aminobutyric acid receptor subunit alpha-4	Homo sapiens (human)	EC50	27.0000	1	1
Gamma-aminobutyric acid receptor subunit alpha-5	Homo sapiens (human)	EC50	10.0033	2	3
Gamma-aminobutyric acid receptor subunit alpha-6	Homo sapiens (human)	EC50	27.0000	1	1
Gamma-aminobutyric acid receptor subunit beta-1	Homo sapiens (human)	EC50	27.0000	1	1
Gamma-aminobutyric acid receptor subunit beta-2	Homo sapiens (human)	EC50	2.1371	9	15
Gamma-aminobutyric acid receptor subunit beta-2	Rattus norvegicus (Norway rat)	EC50	100.0000	1	1
Gamma-aminobutyric acid receptor subunit beta-3	Homo sapiens (human)	EC50	27.0000	1	1
Gamma-aminobutyric acid receptor subunit gamma-2	Homo sapiens (human)	EC50	0.3612	8	14
Gamma-aminobutyric acid receptor subunit gamma-2	Rattus norvegicus (Norway rat)	EC50	100.0000	1	1
Gamma-aminobutyric acid receptor subunit rho-1	Homo sapiens (human)	EC50	1.0806	4	6
Gamma-aminobutyric acid receptor subunit rho-1	Homo sapiens (human)	Kd	2.3000	1	1
Gamma-aminobutyric acid receptor subunit rho-2	Homo sapiens (human)	Kd	1.4000	1	1
Gamma-aminobutyric acid type B receptor subunit 1	Homo sapiens (human)	EC50	1.7000	1	1
Gamma-aminobutyric acid type B receptor subunit 2	Homo sapiens (human)	EC50	1.7000	1	1
Sodium-dependent dopamine transporter	Rattus norvegicus (Norway rat)	EC50	0.1910	1	1

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GABA agonist

Members (8)

Research

Studies (14,722)

Study Types

Protein Targets (116)

Potency Measurements

Inhibition Measurements

Activation Measurements