GABAA receptor agonist

A GABA receptor agonist specific for GABAA receptors, ligand-gated ion channels (also known as ionotropic receptors).

ChEBI ID: 91016

Members (6)

Member	Definition	Class
didesethylflurazepam	A primary amino compound resulting from the dealkylation of both ethyl groups of the anti-insomnia drug flurazepam. It is the major metabolite of flurazepam.	didesethylflurazepam
flunitrazepam	A 1,4-benzodiazepinone that is nitrazepam substituted by a methyl group at position 1 and by a fluoro group at position 2'. It is a potent hypnotic, sedative, and amnestic drug used to treat chronic insomnia.	flunitrazepam
flurazepam	A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a 2-(diethylamino)ethyl group, 2-fluorophenyl group and chloro group at positions 1, 5 and 7, respectively. It is a partial agonist of GABAA receptors and used for the treatment of insomnia.	flurazepam
midazolam	An imidazobenzodiazepine that is 4H-imidazo[1,5-a][1,4]benzodiazepine which is substituted by a methyl, 2-fluorophenyl and chloro groups at positions 1, 6 and 8, respectively.	midazolam
midazolam hydrochloride	The hydrochloride salt of midazolam.	midazolam hydrochloride
pentobarbital	A member of the class of barbiturates, the structure of which is that of barbituric acid substituted at C-5 by ethyl and sec-pentyl groups.	pentobarbital

Research

Studies (21,665)

Timeframe	Studies, Drugs with This Role(%)	All Drugs %
pre-1990	9,553 (44.09)	18.7374
1990's	4,367 (20.16)	18.2507
2000's	3,553 (16.40)	29.6817
2010's	3,149 (14.53)	24.3611
2020's	1,043 (4.81)	2.80

Study Types

Publication Type	Studies, Drugs with this Role (%)	All Drugs (%)
Trials	3,827 (16.19%)	5.53%
Reviews	750 (3.17%)	6.00%
Case Studies	1,030 (4.36%)	4.05%
Observational	127 (0.54%)	0.25%
Other	17,907 (75.75%)	84.16%

Protein Targets (91)

Potency Measurements

Protein	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Drugs
aldehyde dehydrogenase 1 family, member A1	Homo sapiens (human)	Potency	31.6228	1	1
AR protein	Homo sapiens (human)	Potency	13.4481	2	2
aryl hydrocarbon receptor	Homo sapiens (human)	Potency	23.8769	2	4
ATAD5 protein, partial	Homo sapiens (human)	Potency	18.4706	2	2
Ataxin-2	Homo sapiens (human)	Potency	26.6032	1	1
ATPase family AAA domain-containing protein 5	Homo sapiens (human)	Potency	26.6032	2	2
Cellular tumor antigen p53	Homo sapiens (human)	Potency	1.1883	1	1
Chain A, 2-oxoglutarate Oxygenase	Homo sapiens (human)	Potency	39.8107	1	1
Chain A, JmjC domain-containing histone demethylation protein 3A	Homo sapiens (human)	Potency	50.1187	1	1
cytochrome P450 2C9, partial	Homo sapiens (human)	Potency	27.5404	1	1
cytochrome P450 2D6	Homo sapiens (human)	Potency	28.7258	1	2
cytochrome P450 3A4 isoform 1	Homo sapiens (human)	Potency	31.6228	2	2
cytochrome P450 family 3 subfamily A polypeptide 4	Homo sapiens (human)	Potency	4.6553	1	2
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a	Homo sapiens (human)	Potency	7.4978	1	1
estrogen nuclear receptor alpha	Homo sapiens (human)	Potency	12.5010	7	7
estrogen-related nuclear receptor alpha	Homo sapiens (human)	Potency	33.6396	3	3
euchromatic histone-lysine N-methyltransferase 2	Homo sapiens (human)	Potency	1.9953	1	1
farnesoid X nuclear receptor	Homo sapiens (human)	Potency	11.8823	1	1
G	Vesicular stomatitis virus	Potency	27.5404	1	1
GABA theta subunit	Rattus norvegicus (Norway rat)	Potency	31.6228	1	1
Gamma-aminobutyric acid receptor subunit alpha-1	Rattus norvegicus (Norway rat)	Potency	31.6228	1	1
Gamma-aminobutyric acid receptor subunit alpha-2	Rattus norvegicus (Norway rat)	Potency	31.6228	1	1
Gamma-aminobutyric acid receptor subunit alpha-3	Rattus norvegicus (Norway rat)	Potency	31.6228	1	1
Gamma-aminobutyric acid receptor subunit alpha-4	Rattus norvegicus (Norway rat)	Potency	31.6228	1	1
Gamma-aminobutyric acid receptor subunit alpha-5	Rattus norvegicus (Norway rat)	Potency	31.6228	1	1
Gamma-aminobutyric acid receptor subunit alpha-6	Rattus norvegicus (Norway rat)	Potency	31.6228	1	1
Gamma-aminobutyric acid receptor subunit beta-1	Rattus norvegicus (Norway rat)	Potency	31.6228	1	1
Gamma-aminobutyric acid receptor subunit beta-2	Rattus norvegicus (Norway rat)	Potency	31.6228	1	1
Gamma-aminobutyric acid receptor subunit beta-3	Rattus norvegicus (Norway rat)	Potency	31.6228	1	1
Gamma-aminobutyric acid receptor subunit delta	Rattus norvegicus (Norway rat)	Potency	31.6228	1	1
Gamma-aminobutyric acid receptor subunit epsilon	Rattus norvegicus (Norway rat)	Potency	31.6228	1	1
Gamma-aminobutyric acid receptor subunit gamma-1	Rattus norvegicus (Norway rat)	Potency	31.6228	1	1
Gamma-aminobutyric acid receptor subunit gamma-2	Rattus norvegicus (Norway rat)	Potency	31.6228	1	1
Gamma-aminobutyric acid receptor subunit gamma-3	Rattus norvegicus (Norway rat)	Potency	31.6228	1	1
Gamma-aminobutyric acid receptor subunit pi	Rattus norvegicus (Norway rat)	Potency	31.6228	1	1
geminin	Homo sapiens (human)	Potency	18.8375	1	1
GLI family zinc finger 3	Homo sapiens (human)	Potency	17.2732	2	3
glucocorticoid receptor [Homo sapiens]	Homo sapiens (human)	Potency	16.9301	1	1
Glutamate receptor 2	Rattus norvegicus (Norway rat)	Potency	10.5909	1	1
HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)	Potency	27.5404	1	1
IDH1	Homo sapiens (human)	Potency	11.5821	1	1
Inositol hexakisphosphate kinase 1	Homo sapiens (human)	Potency	27.5404	1	2
Interferon beta	Homo sapiens (human)	Potency	27.5404	1	1
nuclear factor erythroid 2-related factor 2 isoform 2	Homo sapiens (human)	Potency	25.9290	1	1
peripheral myelin protein 22	Rattus norvegicus (Norway rat)	Potency	10.1815	1	1
peroxisome proliferator activated receptor gamma	Homo sapiens (human)	Potency	21.3138	1	1
potassium voltage-gated channel subfamily H member 2 isoform d	Homo sapiens (human)	Potency	3.9811	1	1
pregnane X nuclear receptor	Homo sapiens (human)	Potency	17.2234	2	4
progesterone receptor	Homo sapiens (human)	Potency	29.8493	1	1
retinoic acid nuclear receptor alpha variant 1	Homo sapiens (human)	Potency	26.3463	3	3
TDP1 protein	Homo sapiens (human)	Potency	27.6867	2	6
thyroid hormone receptor beta isoform 2	Rattus norvegicus (Norway rat)	Potency	27.1310	2	4
thyrotropin-releasing hormone receptor	Homo sapiens (human)	Potency	14.7263	1	1
vitamin D3 receptor isoform VDRA	Homo sapiens (human)	Potency	56.2341	1	1
Voltage-dependent calcium channel gamma-2 subunit	Mus musculus (house mouse)	Potency	10.5909	1	1

Inhibition Measurements

Protein	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Drugs
ATP-dependent translocase ABCB1	Homo sapiens (human)	IC50	50.0000	3	3
ATP-dependent translocase ABCB1	Mus musculus (house mouse)	IC50	41.5000	4	4
Bile salt export pump	Homo sapiens (human)	IC50	41.7133	3	3
Cholecystokinin receptor type A	Rattus norvegicus (Norway rat)	IC50	100.0000	2	2
Cytochrome P450 3A4	Homo sapiens (human)	IC50	2.7427	3	3
GABA theta subunit	Rattus norvegicus (Norway rat)	IC50	0.0016	3	6
GABA theta subunit	Rattus norvegicus (Norway rat)	Ki	0.0020	1	1
Gamma-aminobutyric acid receptor subunit alpha-1	Homo sapiens (human)	IC50	132,013.5000	2	2
Gamma-aminobutyric acid receptor subunit alpha-1	Rattus norvegicus (Norway rat)	IC50	0.0016	3	6
Gamma-aminobutyric acid receptor subunit alpha-1	Homo sapiens (human)	Ki	0.0026	4	4
Gamma-aminobutyric acid receptor subunit alpha-1	Rattus norvegicus (Norway rat)	Ki	0.0020	1	1
Gamma-aminobutyric acid receptor subunit alpha-2	Homo sapiens (human)	IC50	263,027.0000	1	1
Gamma-aminobutyric acid receptor subunit alpha-2	Rattus norvegicus (Norway rat)	IC50	0.0016	3	6
Gamma-aminobutyric acid receptor subunit alpha-2	Homo sapiens (human)	Ki	0.0022	4	4
Gamma-aminobutyric acid receptor subunit alpha-2	Rattus norvegicus (Norway rat)	Ki	0.0020	1	1
Gamma-aminobutyric acid receptor subunit alpha-3	Homo sapiens (human)	IC50	263,027.0000	1	1
Gamma-aminobutyric acid receptor subunit alpha-3	Rattus norvegicus (Norway rat)	IC50	0.0016	3	6
Gamma-aminobutyric acid receptor subunit alpha-3	Homo sapiens (human)	Ki	0.0048	4	4
Gamma-aminobutyric acid receptor subunit alpha-3	Rattus norvegicus (Norway rat)	Ki	0.0020	1	1
Gamma-aminobutyric acid receptor subunit alpha-4	Homo sapiens (human)	IC50	263,027.0000	1	1
Gamma-aminobutyric acid receptor subunit alpha-4	Rattus norvegicus (Norway rat)	IC50	0.0016	3	6
Gamma-aminobutyric acid receptor subunit alpha-4	Rattus norvegicus (Norway rat)	Ki	0.0020	1	1
Gamma-aminobutyric acid receptor subunit alpha-5	Homo sapiens (human)	IC50	263,027.0000	1	1
Gamma-aminobutyric acid receptor subunit alpha-5	Rattus norvegicus (Norway rat)	IC50	0.0016	3	6
Gamma-aminobutyric acid receptor subunit alpha-5	Homo sapiens (human)	Ki	0.0021	3	3
Gamma-aminobutyric acid receptor subunit alpha-5	Rattus norvegicus (Norway rat)	Ki	0.0020	1	1
Gamma-aminobutyric acid receptor subunit alpha-6	Homo sapiens (human)	IC50	263,027.0000	1	1
Gamma-aminobutyric acid receptor subunit alpha-6	Rattus norvegicus (Norway rat)	IC50	0.0016	3	6
Gamma-aminobutyric acid receptor subunit alpha-6	Homo sapiens (human)	Ki	2.0000	2	2
Gamma-aminobutyric acid receptor subunit alpha-6	Rattus norvegicus (Norway rat)	Ki	0.0020	1	1
Gamma-aminobutyric acid receptor subunit beta-1	Homo sapiens (human)	IC50	263,027.0000	1	1
Gamma-aminobutyric acid receptor subunit beta-1	Rattus norvegicus (Norway rat)	IC50	0.0016	3	6
Gamma-aminobutyric acid receptor subunit beta-1	Rattus norvegicus (Norway rat)	Ki	0.0020	1	1
Gamma-aminobutyric acid receptor subunit beta-2	Homo sapiens (human)	IC50	263,027.0000	1	1
Gamma-aminobutyric acid receptor subunit beta-2	Rattus norvegicus (Norway rat)	IC50	0.0016	3	6
Gamma-aminobutyric acid receptor subunit beta-2	Homo sapiens (human)	Ki	0.0030	5	5
Gamma-aminobutyric acid receptor subunit beta-2	Rattus norvegicus (Norway rat)	Ki	0.0020	1	1
Gamma-aminobutyric acid receptor subunit beta-3	Homo sapiens (human)	IC50	131,557.5000	2	2
Gamma-aminobutyric acid receptor subunit beta-3	Rattus norvegicus (Norway rat)	IC50	0.0016	3	6
Gamma-aminobutyric acid receptor subunit beta-3	Homo sapiens (human)	Ki	0.3358	12	12
Gamma-aminobutyric acid receptor subunit beta-3	Rattus norvegicus (Norway rat)	Ki	0.0020	1	1
Gamma-aminobutyric acid receptor subunit delta	Homo sapiens (human)	IC50	263,027.0000	1	1
Gamma-aminobutyric acid receptor subunit delta	Rattus norvegicus (Norway rat)	IC50	0.0016	3	6
Gamma-aminobutyric acid receptor subunit delta	Rattus norvegicus (Norway rat)	Ki	0.0020	1	1
Gamma-aminobutyric acid receptor subunit epsilon	Homo sapiens (human)	IC50	263,027.0000	1	1
Gamma-aminobutyric acid receptor subunit epsilon	Rattus norvegicus (Norway rat)	IC50	0.0016	3	6
Gamma-aminobutyric acid receptor subunit epsilon	Rattus norvegicus (Norway rat)	Ki	0.0020	1	1
Gamma-aminobutyric acid receptor subunit gamma-1	Homo sapiens (human)	IC50	263,027.0000	1	1
Gamma-aminobutyric acid receptor subunit gamma-1	Rattus norvegicus (Norway rat)	IC50	0.0016	3	6
Gamma-aminobutyric acid receptor subunit gamma-1	Rattus norvegicus (Norway rat)	Ki	0.0020	1	1
Gamma-aminobutyric acid receptor subunit gamma-2	Homo sapiens (human)	IC50	263,027.0000	1	1
Gamma-aminobutyric acid receptor subunit gamma-2	Rattus norvegicus (Norway rat)	IC50	0.0016	3	6
Gamma-aminobutyric acid receptor subunit gamma-2	Homo sapiens (human)	Ki	0.2379	17	17
Gamma-aminobutyric acid receptor subunit gamma-2	Rattus norvegicus (Norway rat)	Ki	0.0020	1	1
Gamma-aminobutyric acid receptor subunit gamma-3	Homo sapiens (human)	IC50	263,027.0000	1	1
Gamma-aminobutyric acid receptor subunit gamma-3	Rattus norvegicus (Norway rat)	IC50	0.0016	3	6
Gamma-aminobutyric acid receptor subunit gamma-3	Rattus norvegicus (Norway rat)	Ki	0.0020	1	1
Gamma-aminobutyric acid receptor subunit pi	Homo sapiens (human)	IC50	263,027.0000	1	1
Gamma-aminobutyric acid receptor subunit pi	Rattus norvegicus (Norway rat)	IC50	0.0016	3	6
Gamma-aminobutyric acid receptor subunit pi	Rattus norvegicus (Norway rat)	Ki	0.0020	1	1
Gamma-aminobutyric acid receptor subunit theta	Homo sapiens (human)	IC50	263,027.0000	1	1
Gastrin/cholecystokinin type B receptor	Rattus norvegicus (Norway rat)	IC50	100.0000	1	1
Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)	IC50	11,465.9130	2	2
Solute carrier family 22 member 1	Homo sapiens (human)	Ki	3.7000	1	1
Translocator protein	Homo sapiens (human)	IC50	263,027.0000	1	1
Translocator protein	Rattus norvegicus (Norway rat)	Ki	0.0020	1	1
UDP-glucuronosyltransferase 1-6	Homo sapiens (human)	IC50	75.5000	1	4
UDP-glucuronosyltransferase 1A1	Homo sapiens (human)	IC50	75.5000	1	4
UDP-glucuronosyltransferase 1A4	Homo sapiens (human)	IC50	75.5000	1	4
UDP-glucuronosyltransferase 2B10	Homo sapiens (human)	IC50	75.5000	1	4
UDP-glucuronosyltransferase 2B7	Homo sapiens (human)	IC50	75.5000	1	4
Voltage-dependent L-type calcium channel subunit alpha-1C	Homo sapiens (human)	IC50	299.0000	1	1
Voltage-dependent L-type calcium channel subunit alpha-1D	Homo sapiens (human)	IC50	299.0000	1	1
Voltage-dependent L-type calcium channel subunit alpha-1F	Homo sapiens (human)	IC50	299.0000	1	1
Voltage-dependent L-type calcium channel subunit alpha-1S	Homo sapiens (human)	IC50	299.0000	1	1

Activation Measurements

Protein	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Drugs
Gamma-aminobutyric acid receptor subunit alpha-1	Homo sapiens (human)	EC50	0.0014	1	1
Gamma-aminobutyric acid receptor subunit alpha-1	Homo sapiens (human)	Kd	0.0045	1	1
Gamma-aminobutyric acid receptor subunit alpha-2	Homo sapiens (human)	EC50	50.0000	1	1
Gamma-aminobutyric acid receptor subunit alpha-5	Homo sapiens (human)	Kd	0.0030	1	1
Gamma-aminobutyric acid receptor subunit beta-2	Homo sapiens (human)	EC50	25.0007	2	2
Gamma-aminobutyric acid receptor subunit gamma-2	Homo sapiens (human)	EC50	25.0007	2	2

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GABAA receptor agonist

Members (6)

Research

Studies (21,665)

Study Types

Protein Targets (91)

Potency Measurements

Inhibition Measurements

Activation Measurements