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