GABA modulator

A substance that does not act as agonist or antagonist but does affect the gamma-aminobutyric acid receptor-ionophore complex. GABA-A receptors appear to have at least three allosteric sites at which modulators act: a site at which benzodiazepines act by increasing the opening frequency of gamma-aminobutyric acid-activated chloride channels; a site at which barbiturates act to prolong the duration of channel opening; and a site at which some steroids may act.

ChEBI ID: 50268

Members (16)

Member	Definition	Class
6,6-dimethyl-2-methylenebicyclo(3.1.1)heptan-3-ol	A pinane monoterpenoid that is a bicyclo[3.1.1]heptane substituted by two methyl groups at position 6, a methylidene group at position 2 and a hydroxy group at position 3.	pinocarveol
alpha-asarone	The trans-isomer of asarone.	alpha-asarone
beta-asarone	The cis-isomer of asarone.	beta-asarone
brexanolone	A 3-hydroxy-5alpha-pregnan-20-one in which the hydroxy group at position 3 has alpha-configuration. It is a metabolite of the sex hormone progesterone and used for the treatment of postpartum depression in women.	brexanolone
chlorazepate	A 1,4-benzodiazepinone in which the oxo group is at position 2, and which is substituted at positions 3, 5, and 7 by carboxy, phenyl and chloro groups, respectively.	clorazepic acid
clobazam	7-Chloro-1H-1,5-benzodiazepine-2,4(3H,5H)-dione in which the hydrogen attached to the nitrogen at position 1 is substituted by a methyl group, whilst that attached to the other nitrogen is substituted by a phenyl group. It is used for the short-term management of acute anxiety and as an adjunct in the treatment of epilepsy in association with other antiepileptics.	clobazam
clonazepam	1,3-Dihydro-2H-1,4-benzodiazepin-2-one in which the hydrogens at positions 5 and 7 are substituted by 2-chlorophenyl and nitro groups, respectively. It is used in the treatment of all types of epilepsy and seizures, as well as myoclonus and associated abnormal movements, and panic disorders. However, its use can be limited by the development of tolerance and by sedation.	clonazepam
clorazepate dipotassium	The compound of monopotassium clorazepate with potassium hydroxide. It is used for the management of anxiety disorders, for the short-term relief of anxiety, as adjunctive therapy in the management of epilepsy, and for the symptomatic relief of acute alcohol withdrawal.	dipotassium clorazepate
estazolam	A triazolo[4,3-a][1,4]benzodiazepine having a phenyl group at position 6 and a chloro substituent at position 8. A short-acting benzodiazepine with general properties similar to diazepam, it is given by mouth as a hypnotic in the short-term management of insomnia.	estazolam
isoliquiritigenin	A member of the class of chalcones that is trans-chalcone hydroxylated at C-2', -4 and -4'.	isoliquiritigenin
nimetazepam	A nitrazepam which is substituted at positions 1 by a methyl group. It is used as an anticonvulsant and as a hypnotic for the short-term management of insomnia.	nimetazepam
nitrazepam	A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one which is substituted at positions 5 and 7 by phenyl and nitro groups, respectively. It is used as a hypnotic for the short-term management of insomnia and for the treatment of epileptic spasms in infants (West's syndrome).	nitrazepam
nordazepam	A 1,4-benzodiazepinone having phenyl and chloro substituents at positions 5 and 7 respectively; it has anticonvulsant, anxiolytic, muscle relaxant and sedative properties but is used primarily in the treatment of anxiety.	nordazepam
secobarbital	A member of the class of barbiturates that is barbituric acid in which the hydrogens at position 5 are substituted by prop-2-en-1-yl and pentan-2-yl groups.	secobarbital
valerenic acid	A monocarboxylic acid that is 2-methylprop-2-enoic acid which is substituted at position 3 by a 3,7-dimethyl-2,4,5,6,7,7a-hexahydro-1H-inden-4-yl group. A bicyclic sesquiterpenoid constituent of the essential oil of the Valerian plant.	valerenic acid
verruculogen	An organic heterohexacyclic compound that is a mycotoxic indole alkaloid isolated from Penicillium and Aspergillus species.	verruculogen

Research

Studies (5,990)

Timeframe	Studies, Drugs with This Role(%)	All Drugs %
pre-1990	2,492 (41.60)	18.7374
1990's	993 (16.58)	18.2507
2000's	886 (14.79)	29.6817
2010's	1,196 (19.97)	24.3611
2020's	423 (7.06)	2.80

Study Types

Publication Type	Studies, Drugs with this Role (%)	All Drugs (%)
Trials	832 (12.21%)	5.53%
Reviews	426 (6.25%)	6.00%
Case Studies	1,098 (16.11%)	4.05%
Observational	11 (0.16%)	0.25%
Other	4,448 (65.27%)	84.16%

Protein Targets (203)

Potency Measurements

Protein	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Drugs
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1	Homo sapiens (human)	Potency	26.6514	1	2
2,3-bisphosphoglycerate-independent phosphoglycerate mutase	Leishmania major strain Friedlin	Potency	37.9330	1	1
67.9K protein	Vaccinia virus	Potency	16.8037	2	2
aldehyde dehydrogenase 1 family, member A1	Homo sapiens (human)	Potency	17.7828	1	1
Alpha-synuclein	Homo sapiens (human)	Potency	32.6427	1	1
Amyloid-beta precursor protein	Homo sapiens (human)	Potency	16.3601	1	1
AR protein	Homo sapiens (human)	Potency	19.5805	7	12
ATAD5 protein, partial	Homo sapiens (human)	Potency	10.9845	4	4
Ataxin-2	Homo sapiens (human)	Potency	17.8549	2	2
ATP-dependent phosphofructokinase	Trypanosoma brucei brucei TREU927	Potency	6.0120	1	1
ATPase family AAA domain-containing protein 5	Homo sapiens (human)	Potency	13.3722	2	2
atrial natriuretic peptide receptor 1 precursor	Homo sapiens (human)	Potency	30.1313	1	1
atrial natriuretic peptide receptor 2 precursor	Homo sapiens (human)	Potency	26.1216	1	1
Bloom syndrome protein isoform 1	Homo sapiens (human)	Potency	50.1187	2	2
Cellular tumor antigen p53	Homo sapiens (human)	Potency	10.3546	1	2
Chain A, Beta-lactamase	Escherichia coli K-12	Potency	112.2020	1	1
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE	Homo sapiens (human)	Potency	7.6110	1	2
chromobox protein homolog 1	Homo sapiens (human)	Potency	62.3032	2	2
cytochrome P450 2C19 precursor	Homo sapiens (human)	Potency	3.9811	1	1
cytochrome P450 2C9 precursor	Homo sapiens (human)	Potency	7.9433	1	1
cytochrome P450 2C9, partial	Homo sapiens (human)	Potency	43.6486	1	1
cytochrome P450 3A4 isoform 1	Homo sapiens (human)	Potency	6.9906	2	4
cytochrome P450 family 3 subfamily A polypeptide 4	Homo sapiens (human)	Potency	13.8029	1	2
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a	Homo sapiens (human)	Potency	4.2765	1	3
D(1A) dopamine receptor	Homo sapiens (human)	Potency	15.8489	1	1
DNA polymerase iota isoform a (long)	Homo sapiens (human)	Potency	85.8943	1	3
DNA polymerase kappa isoform 1	Homo sapiens (human)	Potency	89.1251	1	1
endonuclease IV	Escherichia coli	Potency	0.6310	1	1
estrogen nuclear receptor alpha	Homo sapiens (human)	Potency	34.5733	7	8
estrogen receptor 2 (ER beta)	Homo sapiens (human)	Potency	71.1083	1	1
estrogen-related nuclear receptor alpha	Homo sapiens (human)	Potency	35.4548	7	10
euchromatic histone-lysine N-methyltransferase 2	Homo sapiens (human)	Potency	44.2348	1	3
Fatty-acid amide hydrolase 1	Rattus norvegicus (Norway rat)	Potency	19.9526	1	1
flap endonuclease 1	Homo sapiens (human)	Potency	8.4368	1	1
G	Vesicular stomatitis virus	Potency	43.6486	1	1
GABA theta subunit	Rattus norvegicus (Norway rat)	Potency	6.9906	1	2
Gamma-aminobutyric acid receptor subunit alpha-1	Rattus norvegicus (Norway rat)	Potency	6.9906	1	2
Gamma-aminobutyric acid receptor subunit alpha-2	Rattus norvegicus (Norway rat)	Potency	6.9906	1	2
Gamma-aminobutyric acid receptor subunit alpha-3	Rattus norvegicus (Norway rat)	Potency	6.9906	1	2
Gamma-aminobutyric acid receptor subunit alpha-4	Rattus norvegicus (Norway rat)	Potency	6.9906	1	2
Gamma-aminobutyric acid receptor subunit alpha-5	Rattus norvegicus (Norway rat)	Potency	6.9906	1	2
Gamma-aminobutyric acid receptor subunit alpha-6	Rattus norvegicus (Norway rat)	Potency	6.9906	1	2
Gamma-aminobutyric acid receptor subunit beta-1	Rattus norvegicus (Norway rat)	Potency	6.9906	1	2
Gamma-aminobutyric acid receptor subunit beta-2	Rattus norvegicus (Norway rat)	Potency	6.9906	1	2
Gamma-aminobutyric acid receptor subunit beta-3	Rattus norvegicus (Norway rat)	Potency	6.9906	1	2
Gamma-aminobutyric acid receptor subunit delta	Rattus norvegicus (Norway rat)	Potency	6.9906	1	2
Gamma-aminobutyric acid receptor subunit epsilon	Rattus norvegicus (Norway rat)	Potency	6.9906	1	2
Gamma-aminobutyric acid receptor subunit gamma-1	Rattus norvegicus (Norway rat)	Potency	6.9906	1	2
Gamma-aminobutyric acid receptor subunit gamma-2	Rattus norvegicus (Norway rat)	Potency	6.9906	1	2
Gamma-aminobutyric acid receptor subunit gamma-3	Rattus norvegicus (Norway rat)	Potency	6.9906	1	2
Gamma-aminobutyric acid receptor subunit pi	Rattus norvegicus (Norway rat)	Potency	6.9906	1	2
geminin	Homo sapiens (human)	Potency	13.0472	4	6
GLI family zinc finger 3	Homo sapiens (human)	Potency	40.1510	2	2
glp-1 receptor, partial	Homo sapiens (human)	Potency	17.6316	2	2
GLS protein	Homo sapiens (human)	Potency	10.0000	1	1
glucocerebrosidase	Homo sapiens (human)	Potency	11.2637	6	9
glucocorticoid receptor [Homo sapiens]	Homo sapiens (human)	Potency	4.4866	4	7
Glutamate receptor 2	Rattus norvegicus (Norway rat)	Potency	63.3753	1	1
heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa)	Homo sapiens (human)	Potency	23.7996	1	2
heat shock protein beta-1	Homo sapiens (human)	Potency	58.0918	2	2
Histamine H2 receptor	Cavia porcellus (domestic guinea pig)	Potency	7.9433	1	3
histone acetyltransferase KAT2A isoform 1	Homo sapiens (human)	Potency	39.8107	1	1
histone-lysine N-methyltransferase 2A isoform 2 precursor	Homo sapiens (human)	Potency	31.6228	1	1
HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)	Potency	43.6486	1	1
IDH1	Homo sapiens (human)	Potency	25.9290	1	1
Inositol hexakisphosphate kinase 1	Homo sapiens (human)	Potency	43.6486	1	2
Interferon beta	Homo sapiens (human)	Potency	45.8718	2	4
interleukin 8	Homo sapiens (human)	Potency	74.9780	1	1
lamin isoform A-delta10	Homo sapiens (human)	Potency	8.4168	1	4
Luciferase	Photinus pyralis (common eastern firefly)	Potency	10.6910	1	1
M-phase phosphoprotein 8	Homo sapiens (human)	Potency	35.4813	1	1
Microtubule-associated protein tau	Homo sapiens (human)	Potency	9.7121	1	5
muscleblind-like protein 1 isoform 1	Homo sapiens (human)	Potency	12.5893	1	1
neuropeptide S receptor isoform A	Homo sapiens (human)	Potency	31.6228	1	1
nonstructural protein 1	Influenza A virus (A/WSN/1933(H1N1))	Potency	15.8489	1	1
Nrf2	Homo sapiens (human)	Potency	16.5928	2	2
nuclear factor erythroid 2-related factor 2 isoform 1	Homo sapiens (human)	Potency	68.9281	3	3
Nuclear receptor ROR-gamma	Homo sapiens (human)	Potency	37.5780	1	1
nuclear receptor ROR-gamma isoform 1	Mus musculus (house mouse)	Potency	12.5941	2	6
nuclear receptor subfamily 1, group I, member 2	Rattus norvegicus (Norway rat)	Potency	39.8107	1	1
nuclear receptor subfamily 1, group I, member 3	Homo sapiens (human)	Potency	63.3753	1	1
P53	Homo sapiens (human)	Potency	50.1187	1	1
peptidyl-prolyl cis-trans isomerase NIMA-interacting 1	Homo sapiens (human)	Potency	21.3313	1	1
peripheral myelin protein 22 isoform 1	Homo sapiens (human)	Potency	15.1014	1	1
peroxisome proliferator activated receptor gamma	Homo sapiens (human)	Potency	56.9772	1	1
peroxisome proliferator-activated receptor delta	Homo sapiens (human)	Potency	31.9143	4	4
potassium voltage-gated channel subfamily H member 2 isoform d	Homo sapiens (human)	Potency	3.9811	1	1
PPM1D protein	Homo sapiens (human)	Potency	46.6128	1	2
pregnane X nuclear receptor	Homo sapiens (human)	Potency	25.1555	2	4
progesterone receptor	Homo sapiens (human)	Potency	28.3087	1	1
RAR-related orphan receptor gamma	Mus musculus (house mouse)	Potency	30.4108	2	2
retinoic acid nuclear receptor alpha variant 1	Homo sapiens (human)	Potency	47.4618	3	3
retinoid X nuclear receptor alpha	Homo sapiens (human)	Potency	10.0000	1	1
serine/threonine-protein kinase mTOR isoform 1	Homo sapiens (human)	Potency	26.1216	1	1
SMAD family member 2	Homo sapiens (human)	Potency	41.2140	2	2
SMAD family member 3	Homo sapiens (human)	Potency	41.2140	2	2
Smad3	Homo sapiens (human)	Potency	19.9526	1	1
TDP1 protein	Homo sapiens (human)	Potency	19.3429	2	5
thioredoxin reductase	Rattus norvegicus (Norway rat)	Potency	34.8728	2	2
thyroid hormone receptor beta isoform 2	Rattus norvegicus (Norway rat)	Potency	32.0194	2	5
thyroid stimulating hormone receptor	Homo sapiens (human)	Potency	39.8107	2	2
USP1 protein, partial	Homo sapiens (human)	Potency	62.0506	1	2
v-jun sarcoma virus 17 oncogene homolog (avian)	Homo sapiens (human)	Potency	14.3120	1	1
vitamin D (1,25- dihydroxyvitamin D3) receptor	Homo sapiens (human)	Potency	49.1648	3	3
vitamin D3 receptor isoform VDRA	Homo sapiens (human)	Potency	66.7820	1	3
Voltage-dependent calcium channel gamma-2 subunit	Mus musculus (house mouse)	Potency	63.3753	1	1

Inhibition Measurements

Protein	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Drugs
17-beta-hydroxysteroid dehydrogenase type 1	Homo sapiens (human)	IC50	2.8300	1	1
17-beta-hydroxysteroid dehydrogenase type 2	Homo sapiens (human)	IC50	0.3600	1	1
3-hydroxy-3-methylglutaryl-coenzyme A reductase	Homo sapiens (human)	IC50	2.9482	2	2
3-hydroxy-3-methylglutaryl-coenzyme A reductase	Schizosaccharomyces pombe 972h-	IC50	2,488.0000	1	1
5-hydroxytryptamine receptor 1A	Rattus norvegicus (Norway rat)	IC50	0.0380	1	1
5-hydroxytryptamine receptor 1A	Rattus norvegicus (Norway rat)	Ki	73.0000	1	1
72 kDa type IV collagenase	Homo sapiens (human)	IC50	0.0100	1	1
Aldo-keto reductase family 1 member B1	Homo sapiens (human)	IC50	0.3200	1	1
Amine oxidase [flavin-containing] A	Rattus norvegicus (Norway rat)	IC50	15.6000	2	2
Amine oxidase [flavin-containing] B	Rattus norvegicus (Norway rat)	IC50	47.2000	1	1
Amyloid-beta precursor protein	Homo sapiens (human)	IC50	19.7000	1	1
Aromatase	Homo sapiens (human)	IC50	3.8000	1	1
ATP-binding cassette sub-family C member 3	Homo sapiens (human)	IC50	133.0000	1	2
Beta-secretase 1	Homo sapiens (human)	IC50	42.2500	2	2
Bile salt export pump	Homo sapiens (human)	IC50	133.6667	2	3
Canalicular multispecific organic anion transporter 1	Homo sapiens (human)	IC50	133.0000	1	2
Cholecystokinin receptor type A	Rattus norvegicus (Norway rat)	IC50	100.0000	2	2
Collagenase 3	Homo sapiens (human)	IC50	0.0140	1	1
Cytochrome P450 1A2	Homo sapiens (human)	IC50	0.2690	1	1
Cytochrome P450 2D6	Homo sapiens (human)	IC50	0.2690	1	1
Cytochrome P450 3A4	Homo sapiens (human)	IC50	0.2690	1	1
Estrogen receptor	Homo sapiens (human)	IC50	1.8700	1	1
Estrogen receptor beta	Homo sapiens (human)	IC50	0.2690	1	1
GABA theta subunit	Rattus norvegicus (Norway rat)	IC50	0.0501	6	8
Gamma-aminobutyric acid	Mus musculus (house mouse)	IC50	0.0000	1	1
Gamma-aminobutyric acid	Mus musculus (house mouse)	Ki	73.0000	1	3
Gamma-aminobutyric acid receptor subunit alpha-1	Bos taurus (cattle)	IC50	0.0380	1	2
Gamma-aminobutyric acid receptor subunit alpha-1	Homo sapiens (human)	IC50	190,579.5055	2	4
Gamma-aminobutyric acid receptor subunit alpha-1	Mus musculus (house mouse)	IC50	0.0370	2	2
Gamma-aminobutyric acid receptor subunit alpha-1	Rattus norvegicus (Norway rat)	IC50	0.0501	6	8
Gamma-aminobutyric acid receptor subunit alpha-1	Bos taurus (cattle)	Ki	0.0008	2	2
Gamma-aminobutyric acid receptor subunit alpha-1	Homo sapiens (human)	Ki	0.0008	1	1
Gamma-aminobutyric acid receptor subunit alpha-1	Mus musculus (house mouse)	Ki	73.0000	1	3
Gamma-aminobutyric acid receptor subunit alpha-2	Bos taurus (cattle)	IC50	0.0380	1	2
Gamma-aminobutyric acid receptor subunit alpha-2	Homo sapiens (human)	IC50	190,579.5055	2	4
Gamma-aminobutyric acid receptor subunit alpha-2	Mus musculus (house mouse)	IC50	0.0000	1	1
Gamma-aminobutyric acid receptor subunit alpha-2	Rattus norvegicus (Norway rat)	IC50	0.0501	6	8
Gamma-aminobutyric acid receptor subunit alpha-2	Bos taurus (cattle)	Ki	0.0008	2	2
Gamma-aminobutyric acid receptor subunit alpha-2	Homo sapiens (human)	Ki	0.0008	1	1
Gamma-aminobutyric acid receptor subunit alpha-2	Mus musculus (house mouse)	Ki	73.0000	1	3
Gamma-aminobutyric acid receptor subunit alpha-3	Bos taurus (cattle)	IC50	0.0380	1	2
Gamma-aminobutyric acid receptor subunit alpha-3	Homo sapiens (human)	IC50	190,579.5055	2	4
Gamma-aminobutyric acid receptor subunit alpha-3	Mus musculus (house mouse)	IC50	0.0000	1	1
Gamma-aminobutyric acid receptor subunit alpha-3	Rattus norvegicus (Norway rat)	IC50	0.0501	6	8
Gamma-aminobutyric acid receptor subunit alpha-3	Bos taurus (cattle)	Ki	0.0008	2	2
Gamma-aminobutyric acid receptor subunit alpha-3	Homo sapiens (human)	Ki	0.0008	1	1
Gamma-aminobutyric acid receptor subunit alpha-3	Mus musculus (house mouse)	Ki	73.0000	1	3
Gamma-aminobutyric acid receptor subunit alpha-4	Bos taurus (cattle)	IC50	0.0380	1	2
Gamma-aminobutyric acid receptor subunit alpha-4	Homo sapiens (human)	IC50	190,579.5055	2	4
Gamma-aminobutyric acid receptor subunit alpha-4	Mus musculus (house mouse)	IC50	0.0000	1	1
Gamma-aminobutyric acid receptor subunit alpha-4	Rattus norvegicus (Norway rat)	IC50	0.0501	6	8
Gamma-aminobutyric acid receptor subunit alpha-4	Bos taurus (cattle)	Ki	0.0008	2	2
Gamma-aminobutyric acid receptor subunit alpha-4	Homo sapiens (human)	Ki	0.0008	1	1
Gamma-aminobutyric acid receptor subunit alpha-4	Mus musculus (house mouse)	Ki	73.0000	1	3
Gamma-aminobutyric acid receptor subunit alpha-5	Homo sapiens (human)	IC50	190,579.5055	2	4
Gamma-aminobutyric acid receptor subunit alpha-5	Mus musculus (house mouse)	IC50	0.0000	1	1
Gamma-aminobutyric acid receptor subunit alpha-5	Rattus norvegicus (Norway rat)	IC50	0.0501	6	8
Gamma-aminobutyric acid receptor subunit alpha-5	Homo sapiens (human)	Ki	0.0008	1	1
Gamma-aminobutyric acid receptor subunit alpha-5	Mus musculus (house mouse)	Ki	73.0000	1	3
Gamma-aminobutyric acid receptor subunit alpha-6	Homo sapiens (human)	IC50	190,579.5055	2	4
Gamma-aminobutyric acid receptor subunit alpha-6	Mus musculus (house mouse)	IC50	0.0000	1	1
Gamma-aminobutyric acid receptor subunit alpha-6	Rattus norvegicus (Norway rat)	IC50	0.0501	6	8
Gamma-aminobutyric acid receptor subunit alpha-6	Homo sapiens (human)	Ki	0.0008	1	1
Gamma-aminobutyric acid receptor subunit alpha-6	Mus musculus (house mouse)	Ki	73.0000	1	3
Gamma-aminobutyric acid receptor subunit beta-1	Bos taurus (cattle)	IC50	0.0380	1	2
Gamma-aminobutyric acid receptor subunit beta-1	Homo sapiens (human)	IC50	190,579.5055	2	4
Gamma-aminobutyric acid receptor subunit beta-1	Mus musculus (house mouse)	IC50	0.0000	1	1
Gamma-aminobutyric acid receptor subunit beta-1	Rattus norvegicus (Norway rat)	IC50	0.0501	6	8
Gamma-aminobutyric acid receptor subunit beta-1	Bos taurus (cattle)	Ki	0.0008	2	2
Gamma-aminobutyric acid receptor subunit beta-1	Homo sapiens (human)	Ki	0.0008	1	1
Gamma-aminobutyric acid receptor subunit beta-1	Mus musculus (house mouse)	Ki	73.0000	1	3
Gamma-aminobutyric acid receptor subunit beta-2	Homo sapiens (human)	IC50	190,579.5055	2	4
Gamma-aminobutyric acid receptor subunit beta-2	Rattus norvegicus (Norway rat)	IC50	0.0501	6	8
Gamma-aminobutyric acid receptor subunit beta-2	Homo sapiens (human)	Ki	0.0008	1	1
Gamma-aminobutyric acid receptor subunit beta-3	Homo sapiens (human)	IC50	190,579.5055	2	4
Gamma-aminobutyric acid receptor subunit beta-3	Mus musculus (house mouse)	IC50	0.0000	1	1
Gamma-aminobutyric acid receptor subunit beta-3	Rattus norvegicus (Norway rat)	IC50	0.0501	6	8
Gamma-aminobutyric acid receptor subunit beta-3	Homo sapiens (human)	Ki	0.0008	1	1
Gamma-aminobutyric acid receptor subunit beta-3	Mus musculus (house mouse)	Ki	73.0000	1	3
Gamma-aminobutyric acid receptor subunit delta	Homo sapiens (human)	IC50	190,579.5055	2	4
Gamma-aminobutyric acid receptor subunit delta	Mus musculus (house mouse)	IC50	0.0000	1	1
Gamma-aminobutyric acid receptor subunit delta	Rattus norvegicus (Norway rat)	IC50	0.0501	6	8
Gamma-aminobutyric acid receptor subunit delta	Homo sapiens (human)	Ki	0.0008	1	1
Gamma-aminobutyric acid receptor subunit delta	Mus musculus (house mouse)	Ki	73.0000	1	3
Gamma-aminobutyric acid receptor subunit epsilon	Homo sapiens (human)	IC50	190,579.5055	2	4
Gamma-aminobutyric acid receptor subunit epsilon	Rattus norvegicus (Norway rat)	IC50	0.0501	6	8
Gamma-aminobutyric acid receptor subunit epsilon	Homo sapiens (human)	Ki	0.0008	1	1
Gamma-aminobutyric acid receptor subunit gamma-1	Homo sapiens (human)	IC50	190,579.5055	2	4
Gamma-aminobutyric acid receptor subunit gamma-1	Mus musculus (house mouse)	IC50	0.0000	1	1
Gamma-aminobutyric acid receptor subunit gamma-1	Rattus norvegicus (Norway rat)	IC50	0.0501	6	8
Gamma-aminobutyric acid receptor subunit gamma-1	Homo sapiens (human)	Ki	0.0008	1	1
Gamma-aminobutyric acid receptor subunit gamma-1	Mus musculus (house mouse)	Ki	73.0000	1	3
Gamma-aminobutyric acid receptor subunit gamma-2	Bos taurus (cattle)	IC50	0.0380	1	2
Gamma-aminobutyric acid receptor subunit gamma-2	Homo sapiens (human)	IC50	190,579.5055	2	4
Gamma-aminobutyric acid receptor subunit gamma-2	Mus musculus (house mouse)	IC50	0.0000	1	1
Gamma-aminobutyric acid receptor subunit gamma-2	Rattus norvegicus (Norway rat)	IC50	0.0501	6	8
Gamma-aminobutyric acid receptor subunit gamma-2	Bos taurus (cattle)	Ki	0.0008	2	2
Gamma-aminobutyric acid receptor subunit gamma-2	Homo sapiens (human)	Ki	0.0008	1	1
Gamma-aminobutyric acid receptor subunit gamma-2	Mus musculus (house mouse)	Ki	73.0000	1	3
Gamma-aminobutyric acid receptor subunit gamma-3	Homo sapiens (human)	IC50	190,579.5055	2	4
Gamma-aminobutyric acid receptor subunit gamma-3	Mus musculus (house mouse)	IC50	0.0000	1	1
Gamma-aminobutyric acid receptor subunit gamma-3	Rattus norvegicus (Norway rat)	IC50	0.0501	6	8
Gamma-aminobutyric acid receptor subunit gamma-3	Homo sapiens (human)	Ki	0.0008	1	1
Gamma-aminobutyric acid receptor subunit gamma-3	Mus musculus (house mouse)	Ki	73.0000	1	3
Gamma-aminobutyric acid receptor subunit pi	Homo sapiens (human)	IC50	190,579.5055	2	4
Gamma-aminobutyric acid receptor subunit pi	Mus musculus (house mouse)	IC50	0.0000	1	1
Gamma-aminobutyric acid receptor subunit pi	Rattus norvegicus (Norway rat)	IC50	0.0501	6	8
Gamma-aminobutyric acid receptor subunit pi	Homo sapiens (human)	Ki	0.0008	1	1
Gamma-aminobutyric acid receptor subunit pi	Mus musculus (house mouse)	Ki	73.0000	1	3
Gamma-aminobutyric acid receptor subunit theta	Homo sapiens (human)	IC50	190,579.5055	2	4
Gamma-aminobutyric acid receptor subunit theta	Mus musculus (house mouse)	IC50	0.0000	1	1
Gamma-aminobutyric acid receptor subunit theta	Homo sapiens (human)	Ki	0.0008	1	1
Gamma-aminobutyric acid receptor subunit theta	Mus musculus (house mouse)	Ki	73.0000	1	3
Gastrin/cholecystokinin type B receptor	Rattus norvegicus (Norway rat)	IC50	100.0000	1	1
Glucose-6-phosphate 1-dehydrogenase	Homo sapiens (human)	IC50	66.0000	1	1
Integrase	Human immunodeficiency virus 1	IC50	100.0000	2	2
Interstitial collagenase	Homo sapiens (human)	IC50	0.0160	1	1
Lysine-specific demethylase 4C	Homo sapiens (human)	IC50	200.0000	1	1
Lysine-specific demethylase 4C	Homo sapiens (human)	Ki	200.0000	1	1
Matrilysin	Homo sapiens (human)	IC50	0.0080	1	1
Matrix metalloproteinase-9	Homo sapiens (human)	IC50	1.3265	2	2
Multidrug resistance-associated protein 4	Homo sapiens (human)	IC50	133.0000	1	2
NACHT, LRR and PYD domains-containing protein 3	Homo sapiens (human)	IC50	5.8200	2	2
Neuronal acetylcholine receptor subunit alpha-4	Rattus norvegicus (Norway rat)	Ki	0.0008	1	1
Neuronal acetylcholine receptor subunit beta-2	Rattus norvegicus (Norway rat)	Ki	0.0008	1	1
Nuclear factor NF-kappa-B p100 subunit	Homo sapiens (human)	IC50	32.0000	1	1
Nuclear factor NF-kappa-B p105 subunit	Homo sapiens (human)	IC50	32.0000	1	1
Polyunsaturated fatty acid 5-lipoxygenase	Rattus norvegicus (Norway rat)	IC50	35.0000	1	1
Proteasome subunit beta type-5	Homo sapiens (human)	IC50	4.8800	1	1
Protein disulfide-isomerase	Homo sapiens (human)	Ki	36.1000	1	1
Sodium- and chloride-dependent betaine transporter	Rattus norvegicus (Norway rat)	IC50	0.0910	1	1
Sodium- and chloride-dependent GABA transporter 1	Rattus norvegicus (Norway rat)	IC50	0.0910	1	1
Sodium- and chloride-dependent GABA transporter 2	Rattus norvegicus (Norway rat)	IC50	0.0910	1	1
Sodium- and chloride-dependent GABA transporter 3	Rattus norvegicus (Norway rat)	IC50	0.0910	1	1
Stromelysin-1	Homo sapiens (human)	IC50	0.0810	1	1
Transcription factor p65	Homo sapiens (human)	IC50	32.0000	1	1
Translocator protein	Homo sapiens (human)	IC50	254,106.0000	1	3
Translocator protein	Bos taurus (cattle)	Ki	0.0008	1	1
Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)	IC50	55.0000	2	2
Tyrosyl-DNA phosphodiesterase 1	Homo sapiens (human)	IC50	55.0000	1	1
Xanthine dehydrogenase/oxidase	Bos taurus (cattle)	IC50	47.3000	1	1

Activation Measurements

Protein	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Drugs
bcl-2-like protein 11 isoform 1	Homo sapiens (human)	EC50	350.0000	1	1
Chain A, BCL-2-RELATED PROTEIN A1	Homo sapiens (human)	EC50	350.0000	1	1
Gamma-aminobutyric acid	Mus musculus (house mouse)	EC50	0.8710	1	1
Gamma-aminobutyric acid receptor subunit alpha-1	Homo sapiens (human)	EC50	5.3849	6	6
Gamma-aminobutyric acid receptor subunit alpha-1	Mus musculus (house mouse)	EC50	0.8710	1	1
Gamma-aminobutyric acid receptor subunit alpha-2	Homo sapiens (human)	EC50	0.1562	2	2
Gamma-aminobutyric acid receptor subunit alpha-2	Mus musculus (house mouse)	EC50	0.8710	1	1
Gamma-aminobutyric acid receptor subunit alpha-3	Homo sapiens (human)	EC50	0.1562	2	2
Gamma-aminobutyric acid receptor subunit alpha-3	Mus musculus (house mouse)	EC50	0.8710	1	1
Gamma-aminobutyric acid receptor subunit alpha-4	Homo sapiens (human)	EC50	0.1293	3	3
Gamma-aminobutyric acid receptor subunit alpha-4	Mus musculus (house mouse)	EC50	0.8710	1	1
Gamma-aminobutyric acid receptor subunit alpha-5	Homo sapiens (human)	EC50	0.1562	2	2
Gamma-aminobutyric acid receptor subunit alpha-5	Mus musculus (house mouse)	EC50	0.8710	1	1
Gamma-aminobutyric acid receptor subunit alpha-6	Homo sapiens (human)	EC50	0.1562	2	2
Gamma-aminobutyric acid receptor subunit alpha-6	Mus musculus (house mouse)	EC50	0.8710	1	1
Gamma-aminobutyric acid receptor subunit beta-1	Homo sapiens (human)	EC50	0.1562	2	2
Gamma-aminobutyric acid receptor subunit beta-1	Mus musculus (house mouse)	EC50	0.8710	1	1
Gamma-aminobutyric acid receptor subunit beta-2	Homo sapiens (human)	EC50	2.6619	5	5
Gamma-aminobutyric acid receptor subunit beta-3	Homo sapiens (human)	EC50	4.8470	4	4
Gamma-aminobutyric acid receptor subunit beta-3	Mus musculus (house mouse)	EC50	0.8710	1	1
Gamma-aminobutyric acid receptor subunit delta	Homo sapiens (human)	EC50	0.0755	1	1
Gamma-aminobutyric acid receptor subunit delta	Mus musculus (house mouse)	EC50	0.8710	1	1
Gamma-aminobutyric acid receptor subunit gamma-1	Mus musculus (house mouse)	EC50	0.8710	1	1
Gamma-aminobutyric acid receptor subunit gamma-2	Homo sapiens (human)	EC50	7.9992	4	4
Gamma-aminobutyric acid receptor subunit gamma-2	Mus musculus (house mouse)	EC50	0.8710	1	1
Gamma-aminobutyric acid receptor subunit gamma-3	Mus musculus (house mouse)	EC50	0.8710	1	1
Gamma-aminobutyric acid receptor subunit pi	Mus musculus (house mouse)	EC50	0.8710	1	1
Gamma-aminobutyric acid receptor subunit theta	Mus musculus (house mouse)	EC50	0.8710	1	1
Neuronal acetylcholine receptor subunit alpha-7	Homo sapiens (human)	EC50	11.6000	1	1
Retinoic acid receptor RXR-alpha	Homo sapiens (human)	EC50	27.0000	1	1
Retinoic acid receptor RXR-beta	Homo sapiens (human)	EC50	5.2000	1	1
Retinoic acid receptor RXR-gamma	Homo sapiens (human)	EC50	43.0000	1	1
SWI/SNF related, matrix associated, actin dependent regulator of chromatin, subfamily a, member 2, isoform CRA_a	Homo sapiens (human)	EC50	91.1400	1	1

Other Measurements

Protein	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Drugs
Albumin	Homo sapiens (human)	Activity	17.0000	1	1
Alpha-1-acid glycoprotein 1	Homo sapiens (human)	Activity	9.0000	1	1
Gamma-aminobutyric acid receptor subunit alpha-1	Bos taurus (cattle)	POT	0.1050	1	1
Gamma-aminobutyric acid receptor subunit alpha-2	Bos taurus (cattle)	POT	0.1050	1	1
Gamma-aminobutyric acid receptor subunit alpha-3	Bos taurus (cattle)	POT	0.1050	1	1
Gamma-aminobutyric acid receptor subunit alpha-4	Bos taurus (cattle)	POT	0.1050	1	1
Gamma-aminobutyric acid receptor subunit beta-1	Bos taurus (cattle)	POT	0.1050	1	1
Gamma-aminobutyric acid receptor subunit gamma-2	Bos taurus (cattle)	POT	0.1050	1	1
Mu-type opioid receptor	Cavia porcellus (domestic guinea pig)	Activity	17.0000	1	1
Quinone oxidoreductase	Mus musculus (house mouse)	Activity	4.6433	3	3
Quinone oxidoreductase	Mus musculus (house mouse)	CD	6.2333	3	3
Substance-P receptor	Cavia porcellus (domestic guinea pig)	CD	11.0000	1	1

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