Page last updated: 2024-08-05 15:16:29

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)

MemberDefinitionClass
6,6-dimethyl-2-methylenebicyclo(3.1.1)heptan-3-olA 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-asaroneThe trans-isomer of asarone.alpha-asarone
beta-asaroneThe cis-isomer of asarone.beta-asarone
brexanoloneA 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
chlorazepateA 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
clobazam7-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
clonazepam1,3-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 dipotassiumThe 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
estazolamA 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
isoliquiritigeninA member of the class of chalcones that is trans-chalcone hydroxylated at C-2', -4 and -4'.isoliquiritigenin
nimetazepamA 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
nitrazepamA 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
nordazepamA 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
secobarbitalA 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 acidA 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
verruculogenAn organic heterohexacyclic compound that is a mycotoxic indole alkaloid isolated from Penicillium and Aspergillus species.verruculogen

Research

Studies (5,990)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-19902,492 (41.60)18.7374
1990's993 (16.58)18.2507
2000's886 (14.79)29.6817
2010's1,196 (19.97)24.3611
2020's423 (7.06)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials832 (12.21%)5.53%
Reviews426 (6.25%)6.00%
Case Studies1,098 (16.11%)4.05%
Observational11 (0.16%)0.25%
Other4,448 (65.27%)84.16%

Protein Targets (203)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency26.651412
2,3-bisphosphoglycerate-independent phosphoglycerate mutaseLeishmania major strain FriedlinPotency37.933011
67.9K proteinVaccinia virusPotency16.803722
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency17.782811
Alpha-synucleinHomo sapiens (human)Potency32.642711
Amyloid-beta precursor proteinHomo sapiens (human)Potency16.360111
AR proteinHomo sapiens (human)Potency19.5805712
ATAD5 protein, partialHomo sapiens (human)Potency10.984544
Ataxin-2Homo sapiens (human)Potency17.854922
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency6.012011
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency13.372222
atrial natriuretic peptide receptor 1 precursorHomo sapiens (human)Potency30.131311
atrial natriuretic peptide receptor 2 precursorHomo sapiens (human)Potency26.121611
Bloom syndrome protein isoform 1Homo sapiens (human)Potency50.118722
Cellular tumor antigen p53Homo sapiens (human)Potency10.354612
Chain A, Beta-lactamaseEscherichia coli K-12Potency112.202011
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency7.611012
chromobox protein homolog 1Homo sapiens (human)Potency62.303222
cytochrome P450 2C19 precursorHomo sapiens (human)Potency3.981111
cytochrome P450 2C9 precursorHomo sapiens (human)Potency7.943311
cytochrome P450 2C9, partialHomo sapiens (human)Potency43.648611
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency6.990624
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency13.802912
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency4.276513
D(1A) dopamine receptorHomo sapiens (human)Potency15.848911
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency85.894313
DNA polymerase kappa isoform 1Homo sapiens (human)Potency89.125111
endonuclease IVEscherichia coliPotency0.631011
estrogen nuclear receptor alphaHomo sapiens (human)Potency34.573378
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency71.108311
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency35.4548710
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency44.234813
Fatty-acid amide hydrolase 1Rattus norvegicus (Norway rat)Potency19.952611
flap endonuclease 1Homo sapiens (human)Potency8.436811
GVesicular stomatitis virusPotency43.648611
GABA theta subunitRattus norvegicus (Norway rat)Potency6.990612
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency6.990612
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency6.990612
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency6.990612
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency6.990612
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency6.990612
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency6.990612
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency6.990612
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency6.990612
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency6.990612
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency6.990612
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency6.990612
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency6.990612
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency6.990612
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency6.990612
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency6.990612
gemininHomo sapiens (human)Potency13.047246
GLI family zinc finger 3Homo sapiens (human)Potency40.151022
glp-1 receptor, partialHomo sapiens (human)Potency17.631622
GLS proteinHomo sapiens (human)Potency10.000011
glucocerebrosidaseHomo sapiens (human)Potency11.263769
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency4.486647
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency63.375311
heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa)Homo sapiens (human)Potency23.799612
heat shock protein beta-1Homo sapiens (human)Potency58.091822
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency7.943313
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency39.810711
histone-lysine N-methyltransferase 2A isoform 2 precursorHomo sapiens (human)Potency31.622811
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency43.648611
IDH1Homo sapiens (human)Potency25.929011
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency43.648612
Interferon betaHomo sapiens (human)Potency45.871824
interleukin 8Homo sapiens (human)Potency74.978011
lamin isoform A-delta10Homo sapiens (human)Potency8.416814
LuciferasePhotinus pyralis (common eastern firefly)Potency10.691011
M-phase phosphoprotein 8Homo sapiens (human)Potency35.481311
Microtubule-associated protein tauHomo sapiens (human)Potency9.712115
muscleblind-like protein 1 isoform 1Homo sapiens (human)Potency12.589311
neuropeptide S receptor isoform AHomo sapiens (human)Potency31.622811
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency15.848911
Nrf2Homo sapiens (human)Potency16.592822
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency68.928133
Nuclear receptor ROR-gammaHomo sapiens (human)Potency37.578011
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency12.594126
nuclear receptor subfamily 1, group I, member 2Rattus norvegicus (Norway rat)Potency39.810711
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency63.375311
P53Homo sapiens (human)Potency50.118711
peptidyl-prolyl cis-trans isomerase NIMA-interacting 1Homo sapiens (human)Potency21.331311
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency15.101411
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency56.977211
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency31.914344
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency3.981111
PPM1D proteinHomo sapiens (human)Potency46.612812
pregnane X nuclear receptorHomo sapiens (human)Potency25.155524
progesterone receptorHomo sapiens (human)Potency28.308711
RAR-related orphan receptor gammaMus musculus (house mouse)Potency30.410822
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency47.461833
retinoid X nuclear receptor alphaHomo sapiens (human)Potency10.000011
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency26.121611
SMAD family member 2Homo sapiens (human)Potency41.214022
SMAD family member 3Homo sapiens (human)Potency41.214022
Smad3Homo sapiens (human)Potency19.952611
TDP1 proteinHomo sapiens (human)Potency19.342925
thioredoxin reductaseRattus norvegicus (Norway rat)Potency34.872822
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency32.019425
thyroid stimulating hormone receptorHomo sapiens (human)Potency39.810722
USP1 protein, partialHomo sapiens (human)Potency62.050612
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency14.312011
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency49.164833
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency66.782013
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency63.375311

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
17-beta-hydroxysteroid dehydrogenase type 1Homo sapiens (human)IC502.830011
17-beta-hydroxysteroid dehydrogenase type 2Homo sapiens (human)IC500.360011
3-hydroxy-3-methylglutaryl-coenzyme A reductaseHomo sapiens (human)IC502.948222
3-hydroxy-3-methylglutaryl-coenzyme A reductaseSchizosaccharomyces pombe 972h-IC502,488.000011
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)IC500.038011
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki73.000011
72 kDa type IV collagenaseHomo sapiens (human)IC500.010011
Aldo-keto reductase family 1 member B1Homo sapiens (human)IC500.320011
Amine oxidase [flavin-containing] A Rattus norvegicus (Norway rat)IC5015.600022
Amine oxidase [flavin-containing] BRattus norvegicus (Norway rat)IC5047.200011
Amyloid-beta precursor proteinHomo sapiens (human)IC5019.700011
AromataseHomo sapiens (human)IC503.800011
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50133.000012
Beta-secretase 1Homo sapiens (human)IC5042.250022
Bile salt export pumpHomo sapiens (human)IC50133.666723
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50133.000012
Cholecystokinin receptor type ARattus norvegicus (Norway rat)IC50100.000022
Collagenase 3Homo sapiens (human)IC500.014011
Cytochrome P450 1A2Homo sapiens (human)IC500.269011
Cytochrome P450 2D6Homo sapiens (human)IC500.269011
Cytochrome P450 3A4Homo sapiens (human)IC500.269011
Estrogen receptorHomo sapiens (human)IC501.870011
Estrogen receptor betaHomo sapiens (human)IC500.269011
GABA theta subunitRattus norvegicus (Norway rat)IC500.050168
Gamma-aminobutyric acid Mus musculus (house mouse)IC500.000011
Gamma-aminobutyric acid Mus musculus (house mouse)Ki73.000013
Gamma-aminobutyric acid receptor subunit alpha-1Bos taurus (cattle)IC500.038012
Gamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)IC50190,579.505524
Gamma-aminobutyric acid receptor subunit alpha-1Mus musculus (house mouse)IC500.037022
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)IC500.050168
Gamma-aminobutyric acid receptor subunit alpha-1Bos taurus (cattle)Ki0.000822
Gamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)Ki0.000811
Gamma-aminobutyric acid receptor subunit alpha-1Mus musculus (house mouse)Ki73.000013
Gamma-aminobutyric acid receptor subunit alpha-2Bos taurus (cattle)IC500.038012
Gamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)IC50190,579.505524
Gamma-aminobutyric acid receptor subunit alpha-2Mus musculus (house mouse)IC500.000011
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)IC500.050168
Gamma-aminobutyric acid receptor subunit alpha-2Bos taurus (cattle)Ki0.000822
Gamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)Ki0.000811
Gamma-aminobutyric acid receptor subunit alpha-2Mus musculus (house mouse)Ki73.000013
Gamma-aminobutyric acid receptor subunit alpha-3Bos taurus (cattle)IC500.038012
Gamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)IC50190,579.505524
Gamma-aminobutyric acid receptor subunit alpha-3Mus musculus (house mouse)IC500.000011
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)IC500.050168
Gamma-aminobutyric acid receptor subunit alpha-3Bos taurus (cattle)Ki0.000822
Gamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)Ki0.000811
Gamma-aminobutyric acid receptor subunit alpha-3Mus musculus (house mouse)Ki73.000013
Gamma-aminobutyric acid receptor subunit alpha-4Bos taurus (cattle)IC500.038012
Gamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)IC50190,579.505524
Gamma-aminobutyric acid receptor subunit alpha-4Mus musculus (house mouse)IC500.000011
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)IC500.050168
Gamma-aminobutyric acid receptor subunit alpha-4Bos taurus (cattle)Ki0.000822
Gamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)Ki0.000811
Gamma-aminobutyric acid receptor subunit alpha-4Mus musculus (house mouse)Ki73.000013
Gamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)IC50190,579.505524
Gamma-aminobutyric acid receptor subunit alpha-5Mus musculus (house mouse)IC500.000011
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)IC500.050168
Gamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)Ki0.000811
Gamma-aminobutyric acid receptor subunit alpha-5Mus musculus (house mouse)Ki73.000013
Gamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)IC50190,579.505524
Gamma-aminobutyric acid receptor subunit alpha-6Mus musculus (house mouse)IC500.000011
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)IC500.050168
Gamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)Ki0.000811
Gamma-aminobutyric acid receptor subunit alpha-6Mus musculus (house mouse)Ki73.000013
Gamma-aminobutyric acid receptor subunit beta-1Bos taurus (cattle)IC500.038012
Gamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)IC50190,579.505524
Gamma-aminobutyric acid receptor subunit beta-1Mus musculus (house mouse)IC500.000011
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)IC500.050168
Gamma-aminobutyric acid receptor subunit beta-1Bos taurus (cattle)Ki0.000822
Gamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)Ki0.000811
Gamma-aminobutyric acid receptor subunit beta-1Mus musculus (house mouse)Ki73.000013
Gamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)IC50190,579.505524
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)IC500.050168
Gamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)Ki0.000811
Gamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)IC50190,579.505524
Gamma-aminobutyric acid receptor subunit beta-3Mus musculus (house mouse)IC500.000011
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)IC500.050168
Gamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)Ki0.000811
Gamma-aminobutyric acid receptor subunit beta-3Mus musculus (house mouse)Ki73.000013
Gamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)IC50190,579.505524
Gamma-aminobutyric acid receptor subunit deltaMus musculus (house mouse)IC500.000011
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)IC500.050168
Gamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)Ki0.000811
Gamma-aminobutyric acid receptor subunit deltaMus musculus (house mouse)Ki73.000013
Gamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)IC50190,579.505524
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)IC500.050168
Gamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)Ki0.000811
Gamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)IC50190,579.505524
Gamma-aminobutyric acid receptor subunit gamma-1Mus musculus (house mouse)IC500.000011
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)IC500.050168
Gamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)Ki0.000811
Gamma-aminobutyric acid receptor subunit gamma-1Mus musculus (house mouse)Ki73.000013
Gamma-aminobutyric acid receptor subunit gamma-2Bos taurus (cattle)IC500.038012
Gamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)IC50190,579.505524
Gamma-aminobutyric acid receptor subunit gamma-2Mus musculus (house mouse)IC500.000011
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)IC500.050168
Gamma-aminobutyric acid receptor subunit gamma-2Bos taurus (cattle)Ki0.000822
Gamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)Ki0.000811
Gamma-aminobutyric acid receptor subunit gamma-2Mus musculus (house mouse)Ki73.000013
Gamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)IC50190,579.505524
Gamma-aminobutyric acid receptor subunit gamma-3Mus musculus (house mouse)IC500.000011
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)IC500.050168
Gamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)Ki0.000811
Gamma-aminobutyric acid receptor subunit gamma-3Mus musculus (house mouse)Ki73.000013
Gamma-aminobutyric acid receptor subunit piHomo sapiens (human)IC50190,579.505524
Gamma-aminobutyric acid receptor subunit piMus musculus (house mouse)IC500.000011
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)IC500.050168
Gamma-aminobutyric acid receptor subunit piHomo sapiens (human)Ki0.000811
Gamma-aminobutyric acid receptor subunit piMus musculus (house mouse)Ki73.000013
Gamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)IC50190,579.505524
Gamma-aminobutyric acid receptor subunit thetaMus musculus (house mouse)IC500.000011
Gamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)Ki0.000811
Gamma-aminobutyric acid receptor subunit thetaMus musculus (house mouse)Ki73.000013
Gastrin/cholecystokinin type B receptorRattus norvegicus (Norway rat)IC50100.000011
Glucose-6-phosphate 1-dehydrogenaseHomo sapiens (human)IC5066.000011
Integrase Human immunodeficiency virus 1IC50100.000022
Interstitial collagenaseHomo sapiens (human)IC500.016011
Lysine-specific demethylase 4CHomo sapiens (human)IC50200.000011
Lysine-specific demethylase 4CHomo sapiens (human)Ki200.000011
MatrilysinHomo sapiens (human)IC500.008011
Matrix metalloproteinase-9Homo sapiens (human)IC501.326522
Multidrug resistance-associated protein 4Homo sapiens (human)IC50133.000012
NACHT, LRR and PYD domains-containing protein 3 Homo sapiens (human)IC505.820022
Neuronal acetylcholine receptor subunit alpha-4Rattus norvegicus (Norway rat)Ki0.000811
Neuronal acetylcholine receptor subunit beta-2Rattus norvegicus (Norway rat)Ki0.000811
Nuclear factor NF-kappa-B p100 subunit Homo sapiens (human)IC5032.000011
Nuclear factor NF-kappa-B p105 subunitHomo sapiens (human)IC5032.000011
Polyunsaturated fatty acid 5-lipoxygenaseRattus norvegicus (Norway rat)IC5035.000011
Proteasome subunit beta type-5Homo sapiens (human)IC504.880011
Protein disulfide-isomeraseHomo sapiens (human)Ki36.100011
Sodium- and chloride-dependent betaine transporterRattus norvegicus (Norway rat)IC500.091011
Sodium- and chloride-dependent GABA transporter 1Rattus norvegicus (Norway rat)IC500.091011
Sodium- and chloride-dependent GABA transporter 2Rattus norvegicus (Norway rat)IC500.091011
Sodium- and chloride-dependent GABA transporter 3Rattus norvegicus (Norway rat)IC500.091011
Stromelysin-1Homo sapiens (human)IC500.081011
Transcription factor p65Homo sapiens (human)IC5032.000011
Translocator proteinHomo sapiens (human)IC50254,106.000013
Translocator proteinBos taurus (cattle)Ki0.000811
Tyrosine-protein phosphatase non-receptor type 1Homo sapiens (human)IC5055.000022
Tyrosyl-DNA phosphodiesterase 1Homo sapiens (human)IC5055.000011
Xanthine dehydrogenase/oxidaseBos taurus (cattle)IC5047.300011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
bcl-2-like protein 11 isoform 1Homo sapiens (human)EC50350.000011
Chain A, BCL-2-RELATED PROTEIN A1Homo sapiens (human)EC50350.000011
Gamma-aminobutyric acid Mus musculus (house mouse)EC500.871011
Gamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)EC505.384966
Gamma-aminobutyric acid receptor subunit alpha-1Mus musculus (house mouse)EC500.871011
Gamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)EC500.156222
Gamma-aminobutyric acid receptor subunit alpha-2Mus musculus (house mouse)EC500.871011
Gamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)EC500.156222
Gamma-aminobutyric acid receptor subunit alpha-3Mus musculus (house mouse)EC500.871011
Gamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)EC500.129333
Gamma-aminobutyric acid receptor subunit alpha-4Mus musculus (house mouse)EC500.871011
Gamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)EC500.156222
Gamma-aminobutyric acid receptor subunit alpha-5Mus musculus (house mouse)EC500.871011
Gamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)EC500.156222
Gamma-aminobutyric acid receptor subunit alpha-6Mus musculus (house mouse)EC500.871011
Gamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)EC500.156222
Gamma-aminobutyric acid receptor subunit beta-1Mus musculus (house mouse)EC500.871011
Gamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)EC502.661955
Gamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)EC504.847044
Gamma-aminobutyric acid receptor subunit beta-3Mus musculus (house mouse)EC500.871011
Gamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)EC500.075511
Gamma-aminobutyric acid receptor subunit deltaMus musculus (house mouse)EC500.871011
Gamma-aminobutyric acid receptor subunit gamma-1Mus musculus (house mouse)EC500.871011
Gamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)EC507.999244
Gamma-aminobutyric acid receptor subunit gamma-2Mus musculus (house mouse)EC500.871011
Gamma-aminobutyric acid receptor subunit gamma-3Mus musculus (house mouse)EC500.871011
Gamma-aminobutyric acid receptor subunit piMus musculus (house mouse)EC500.871011
Gamma-aminobutyric acid receptor subunit thetaMus musculus (house mouse)EC500.871011
Neuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)EC5011.600011
Retinoic acid receptor RXR-alphaHomo sapiens (human)EC5027.000011
Retinoic acid receptor RXR-betaHomo sapiens (human)EC505.200011
Retinoic acid receptor RXR-gammaHomo sapiens (human)EC5043.000011
SWI/SNF related, matrix associated, actin dependent regulator of chromatin, subfamily a, member 2, isoform CRA_aHomo sapiens (human)EC5091.140011

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
AlbuminHomo sapiens (human)Activity17.000011
Alpha-1-acid glycoprotein 1Homo sapiens (human)Activity9.000011
Gamma-aminobutyric acid receptor subunit alpha-1Bos taurus (cattle)POT0.105011
Gamma-aminobutyric acid receptor subunit alpha-2Bos taurus (cattle)POT0.105011
Gamma-aminobutyric acid receptor subunit alpha-3Bos taurus (cattle)POT0.105011
Gamma-aminobutyric acid receptor subunit alpha-4Bos taurus (cattle)POT0.105011
Gamma-aminobutyric acid receptor subunit beta-1Bos taurus (cattle)POT0.105011
Gamma-aminobutyric acid receptor subunit gamma-2Bos taurus (cattle)POT0.105011
Mu-type opioid receptorCavia porcellus (domestic guinea pig)Activity17.000011
Quinone oxidoreductaseMus musculus (house mouse)Activity4.643333
Quinone oxidoreductaseMus musculus (house mouse)CD6.233333
Substance-P receptorCavia porcellus (domestic guinea pig)CD11.000011