Page last updated: 2024-08-05 15:20:40

GABA antagonist

A compound that inhibits the action of gamma-aminobutyric acid.

ChEBI ID: 65259

Members (7)

MemberDefinitionClass
clozapineA benzodiazepine that is 5H-dibenzo[b,e][1,4]diazepine substituted by a chloro group at position 8 and a 4-methylpiperazin-1-yl group at position 11. It is a second generation antipsychotic used in the treatment of psychiatric disorders like schizophrenia.clozapine
flumazenilAn organic heterotricyclic compound that is 5,6-dihydro-4H-imidazo[1,5-a][1,4]benzodiazepine which is substituted at positions 3, 5, 6, and 8 by ethoxycarbonyl, methyl, oxo, and fluoro groups, respectively. It is used as an antidote to benzodiazepine overdose.flumazenil
megestrol acetateA sesquiterpene lactone with formula C15H20O8. It is a neurotoxic natural product found in plants of the family Illiciaceae.anisatin
picrotoxininA picrotoxane sesquiterpenoid that is 3a,4,5,6,7,7a-hexahydro-1H-indene-3,7-dicarboxylic acid which is substituted at positions 3a, 6, and 7a by methyl, isopropenyl, and hydroxy groups, respectively; in which the double bond at position 2-3 has been epoxidised; and in which the carboxy groups at positions 3 and 7 have undergone gamma-lactone formation by O-alkylation to positions 4 and 5, respectively. A component of picrotoxin.picrotoxinin
suraminA member of the class of phenylureas that is urea in which each of the amino groups has been substituted by a 3-({2-methyl-5-[(4,6,8-trisulfo-1-naphthyl)carbamoyl]phenyl}carbamoyl)phenyl group. An activator of both the rabbit skeletal muscle RyR1 and sheep cardiac RyR2 isoform ryanodine receptor channels, it has been used for the treatment of human African trypanosomiasis for over 100 years.suramin
suramin sodiumAn organic sodium salt that is the hexasodium salt of suramin. It is an FDA approved drug for African sleeping sickness and river blindness.suramin sodium
xenovulene aA sesquiterpenoid based on a humulene skeleton. It is isolated from Sarocladium strictum and has been shown to exhibit inhibitory activity against GABA receptor.xenovulene A

Research

Studies (16,378)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-19902,200 (13.43)18.7374
1990's4,992 (30.48)18.2507
2000's4,249 (25.94)29.6817
2010's3,626 (22.14)24.3611
2020's1,311 (8.00)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials1,265 (7.25%)5.53%
Reviews1,615 (9.25%)6.00%
Case Studies2,308 (13.22%)4.05%
Observational78 (0.45%)0.25%
Other12,189 (69.83%)84.16%

Protein Targets (324)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
acetylcholinesteraseHomo sapiens (human)Potency12.301811
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency35.481311
AR proteinHomo sapiens (human)Potency19.358666
arylsulfatase AHomo sapiens (human)Potency0.095311
ATAD5 protein, partialHomo sapiens (human)Potency2.310011
Ataxin-2Homo sapiens (human)Potency15.271822
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency7.079511
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency10.590911
atrial natriuretic peptide receptor 2 precursorHomo sapiens (human)Potency10.399211
Bloom syndrome protein isoform 1Homo sapiens (human)Potency0.253525
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency79.432811
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency33.491511
caspase-1 isoform alpha precursorHomo sapiens (human)Potency39.810711
caspase-3Homo sapiens (human)Potency33.491511
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency12.589311
Chain A, ATP-DEPENDENT DNA HELICASE Q1Homo sapiens (human)Potency23.587035
Chain A, Breast cancer type 1 susceptibility proteinHomo sapiens (human)Potency14.219112
Chain A, CruzipainTrypanosoma cruziPotency17.900812
Chain A, HADH2 proteinHomo sapiens (human)Potency23.444125
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency79.432811
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency13.754436
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency4.398127
Chain B, HADH2 proteinHomo sapiens (human)Potency23.444125
chromobox protein homolog 1Homo sapiens (human)Potency79.432811
cytochrome P450 2C19 precursorHomo sapiens (human)Potency13.351912
cytochrome P450 2C9 precursorHomo sapiens (human)Potency39.810711
cytochrome P450 2C9, partialHomo sapiens (human)Potency26.176112
cytochrome P450 2D6Homo sapiens (human)Potency13.802911
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency11.264113
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency23.735824
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency17.376811
D(1A) dopamine receptorHomo sapiens (human)Potency4.468033
DNA polymerase betaHomo sapiens (human)Potency40.162012
DNA polymerase eta isoform 1Homo sapiens (human)Potency0.223911
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency40.422612
DNA polymerase kappa isoform 1Homo sapiens (human)Potency0.065812
endonuclease IVEscherichia coliPotency9.530723
estrogen nuclear receptor alphaHomo sapiens (human)Potency25.290955
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency33.491511
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency20.836466
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency0.897913
EWS/FLI fusion proteinHomo sapiens (human)Potency23.093147
flap endonuclease 1Homo sapiens (human)Potency29.934911
Fumarate hydrataseHomo sapiens (human)Potency24.905312
GVesicular stomatitis virusPotency26.176112
GABA theta subunitRattus norvegicus (Norway rat)Potency23.735812
galactokinaseHomo sapiens (human)Potency17.782811
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency23.735812
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency23.735812
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency23.735812
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency23.735812
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency23.735812
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency23.735812
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency23.735812
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency23.735812
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency23.735812
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency23.735812
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency23.735812
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency23.735812
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency23.735812
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency23.735812
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency23.735812
gemininHomo sapiens (human)Potency0.326411
GLI family zinc finger 3Homo sapiens (human)Potency7.955222
GLS proteinHomo sapiens (human)Potency19.506413
glucocerebrosidaseHomo sapiens (human)Potency15.757914
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency2.683211
Glutamate receptor 1Rattus norvegicus (Norway rat)Potency8.912511
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency21.202022
Glutamate receptor 3Rattus norvegicus (Norway rat)Potency8.912511
Glutamate receptor 4Rattus norvegicus (Norway rat)Potency8.912511
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency17.473329
Histone H2A.xCricetulus griseus (Chinese hamster)Potency61.931511
histone-lysine N-methyltransferase 2A isoform 2 precursorHomo sapiens (human)Potency11.034412
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency26.176112
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency2.131411
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency12.589322
IDH1Homo sapiens (human)Potency10.322511
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency26.176114
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency4.417513
Integrin alpha-IIbHomo sapiens (human)Potency12.589311
Integrin beta-3Homo sapiens (human)Potency12.589311
Interferon betaHomo sapiens (human)Potency26.176112
lamin isoform A-delta10Homo sapiens (human)Potency3.702524
lethal factor (plasmid)Bacillus anthracis str. A2012Potency31.622811
LuciferasePhotinus pyralis (common eastern firefly)Potency31.868623
M-phase phosphoprotein 8Homo sapiens (human)Potency22.196912
Microtubule-associated protein tauHomo sapiens (human)Potency23.458927
mitogen-activated protein kinase 1Homo sapiens (human)Potency31.622811
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency1.133724
muscleblind-like protein 1 isoform 1Homo sapiens (human)Potency0.112211
NFKB1 protein, partialHomo sapiens (human)Potency0.677424
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency16.784211
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency4.683722
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency19.955412
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency14.506334
Ornithine decarboxylaseRattus norvegicus (Norway rat)Potency31.622811
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency18.069112
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency47.754811
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency0.075011
phosphopantetheinyl transferaseBacillus subtilisPotency69.692613
Platelet-activating factor receptorHomo sapiens (human)Potency14.219112
polyproteinZika virusPotency24.905312
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency6.304613
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency17.559412
progesterone receptorHomo sapiens (human)Potency22.553133
pyruvate kinaseLeishmania mexicana mexicanaPotency0.794322
pyruvate kinase PKM isoform bHomo sapiens (human)Potency31.622822
RAR-related orphan receptor gammaMus musculus (house mouse)Potency6.682411
regulator of G-protein signaling 4Homo sapiens (human)Potency0.006812
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency29.849311
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency17.782811
survival motor neuron protein isoform dHomo sapiens (human)Potency8.356113
TAR DNA-binding protein 43Homo sapiens (human)Potency35.481311
TDP1 proteinHomo sapiens (human)Potency19.2440212
thioredoxin reductaseRattus norvegicus (Norway rat)Potency13.114536
ThrombopoietinHomo sapiens (human)Potency3.981122
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency21.640322
thyroid stimulating hormone receptorHomo sapiens (human)Potency11.068424
transient receptor potential cation channel subfamily V member 1Homo sapiens (human)Potency12.589311
USP1 protein, partialHomo sapiens (human)Potency7.943311
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency0.595511
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency35.481311
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency33.491511

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
3-hydroxy-3-methylglutaryl-coenzyme A reductase Rattus norvegicus (Norway rat)Ki0.015011
5-hydroxytryptamine receptor 1AHomo sapiens (human)IC500.150011
5-hydroxytryptamine receptor 1AMus musculus (house mouse)IC502.000011
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)IC501.269534
5-hydroxytryptamine receptor 1AHomo sapiens (human)Ki0.16571518
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki0.145199
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)IC500.373033
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)Ki0.152122
5-hydroxytryptamine receptor 1DRattus norvegicus (Norway rat)IC500.587011
5-hydroxytryptamine receptor 1DRattus norvegicus (Norway rat)Ki0.023211
5-hydroxytryptamine receptor 1FRattus norvegicus (Norway rat)IC500.587011
5-hydroxytryptamine receptor 1FRattus norvegicus (Norway rat)Ki0.023211
5-hydroxytryptamine receptor 2AHomo sapiens (human)IC500.065835
5-hydroxytryptamine receptor 2AMus musculus (house mouse)IC500.028011
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)IC500.08861111
5-hydroxytryptamine receptor 2AHomo sapiens (human)Ki0.01563438
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)Ki0.01232223
5-hydroxytryptamine receptor 2BHomo sapiens (human)IC500.081024
5-hydroxytryptamine receptor 2BMus musculus (house mouse)IC500.028011
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)IC500.033877
5-hydroxytryptamine receptor 2BHomo sapiens (human)Ki0.005133
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)Ki0.013777
5-hydroxytryptamine receptor 2CHomo sapiens (human)IC500.065835
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)IC500.031088
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki0.01542326
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)Ki0.01351010
5-hydroxytryptamine receptor 2C Mus musculus (house mouse)IC500.028011
5-hydroxytryptamine receptor 3ACavia porcellus (domestic guinea pig)IC50110.000011
5-hydroxytryptamine receptor 3AHomo sapiens (human)Ki0.334833
5-hydroxytryptamine receptor 3AMus musculus (house mouse)Ki0.032011
5-hydroxytryptamine receptor 3ARattus norvegicus (Norway rat)Ki0.053011
5-hydroxytryptamine receptor 3BHomo sapiens (human)Ki0.409122
5-hydroxytryptamine receptor 3BRattus norvegicus (Norway rat)Ki0.053011
5-hydroxytryptamine receptor 3CHomo sapiens (human)Ki0.409122
5-hydroxytryptamine receptor 3DHomo sapiens (human)Ki0.409122
5-hydroxytryptamine receptor 3EHomo sapiens (human)Ki0.409122
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)IC500.032022
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)Ki0.009522
5-hydroxytryptamine receptor 4Homo sapiens (human)Ki0.223911
5-hydroxytryptamine receptor 5AHomo sapiens (human)Ki1.000011
5-hydroxytryptamine receptor 6Homo sapiens (human)IC500.017144
5-hydroxytryptamine receptor 6Homo sapiens (human)Ki0.01701720
5-hydroxytryptamine receptor 7Homo sapiens (human)Ki0.33382833
5-hydroxytryptamine receptor 7 Rattus norvegicus (Norway rat)Ki0.009422
Adenosine receptor A1Rattus norvegicus (Norway rat)Ki0.353011
Adenylate cyclase type 1 Rattus norvegicus (Norway rat)IC500.140011
Adenylate cyclase type 2Rattus norvegicus (Norway rat)IC500.140011
Adenylate cyclase type 3Rattus norvegicus (Norway rat)IC500.140011
Adenylate cyclase type 4Rattus norvegicus (Norway rat)IC500.140011
Adenylate cyclase type 5Rattus norvegicus (Norway rat)IC500.140011
Adenylate cyclase type 6Rattus norvegicus (Norway rat)IC500.140011
Adenylate cyclase type 8Rattus norvegicus (Norway rat)IC500.140011
Adenylyl cyclase 7 Rattus norvegicus (Norway rat)IC500.140011
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)IC501.470011
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)Ki1.458011
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC500.056778
Alpha-1A adrenergic receptorHomo sapiens (human)Ki0.020166
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Ki0.0865911
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)IC500.056778
Alpha-1B adrenergic receptorHomo sapiens (human)Ki0.020355
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Ki0.08581011
Alpha-1D adrenergic receptorHomo sapiens (human)IC500.035011
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)IC500.056778
Alpha-1D adrenergic receptorHomo sapiens (human)Ki0.019866
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Ki0.100889
Alpha-2A adrenergic receptorHomo sapiens (human)IC500.090011
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)IC503.577222
Alpha-2A adrenergic receptorHomo sapiens (human)Ki0.090855
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)Ki0.075867
Alpha-2B adrenergic receptorHomo sapiens (human)IC500.023011
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)IC503.577222
Alpha-2B adrenergic receptorHomo sapiens (human)Ki0.074033
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)Ki0.082345
Alpha-2C adrenergic receptorHomo sapiens (human)IC500.007911
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)IC503.577222
Alpha-2C adrenergic receptorHomo sapiens (human)Ki0.053844
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)Ki0.082345
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)IC506.285522
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)Ki8.660611
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50133.000012
ATP-dependent 6-phosphofructokinaseTrypanosoma brucei bruceiIC503.000011
Beta-1 adrenergic receptorRattus norvegicus (Norway rat)Ki18.000022
Beta-1 adrenergic receptor Cavia porcellus (domestic guinea pig)Ki0.150011
Beta-2 adrenergic receptorRattus norvegicus (Norway rat)IC500.140011
Beta-2 adrenergic receptorRattus norvegicus (Norway rat)Ki10.000011
Beta-3 adrenergic receptorRattus norvegicus (Norway rat)Ki10.000011
Bile salt export pumpHomo sapiens (human)IC50285.637859
Bile salt export pumpRattus norvegicus (Norway rat)IC50598.250012
Calmodulin-1Homo sapiens (human)IC5080.000022
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50133.000012
Cathepsin BHomo sapiens (human)IC5030.000011
Cholecystokinin receptor type ACavia porcellus (domestic guinea pig)Ki0.060011
Cytochrome P450 2C9 Homo sapiens (human)IC5014.100011
Cytochrome P450 2J2Homo sapiens (human)IC5014.100011
Cytochrome P450 3A4Homo sapiens (human)Ki0.017012
DBos taurus (cattle)IC504.090022
DRattus norvegicus (Norway rat)IC501.0660812
DBos taurus (cattle)Ki0.4200813
DRattus norvegicus (Norway rat)Ki0.23691316
D(1A) dopamine receptorHomo sapiens (human)IC500.107011
D(1A) dopamine receptorHomo sapiens (human)Ki0.13421212
D(1B) dopamine receptorRattus norvegicus (Norway rat)IC500.931257
D(1B) dopamine receptorHomo sapiens (human)Ki0.489022
D(1B) dopamine receptorRattus norvegicus (Norway rat)Ki0.174222
D(2) dopamine receptorBos taurus (cattle)IC501.804055
D(2) dopamine receptorHomo sapiens (human)IC500.204489
D(2) dopamine receptorMus musculus (house mouse)IC500.290012
D(2) dopamine receptorRattus norvegicus (Norway rat)IC500.67591925
D(2) dopamine receptorBos taurus (cattle)Ki0.690011
D(2) dopamine receptorChlorocebus aethiops (grivet)Ki0.254022
D(2) dopamine receptorHomo sapiens (human)Ki0.12966972
D(2) dopamine receptorRattus norvegicus (Norway rat)Ki0.16932537
D(3) dopamine receptorHomo sapiens (human)IC500.354022
D(3) dopamine receptorRattus norvegicus (Norway rat)IC503.077368
D(3) dopamine receptorChlorocebus aethiops (grivet)Ki0.466011
D(3) dopamine receptorHomo sapiens (human)Ki0.48313434
D(3) dopamine receptorRattus norvegicus (Norway rat)Ki0.329855
D(4) dopamine receptorHomo sapiens (human)IC500.07961212
D(4) dopamine receptorRattus norvegicus (Norway rat)IC500.931257
D(4) dopamine receptorHomo sapiens (human)Ki0.20285151
D(4) dopamine receptorRattus norvegicus (Norway rat)Ki0.097544
DNA primaseMycobacterium tuberculosis CDC1551IC508.200011
DNA-dependent protein kinase catalytic subunitHomo sapiens (human)IC501.700011
Dual specificity protein phosphatase 5Homo sapiens (human)Ki0.025011
Ectonucleoside triphosphate diphosphohydrolase 1Rattus norvegicus (Norway rat)Ki300.000022
Ectonucleoside triphosphate diphosphohydrolase 2Rattus norvegicus (Norway rat)Ki65.400022
Ectonucleoside triphosphate diphosphohydrolase 3 Rattus norvegicus (Norway rat)Ki12.700011
Ectonucleoside triphosphate diphosphohydrolase 8Homo sapiens (human)Ki100.000011
Endothelin receptor type BHomo sapiens (human)Ki0.012622
Endothelin receptor type BRattus norvegicus (Norway rat)Ki0.012611
GABA theta subunitRattus norvegicus (Norway rat)IC500.667923
GABA theta subunitRattus norvegicus (Norway rat)Ki0.025577
Gamma-aminobutyric acid receptor subunit alpha-1Bos taurus (cattle)IC500.000512
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)IC500.667923
Gamma-aminobutyric acid receptor subunit alpha-1Bos taurus (cattle)Ki0.000855
Gamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)Ki0.0049732
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Ki0.031799
Gamma-aminobutyric acid receptor subunit alpha-2Bos taurus (cattle)IC500.000512
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)IC500.667923
Gamma-aminobutyric acid receptor subunit alpha-2Bos taurus (cattle)Ki0.000855
Gamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)Ki0.0049732
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Ki0.025577
Gamma-aminobutyric acid receptor subunit alpha-3Bos taurus (cattle)IC500.000512
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)IC500.667923
Gamma-aminobutyric acid receptor subunit alpha-3Bos taurus (cattle)Ki0.000855
Gamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)Ki0.0050732
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Ki0.022488
Gamma-aminobutyric acid receptor subunit alpha-4Bos taurus (cattle)IC500.000512
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)IC500.667923
Gamma-aminobutyric acid receptor subunit alpha-4Bos taurus (cattle)Ki0.000855
Gamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)Ki0.0052429
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Ki0.025577
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)IC500.667923
Gamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)Ki0.0049631
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Ki0.025577
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)IC500.667923
Gamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)Ki0.0195631
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Ki0.02921212
Gamma-aminobutyric acid receptor subunit beta-1Bos taurus (cattle)IC500.000512
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)IC500.667923
Gamma-aminobutyric acid receptor subunit beta-1Bos taurus (cattle)Ki0.000855
Gamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)Ki0.000922
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Ki0.025577
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)IC500.667923
Gamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)Ki0.0055530
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Ki0.03051515
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)IC500.667923
Gamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)Ki0.02541212
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Ki0.025577
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)IC500.667923
Gamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)Ki0.000922
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Ki0.025577
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)IC500.667923
Gamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)Ki0.000922
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Ki0.025577
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)IC500.751024
Gamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)Ki0.000922
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Ki0.025577
Gamma-aminobutyric acid receptor subunit gamma-2Bos taurus (cattle)IC500.000512
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)IC500.667923
Gamma-aminobutyric acid receptor subunit gamma-2Bos taurus (cattle)Ki0.000855
Gamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)Ki0.01171540
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Ki0.03051515
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)IC500.667923
Gamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)Ki0.000922
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Ki0.025577
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)IC500.667923
Gamma-aminobutyric acid receptor subunit piHomo sapiens (human)Ki0.000922
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Ki0.025577
Gamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)Ki0.000922
Gastrin/cholecystokinin type B receptorMus musculus (house mouse)Ki0.003812
Glycine receptor subunit alpha-2Rattus norvegicus (Norway rat)IC502.400011
Histamine H1 receptorHomo sapiens (human)IC500.004911
Histamine H1 receptorRattus norvegicus (Norway rat)IC500.023012
Histamine H1 receptorCavia porcellus (domestic guinea pig)Ki0.012611
Histamine H1 receptorHomo sapiens (human)Ki0.003588
Histamine H1 receptorRattus norvegicus (Norway rat)Ki0.005012
Histamine H2 receptorHomo sapiens (human)IC503.610011
Histamine H2 receptorHomo sapiens (human)Ki3.550011
Histamine H3 receptorHomo sapiens (human)Ki0.815522
Histamine H4 receptorHomo sapiens (human)Ki0.192533
Multidrug resistance-associated protein 4Homo sapiens (human)IC50133.000012
Muscarinic acetylcholine receptor M1Homo sapiens (human)IC500.009633
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)IC500.123347
Muscarinic acetylcholine receptor M1Homo sapiens (human)Ki0.007966
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Ki0.013622
Muscarinic acetylcholine receptor M2Homo sapiens (human)IC500.476011
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)IC500.153445
Muscarinic acetylcholine receptor M2Homo sapiens (human)Ki0.101522
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)Ki0.035622
Muscarinic acetylcholine receptor M3Homo sapiens (human)IC500.078011
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)IC500.153445
Muscarinic acetylcholine receptor M3Homo sapiens (human)Ki0.025522
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)Ki0.025111
Muscarinic acetylcholine receptor M4Homo sapiens (human)IC500.045011
Muscarinic acetylcholine receptor M4Rattus norvegicus (Norway rat)IC500.153445
Muscarinic acetylcholine receptor M4Homo sapiens (human)Ki0.017633
Muscarinic acetylcholine receptor M4Rattus norvegicus (Norway rat)Ki0.025111
Muscarinic acetylcholine receptor M5Homo sapiens (human)IC500.013011
Muscarinic acetylcholine receptor M5Rattus norvegicus (Norway rat)IC500.153445
Muscarinic acetylcholine receptor M5Homo sapiens (human)Ki0.021822
Muscarinic acetylcholine receptor M5Rattus norvegicus (Norway rat)Ki0.025111
NAD-dependent protein deacetylase HST2Saccharomyces cerevisiae S288CIC50240.000011
NAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)IC501.385777
NAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)IC501.175044
NAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)IC5020.600088
Neuronal acetylcholine receptor subunit alpha-4Rattus norvegicus (Norway rat)Ki0.000911
Neuronal acetylcholine receptor subunit alpha-7Rattus norvegicus (Norway rat)Ki0.090011
Neuronal acetylcholine receptor subunit beta-2Rattus norvegicus (Norway rat)Ki0.000911
Nuclear receptor subfamily 3 group C member 3 Bos taurus (cattle)IC5010.571011
Nuclear receptor subfamily 3 group C member 3 Bos taurus (cattle)Ki8.660611
P2X purinoceptor 2Rattus norvegicus (Norway rat)IC5021.905412
P2Y purinoceptor 11Homo sapiens (human)Ki0.207122
P2Y purinoceptor 2Homo sapiens (human)IC5075.000022
P2Y purinoceptor 6Homo sapiens (human)IC5027.000011
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC502.17911112
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)Ki9.960155
Protein arginine N-methyltransferase 1Homo sapiens (human)IC50344.810033
Protein kinase C alpha typeHomo sapiens (human)IC5029.000011
Protein kinase C beta typeHomo sapiens (human)IC5029.000011
Protein kinase C delta typeHomo sapiens (human)IC5029.000011
Protein kinase C epsilon typeHomo sapiens (human)IC5029.000011
Protein kinase C eta typeHomo sapiens (human)IC5029.000011
Protein kinase C gamma typeHomo sapiens (human)IC5029.000011
Protein kinase C iota typeHomo sapiens (human)IC5029.000011
Protein kinase C theta typeHomo sapiens (human)IC5029.000011
Protein kinase C zeta typeHomo sapiens (human)IC5029.000011
Reverse transcriptase/RNaseH Human immunodeficiency virus 1IC5012.200022
RmtAAspergillus nidulansIC505.900011
Serine/threonine-protein kinase D1Homo sapiens (human)IC5029.000011
Serine/threonine-protein kinase D3Homo sapiens (human)IC5029.000011
Sigma non-opioid intracellular receptor 1Rattus norvegicus (Norway rat)IC501.000011
Sigma non-opioid intracellular receptor 1Homo sapiens (human)Ki8.500011
Signal transducer and activator of transcription 1-alpha/betaHomo sapiens (human)IC509.100011
Signal transducer and activator of transcription 3 Mus musculus (house mouse)IC50100.000011
Signal transducer and activator of transcription 5AHomo sapiens (human)IC509.400011
Signal transducer and activator of transcription 5BHomo sapiens (human)IC5010.400011
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)IC505.754412
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)Ki0.239245
Sodium-dependent dopamine transporter Homo sapiens (human)Ki0.021012
Sodium-dependent noradrenaline transporter Homo sapiens (human)IC501.470011
Sodium-dependent noradrenaline transporter Homo sapiens (human)Ki1.458011
Sodium-dependent serotonin transporterHomo sapiens (human)IC500.546011
Sodium-dependent serotonin transporterHomo sapiens (human)Ki2.095022
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)Ki0.021011
TransporterRattus norvegicus (Norway rat)Ki0.543522
Tyrosine-protein phosphatase non-receptor type 1Homo sapiens (human)IC509.760011
Uracil nucleotide/cysteinyl leukotriene receptorHomo sapiens (human)IC50100.000011
Voltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)IC503.600011
Voltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)IC503.600011
Voltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)IC503.600011
Voltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)IC503.600011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 2BHomo sapiens (human)EC500.020011
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)Kd0.125912
5-hydroxytryptamine receptor 2CHomo sapiens (human)EC500.250011
AlbuminRattus norvegicus (Norway rat)Kd78.800011
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Kd0.512911
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Kd0.512911
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Kd0.512911
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)Kd20.417411
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)Kd20.417411
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)Kd20.417411
Calmodulin Bos taurus (cattle)Kd61.000011
Delta-type opioid receptorHomo sapiens (human)EC50100.000011
Gamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)Kd0.002011
Gamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)Kd0.000411
Gamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)Kd0.000511
Gamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)Kd0.000411
Gamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)Kd0.000411
Histamine H1 receptorHomo sapiens (human)EC500.000411
Histamine H1 receptorHomo sapiens (human)Kd0.003111
Histamine H4 receptorHomo sapiens (human)Kd0.029444
Kappa-type opioid receptorHomo sapiens (human)EC50100.000011
Mu-type opioid receptorHomo sapiens (human)EC50100.000011
Muscarinic acetylcholine receptor M1Homo sapiens (human)EC5010.000011
Muscarinic acetylcholine receptor M2Homo sapiens (human)EC5010.000011
Muscarinic acetylcholine receptor M3Homo sapiens (human)EC5010.000011
Muscarinic acetylcholine receptor M4Homo sapiens (human)EC5010.000011
Nuclear receptor subfamily 1 group I member 2Homo sapiens (human)EC501.300011
P2X purinoceptor 1Rattus norvegicus (Norway rat)EC501.000011
P2X purinoceptor 2Rattus norvegicus (Norway rat)EC5010.400011
P2X purinoceptor 3Homo sapiens (human)EC508.950022
P2X purinoceptor 4Rattus norvegicus (Norway rat)EC50100.000011
P2X purinoceptor 5Rattus norvegicus (Norway rat)EC504.000011
P2X purinoceptor 6Rattus norvegicus (Norway rat)EC50100.000011
P2X purinoceptor 7Homo sapiens (human)EC5092.000011
P2Y purinoceptor 1Meleagris gallopavo (turkey)EC5010.000011
P2Y purinoceptor 11Homo sapiens (human)EC5016.000011
P2Y purinoceptor 12Rattus norvegicus (Norway rat)EC504.000011
P2Y purinoceptor 2Homo sapiens (human)EC5048.000011
P2Y purinoceptor 4Homo sapiens (human)EC50100.000011
short transient receptor potential channel 6 isoform 1Mus musculus (house mouse)EC5015.850011

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 2AHomo sapiens (human)Activity0.005411
5-hydroxytryptamine receptor 2AHomo sapiens (human)INH0.005411
5-hydroxytryptamine receptor 6Homo sapiens (human)INH0.006411
ATP-dependent translocase ABCB1Homo sapiens (human)Km58.000011
Cytochrome P450 2C19Homo sapiens (human)Km25.300011
Cytochrome P450 2C9 Homo sapiens (human)Km25.300011
Cytochrome P450 2D6Homo sapiens (human)Km43.766733
Cytochrome P450 2J2Homo sapiens (human)Km25.300011
Cytochrome P450 3A4Homo sapiens (human)Km45.240045
D(1A) dopamine receptorHomo sapiens (human)Kb10.000011
D(1B) dopamine receptorHomo sapiens (human)Kb10.000011
D(2) dopamine receptorHomo sapiens (human)Activity0.256011
D(2) dopamine receptorHomo sapiens (human)Kb10.000011
D(2) dopamine receptorHomo sapiens (human)pKi0.006911
D(3) dopamine receptorHomo sapiens (human)Kb10.000011
D(3) dopamine receptorHomo sapiens (human)pKi0.006611
D(4) dopamine receptorHomo sapiens (human)Kb10.000011
D(4) dopamine receptorHomo sapiens (human)pKi0.007311
Histamine H1 receptorHomo sapiens (human)Activity0.001211
Histamine H1 receptorHomo sapiens (human)INH0.001211
UDP-glucuronosyltransferase 1A4Homo sapiens (human)Km62.000011