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sympathomimetic agent

A drug that mimics the effects of stimulating postganglionic adrenergic sympathetic nerves. Included in this class are drugs that directly stimulate adrenergic receptors and drugs that act indirectly by provoking the release of adrenergic transmitters.

ChEBI ID: 35524

Members (33)

MemberDefinitionClass
acebutololAn ether that is the 2-acetyl-4-(butanoylamino)phenyl ether of the primary hydroxy group of 3-(propan-2-ylamino)propane-1,2-diol.acebutolol
acebutolol hydrochlorideThe hydrochloride salt of acebutolol, prepared using equimolar amounts of acebutolol and hydrogen chloride.acebutolol hydrochloride
ameziniumA pyridazinium ion that is pyridazin-1-ium which is substituted by a phenyl, amino and methoxy groups at positions 1, 4 and 6, respectively.amezinium
bambuterolA carbamate ester that is terbutaline in which both of the phenolic hydroxy groups have been protected as the corresponding N,N-dimethylcarbamates. A long acting beta-adrenoceptor agonist used in the treatment of asthma, it is a prodrug for terbutaline.bambuterol
bambuterol hydrochlorideThe hydrochloride salt of bambuterol. A long acting beta-adrenoceptor agonist used in the treatment of asthma, it is a prodrug for terbutaline.bambuterol hydrochloride
benzphetamineDextroamphetamine in which the the hydrogens attached to the amino group are substituted by a methyl and a benzyl group. A sympathomimetic agent with properties similar to dextroamphetamine, it is used as its hydrochloride salt in the treatment of obesity.benzphetamine
berotekA member of the class resorcinols that is 5-(1-hydroxyethyl)benzene-1,3-diol in which one of the methyl hydrogens is replaced by a 1-(4-hydroxyphenyl)propan-2-amino group. A beta2-adrenergic agonist, it is used (as the hydrobromide salt) as a bronchodilator in the management of reversible airway obstruction.fenoterol
clenbuterolA substituted aniline that is 2,6-dichloroaniline in which the hydrogen at position 4 has been replaced by a 2-(tert-butylamino)-1-hydroxyethyl group.clenbuterol
cocaineA tropane alkaloid obtained from leaves of the South American shrub Erythroxylon coca.cocaine
dextroamphetamineA 1-phenylpropan-2-amine that has S configuration.(S)-amphetamine
diazoxideA benzothiadiazine that is the S,S-dioxide of 2H-1,2,4-benzothiadiazine which is substituted at position 3 by a methyl group and at position 7 by chlorine. A peripheral vasodilator, it increases the concentration of glucose in the plasma and inhibits the secretion of insulin by the beta- cells of the pancreas. It is used orally in the management of intractable hypoglycaemia and intravenously in the management of hypertensive emergencies.diazoxide
dipivefrinThe dipivalate ester of (+-)-epinephrine (racepinephrine). A pro-drug of epinephrine, the hydrochloride is used topically as eye drops to reduce intra-ocular pressure in the treatment of open-angle glaucoma or ocular hypertension.dipivefrin
dipivefrin hydrochlorideThe hydrochloride salt of dipivefrin. It is used topically as eye drops to reduce intra-ocular pressure in the treatment of open-angle glaucoma or ocular hypertension.dipivefrin hydrochloride
dobutamineA catecholamine that is 4-(3-aminobutyl)phenol in which one of the hydrogens attached to the nitrogen is substituted by a 2-(3,4-dihydroxyphenyl)ethyl group. A beta1-adrenergic receptor agonist that has cardiac stimulant action without evoking vasoconstriction or tachycardia, it is used as the hydrochloride to increase the contractility of the heart in the management of acute heart failure.dobutamine
dobutamine hydrochlorideThe hydrochloride salt of dobutamine. A beta1-adrenergic receptor agonist that has cardiac stimulant action without evoking vasoconstriction or tachycardia, it is used to increase the contractility of the heart in the management of acute heart failure.dobutamine hydrochloride
ephedrineA phenethylamine alkaloid that is 2-phenylethanamine substituted by a methyl group at the amino nitrogen and a methyl and a hydroxy group at position 2 and 1 respectively.(-)-ephedrine
fenoterolThe hydrobromide salt of fenoterol. A beta2-adrenergic agonist, it is used as a bronchodilator in the management of reversible airway obstruction.fenoterol hydrobromide
isoproterenolA secondary amino compound that is noradrenaline in which one of the hydrogens attached to the nitrogen is replaced by an isopropyl group. A sympathomimetic acting almost exclusively on beta-adrenergic receptors, it is used (mainly as the hydrochloride salt) as a bronghodilator and heart stimulant for the management of a variety of cardiac disorders.isoprenaline
L-isoprenalineAn optically active phenylethanolamine compound having an isopropyl substituent attached to the nitrogen atom.L-isoprenaline
metaraminolA member of the class of phenylethanolamines that is 2-amino-1-phenylethanol substituted by a methyl group at position 2 and a phenolic hydroxy group at position 1. A sympathomimetic agent , it is used in the treatment of hypotension.metaraminol
midodrineAn aromatic ether that is 1,4-dimethoxybenzene which is substituted at position 2 by a 2-(glycylamino)-1-hydroxyethyl group. A direct-acting sympathomimetic with selective alpha-adrenergic agonist activity, it is used (generally as its hydrochloride salt) as a peripheral vasoconstrictor in the treatment of certain hypotensive states. The main active moiety is its major metabolite, deglymidodrine.midodrine
midodrine hydrochlorideA hydrochloride resulting from the combination of equimolar amounts of midodrine and hydrogen chloride. Midodrine is a direct-acting sympathomimetic with selective alpha-adrenergic agonist activity. The hydrochloride salt is used as a peripheral vasoconstrictor in the treatment of certain hypotensive states. The main active moiety is its major metabolite, deglymidodrine.midodrine hydrochloride
nab-365A hydrochloride that is the monohydrochloride salt of clenbuterol.clenbuterol hydrochloride
oxymetazolineA member of the class of phenols that is 2,4-dimethylphenol which is substituted at positions 3 and 6 by 4,5-dihydro-1H-imidazol-2-ylmethyl and tert-butyl groups, respectively. A direct-acting sympathomimetic with marked alpha-adrenergic activity, it is a vasoconstrictor that is used (generally as the hydrochloride salt) to relieve nasal congestion.oxymetazoline
oxymetazoline hydrochlorideA hydrochloride salt resulting from the reaction of equimolar quantities of oxymetazoline and hydrogen chloride. A direct-acting sympathomimetic with marked alpha-adrenergic activity, it is a vasoconstrictor that is used to relieve nasal congestion.oxymetazoline hydrochloride
phenmetrazineA member of the class of morpholines that is morpholine substituted with a phenyl group at position 2 and a methyl group at position 3.phenmetrazine
phenterminephentermine
phenylephrineA member of the class of the class of phenylethanolamines that is (1R)-2-(methylamino)-1-phenylethan-1-ol carrying an additional hydroxy substituent at position 3 on the phenyl ring.phenylephrine
pseudoephedrineA member of the class of the class of phenylethanolamines that is (1S)-2-(methylamino)-1-phenylethan-1-ol in which the pro-S hydrogen at position 2 is replaced by a methyl group.pseudoephedrine
st 1059An aromatic ether that is 1,4-dimethoxybenzene which is substituted at position 2 by a 2-amino-1-hydroxyethyl group. The immediate and active metabolite of midrodine, it is a direct-acting sympathomimetic with selective alpha-adrenergic agonist activity. Midrodine is used (generally as its hydrochloride salt) as a prodrug for deglymidodrine, which acts as a peripheral vasoconstrictor in the treatment of certain hypotensive states.deglymidodrine
terbutalineA member of the class of phenylethanolamines that is catechol substituted at position 5 by a 2-(tert-butylamino)-1-hydroxyethyl group.terbutaline
tetrahydrozolinetetryzoline
tetrahydrozoline hydrochlorideThe hydrochloride salt of tetryzoline. It is used as a nasal decongestant.tetrahydrozoline hydrochloride

Research

Studies (98,799)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-199038,175 (38.64)18.7374
1990's22,719 (23.00)18.2507
2000's18,184 (18.41)29.6817
2010's15,281 (15.47)24.3611
2020's4,440 (4.49)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials7,348 (6.63%)5.53%
Reviews4,890 (4.42%)6.00%
Case Studies4,934 (4.45%)4.05%
Observational139 (0.13%)0.25%
Other93,445 (84.37%)84.16%

Protein Targets (337)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency39.810711
15-lipoxygenase, partialHomo sapiens (human)Potency0.398111
2,3-bisphosphoglycerate-independent phosphoglycerate mutaseLeishmania major strain FriedlinPotency28.871012
67.9K proteinVaccinia virusPotency0.446711
acetylcholinesteraseHomo sapiens (human)Potency19.252222
activating transcription factor 6Homo sapiens (human)Potency26.465913
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency21.259613
alpha-galactosidaseHomo sapiens (human)Potency32.464822
apical membrane antigen 1, AMA1Plasmodium falciparum 3D7Potency10.000011
AR proteinHomo sapiens (human)Potency29.052233
aryl hydrocarbon receptorHomo sapiens (human)Potency26.603211
arylsulfatase AHomo sapiens (human)Potency14.900613
ATAD5 protein, partialHomo sapiens (human)Potency1.834911
Ataxin-2Homo sapiens (human)Potency16.574526
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency9.922514
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency4.682923
beta-2 adrenergic receptorHomo sapiens (human)Potency4.3192413
Bloom syndrome protein isoform 1Homo sapiens (human)Potency0.003424
Cellular tumor antigen p53Homo sapiens (human)Potency17.412412
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency16.461315
Chain A, Beta-lactamaseEscherichia coli K-12Potency6.593116
Chain A, Ferritin light chainEquus caballus (horse)Potency5.112012
Chain A, HADH2 proteinHomo sapiens (human)Potency4.372628
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency12.459714
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency6.974012
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency49.168713
Chain B, HADH2 proteinHomo sapiens (human)Potency4.372628
chaperonin GroELMethanococcus maripaludis S2Potency100.000011
chromobox protein homolog 1Homo sapiens (human)Potency76.947728
cytochrome P450 2C19 precursorHomo sapiens (human)Potency9.282413
cytochrome P450 2C9 precursorHomo sapiens (human)Potency0.794311
cytochrome P450 2D6Homo sapiens (human)Potency17.591618
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency7.428615
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency22.6694216
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency0.475413
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency33.491511
D(1A) dopamine receptorHomo sapiens (human)Potency2.244526
D(1A) dopamine receptorSus scrofa (pig)Potency18.492711
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency89.125111
DNA polymerase kappa isoform 1Homo sapiens (human)Potency10.990313
dopamine D1 receptorHomo sapiens (human)Potency3.083214
endonuclease IVEscherichia coliPotency25.118911
estrogen nuclear receptor alphaHomo sapiens (human)Potency12.877944
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency31.670422
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency5.8216610
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency5.2344110
EWS/FLI fusion proteinHomo sapiens (human)Potency23.1541413
Fumarate hydrataseHomo sapiens (human)Potency2.238711
GABA theta subunitRattus norvegicus (Norway rat)Potency22.669418
GALC proteinHomo sapiens (human)Potency0.707911
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency22.669418
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency22.669418
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency22.669418
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency22.669418
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency22.669418
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency22.669418
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency22.669418
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency22.669418
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency22.669418
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency22.669418
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency22.669418
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency22.669418
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency22.669418
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency22.669418
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency22.669418
gemininHomo sapiens (human)Potency8.7590314
GLI family zinc finger 3Homo sapiens (human)Potency6.188226
glp-1 receptor, partialHomo sapiens (human)Potency4.4958313
GLS proteinHomo sapiens (human)Potency10.2163212
glucocerebrosidaseHomo sapiens (human)Potency35.481311
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency6.441811
glucokinase regulatory proteinHomo sapiens (human)Potency19.702012
GTP-binding nuclear protein Ran isoform 1Homo sapiens (human)Potency2.310713
Guanine nucleotide-binding protein GHomo sapiens (human)Potency7.079511
guanine nucleotide-binding protein G(i) subunit alpha-1 isoform 1Homo sapiens (human)Potency7.943311
heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa)Homo sapiens (human)Potency23.280911
hexokinase-4 isoform 1Homo sapiens (human)Potency19.702012
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency6.221427
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency28.643713
Histone H2A.xCricetulus griseus (Chinese hamster)Potency51.836323
huntingtin isoform 2Homo sapiens (human)Potency35.481311
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency0.270328
IDH1Homo sapiens (human)Potency29.092912
importin subunit beta-1 isoform 1Homo sapiens (human)Potency2.310713
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency5.011911
lamin isoform A-delta10Homo sapiens (human)Potency11.155729
lethal factor (plasmid)Bacillus anthracis str. A2012Potency6.301012
LuciferasePhotinus pyralis (common eastern firefly)Potency39.810711
M-phase phosphoprotein 8Homo sapiens (human)Potency37.052913
Microtubule-associated protein tauHomo sapiens (human)Potency6.945623
mitogen-activated protein kinase 1Homo sapiens (human)Potency4.087525
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency9.106322
neuropeptide S receptor isoform AHomo sapiens (human)Potency5.145412
NFKB1 protein, partialHomo sapiens (human)Potency8.341728
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency43.774422
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency0.154911
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency12.589311
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency19.335122
Ornithine decarboxylaseRattus norvegicus (Norway rat)Potency7.943311
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency2.030713
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency2.254114
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency67.903112
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency30.160722
phosphopantetheinyl transferaseBacillus subtilisPotency44.979315
plasminogen precursorMus musculus (house mouse)Potency7.943311
polyproteinZika virusPotency2.238711
polyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)Potency3.162311
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency10.291812
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency10.205713
pyruvate kinaseLeishmania mexicana mexicanaPotency10.000022
pyruvate kinase PKM isoform bHomo sapiens (human)Potency7.943322
Rap guanine nucleotide exchange factor 4Homo sapiens (human)Potency11.220211
RAR-related orphan receptor gammaMus musculus (house mouse)Potency15.328113
ras-related protein Rab-9AHomo sapiens (human)Potency47.990412
regulator of G-protein signaling 4Homo sapiens (human)Potency13.631016
RGS12Homo sapiens (human)Potency7.943311
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency18.288523
Smad3Homo sapiens (human)Potency0.854012
snurportin-1Homo sapiens (human)Potency2.310713
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency18.257915
survival motor neuron protein isoform dHomo sapiens (human)Potency1.584911
TDP1 proteinHomo sapiens (human)Potency18.5089221
thioredoxin reductaseRattus norvegicus (Norway rat)Potency11.9827213
ThrombopoietinHomo sapiens (human)Potency3.162322
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency10.963422
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency6.309611
thyroid stimulating hormone receptorHomo sapiens (human)Potency7.1169525
transcriptional regulator ERG isoform 3Homo sapiens (human)Potency17.546413
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency7.943311
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency7.943311
USP1 protein, partialHomo sapiens (human)Potency25.294024
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency2.684412
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency56.454113

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)IC501.328812
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki2.954834
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)IC501.328812
5-hydroxytryptamine receptor 1BHomo sapiens (human)Ki0.000311
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)Ki0.606423
5-hydroxytryptamine receptor 1DHomo sapiens (human)Ki0.000411
5-hydroxytryptamine receptor 1DRattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 1FRattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 2AHomo sapiens (human)IC501.285011
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)IC500.085522
5-hydroxytryptamine receptor 2AHomo sapiens (human)Ki0.367011
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 2BHomo sapiens (human)IC503.056011
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)IC500.085522
5-hydroxytryptamine receptor 2BHomo sapiens (human)Ki1.945011
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 2CHomo sapiens (human)IC500.578011
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)IC500.085522
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki0.303011
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 3ARattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 3BRattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)IC500.578011
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)Ki0.303011
5-hydroxytryptamine receptor 4 Rattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 5ARattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 5BRattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 6Homo sapiens (human)IC501.670011
5-hydroxytryptamine receptor 6Homo sapiens (human)Ki0.775011
5-hydroxytryptamine receptor 6Rattus norvegicus (Norway rat)Ki0.301011
5-hydroxytryptamine receptor 7 Rattus norvegicus (Norway rat)Ki0.301011
AcetylcholinesteraseElectrophorus electricus (electric eel)IC50100.000011
AcetylcholinesteraseHomo sapiens (human)IC5025.000044
AcetylcholinesteraseRattus norvegicus (Norway rat)IC5030.000011
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)IC500.383011
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)Ki0.380011
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC50100.000011
Alpha-1A adrenergic receptorBos taurus (cattle)Ki0.473212
Alpha-1A adrenergic receptorHomo sapiens (human)Ki0.137834
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Ki6.869857
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)IC50100.000011
Alpha-1B adrenergic receptorHomo sapiens (human)Ki0.584234
Alpha-1B adrenergic receptorMesocricetus auratus (golden hamster)Ki3.820434
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Ki20.800022
Alpha-1D adrenergic receptorHomo sapiens (human)IC501.479012
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)IC50100.000011
Alpha-1D adrenergic receptorHomo sapiens (human)Ki0.711234
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Ki7.575556
Alpha-2A adrenergic receptorHomo sapiens (human)IC500.023011
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)IC5052.877222
Alpha-2A adrenergic receptorBos taurus (cattle)Ki0.001511
Alpha-2A adrenergic receptorHomo sapiens (human)Ki0.16101923
Alpha-2A adrenergic receptorMus musculus (house mouse)Ki0.091333
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)Ki1.83851517
Alpha-2A adrenergic receptorSus scrofa (pig)Ki0.021011
Alpha-2B adrenergic receptorHomo sapiens (human)IC502.119512
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)IC5052.877222
Alpha-2B adrenergic receptorHomo sapiens (human)Ki0.45411721
Alpha-2B adrenergic receptorMus musculus (house mouse)Ki0.091333
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)Ki1.74871719
Alpha-2C adrenergic receptorHomo sapiens (human)IC502.633011
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)IC5052.877222
Alpha-2C adrenergic receptorHomo sapiens (human)Ki0.12181822
Alpha-2C adrenergic receptorMus musculus (house mouse)Ki0.091333
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)Ki1.83851517
Amine oxidase [flavin-containing] AHomo sapiens (human)Ki14.400011
Amine oxidase [flavin-containing] BBos taurus (cattle)Ki300.000011
Amine oxidase [flavin-containing] BHomo sapiens (human)Ki280.000011
Amine oxidase [flavin-containing] BRattus norvegicus (Norway rat)Ki370.000022
Amyloid-beta precursor proteinHomo sapiens (human)IC500.338011
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50133.000012
ATP-binding cassette sub-family C member 8Homo sapiens (human)IC50470.500044
ATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)IC50470.500044
Beta-1 adrenergic receptorHomo sapiens (human)IC500.782014
Beta-1 adrenergic receptorRattus norvegicus (Norway rat)IC500.212522
Beta-1 adrenergic receptorHomo sapiens (human)Ki0.678425
Beta-1 adrenergic receptorMus musculus (house mouse)Ki0.220022
Beta-1 adrenergic receptorRattus norvegicus (Norway rat)Ki4.583333
Beta-2 adrenergic receptorCanis lupus familiaris (dog)IC500.666723
Beta-2 adrenergic receptorCavia porcellus (domestic guinea pig)IC500.060011
Beta-2 adrenergic receptorHomo sapiens (human)IC500.776024
Beta-2 adrenergic receptorRattus norvegicus (Norway rat)IC500.212522
Beta-2 adrenergic receptorHomo sapiens (human)Ki0.30041012
Beta-2 adrenergic receptorMesocricetus auratus (golden hamster)Ki0.136011
Beta-2 adrenergic receptorRattus norvegicus (Norway rat)Ki0.676111
Beta-2 adrenergic receptor Bos taurus (cattle)Ki0.110022
Beta-3 adrenergic receptorRattus norvegicus (Norway rat)IC500.212522
Beta-3 adrenergic receptorHomo sapiens (human)Ki18.620911
Bile salt export pumpHomo sapiens (human)IC50602.0182511
Bile salt export pumpRattus norvegicus (Norway rat)IC501,000.000011
cAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)Ki1.115011
cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)Ki1.115011
cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)Ki1.115011
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50133.000012
Carbonic anhydrase 1Homo sapiens (human)Ki1.920011
Carbonic anhydrase 12Homo sapiens (human)Ki4.350011
Carbonic anhydrase 13Homo sapiens (human)Ki9.530011
Carbonic anhydrase 14Homo sapiens (human)Ki12.020011
Carbonic anhydrase 15Mus musculus (house mouse)Ki0.390011
Carbonic anhydrase 2Homo sapiens (human)Ki0.480011
Carbonic anhydrase 3Homo sapiens (human)Ki7.400011
Carbonic anhydrase 4Homo sapiens (human)Ki8.980011
Carbonic anhydrase 5A, mitochondrialHomo sapiens (human)Ki0.730011
Carbonic anhydrase 5B, mitochondrialHomo sapiens (human)Ki0.890011
Carbonic anhydrase 6Homo sapiens (human)Ki9.470011
Carbonic anhydrase 7Homo sapiens (human)Ki4.300011
Carbonic anhydrase 9Homo sapiens (human)Ki9.820011
Carboxylic ester hydrolase Rattus norvegicus (Norway rat)IC500.003011
CholinesteraseEquus caballus (horse)IC500.119311
CholinesteraseHomo sapiens (human)IC500.003344
Coagulation factor VIIHomo sapiens (human)IC50740.000011
Cytochrome P450 2D6Homo sapiens (human)IC501.100012
DRattus norvegicus (Norway rat)IC505.754411
D(1A) dopamine receptorHomo sapiens (human)Ki50.000011
D(2) dopamine receptorHomo sapiens (human)Ki30.000022
D(2) dopamine receptorRattus norvegicus (Norway rat)Ki0.330011
D(3) dopamine receptorHomo sapiens (human)IC504.985011
D(3) dopamine receptorHomo sapiens (human)Ki3.196522
D(4) dopamine receptorHomo sapiens (human)Ki2.900011
Epidermal growth factor receptorHomo sapiens (human)IC505.551011
Fatty acid-binding protein, heartHomo sapiens (human)IC500.367011
Gamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)IC50127.000011
Gamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)IC50127.000011
Gamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)IC50127.000011
Gamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)IC50127.000011
Gamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)IC50127.000011
Gamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)IC50127.000011
Gamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)IC50127.000011
Gamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)IC50127.000011
Gamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)IC50127.000011
Gamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)IC50127.000011
Gamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)IC50127.000011
Gamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)IC50127.000011
Gamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)IC50127.000011
Gamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)IC50127.000011
Gamma-aminobutyric acid receptor subunit piHomo sapiens (human)IC50127.000011
Gamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)IC50127.000011
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)Ki10.000011
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)Ki10.000011
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)Ki10.000011
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)Ki10.000011
Glutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)Ki10.000011
Glutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)Ki10.000011
Glutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)Ki10.000011
guanine nucleotide-binding protein subunit alpha-15Homo sapiens (human)IC5029.868011
high affinity choline transporter 1 isoform aHomo sapiens (human)IC500.060026
Leukotriene B4 receptor 1Homo sapiens (human)Ki0.524011
Leukotriene B4 receptor 2Homo sapiens (human)Ki0.524011
Lysosomal Pro-X carboxypeptidaseHomo sapiens (human)Ki10.000011
Macrophage migration inhibitory factorHomo sapiens (human)IC5098.100011
Macrophage migration inhibitory factorHomo sapiens (human)Ki77.100011
Multidrug resistance-associated protein 4Homo sapiens (human)IC50133.000012
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Ki61.398522
Muscarinic acetylcholine receptor M2Sus scrofa (pig)Ki0.234411
Muscarinic acetylcholine receptor M4Homo sapiens (human)IC503.261011
Muscarinic acetylcholine receptor M4Homo sapiens (human)Ki0.455011
Muscarinic acetylcholine receptor M5Homo sapiens (human)IC501.332011
Muscarinic acetylcholine receptor M5Homo sapiens (human)Ki0.957011
NischarinHomo sapiens (human)Ki0.006212
Phenylethanolamine N-methyltransferaseBos taurus (cattle)Ki435.333323
Polyunsaturated fatty acid lipoxygenase ALOX15Oryctolagus cuniculus (rabbit)IC501.184512
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC505.541066
Sigma non-opioid intracellular receptor 1Homo sapiens (human)IC501.539323
Sigma non-opioid intracellular receptor 1Homo sapiens (human)Ki4.944022
Sodium-dependent dopamine transporterMus musculus (house mouse)IC500.200011
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)IC501.34964767
Sodium-dependent dopamine transporterMus musculus (house mouse)Ki0.850011
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)Ki25.87682540
Sodium-dependent dopamine transporter Homo sapiens (human)IC500.37083536
Sodium-dependent dopamine transporter Homo sapiens (human)Ki0.41033135
Sodium-dependent noradrenaline transporter Homo sapiens (human)IC501.22122324
Sodium-dependent noradrenaline transporter Homo sapiens (human)Ki1.53543134
Sodium-dependent serotonin transporterHomo sapiens (human)IC501.24032425
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)IC500.88851518
Sodium-dependent serotonin transporterHomo sapiens (human)Ki0.54523236
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)Ki0.55211827
Solute carrier family 22 member 1 Homo sapiens (human)IC504.170011
Solute carrier family 22 member 1 Homo sapiens (human)Ki95.800011
Tissue factorHomo sapiens (human)IC50740.000011
trace amine-associated receptor 1Homo sapiens (human)IC500.157111
TransporterRattus norvegicus (Norway rat)IC503.22771315
TransporterRattus norvegicus (Norway rat)Ki2.36431518
Tryptophan 5-hydroxylase 1Rattus norvegicus (Norway rat)Ki0.490011
Tyrosine-protein kinase FynHomo sapiens (human)IC503.975011
Tyrosine-protein kinase LckHomo sapiens (human)IC505.519011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 1AHomo sapiens (human)EC500.070011
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)EC5012.569422
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Kd4.466812
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)EC500.020011
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)Kd4.466812
5-hydroxytryptamine receptor 1DRattus norvegicus (Norway rat)EC500.020011
5-hydroxytryptamine receptor 1DRattus norvegicus (Norway rat)Kd4.466812
5-hydroxytryptamine receptor 1FRattus norvegicus (Norway rat)EC500.020011
5-hydroxytryptamine receptor 1FRattus norvegicus (Norway rat)Kd4.466812
5-hydroxytryptamine receptor 2AMus musculus (house mouse)EC5038.115222
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)Kd4.466812
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)Kd4.466812
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)Kd4.466812
5-hydroxytryptamine receptor 3ARattus norvegicus (Norway rat)Kd4.466812
5-hydroxytryptamine receptor 3BRattus norvegicus (Norway rat)Kd4.466812
5-hydroxytryptamine receptor 4 Rattus norvegicus (Norway rat)Kd4.466812
5-hydroxytryptamine receptor 5ARattus norvegicus (Norway rat)Kd4.466812
5-hydroxytryptamine receptor 5BRattus norvegicus (Norway rat)Kd4.466812
5-hydroxytryptamine receptor 6Rattus norvegicus (Norway rat)Kd4.466812
5-hydroxytryptamine receptor 7 Rattus norvegicus (Norway rat)Kd4.466812
Alpha-1A adrenergic receptorBos taurus (cattle)EC500.009011
Alpha-1A adrenergic receptorHomo sapiens (human)EC501.039077
Alpha-1B adrenergic receptorHomo sapiens (human)EC505.858566
Alpha-1B adrenergic receptor Cricetulus griseus (Chinese hamster)EC500.010011
Alpha-1D adrenergic receptorHomo sapiens (human)EC508.786044
Alpha-2A adrenergic receptorHomo sapiens (human)EC500.154722
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)EC5025.118911
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)EC5025.118911
Alpha-2C adrenergic receptorHomo sapiens (human)EC500.340011
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)EC5025.118911
alternatively spliced Trp4Mus musculus (house mouse)EC503.350011
ATP-binding cassette sub-family C member 8Homo sapiens (human)EC5023.016766
ATP-sensitive inward rectifier potassium channel 11Homo sapiens (human)EC5023.016766
Beta-1 adrenergic receptorHomo sapiens (human)EC500.29932728
Beta-1 adrenergic receptorMus musculus (house mouse)EC500.980011
Beta-1 adrenergic receptorRattus norvegicus (Norway rat)EC500.007011
Beta-1 adrenergic receptorHomo sapiens (human)Kd63.660717
Beta-1 adrenergic receptor Cavia porcellus (domestic guinea pig)EC500.022926
Beta-2 adrenergic receptorCavia porcellus (domestic guinea pig)EC500.7588811
Beta-2 adrenergic receptorHomo sapiens (human)EC500.50043336
Beta-2 adrenergic receptorMesocricetus auratus (golden hamster)EC500.020011
Beta-2 adrenergic receptorMus musculus (house mouse)EC500.980011
Beta-2 adrenergic receptorRattus norvegicus (Norway rat)EC500.007011
Beta-2 adrenergic receptorCavia porcellus (domestic guinea pig)Kd0.025111
Beta-2 adrenergic receptorHomo sapiens (human)Kd28.2546616
Beta-2 adrenergic receptor Bos taurus (cattle)Kd1.448713
Beta-3 adrenergic receptorHomo sapiens (human)EC500.29132627
Beta-3 adrenergic receptorMus musculus (house mouse)EC500.980011
Beta-3 adrenergic receptorRattus norvegicus (Norway rat)EC500.047022
Beta-3 adrenergic receptorHomo sapiens (human)Kd63.660717
Beta-adrenergic receptor kinase 1Homo sapiens (human)Kd3.800012
Chain A, CHIMERA OF IG KAPPA CHAIN: HUMAN CONSTANT REGION AND MOUSE VARIABLE REGIONsynthetic constructKd0.400011
Chain B, CHIMERA OF IG GAMMA-1 CHAIN: HUMAN CONSTANT REGION AND MOUSE VARIABLE REGIONsynthetic constructKd0.400011
Chain H, Fab M82G2, Heavy chainMus musculus (house mouse)Kd0.140012
Chain L, Fab M82G2, Light chainMus musculus (house mouse)Kd0.140012
Delta-type opioid receptorRattus norvegicus (Norway rat)EC500.013011
GABA theta subunitRattus norvegicus (Norway rat)EC500.070012
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)EC500.070012
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)EC500.070012
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)EC500.070012
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)EC500.070012
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)EC500.070012
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)EC500.070012
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)EC500.070012
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)EC500.070012
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)EC500.070012
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)EC500.070012
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)EC500.070012
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)EC500.070012
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)EC500.070012
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)EC500.070012
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)EC500.070012
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)EC500.003011
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)EC500.003011
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)EC500.003011
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)EC500.003011
Glutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)EC500.003011
Glutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)EC500.003011
Glutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)EC500.003011
guanine nucleotide-binding protein subunit alpha-15Homo sapiens (human)EC5029.868012
Histamine H2 receptorCavia porcellus (domestic guinea pig)EC500.039811
mu-type opioid receptor isoform MOR-1Homo sapiens (human)EC5092.491723
Nicotinamide phosphoribosyltransferaseHomo sapiens (human)Kd230.000011
NPYLR7BAedes aegypti (yellow fever mosquito)EC500.039014
Oxytocin receptorRattus norvegicus (Norway rat)EC500.003011
Sigma non-opioid intracellular receptor 1Rattus norvegicus (Norway rat)EC500.990011
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)EC500.025011
Sodium-dependent dopamine transporter Homo sapiens (human)EC500.990011
Sodium-dependent noradrenaline transporter Homo sapiens (human)EC500.210011
Sodium-dependent serotonin transporterHomo sapiens (human)EC500.140011
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)EC501.765011
Taste receptor type 2 member 1Homo sapiens (human)EC500.004911
Taste receptor type 2 member 10Homo sapiens (human)EC500.004911
Taste receptor type 2 member 13Homo sapiens (human)EC500.004911
Taste receptor type 2 member 14Homo sapiens (human)EC500.004911
Taste receptor type 2 member 16Homo sapiens (human)EC500.004911
Taste receptor type 2 member 19Homo sapiens (human)EC500.004911
Taste receptor type 2 member 20Homo sapiens (human)EC500.004911
Taste receptor type 2 member 3Homo sapiens (human)EC500.004911
Taste receptor type 2 member 30Homo sapiens (human)EC500.004911
Taste receptor type 2 member 31Homo sapiens (human)EC500.004911
Taste receptor type 2 member 38Homo sapiens (human)EC500.004911
Taste receptor type 2 member 39Homo sapiens (human)EC500.004911
Taste receptor type 2 member 4Homo sapiens (human)EC500.004911
Taste receptor type 2 member 40Homo sapiens (human)EC500.004911
Taste receptor type 2 member 41Homo sapiens (human)EC500.004911
Taste receptor type 2 member 42Homo sapiens (human)EC500.004911
Taste receptor type 2 member 43Homo sapiens (human)EC500.004911
Taste receptor type 2 member 45Homo sapiens (human)EC500.004911
Taste receptor type 2 member 46Homo sapiens (human)EC500.004911
Taste receptor type 2 member 5Homo sapiens (human)EC500.004911
Taste receptor type 2 member 50Homo sapiens (human)EC500.004911
Taste receptor type 2 member 60Homo sapiens (human)EC500.004911
Taste receptor type 2 member 7Homo sapiens (human)EC500.004911
Taste receptor type 2 member 8Homo sapiens (human)EC500.004911
Taste receptor type 2 member 9Homo sapiens (human)EC500.004911
Trace amine-associated receptor 1Homo sapiens (human)EC501.381656
Trace amine-associated receptor 1Macaca mulatta (Rhesus monkey)EC501.010011
Trace amine-associated receptor 1Mus musculus (house mouse)EC500.103955
Trace amine-associated receptor 1Rattus norvegicus (Norway rat)EC500.532866
Vasopressin V1a receptorRattus norvegicus (Norway rat)EC501.000011

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Alpha-2A adrenergic receptorMus musculus (house mouse)IC400.078011
Alpha-2B adrenergic receptorMus musculus (house mouse)IC400.078011
Alpha-2C adrenergic receptorMus musculus (house mouse)IC400.078011
Beta-1 adrenergic receptorRattus norvegicus (Norway rat)EC200.000111
Beta-1 adrenergic receptor Cavia porcellus (domestic guinea pig)ED250.003411
Beta-2 adrenergic receptorHomo sapiens (human)Km0.050011
Beta-2 adrenergic receptor Bos taurus (cattle)Concentration500,000.500012
Beta-2 adrenergic receptor Bos taurus (cattle)KD app2.258512
Glutamate receptor 1Rattus norvegicus (Norway rat)EC2x448.000011
Glutamate receptor 1Rattus norvegicus (Norway rat)EC5X1,000.000012
Glutamate receptor 2Rattus norvegicus (Norway rat)EC2x448.000011
Glutamate receptor 2Rattus norvegicus (Norway rat)EC5X1,000.000012
Glutamate receptor 3Rattus norvegicus (Norway rat)EC2x448.000011
Glutamate receptor 3Rattus norvegicus (Norway rat)EC5X1,000.000012
Glutamate receptor 4Rattus norvegicus (Norway rat)EC2x448.000011
Glutamate receptor 4Rattus norvegicus (Norway rat)EC5X1,000.000012
Liver carboxylesterase 1Homo sapiens (human)Km120.000011
POU domain, class 2, transcription factor 1Homo sapiens (human)Km124.800012
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)Km0.200011