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adrenergic antagonist

An agent that binds to but does not activate adrenergic receptors thereby blocking the actions of endogenous or exogenous adrenergic agonists.

ChEBI ID: 37887

Members (20)

MemberDefinitionClass
bethanidinebethanidine
bretyliumA quaternary ammonium cation having 2-bromobenzyl, ethyl and two methyl groups attached to the nitrogen. It blocks noradrenaline release from the peripheral sympathetic nervous system, and is used in emergency medicine, cardiology, and other specialties for the acute management of ventricular tachycardia and ventricular fibrillation.bretylium
bretylium tosylateThe tosylate salt of bretylium. It blocks noradrenaline release from the peripheral sympathetic nervous system, and is used in emergency medicine, cardiology, and other specialties for the acute management of ventricular tachycardia and ventricular fibrillation.bretylium tosylate
bupivacaine hydrochlorideA racemate composed of equimolar amounts of dextrobupivacaine hydrochloride and levobupivacaine hydrochloride. The monohydrate form is commonly used as a local anaesthetic.1-butyl-N-(2,6-dimethylphenyl)piperidine-2-carboxamide hydrochloride; bupivacaine hydrochloride (anhydrous)
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
dihydroergocristineErgocristine in which a single bond replaces the double bond between positions 9 and 10. It is used as the mesylate salt for the symptomatic treatment of mental deterioration associated with cerebrovascular insufficiency and in peripheral vascular disease.dihydroergocristine
guanadrelA spiroketal resulting from the formal condensation of the keto group of cyclohexanone with the hydroxy groups of 1-(2,3-dihydroxypropyl)guanidine. A postganglionic adrenergic blocking agent formerly used (generally as the sulfate salt) for the management of hypertension, it has been largely superseded by other drugs less likely to cause orthostatic hypotension (dizzy spells on standing up or stretching).guanadrel
guanadrel sulfateAn organic sulfate salt resulting from the reaction of 2 eq. guanadrel with 1 eq. sulfuric acid. A postganglionic adrenergic blocking agent formerly used for the management of hypertension, it has been largely superseded by other drugs less likely to cause orthostatic hypotension (dizzy spells on standing up or stretching).guanadrel sulfate
guanethidineA member of the class of guanidines in which one of the hydrogens of the amino group has been replaced by a 2-azocan-1-ylethyl group.guanethidine
hordatine aA member of the calss of benzofurans that is a homodimer of para-coumarylagmatine where a hydroxy group of one molecule has reacted across the other molecule's ethene double bond to combine the two molecules and form a furan ring.hordatine A
levobupivacaineThe (S)-(-)-enantiomer of bupivacaine.levobupivacaine
levobupivacaine hydrochlorideThe monohydrochloride salt of levobupivacaine.levobupivacaine hydrochloride (anhydrous)
lurasidoneAn N-arylpiperazine that is (3aR,4S,7R,7aS)-2-{[(1R,2R)-2-(piperazin-1-ylmethyl)cyclohexyl]methyl}hexahydro-1H-4,7-methanoisoindole-1,3(2H)-dione in which position N4 of the piperazine ring is substituted by a 1,2-benzothiazol-3-yl group. Lurasidone is used (generally as the hydrochloride salt) as an atypical antipsychotic for the treatment of schizophrenia.lurasidone
lurasidone hydrochlorideA hydrochloride obtained by reaction of lurasidone with one equivalent of hydrochloric acid. An atypical antipsychotic agent used for the treatment of schizophrenia.lurasidone hydrochloride
periciazineA member of the class of phenothiazines that is 10H-phenothiazine substituted by a 3-(4-hydroxypiperidin-1-yl)propyl group at the nitrogen atom and a carbonitrile group at position 2. Periciazine is a first generation antipsychotic.periciazine
profenamineA member of the class of phenothiazines that is phenothiazine in which the hydrogen attached to the nitrogen is substituted by a 2-(diethylamino)propyl group. An antimuscarinic, it is used as the hydrochloride for the symptomatic treatment of Parkinson's disease.profenamine
profenamine hydrochlorideThe monohydrochloride salt of profenamine. An antimuscarinic, it is used for the symptomatic treatment of Parkinson's disease.profenamine hydrochloride
quetiapinequetiapine
trazodoneAn N-arylpiperazine in which one nitrogen is substituted by a 3-chlorophenyl group, while the other is substituted by a 3-(3-oxo[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)propyl group.trazodone
trazodone hydrochlorideA hydrochloride salt prepared from equimolar amounts of trazodone and hydrogen chloride.trazodone hydrochloride

Research

Studies (49,610)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-19909,275 (18.70)18.7374
1990's5,389 (10.86)18.2507
2000's10,233 (20.63)29.6817
2010's16,770 (33.80)24.3611
2020's7,943 (16.01)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials2,461 (4.68%)5.53%
Reviews2,882 (5.48%)6.00%
Case Studies2,642 (5.02%)4.05%
Observational103 (0.20%)0.25%
Other44,547 (84.63%)84.16%

Protein Targets (259)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency24.444215
15-lipoxygenase, partialHomo sapiens (human)Potency25.118911
67.9K proteinVaccinia virusPotency6.256012
acetylcholinesteraseHomo sapiens (human)Potency25.601812
acid sphingomyelinaseHomo sapiens (human)Potency19.952611
activating transcription factor 6Homo sapiens (human)Potency0.013411
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency23.567614
AR proteinHomo sapiens (human)Potency20.5670820
arylsulfatase AHomo sapiens (human)Potency11.995511
ATAD5 protein, partialHomo sapiens (human)Potency3.001323
Ataxin-2Homo sapiens (human)Potency20.961624
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency4.341112
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)Potency0.003522
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency79.432811
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency33.491511
caspase-3Homo sapiens (human)Potency33.491511
Cellular tumor antigen p53Homo sapiens (human)Potency21.800325
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency25.118911
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency25.059315
Chain A, Beta-lactamaseEscherichia coli K-12Potency10.682622
Chain A, Ferritin light chainEquus caballus (horse)Potency24.905422
Chain A, HADH2 proteinHomo sapiens (human)Potency29.112527
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency79.432811
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency30.668713
Chain B, HADH2 proteinHomo sapiens (human)Potency29.112527
chromobox protein homolog 1Homo sapiens (human)Potency65.916325
cytochrome P450 2C19 precursorHomo sapiens (human)Potency25.118911
cytochrome P450 2C9 precursorHomo sapiens (human)Potency39.810711
cytochrome P450 2C9, partialHomo sapiens (human)Potency38.901811
cytochrome P450 2D6Homo sapiens (human)Potency10.688215
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency13.701115
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency18.3411214
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency15.100429
D(1A) dopamine receptorHomo sapiens (human)Potency4.671937
DNA polymerase betaHomo sapiens (human)Potency79.432811
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency79.432811
DNA polymerase kappa isoform 1Homo sapiens (human)Potency28.183811
dopamine D1 receptorHomo sapiens (human)Potency0.051711
estrogen nuclear receptor alphaHomo sapiens (human)Potency24.9092722
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency33.491511
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency37.5753916
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency9.854915
EWS/FLI fusion proteinHomo sapiens (human)Potency34.669433
farnesoid X nuclear receptorHomo sapiens (human)Potency23.410622
Fumarate hydrataseHomo sapiens (human)Potency24.905312
GVesicular stomatitis virusPotency38.901811
GABA theta subunitRattus norvegicus (Norway rat)Potency18.341117
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency18.341117
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency18.341117
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency18.341117
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency18.341117
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency18.341117
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency18.341117
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency18.341117
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency18.341117
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency18.341117
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency18.341117
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency18.341117
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency18.341117
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency18.341117
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency18.341117
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency18.341117
gemininHomo sapiens (human)Potency8.654924
GLI family zinc finger 3Homo sapiens (human)Potency20.243126
GLS proteinHomo sapiens (human)Potency21.486424
glucocerebrosidaseHomo sapiens (human)Potency13.548113
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency11.451627
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency33.491511
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency18.8920211
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency19.723417
Histone H2A.xCricetulus griseus (Chinese hamster)Potency61.931511
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency38.901811
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)Potency38.901812
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency3.366723
Interferon betaHomo sapiens (human)Potency38.901811
lamin isoform A-delta10Homo sapiens (human)Potency8.733017
lethal factor (plasmid)Bacillus anthracis str. A2012Potency31.622811
LuciferasePhotinus pyralis (common eastern firefly)Potency40.533411
M-phase phosphoprotein 8Homo sapiens (human)Potency18.137812
Microtubule-associated protein tauHomo sapiens (human)Potency27.724014
mitogen-activated protein kinase 1Homo sapiens (human)Potency21.159126
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency9.021625
NFKB1 protein, partialHomo sapiens (human)Potency1.000022
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency33.020923
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency17.949813
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency19.287235
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency20.273112
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency47.754811
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency18.582025
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency1.916222
polyproteinZika virusPotency24.905312
polyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)Potency12.589311
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency11.047514
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency12.205718
pregnane X nuclear receptorHomo sapiens (human)Potency16.365728
progesterone receptorHomo sapiens (human)Potency27.059213
Rap guanine nucleotide exchange factor 3Homo sapiens (human)Potency125.892011
RAR-related orphan receptor gammaMus musculus (house mouse)Potency3.400622
regulator of G-protein signaling 4Homo sapiens (human)Potency26.679511
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency29.014422
retinoid X nuclear receptor alphaHomo sapiens (human)Potency18.491522
serine/threonine-protein kinase PLK1Homo sapiens (human)Potency29.934911
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency21.441117
survival motor neuron protein isoform dHomo sapiens (human)Potency12.589312
TDP1 proteinHomo sapiens (human)Potency20.8406229
thioredoxin reductaseRattus norvegicus (Norway rat)Potency32.3600412
ThrombopoietinHomo sapiens (human)Potency12.589322
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency22.1192313
thyroid stimulating hormone receptorHomo sapiens (human)Potency14.747323
transcriptional regulator ERG isoform 3Homo sapiens (human)Potency3.981111
transient receptor potential cation channel subfamily V member 1Homo sapiens (human)Potency12.589311
USP1 protein, partialHomo sapiens (human)Potency38.700613
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency3.076122
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency7.842222
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency72.334212
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)IC501.135936
5-hydroxytryptamine receptor 1AHomo sapiens (human)Ki0.18201725
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki0.2292911
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)IC500.571335
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)Ki0.324324
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)IC500.088748
5-hydroxytryptamine receptor 2AMus musculus (house mouse)IC500.028011
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)IC500.07761213
5-hydroxytryptamine receptor 2AHomo sapiens (human)Ki0.03633749
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)Ki0.01192324
5-hydroxytryptamine receptor 2BHomo sapiens (human)IC500.107426
5-hydroxytryptamine receptor 2BMus musculus (house mouse)IC500.028011
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)IC500.033877
5-hydroxytryptamine receptor 2BHomo sapiens (human)Ki0.098657
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)Ki0.013777
5-hydroxytryptamine receptor 2CHomo sapiens (human)IC500.531537
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)IC500.031088
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki0.28492432
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)IC500.864024
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)Ki0.448824
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)Ki0.08281721
5-hydroxytryptamine receptor 7Homo sapiens (human)IC500.015711
5-hydroxytryptamine receptor 7Homo sapiens (human)Ki0.30783036
5-hydroxytryptamine receptor 7 Rattus norvegicus (Norway rat)Ki0.009422
AcetylcholinesteraseHomo sapiens (human)IC50437.297167
AcetylcholinesteraseHomo sapiens (human)Ki3,492.517167
Acetylcholinesterase Bos taurus (cattle)IC507.000011
Acetylcholinesterase Bos taurus (cattle)Ki173.200022
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)IC500.081689
Alpha-1A adrenergic receptorHomo sapiens (human)Ki0.021179
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Ki0.1484912
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)IC500.081689
Alpha-1B adrenergic receptorHomo sapiens (human)Ki0.021468
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Ki0.14781012
Alpha-1D adrenergic receptorHomo sapiens (human)IC500.132213
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)IC500.081689
Alpha-1D adrenergic receptorHomo sapiens (human)Ki0.0332711
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Ki0.1737810
Alpha-2A adrenergic receptorHomo sapiens (human)IC501.163513
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)IC503.577222
Alpha-2A adrenergic receptorHomo sapiens (human)Ki0.324059
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)Ki0.116168
Alpha-2B adrenergic receptorHomo sapiens (human)IC500.170813
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)IC503.577222
Alpha-2B adrenergic receptorHomo sapiens (human)Ki0.233337
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)Ki0.134946
Alpha-2C adrenergic receptorHomo sapiens (human)IC500.790213
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)IC503.577222
Alpha-2C adrenergic receptorHomo sapiens (human)Ki0.218148
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)Ki0.134946
Androgen receptorRattus norvegicus (Norway rat)Ki3.000011
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)IC506.285522
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)Ki8.660611
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50133.000014
ATP-dependent translocase ABCB1Homo sapiens (human)Ki263.500022
ATP-dependent translocase ABCB1Mus musculus (house mouse)Ki139.100022
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)IC50269.3700512
Bile salt export pumpRattus norvegicus (Norway rat)IC50196.500011
Calmodulin-1Homo sapiens (human)IC5080.000022
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50133.000012
Carboxylic ester hydrolase Equus caballus (horse)Ki0.020011
Cholecystokinin receptor type ACavia porcellus (domestic guinea pig)Ki0.060011
CholinesteraseEquus caballus (horse)IC500.475012
CholinesteraseHomo sapiens (human)IC500.703333
CholinesteraseHomo sapiens (human)Ki4,033.346733
Cytochrome P450 2C9 Homo sapiens (human)IC5014.100011
Cytochrome P450 2D6Homo sapiens (human)IC500.298212
Cytochrome P450 2J2Homo sapiens (human)IC5014.100011
Cytochrome P450 3A4Homo sapiens (human)Ki0.017012
DBos taurus (cattle)IC504.090022
DRattus norvegicus (Norway rat)IC501.0661812
DBos taurus (cattle)Ki0.4200813
DRattus norvegicus (Norway rat)Ki0.23691316
D(1A) dopamine receptorHomo sapiens (human)IC500.268212
D(1A) dopamine receptorHomo sapiens (human)Ki0.48471216
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)IC500.6958911
D(2) dopamine receptorMus musculus (house mouse)IC500.290012
D(2) dopamine receptorRattus norvegicus (Norway rat)IC500.65031927
D(2) dopamine receptorBos taurus (cattle)Ki0.690011
D(2) dopamine receptorChlorocebus aethiops (grivet)Ki0.254022
D(2) dopamine receptorHomo sapiens (human)Ki0.13567180
D(2) dopamine receptorRattus norvegicus (Norway rat)Ki0.16932537
D(3) dopamine receptorHomo sapiens (human)IC501.403524
D(3) dopamine receptorRattus norvegicus (Norway rat)IC500.931257
D(3) dopamine receptorChlorocebus aethiops (grivet)Ki0.466011
D(3) dopamine receptorHomo sapiens (human)Ki0.49133440
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)Ki0.30455155
D(4) dopamine receptorRattus norvegicus (Norway rat)Ki0.097544
Dihydrofolate reductase Bacillus anthracisIC50102.000011
Endothelin receptor type BHomo sapiens (human)Ki0.012622
Endothelin receptor type BRattus norvegicus (Norway rat)Ki0.012611
GABA theta subunitRattus norvegicus (Norway rat)IC501.000012
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)IC501.000012
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)IC501.000012
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)IC501.000012
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)IC501.000012
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)IC501.000012
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)IC501.000012
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)IC501.000012
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)IC501.000012
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)IC501.000012
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)IC501.000012
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)IC501.000012
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)IC501.000013
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)IC501.000012
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)IC501.000012
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)IC501.000012
Gastrin/cholecystokinin type B receptorMus musculus (house mouse)Ki0.003812
Histamine H1 receptorHomo sapiens (human)IC500.135213
Histamine H1 receptorRattus norvegicus (Norway rat)IC500.023012
Histamine H1 receptorCavia porcellus (domestic guinea pig)Ki0.069212
Histamine H1 receptorHomo sapiens (human)Ki0.00961014
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)IC50133.000014
Muscarinic acetylcholine receptor M1Homo sapiens (human)IC500.660934
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)IC500.201459
Muscarinic acetylcholine receptor M1Homo sapiens (human)Ki0.2047711
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Ki0.013622
Muscarinic acetylcholine receptor M2Homo sapiens (human)IC501.910412
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)IC500.245357
Muscarinic acetylcholine receptor M2Homo sapiens (human)Ki0.603124
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)Ki0.035622
Muscarinic acetylcholine receptor M3Homo sapiens (human)IC500.078011
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)IC500.245357
Muscarinic acetylcholine receptor M3Homo sapiens (human)Ki0.357023
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)Ki0.025111
Muscarinic acetylcholine receptor M4Homo sapiens (human)IC500.811812
Muscarinic acetylcholine receptor M4Rattus norvegicus (Norway rat)IC500.245357
Muscarinic acetylcholine receptor M4Homo sapiens (human)Ki0.236536
Muscarinic acetylcholine receptor M4Rattus norvegicus (Norway rat)Ki0.025111
Muscarinic acetylcholine receptor M5Homo sapiens (human)IC501.506812
Muscarinic acetylcholine receptor M5Rattus norvegicus (Norway rat)IC500.245357
Muscarinic acetylcholine receptor M5Homo sapiens (human)Ki0.804924
Muscarinic acetylcholine receptor M5Rattus norvegicus (Norway rat)Ki0.025111
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
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50109.54381725
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)Ki9.960155
Sigma non-opioid intracellular receptor 1Homo sapiens (human)IC502.248212
Sigma non-opioid intracellular receptor 1Rattus norvegicus (Norway rat)IC501.000011
Sigma non-opioid intracellular receptor 1Homo sapiens (human)Ki3.463323
Sodium channel protein type 5 subunit alphaHomo sapiens (human)IC5016.900011
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)IC500.369012
Sodium-dependent serotonin transporterHomo sapiens (human)Ki5.573024
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)Ki0.021011
Solute carrier family 22 member 1 Homo sapiens (human)IC5020.460011
TransporterRattus norvegicus (Norway rat)Ki0.589023
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 1AHomo sapiens (human)EC500.785011
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)Kd43.375012
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
Histamine H1 receptorHomo sapiens (human)EC500.000411
Histamine H1 receptorHomo sapiens (human)Kd0.003111
Histamine H4 receptorHomo sapiens (human)Kd0.029444
HLA class I histocompatibility antigen, A alpha chain Homo sapiens (human)Kd2.500011
Muscarinic acetylcholine receptor M1Homo sapiens (human)EC5010.000012
Muscarinic acetylcholine receptor M2Homo sapiens (human)EC5010.000011
Muscarinic acetylcholine receptor M3Homo sapiens (human)EC5010.000011
Muscarinic acetylcholine receptor M4Homo sapiens (human)EC5010.000011
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)Km35.150012
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
Nitric oxide synthase, brain Rattus norvegicus (Norway rat)Activity0.100012
Nitric oxide synthase, inducibleHomo sapiens (human)Activity0.100012
UDP-glucuronosyltransferase 1A4Homo sapiens (human)Km62.000011