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beta-adrenergic antagonist

An agent that binds to but does not activate beta-adrenergic receptors thereby blocking the actions of endogenous or exogenous beta-adrenergic agonists. beta-Adrenergic antagonists are used for treatment of hypertension, cardiac arrhythmias, angina pectoris, glaucoma, migraine headaches and anxiety.

ChEBI ID: 35530

Members (30)

MemberDefinitionClass
1-0-octadecyl 2-0-acetyl sn-glycero-3-phosphorylcholineA 2-acetyl-1-alkyl-sn-glycero-3-phosphocholine betaine which has octadecyl as the alkyl group. PAF is a potent phospholipid activator and mediator of many leukocyte functions, including platelet aggregation, inflammation, and anaphylaxis.2-O-acetyl-1-O-octadecyl-sn-glycero-3-phosphocholine
1-hexadecyl-2-acetyl-glycero-3-phosphocholineA 2-acetyl-1-alkyl-sn-glycero-3-phosphocholine betaine which has hexadecyl as the alkyl group. PAF is a potent phospholipid activator and mediator of many leukocyte functions, including platelet aggregation, inflammation, and anaphylaxis.2-O-acetyl-1-O-hexadecyl-sn-glycero-3-phosphocholine
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
ag 1879A member of the class of pyrazolopyrimidine that is pyrazolo[3,4-d]pyrimidin-4-amine bearing additional tert-butyl and 4-chlorophenyl substituents at positions 1 and 3 respectively. It is a potent ATP-competitive inhibitor of the Src family of protein tyrosine kinases.PP2
alprenololA secondary alcohol that is propan-2-ol substituted by a 2-allylphenoxy group at position 1 and an isopropylamino group at position 3. It is a beta-adrenergic antagonist used as a antihypertensive, anti-arrhythmia and a sympatholytic agent.alprenolol
asl 8052The hydrochloride salt of esmolol. A cardioselective and short-acting beta1 receptor blocker with rapid onset but lacking intrinsic sympathomimetic and membrane-stabilising properties, it is used in the management of supraventricular arrhythmias, and for the control of hypertension and tachycardia during surgery.esmolol hydrochloride
atenololAn ethanolamine compound having a (4-carbamoylmethylphenoxy)methyl group at the 1-position and an N-isopropyl substituent.atenolol
betaxololA propanolamine that is 3-aminopropane-1,2-diol in which the hydrogen of the primary hydoxy is substituted by a 4-[2-(cyclopropylmethoxy)ethyl]phenyl group and one of the hydrogens attached to the amino group is substituted by isopropyl. It is a selective beta1-receptor blocker and is used in the treatment of glaucoma as well as hypertension, arrhythmias, and coronary heart disease. It is also used to reduce non-fatal cardiac events in patients with heart failure.betaxolol
betaxolol hydrochlorideThe hydrochloride salt of betaxolol.betaxolol hydrochloride
bevantololA propanolamine that is 3-aminopropane-1,2-diol in which the hydrogen of the primary hydroxy group is substituted by 3-methylphenyl and one of the hydrogens attached to the nitrogen is substituted by 2-(3,4-dimethoxyphenyl)ethyl. A beta1 adrenoceptor antagonist, it has been shown to be as effective as other beta-blockers for the treatment of angina pectoris and hypertension.bevantolol
bisoprololbisoprolol
carteololcarteolol
carteolol hydrochloridecarteolol hydrochloride
carvedilolA member of the class of carbazoles that is an adrenergic antagonist with non-selective beta- and alpha-1 receptor blocking properties which helps in the management of congestive heart failure.carvedilol
cgp 12177A benzimidazole that is benzimidazol-2-one substituted at position 4 by a 3-(tert-butylamino)-2-hydroxypropoxy group.CGP 12177
esatenololThe (S)-enantiomer of atenolol.esatenolol
icatibantA ten-membered synthetic oligopeptide consisting of D-Arg, Arg, Pro, Hyp, Gly, Thi, Ser, D-Tic, Oic, and Arg residues joined in sequrence. A bradykinin receptor antagonist used as its acetate salt for the treatment of acute attacks of hereditary angioedema in adult patients.icatibant
ici 118551An indane substituted at position 7 by a methyl group and at position 4 by a 3-(isopropylamino)-2-hydroxybutoxy group (the 2R,3S-diastereomer).ICI 118551
levobunololA cyclic ketone that is 3,4-dihydronaphthalen-1-one substituted at position 5 by a 3-(tert-butylamino)-2-hydroxypropoxy group (the S-enantiomer). A non-selective beta-adrenergic antagonist used (as its hydrochloride salt) for treatment of glaucoma.levobunolol
levobunolol hydrochlorideA hydrochloride obtained by combining equimolar amounts of levobunolol and hydrochloric acid. A non-selective beta-adrenergic antagonist used for treatment of glaucoma.levobunolol hydrochloride
metipranolol3-(Propan-2-ylamino)propane-1,2-diol in which the hydrogen of the primary hydroxy group is substituted by a 4-acetoxy-2,3,5-trimethylphenoxy group. A non-cardioselective beta-blocker, it is used to lower intra-ocular pressure in the management of open-angle glaucoma.metipranolol
metoprololA propanolamine that is 1-(propan-2-ylamino)propan-2-ol substituted by a 4-(2-methoxyethyl)phenoxy group at position 1.metoprolol
pindololA member of the class of indols which is the 2-hydroxy-3-(isopropylamino)propyl ether derivative of 1H-indol-4-ol.pindolol
practololN-(4-Hydroxyphenyl)acetamide in which the hydrogen of the phenolic hydroxy group is substituted by a 3-(isopropylaminoamino)-2-hydroxypropyl group. A selective beta blocker, it has been used in the emergency treatment of cardiac arrhythmias.practolol
propranololA propanolamine that is propan-2-ol substituted by a propan-2-ylamino group at position 1 and a naphthalen-1-yloxy group at position 3.propranolol
sotalolA sulfonamide that is N-phenylmethanesulfonamide in which the phenyl group is substituted at position 4 by a 1-hydroxy-2-(isopropylamino)ethyl group. It has both beta-adrenoreceptor blocking (Vaughan Williams Class II) and cardiac action potential duration prolongation (Vaughan Williams Class III) antiarrhythmic properties. It is used (usually as the hydrochloride salt) for the management of ventricular and supraventricular arrhythmias.sotalol
sotalol hydrochlorideA hydrochloride salt that is the monohydrochloride of sotalol. It has both beta-adrenoreceptor blocking (Vaughan Williams Class II) and cardiac action potential duration prolongation (Vaughan Williams Class III) antiarrhythmic properties. It is used (usually as the hydrochloride salt) for the management of ventricular and supraventricular arrhythmias.sotalol hydrochloride
timololThe (S)-(-) (more active) enantiomer of timolol. A beta-adrenergic antagonist, both the hemihydrate and the maleate salt are used in the mangement of glaucoma, hypertension, angina pectoris and myocardial infarction, and for the prevention of migraine.(S)-timolol (anhydrous)
timolol maleateThe maleic acid salt of the active (S)-enantiomer of timolol, comprising equimolar amounts of (S)-timolol and maleic acid.(S)-timolol maleate

Research

Studies (62,773)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-199030,224 (48.15)18.7374
1990's14,306 (22.79)18.2507
2000's9,122 (14.53)29.6817
2010's7,262 (11.57)24.3611
2020's1,859 (2.96)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials11,648 (15.49%)5.53%
Reviews4,072 (5.42%)6.00%
Case Studies4,063 (5.40%)4.05%
Observational121 (0.16%)0.25%
Other55,269 (73.52%)84.16%

Protein Targets (252)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-lipoxygenase, partialHomo sapiens (human)Potency39.810711
67.9K proteinVaccinia virusPotency4.170712
acetylcholinesteraseHomo sapiens (human)Potency41.993622
alpha-galactosidaseHomo sapiens (human)Potency4.575313
Alpha-synucleinHomo sapiens (human)Potency2.375312
AR proteinHomo sapiens (human)Potency28.623767
aryl hydrocarbon receptorHomo sapiens (human)Potency29.849322
arylsulfatase AHomo sapiens (human)Potency6.514618
ATAD5 protein, partialHomo sapiens (human)Potency21.799425
Ataxin-2Homo sapiens (human)Potency23.887524
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency19.525915
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency29.849311
Bloom syndrome protein isoform 1Homo sapiens (human)Potency124.424228
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency44.964712
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency17.559412
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency25.360614
Chain A, Beta-lactamaseEscherichia coli K-12Potency21.314512
Chain A, CruzipainTrypanosoma cruziPotency39.810711
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency6.423814
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency23.128815
chromobox protein homolog 1Homo sapiens (human)Potency48.574527
cytochrome P450 2D6Homo sapiens (human)Potency16.767816
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency17.001114
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency21.5102210
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency27.595713
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency13.333211
D(1A) dopamine receptorHomo sapiens (human)Potency5.092536
D(1A) dopamine receptorSus scrofa (pig)Potency14.689211
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency89.420814
DNA polymerase kappa isoform 1Homo sapiens (human)Potency44.059613
endonuclease IVEscherichia coliPotency14.125411
estrogen nuclear receptor alphaHomo sapiens (human)Potency12.261247
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency43.277111
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency41.131244
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency11.0965110
EWS/FLI fusion proteinHomo sapiens (human)Potency17.654048
flap endonuclease 1Homo sapiens (human)Potency19.780212
GABA theta subunitRattus norvegicus (Norway rat)Potency21.510215
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency21.510215
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency21.510215
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency21.510215
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency21.510215
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency21.510215
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency21.510215
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency21.510215
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency21.510215
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency21.510215
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency21.510215
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency21.510215
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency21.510215
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency21.510215
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency21.510215
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency21.510215
gemininHomo sapiens (human)Potency9.7887211
GLI family zinc finger 3Homo sapiens (human)Potency8.628223
glp-1 receptor, partialHomo sapiens (human)Potency5.623411
GLS proteinHomo sapiens (human)Potency21.951123
glucocerebrosidaseHomo sapiens (human)Potency11.220211
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency16.634423
glucokinase regulatory proteinHomo sapiens (human)Potency19.952611
Guanine nucleotide-binding protein GHomo sapiens (human)Potency28.183811
hexokinase-4 isoform 1Homo sapiens (human)Potency19.952611
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency5.011912
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency39.810711
Histone H2A.xCricetulus griseus (Chinese hamster)Potency61.931511
histone-lysine N-methyltransferase 2A isoform 2 precursorHomo sapiens (human)Potency25.118911
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency12.589322
importin subunit beta-1 isoform 1Homo sapiens (human)Potency125.892011
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency2.238711
lamin isoform A-delta10Homo sapiens (human)Potency9.0672111
lethal factor (plasmid)Bacillus anthracis str. A2012Potency22.106012
lysosomal alpha-glucosidase preproproteinHomo sapiens (human)Potency26.224833
M-phase phosphoprotein 8Homo sapiens (human)Potency25.118911
Microtubule-associated protein tauHomo sapiens (human)Potency22.387212
mitogen-activated protein kinase 1Homo sapiens (human)Potency19.955422
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency4.064825
Neuronal acetylcholine receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency11.220211
Neuronal acetylcholine receptor subunit beta-2Rattus norvegicus (Norway rat)Potency11.220211
NFKB1 protein, partialHomo sapiens (human)Potency4.261728
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency4.280012
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency26.601111
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency16.360111
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency6.007011
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency17.044824
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency29.849311
ParkinHomo sapiens (human)Potency16.360111
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency17.324612
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency84.921411
phosphopantetheinyl transferaseBacillus subtilisPotency44.964712
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency5.011911
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency13.512015
progesterone receptorHomo sapiens (human)Potency61.752811
RAR-related orphan receptor gammaMus musculus (house mouse)Potency0.472412
regulator of G-protein signaling 4Homo sapiens (human)Potency5.671417
retinoid X nuclear receptor alphaHomo sapiens (human)Potency49.291122
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency14.689222
Smad3Homo sapiens (human)Potency2.058513
snurportin-1Homo sapiens (human)Potency125.892011
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency29.950315
survival motor neuron protein isoform dHomo sapiens (human)Potency11.690213
TAR DNA-binding protein 43Homo sapiens (human)Potency23.433414
TDP1 proteinHomo sapiens (human)Potency16.0644214
thioredoxin reductaseRattus norvegicus (Norway rat)Potency13.049027
ThrombopoietinHomo sapiens (human)Potency5.011922
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency31.253024
thyroid stimulating hormone receptorHomo sapiens (human)Potency19.111625
transcriptional regulator ERG isoform 3Homo sapiens (human)Potency22.106012
USP1 protein, partialHomo sapiens (human)Potency39.810712
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency1.492622
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency37.646012

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 1AHomo sapiens (human)IC502.305522
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)IC500.6003510
5-hydroxytryptamine receptor 1AHomo sapiens (human)Ki0.051855
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki2.6336313
5-hydroxytryptamine receptor 1BHomo sapiens (human)IC505.011911
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)IC501.182015
5-hydroxytryptamine receptor 1BHomo sapiens (human)Ki7.533313
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)Ki0.450948
5-hydroxytryptamine receptor 1DRattus norvegicus (Norway rat)Ki0.100011
5-hydroxytryptamine receptor 1FRattus norvegicus (Norway rat)Ki0.100011
5-hydroxytryptamine receptor 2AHomo sapiens (human)IC502.296023
5-hydroxytryptamine receptor 2AHomo sapiens (human)Ki0.268012
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)Ki114.750022
5-hydroxytryptamine receptor 2BHomo sapiens (human)IC501.792323
5-hydroxytryptamine receptor 2BHomo sapiens (human)Ki0.116512
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)Ki114.750022
5-hydroxytryptamine receptor 2CHomo sapiens (human)IC502.473623
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki18.420723
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)Ki114.750022
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)IC501.204512
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)Ki0.631012
5-hydroxytryptamine receptor 6Homo sapiens (human)IC503.198623
5-hydroxytryptamine receptor 6Homo sapiens (human)Ki1.064012
5-hydroxytryptamine receptor 7Cavia porcellus (domestic guinea pig)IC5063.200012
5-hydroxytryptamine receptor 7Homo sapiens (human)IC505.011911
Adenosine receptor A2aHomo sapiens (human)IC505.011911
Adenosine receptor A3Homo sapiens (human)IC505.011911
AlbuminHomo sapiens (human)Ki354,813,000.000011
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)IC500.538011
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)Ki0.533011
Alpha-1A adrenergic receptorHomo sapiens (human)IC502.620922
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC50100.000011
Alpha-1B adrenergic receptorHomo sapiens (human)IC500.230011
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)IC50100.000011
Alpha-1D adrenergic receptorHomo sapiens (human)IC500.115922
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)IC50100.000011
Alpha-1D adrenergic receptorHomo sapiens (human)Ki0.000911
Alpha-2A adrenergic receptorHomo sapiens (human)IC502.558922
Alpha-2A adrenergic receptorHomo sapiens (human)Ki0.040011
Alpha-2B adrenergic receptorHomo sapiens (human)IC500.094011
Alpha-2B adrenergic receptorHomo sapiens (human)Ki0.043011
Alpha-2C adrenergic receptorHomo sapiens (human)IC502.550922
Alpha-2C adrenergic receptorHomo sapiens (human)Ki0.013011
Amyloid-beta precursor proteinHomo sapiens (human)IC5030.000011
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)IC504.119311
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)Ki3.374911
Angiotensin-converting enzymeRattus norvegicus (Norway rat)Ki0.024014
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50133.000018
ATP-dependent translocase ABCB1Homo sapiens (human)IC50378.040045
ATP-dependent translocase ABCB1Homo sapiens (human)Ki124.000012
B2 bradykinin receptorCavia porcellus (domestic guinea pig)IC500.002523
B2 bradykinin receptorHomo sapiens (human)IC500.001944
B2 bradykinin receptorHomo sapiens (human)Ki0.000144
B2 bradykinin receptorRattus norvegicus (Norway rat)Ki0.000111
Beta-1 adrenergic receptorHomo sapiens (human)IC501.72351929
Beta-1 adrenergic receptorRattus norvegicus (Norway rat)IC500.012023
Beta-1 adrenergic receptorHomo sapiens (human)Ki0.2127921
Beta-1 adrenergic receptorMus musculus (house mouse)Ki0.018913
Beta-1 adrenergic receptorRattus norvegicus (Norway rat)Ki0.8031717
Beta-1 adrenergic receptor Cavia porcellus (domestic guinea pig)IC500.034711
Beta-2 adrenergic receptorCanis lupus familiaris (dog)IC503.804234
Beta-2 adrenergic receptorCavia porcellus (domestic guinea pig)IC500.028811
Beta-2 adrenergic receptorHomo sapiens (human)IC501.60621220
Beta-2 adrenergic receptorRattus norvegicus (Norway rat)IC500.012023
Beta-2 adrenergic receptorHomo sapiens (human)Ki1.00741022
Beta-2 adrenergic receptorMus musculus (house mouse)Ki13.500011
Beta-2 adrenergic receptorRattus norvegicus (Norway rat)Ki1.600011
Beta-3 adrenergic receptorHomo sapiens (human)IC501.5434510
Beta-3 adrenergic receptorRattus norvegicus (Norway rat)IC500.012023
Beta-3 adrenergic receptorHomo sapiens (human)Ki0.152415
Beta-3 adrenergic receptorRattus norvegicus (Norway rat)Ki1.600011
Bile salt export pumpHomo sapiens (human)IC50393.7000420
Bile salt export pumpRattus norvegicus (Norway rat)IC501,000.000012
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50133.000018
Casein kinase I isoform deltaHomo sapiens (human)IC500.041011
Chain A, Lck KinaseHomo sapiens (human)IC500.020011
Chain A, Tyrosine-protein kinase LynMus musculus (house mouse)IC500.009012
Cholecystokinin receptor type AHomo sapiens (human)IC505.011911
Cytochrome P450 1A2Homo sapiens (human)IC507.000022
Cytochrome P450 1B1Homo sapiens (human)IC501.100011
Cytochrome P450 2C19Homo sapiens (human)IC5010.000011
Cytochrome P450 2C8Homo sapiens (human)IC5010.000011
Cytochrome P450 2C9 Homo sapiens (human)IC5028.717524
Cytochrome P450 2D6Homo sapiens (human)IC5018.318636
Cytochrome P450 2J2Homo sapiens (human)IC5034.956713
Cytochrome P450 3A4Homo sapiens (human)IC5010.000011
D(1A) dopamine receptorHomo sapiens (human)IC503.254922
D(1A) dopamine receptorHomo sapiens (human)Ki0.749011
D(2) dopamine receptorHomo sapiens (human)IC502.578922
D(2) dopamine receptorHomo sapiens (human)Ki0.049011
D(3) dopamine receptorHomo sapiens (human)IC500.577011
D(3) dopamine receptorHomo sapiens (human)Ki0.196011
D(3) dopamine receptorRattus norvegicus (Norway rat)Ki5.000011
Delta-type opioid receptorHomo sapiens (human)IC505.011911
Endothelin-1 receptorHomo sapiens (human)IC505.011911
Ephrin type-B receptor 2Homo sapiens (human)IC5052.000011
Epidermal growth factor receptorHomo sapiens (human)IC500.480011
Epidermal growth factor receptorHomo sapiens (human)Ki10.000011
Fatty acid-binding protein, liverRattus norvegicus (Norway rat)Ki717.000011
GABA theta subunitRattus norvegicus (Norway rat)IC500.028812
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)IC500.028812
Gamma-aminobutyric acid receptor subunit alpha-1Bos taurus (cattle)Ki0.000111
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)IC500.028812
Gamma-aminobutyric acid receptor subunit alpha-2Bos taurus (cattle)Ki0.000111
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)IC500.028812
Gamma-aminobutyric acid receptor subunit alpha-3Bos taurus (cattle)Ki0.000111
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)IC500.028812
Gamma-aminobutyric acid receptor subunit alpha-4Bos taurus (cattle)Ki0.000111
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)IC500.028812
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)IC500.028812
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)IC500.028812
Gamma-aminobutyric acid receptor subunit beta-1Bos taurus (cattle)Ki0.000111
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)IC500.028812
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)IC500.028812
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)IC500.028812
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)IC500.028812
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)IC500.028812
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)IC500.028812
Gamma-aminobutyric acid receptor subunit gamma-2Bos taurus (cattle)Ki0.000111
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)IC500.028812
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)IC500.028812
Kappa-type opioid receptorHomo sapiens (human)IC505.011911
Mitogen-activated protein kinase 14Homo sapiens (human)IC504.230011
Mu-type opioid receptorHomo sapiens (human)IC505.011911
Multidrug and toxin extrusion protein 1Homo sapiens (human)IC5092.400011
Multidrug resistance-associated protein 4Homo sapiens (human)IC50133.000018
Muscarinic acetylcholine receptor M1Homo sapiens (human)IC505.011911
Muscarinic acetylcholine receptor M2Homo sapiens (human)IC505.011911
Muscarinic acetylcholine receptor M3Homo sapiens (human)IC505.011911
Nuclear receptor subfamily 3 group C member 3 Bos taurus (cattle)IC504.119311
Nuclear receptor subfamily 3 group C member 3 Bos taurus (cattle)Ki3.374911
Platelet-activating factor receptorHomo sapiens (human)IC500.000311
Platelet-activating factor receptorHomo sapiens (human)Ki0.000111
Potassium channel subfamily K member 10Homo sapiens (human)IC5015.800022
Potassium channel subfamily K member 2Homo sapiens (human)IC5010.950022
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC507.328677
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)Ki3.374911
Proto-oncogene tyrosine-protein kinase LCK Mus musculus (house mouse)IC500.031011
Proto-oncogene tyrosine-protein kinase SrcGallus gallus (chicken)IC500.036011
Proto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)IC501.181488
Proto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)Ki0.500022
Receptor-interacting serine/threonine-protein kinase 2Homo sapiens (human)IC500.019011
Renin Rattus norvegicus (Norway rat)Ki13.500012
Sigma non-opioid intracellular receptor 1Homo sapiens (human)IC501.821512
Sigma non-opioid intracellular receptor 1Homo sapiens (human)Ki0.765512
Sodium channel protein type 5 subunit alphaHomo sapiens (human)IC502.100011
Sodium-dependent dopamine transporter Homo sapiens (human)IC500.845011
Sodium-dependent dopamine transporter Homo sapiens (human)Ki0.671011
Sodium-dependent noradrenaline transporter Homo sapiens (human)IC500.538011
Sodium-dependent noradrenaline transporter Homo sapiens (human)Ki0.533011
Sodium-dependent serotonin transporterHomo sapiens (human)IC501.833013
Sodium-dependent serotonin transporterHomo sapiens (human)Ki0.974013
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)Ki7.000011
Sodium/bile acid cotransporterHomo sapiens (human)IC505.500011
Solute carrier family 22 member 1 Homo sapiens (human)IC5033.300022
Solute carrier family 22 member 1 Homo sapiens (human)Ki95.800011
Solute carrier family 22 member 2Homo sapiens (human)IC507.500011
Squalene synthaseRattus norvegicus (Norway rat)IC504.200011
Toll-like receptor 4Homo sapiens (human)IC5032.220011
Type-1 angiotensin II receptorHomo sapiens (human)IC505.011911
Tyrosine-protein kinase ABL1Homo sapiens (human)Ki0.500011
Tyrosine-protein kinase CSKHomo sapiens (human)IC500.500011
Tyrosine-protein kinase FynHomo sapiens (human)IC500.005222
Tyrosine-protein kinase HCKHomo sapiens (human)IC500.005011
Tyrosine-protein kinase JAK2Homo sapiens (human)IC5050,000.000011
Tyrosine-protein kinase LckHomo sapiens (human)IC500.004011
Tyrosine-protein kinase LckHomo sapiens (human)Ki0.000811
Tyrosine-protein kinase LynHomo sapiens (human)IC500.000511
Tyrosine-protein kinase ZAP-70Homo sapiens (human)IC50100,000.000011
UDP-glucuronosyltransferase 1A1 Homo sapiens (human)IC5019.500022
UreaseCanavalia ensiformis (jack bean)IC5064.360011
Vasopressin V1a receptorHomo sapiens (human)IC505.011911
Voltage-dependent L-type calcium channel subunit alpha-1CCavia porcellus (domestic guinea pig)IC5021.000014
Voltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)IC50412.433333
Voltage-dependent L-type calcium channel subunit alpha-1CRattus norvegicus (Norway rat)IC5021.000011
Voltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)IC50193.300011
Voltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)IC50193.300011
Voltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)IC50193.300011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 1AHomo sapiens (human)EC500.027011
5-hydroxytryptamine receptor 1AHomo sapiens (human)Kd0.063111
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Kd0.9098213
5-hydroxytryptamine receptor 1BHomo sapiens (human)EC505.011911
5-hydroxytryptamine receptor 2AHomo sapiens (human)EC505.011911
5-hydroxytryptamine receptor 2BHomo sapiens (human)EC505.011911
5-hydroxytryptamine receptor 2CHomo sapiens (human)EC505.011911
5-hydroxytryptamine receptor 6Homo sapiens (human)EC505.011911
5-hydroxytryptamine receptor 7Homo sapiens (human)EC505.011911
Adenosine receptor A2aHomo sapiens (human)EC505.011911
Adenosine receptor A3Homo sapiens (human)EC505.011911
AlbuminHomo sapiens (human)Kd520.342566
Alpha-1A adrenergic receptorHomo sapiens (human)EC505.011911
Alpha-1A adrenergic receptorHomo sapiens (human)Kd100.000011
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Kd0.014811
Alpha-1B adrenergic receptorHomo sapiens (human)Kd100.000011
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Kd0.014811
Alpha-1D adrenergic receptorHomo sapiens (human)Kd100.000011
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Kd0.014811
Alpha-2A adrenergic receptorHomo sapiens (human)EC505.011911
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)EC500.027012
Alpha-2A adrenergic receptorHomo sapiens (human)Kd100.000011
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)Kd0.014811
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)EC500.027012
Alpha-2B adrenergic receptorHomo sapiens (human)Kd100.000011
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)Kd0.014811
Alpha-2C adrenergic receptorHomo sapiens (human)EC505.011911
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)EC500.027012
Alpha-2C adrenergic receptorHomo sapiens (human)Kd100.000011
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)Kd0.014811
amino acid transporter AGP1Saccharomyces cerevisiae S288CEC5010.800011
B2 bradykinin receptorHomo sapiens (human)Kd0.000311
bcl-2-like protein 11 isoform 1Homo sapiens (human)EC50350.000011
Beta-1 adrenergic receptorHomo sapiens (human)EC500.012311
Beta-1 adrenergic receptorHomo sapiens (human)Kd5.26521050
Beta-1 adrenergic receptorRattus norvegicus (Norway rat)Kd0.0551410
Beta-1 adrenergic receptor Cavia porcellus (domestic guinea pig)Kd0.63721729
Beta-2 adrenergic receptorCanis lupus familiaris (dog)Kd0.186211
Beta-2 adrenergic receptorCavia porcellus (domestic guinea pig)Kd0.6115622
Beta-2 adrenergic receptorHomo sapiens (human)Kd5.05121360
Beta-2 adrenergic receptor Bos taurus (cattle)Kd69.069013
Beta-3 adrenergic receptorHomo sapiens (human)Kd5.7821744
Chain A, BCL-2-RELATED PROTEIN A1Homo sapiens (human)EC50350.000011
Cholecystokinin receptor type AHomo sapiens (human)EC505.011911
D(1A) dopamine receptorHomo sapiens (human)EC505.011911
D(2) dopamine receptorHomo sapiens (human)EC505.011911
Delta-type opioid receptorHomo sapiens (human)EC505.011911
Endothelin-1 receptorHomo sapiens (human)EC505.011911
Ephrin type-A receptor 3Homo sapiens (human)Kd200.000011
Ephrin type-B receptor 2Homo sapiens (human)Kd36.500011
GABA theta subunitRattus norvegicus (Norway rat)Kd0.985316
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Kd0.985316
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Kd0.985316
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Kd0.985316
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Kd0.985316
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Kd0.985316
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Kd0.985316
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Kd0.985316
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Kd0.985316
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Kd0.985316
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Kd0.985316
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Kd0.985316
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Kd0.985316
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Kd0.985316
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Kd0.985316
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Kd0.985316
Kappa-type opioid receptorHomo sapiens (human)EC505.011911
LAP4Saccharomyces cerevisiae (brewer's yeast)EC504.823011
Mu-type opioid receptorHomo sapiens (human)EC505.011911
Muscarinic acetylcholine receptor M1Homo sapiens (human)EC505.011911
Muscarinic acetylcholine receptor M2Homo sapiens (human)EC505.011911
Muscarinic acetylcholine receptor M3Homo sapiens (human)EC505.011911
Neuromedin-K receptorCavia porcellus (domestic guinea pig)Kd0.002411
Nuclear receptor subfamily 2 group E member 1Homo sapiens (human)EC5033.666733
Nuclear receptor subfamily 2 group E member 1Homo sapiens (human)Kd0.500011
Proto-oncogene tyrosine-protein kinase SrcGallus gallus (chicken)Kd0.296011
RPL19ASaccharomyces cerevisiae (brewer's yeast)EC500.852522
short transient receptor potential channel 6 isoform 1Mus musculus (house mouse)EC5044.670011
Type-1 angiotensin II receptorHomo sapiens (human)EC505.011911
Vasopressin V1a receptorHomo sapiens (human)EC505.011911

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Affinity constant0.013011
Alpha-1A adrenergic receptorHomo sapiens (human)Kapp78.282814
Alpha-1B adrenergic receptorHomo sapiens (human)Kapp78.282814
Alpha-1D adrenergic receptorHomo sapiens (human)Kapp78.282714
Alpha-2A adrenergic receptorHomo sapiens (human)Kapp78.282714
Alpha-2B adrenergic receptorHomo sapiens (human)Kapp78.282714
Alpha-2C adrenergic receptorHomo sapiens (human)Kapp78.282814
ATP-dependent translocase ABCB1Homo sapiens (human)Ki1200.000011
ATP-dependent translocase ABCB1Homo sapiens (human)Ki21,750.000011
Beta-1 adrenergic receptorRattus norvegicus (Norway rat)Kapp4.508214
Beta-1 adrenergic receptor Cavia porcellus (domestic guinea pig)Affinity constant0.013011
Beta-2 adrenergic receptorCavia porcellus (domestic guinea pig)Affinity constant0.000611
Beta-2 adrenergic receptorRattus norvegicus (Norway rat)Kapp78.282714
Chain A, BCL-2-RELATED PROTEIN A1Homo sapiens (human)AC50697.450022
HSP40, subfamily A [Plasmodium falciparum 3D7]Plasmodium falciparum 3D7AbsAC1000_uM1.558011
POU domain, class 2, transcription factor 1Homo sapiens (human)Km195.900011
Skn7pSaccharomyces cerevisiae (brewer's yeast)AbsAC40_uM12.610011
Solute carrier family 22 member 1 Homo sapiens (human)Activity9.700011