Page last updated: 2024-08-05 15:11:25
alpha-adrenergic agonist
An agent that selectively binds to and activates alpha-adrenergic receptors.
ChEBI ID: 35569
Members (22)
| Member | Definition | Class |
|---|---|---|
| alo 2145 | The hydrochloride salt of apraclonidine. | apraclonidine hydrochloride |
| apraclonidine | An imidazoline that is 2-amino 4,5-dihydro-1H-imidazoline in which one of the exocyclic amino hydrogens has been replaced by a 4-amino-2,6-dichlorophenyl group. | apraclonidine |
| brimonidine | brimonidine | |
| corbadrine | A catecholamine in which the 2-aminoethyl group is substituted with a hydroxy group at C-1 and a methyl group at C-2, with configurations 1R,2S. A metabolite of alpha-methyl-L-dopa, it is an alpha2-adrenergic agonist and acts as a topical nasal decongestant and vasoconstrictor, most often used in dentistry. | (-)-alpha-Methylnoradrenaline; alpha-methylnoradrenaline |
| dabuzalgron | A sulfonamide that is N-phenylmethanesulfonamide which carries a chloro group at position 2, 4,5-dihydro-1H-imidazol-2-ylmethoxy group at position 5, and a methyl group at position 6. Its is a selective alpha-adrenoceptor agonist that is used in the treatment of urinary incontinence. | dabuzalgron |
| dexmedetomidine | dexmedetomidine | |
| dibromophakellin | An alkaloid isolated from the marine sponge Phakellia flabellata and Acanthella costata. It acts as an alpha2B adrenoceptor agonist. | (-)-dibromophakellin |
| ergotamine | A peptide ergot alkaloid that is dihydroergotamine in which a double bond replaces the single bond between positions 9 and 10. | ergotamine |
| fenoldopam | fenoldopam | |
| lofexidine | lofexidine | |
| metaraminol | A 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 |
| methoxamine | An amphetamine in which the parent 1-phenylpropan-2-amine skeleton is substituted at position 1 with an hydroxy group and the phenyl ring is 2- and 5-substituted with methoxy groups. It is an antihypotensive agent (pressor), an agonist acting directly at alpha-adrenoceptors with selectivity for the alpha-1 adrenoceptor subtype similar to phenylephrine . | methoxamine |
| methyldopa | A derivative of L-tyrosine having a methyl group at the alpha-position and an additional hydroxy group at the 3-position on the phenyl ring. | alpha-methyl-L-dopa |
| midodrine | An 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 hydrochloride | A 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 |
| oxymetazoline | A 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 hydrochloride | A 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 |
| phenylephrine | A 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 |
| st 1059 | An 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 |
| synephrine | A phenethylamine alkaloid that is 4-(2-aminoethyl)phenol substituted by a hydroxy group at position 1 and a methyl group at the amino nitrogen. | synephrine |
| tizanidine | 2,1,3-Benzothiadiazole substituted at C-4 by a Delta(1)-imidazolin-2-ylamino group and at C-4 by a chloro group. It is an agonist at alpha2-adrenergic receptor sites. | tizanidine |
| xylazine | A methyl benzene that is 1,3-dimethylbenzene which is substituted by a 5,6-dihydro-4H-1,3-thiazin-2-ylnitrilo group at position 2. It is an alpha2 adrenergic receptor agonist and frequently used in veterinary medicine as an emetic and sedative with analgesic and muscle relaxant properties. | xylazine |
Research
Studies (30,799)
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 11,842 (38.45) | 18.7374 |
| 1990's | 5,599 (18.18) | 18.2507 |
| 2000's | 5,050 (16.40) | 29.6817 |
| 2010's | 5,754 (18.68) | 24.3611 |
| 2020's | 2,554 (8.29) | 2.80 |
Study Types
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 3,925 (11.61%) | 5.53% |
| Reviews | 1,791 (5.30%) | 6.00% |
| Case Studies | 1,895 (5.61%) | 4.05% |
| Observational | 159 (0.47%) | 0.25% |
| Other | 26,031 (77.01%) | 84.16% |
Protein Targets (217)
Potency Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1 | Homo sapiens (human) | Potency | 26.6602 | 1 | 3 |
| 15-lipoxygenase, partial | Homo sapiens (human) | Potency | 6.7567 | 1 | 3 |
| 2,3-bisphosphoglycerate-independent phosphoglycerate mutase | Leishmania major strain Friedlin | Potency | 37.9330 | 1 | 1 |
| acetylcholinesterase | Homo sapiens (human) | Potency | 34.1886 | 2 | 7 |
| activating transcription factor 6 | Homo sapiens (human) | Potency | 34.1979 | 1 | 2 |
| aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 16.8059 | 1 | 5 |
| apical membrane antigen 1, AMA1 | Plasmodium falciparum 3D7 | Potency | 11.2202 | 1 | 1 |
| AR protein | Homo sapiens (human) | Potency | 26.6032 | 4 | 4 |
| aryl hydrocarbon receptor | Homo sapiens (human) | Potency | 68.4501 | 2 | 2 |
| arylsulfatase A | Homo sapiens (human) | Potency | 13.1922 | 1 | 8 |
| ATAD5 protein, partial | Homo sapiens (human) | Potency | 6.0542 | 3 | 3 |
| Ataxin-2 | Homo sapiens (human) | Potency | 17.4882 | 1 | 2 |
| ATP-dependent phosphofructokinase | Trypanosoma brucei brucei TREU927 | Potency | 10.5634 | 4 | 8 |
| atrial natriuretic peptide receptor 1 precursor | Homo sapiens (human) | Potency | 37.9330 | 1 | 1 |
| Bloom syndrome protein isoform 1 | Homo sapiens (human) | Potency | 16.7062 | 2 | 11 |
| bromodomain adjacent to zinc finger domain 2B | Homo sapiens (human) | Potency | 57.9244 | 1 | 2 |
| cellular tumor antigen p53 isoform a | Homo sapiens (human) | Potency | 25.1189 | 1 | 1 |
| Chain A, 2-oxoglutarate Oxygenase | Homo sapiens (human) | Potency | 12.1527 | 1 | 6 |
| Chain A, ATP-DEPENDENT DNA HELICASE Q1 | Homo sapiens (human) | Potency | 12.6803 | 2 | 6 |
| Chain A, Beta-lactamase | Escherichia coli K-12 | Potency | 29.2520 | 2 | 5 |
| Chain A, Ferritin light chain | Equus caballus (horse) | Potency | 42.2395 | 2 | 2 |
| Chain A, HADH2 protein | Homo sapiens (human) | Potency | 5.1277 | 2 | 6 |
| Chain A, JmjC domain-containing histone demethylation protein 3A | Homo sapiens (human) | Potency | 19.9526 | 1 | 1 |
| Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE | Homo sapiens (human) | Potency | 3.5741 | 2 | 9 |
| Chain A, Putative fructose-1,6-bisphosphate aldolase | Giardia intestinalis | Potency | 13.1705 | 1 | 6 |
| Chain A, TYROSYL-DNA PHOSPHODIESTERASE | Homo sapiens (human) | Potency | 21.2643 | 1 | 6 |
| Chain B, HADH2 protein | Homo sapiens (human) | Potency | 5.1277 | 2 | 6 |
| chaperonin GroEL | Methanococcus maripaludis S2 | Potency | 100.0000 | 1 | 1 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 31.7730 | 2 | 6 |
| cytochrome P450 2C19 precursor | Homo sapiens (human) | Potency | 5.6608 | 1 | 2 |
| cytochrome P450 2C9 precursor | Homo sapiens (human) | Potency | 0.1995 | 1 | 1 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 27.5404 | 1 | 1 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 10.9875 | 1 | 7 |
| cytochrome P450 2D6 isoform 1 | Homo sapiens (human) | Potency | 16.9744 | 1 | 7 |
| cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 10.4617 | 2 | 14 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 8.3903 | 1 | 3 |
| D(1A) dopamine receptor | Homo sapiens (human) | Potency | 1.4382 | 3 | 4 |
| D(1A) dopamine receptor | Sus scrofa (pig) | Potency | 23.2809 | 1 | 1 |
| DNA polymerase beta | Homo sapiens (human) | Potency | 1.2673 | 1 | 2 |
| DNA polymerase eta isoform 1 | Homo sapiens (human) | Potency | 15.6730 | 1 | 2 |
| DNA polymerase III, partial | Bacillus subtilis | Potency | 26.6795 | 1 | 1 |
| DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 14.5133 | 1 | 4 |
| DNA polymerase kappa isoform 1 | Homo sapiens (human) | Potency | 5.6939 | 1 | 5 |
| dopamine D1 receptor | Homo sapiens (human) | Potency | 3.3478 | 1 | 3 |
| endonuclease IV | Escherichia coli | Potency | 12.8361 | 2 | 4 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 14.2956 | 3 | 6 |
| estrogen receptor 2 (ER beta) | Homo sapiens (human) | Potency | 19.7236 | 2 | 2 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 12.3153 | 4 | 8 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 15.3235 | 1 | 15 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 17.1620 | 4 | 8 |
| farnesoid X nuclear receptor | Homo sapiens (human) | Potency | 61.5619 | 1 | 1 |
| flap endonuclease 1 | Homo sapiens (human) | Potency | 23.8441 | 3 | 7 |
| G | Vesicular stomatitis virus | Potency | 27.5404 | 1 | 1 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 10.4617 | 1 | 7 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 10.4617 | 1 | 7 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 10.4617 | 1 | 7 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 10.4617 | 1 | 7 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 10.4617 | 1 | 7 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 10.4617 | 1 | 7 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 10.4617 | 1 | 7 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 10.4617 | 1 | 7 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 10.4617 | 1 | 7 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 10.4617 | 1 | 7 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 10.4617 | 1 | 7 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 10.4617 | 1 | 7 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 10.4617 | 1 | 7 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 10.4617 | 1 | 7 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 10.4617 | 1 | 7 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 10.4617 | 1 | 7 |
| geminin | Homo sapiens (human) | Potency | 2.8579 | 2 | 3 |
| GLI family zinc finger 3 | Homo sapiens (human) | Potency | 23.3314 | 2 | 7 |
| glp-1 receptor, partial | Homo sapiens (human) | Potency | 7.8570 | 3 | 5 |
| GLS protein | Homo sapiens (human) | Potency | 10.4503 | 2 | 10 |
| glucocerebrosidase | Homo sapiens (human) | Potency | 17.7584 | 1 | 2 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 5.6279 | 1 | 3 |
| heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa) | Homo sapiens (human) | Potency | 20.4054 | 1 | 2 |
| heat shock protein beta-1 | Homo sapiens (human) | Potency | 33.4889 | 1 | 1 |
| Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 8.1007 | 2 | 5 |
| histone acetyltransferase KAT2A isoform 1 | Homo sapiens (human) | Potency | 9.4594 | 1 | 3 |
| Histone H2A.x | Cricetulus griseus (Chinese hamster) | Potency | 61.0782 | 2 | 4 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 27.5404 | 1 | 1 |
| hypothetical protein, conserved | Trypanosoma brucei | Potency | 17.9232 | 2 | 2 |
| hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor) | Homo sapiens (human) | Potency | 1.3049 | 2 | 6 |
| importin subunit beta-1 isoform 1 | Homo sapiens (human) | Potency | 112.2020 | 1 | 1 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 27.5404 | 1 | 2 |
| Inositol monophosphatase 1 | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1 | 1 |
| Interferon beta | Homo sapiens (human) | Potency | 21.2062 | 2 | 2 |
| interleukin 8 | Homo sapiens (human) | Potency | 42.1632 | 1 | 1 |
| lamin isoform A-delta10 | Homo sapiens (human) | Potency | 11.8086 | 1 | 7 |
| lethal factor (plasmid) | Bacillus anthracis str. A2012 | Potency | 22.1060 | 1 | 2 |
| lysosomal alpha-glucosidase preproprotein | Homo sapiens (human) | Potency | 3.5481 | 1 | 1 |
| M-phase phosphoprotein 8 | Homo sapiens (human) | Potency | 23.2786 | 1 | 2 |
| Microtubule-associated protein tau | Homo sapiens (human) | Potency | 19.8019 | 2 | 9 |
| mitogen-activated protein kinase 1 | Homo sapiens (human) | Potency | 39.8107 | 1 | 1 |
| muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | Potency | 12.4174 | 2 | 6 |
| muscleblind-like protein 1 isoform 1 | Homo sapiens (human) | Potency | 43.4820 | 1 | 4 |
| neuropeptide S receptor isoform A | Homo sapiens (human) | Potency | 3.9811 | 1 | 1 |
| NFKB1 protein, partial | Homo sapiens (human) | Potency | 15.2858 | 2 | 6 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 42.0223 | 1 | 4 |
| nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_a | Homo sapiens (human) | Potency | 0.1549 | 1 | 1 |
| Nuclear receptor ROR-gamma | Homo sapiens (human) | Potency | 2.6603 | 1 | 1 |
| nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 29.1110 | 2 | 4 |
| peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 | Homo sapiens (human) | Potency | 50.1187 | 1 | 1 |
| peripheral myelin protein 22 | Rattus norvegicus (Norway rat) | Potency | 17.2648 | 1 | 3 |
| peripheral myelin protein 22 isoform 1 | Homo sapiens (human) | Potency | 80.3039 | 1 | 2 |
| peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 28.1931 | 2 | 3 |
| peroxisome proliferator-activated receptor delta | Homo sapiens (human) | Potency | 1.0947 | 1 | 1 |
| phosphoglycerate kinase | Trypanosoma brucei brucei TREU927 | Potency | 2.1331 | 1 | 1 |
| phosphopantetheinyl transferase | Bacillus subtilis | Potency | 42.1101 | 3 | 8 |
| Polyunsaturated fatty acid lipoxygenase ALOX15B | Homo sapiens (human) | Potency | 19.9526 | 1 | 1 |
| potassium voltage-gated channel subfamily H member 2 isoform d | Homo sapiens (human) | Potency | 10.5965 | 1 | 5 |
| pregnane X nuclear receptor | Homo sapiens (human) | Potency | 37.5311 | 1 | 2 |
| progesterone receptor | Homo sapiens (human) | Potency | 33.4915 | 1 | 1 |
| pyruvate kinase | Leishmania mexicana mexicana | Potency | 1.7415 | 2 | 5 |
| Rap guanine nucleotide exchange factor 3 | Homo sapiens (human) | Potency | 10.0000 | 1 | 1 |
| RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 15.6236 | 1 | 3 |
| ras-related protein Rab-9A | Homo sapiens (human) | Potency | 33.1763 | 1 | 3 |
| regulator of G-protein signaling 4 | Homo sapiens (human) | Potency | 17.5416 | 1 | 6 |
| retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 15.5675 | 3 | 6 |
| serine/threonine-protein kinase mTOR isoform 1 | Homo sapiens (human) | Potency | 23.0014 | 4 | 4 |
| SMAD family member 2 | Homo sapiens (human) | Potency | 3.6722 | 2 | 3 |
| SMAD family member 3 | Homo sapiens (human) | Potency | 3.6722 | 2 | 3 |
| Smad3 | Homo sapiens (human) | Potency | 2.4906 | 1 | 2 |
| snurportin-1 | Homo sapiens (human) | Potency | 112.2020 | 1 | 1 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 14.5891 | 1 | 3 |
| survival motor neuron protein isoform d | Homo sapiens (human) | Potency | 0.7079 | 1 | 1 |
| TDP1 protein | Homo sapiens (human) | Potency | 24.6200 | 2 | 13 |
| thioredoxin glutathione reductase | Schistosoma mansoni | Potency | 22.3872 | 1 | 1 |
| thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 16.0545 | 4 | 19 |
| Thrombopoietin | Homo sapiens (human) | Potency | 11.2947 | 2 | 4 |
| thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 27.3914 | 2 | 2 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 27.4220 | 5 | 13 |
| transcriptional regulator ERG isoform 3 | Homo sapiens (human) | Potency | 7.0795 | 1 | 1 |
| transient receptor potential cation channel subfamily V member 1 | Homo sapiens (human) | Potency | 31.6228 | 1 | 1 |
| ubiquitin carboxyl-terminal hydrolase 2 isoform a | Homo sapiens (human) | Potency | 22.3872 | 1 | 1 |
| v-jun sarcoma virus 17 oncogene homolog (avian) | Homo sapiens (human) | Potency | 26.8325 | 1 | 1 |
| vitamin D (1,25- dihydroxyvitamin D3) receptor | Homo sapiens (human) | Potency | 7.7394 | 1 | 2 |
| vitamin D3 receptor isoform VDRA | Homo sapiens (human) | Potency | 37.7887 | 1 | 4 |
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 1A | Rattus norvegicus (Norway rat) | IC50 | 0.8525 | 1 | 3 |
| 5-hydroxytryptamine receptor 1A | Homo sapiens (human) | Ki | 0.1259 | 1 | 1 |
| 5-hydroxytryptamine receptor 1A | Rattus norvegicus (Norway rat) | Ki | 0.4872 | 1 | 3 |
| 5-hydroxytryptamine receptor 1B | Rattus norvegicus (Norway rat) | IC50 | 0.8525 | 1 | 3 |
| 5-hydroxytryptamine receptor 1B | Homo sapiens (human) | Ki | 0.0021 | 3 | 4 |
| 5-hydroxytryptamine receptor 1B | Rattus norvegicus (Norway rat) | Ki | 0.4872 | 1 | 3 |
| 5-hydroxytryptamine receptor 1D | Homo sapiens (human) | Ki | 0.0027 | 5 | 6 |
| 5-hydroxytryptamine receptor 2A | Homo sapiens (human) | IC50 | 0.6457 | 1 | 2 |
| 5-hydroxytryptamine receptor 2A | Homo sapiens (human) | Ki | 0.1844 | 1 | 2 |
| 5-hydroxytryptamine receptor 2B | Homo sapiens (human) | IC50 | 1.5297 | 1 | 2 |
| 5-hydroxytryptamine receptor 2B | Homo sapiens (human) | Ki | 0.9736 | 1 | 2 |
| 5-hydroxytryptamine receptor 2C | Homo sapiens (human) | IC50 | 0.3170 | 1 | 2 |
| 5-hydroxytryptamine receptor 2C | Homo sapiens (human) | Ki | 0.1660 | 1 | 2 |
| 5-hydroxytryptamine receptor 4 | Cavia porcellus (domestic guinea pig) | IC50 | 0.3170 | 1 | 2 |
| 5-hydroxytryptamine receptor 4 | Cavia porcellus (domestic guinea pig) | Ki | 0.1660 | 1 | 2 |
| 5-hydroxytryptamine receptor 5A | Homo sapiens (human) | Ki | 0.0215 | 4 | 5 |
| 5-hydroxytryptamine receptor 6 | Homo sapiens (human) | IC50 | 0.8360 | 1 | 2 |
| 5-hydroxytryptamine receptor 6 | Homo sapiens (human) | Ki | 0.3880 | 1 | 2 |
| Adenylate cyclase | Arthrospira platensis | IC50 | 70.0000 | 1 | 1 |
| Alpha-1A adrenergic receptor | Bos taurus (cattle) | Ki | 0.4732 | 1 | 2 |
| Alpha-1A adrenergic receptor | Homo sapiens (human) | Ki | 0.1462 | 4 | 5 |
| Alpha-1A adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 1.6667 | 6 | 8 |
| Alpha-1B adrenergic receptor | Homo sapiens (human) | Ki | 0.5034 | 4 | 5 |
| Alpha-1B adrenergic receptor | Mesocricetus auratus (golden hamster) | Ki | 3.8204 | 3 | 4 |
| Alpha-1B adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 2.2817 | 3 | 3 |
| Alpha-1D adrenergic receptor | Homo sapiens (human) | IC50 | 1.5377 | 1 | 3 |
| Alpha-1D adrenergic receptor | Homo sapiens (human) | Ki | 0.5484 | 5 | 7 |
| Alpha-1D adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 1.5283 | 6 | 7 |
| Alpha-2A adrenergic receptor | Homo sapiens (human) | IC50 | 0.0660 | 2 | 5 |
| Alpha-2A adrenergic receptor | Bos taurus (cattle) | Ki | 0.0015 | 1 | 1 |
| Alpha-2A adrenergic receptor | Homo sapiens (human) | Ki | 0.1236 | 24 | 31 |
| Alpha-2A adrenergic receptor | Mus musculus (house mouse) | Ki | 0.0913 | 3 | 3 |
| Alpha-2A adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 0.4365 | 20 | 25 |
| Alpha-2A adrenergic receptor | Sus scrofa (pig) | Ki | 0.0210 | 1 | 1 |
| Alpha-2B adrenergic receptor | Homo sapiens (human) | IC50 | 0.4662 | 2 | 5 |
| Alpha-2B adrenergic receptor | Homo sapiens (human) | Ki | 0.3493 | 19 | 25 |
| Alpha-2B adrenergic receptor | Mus musculus (house mouse) | Ki | 0.0913 | 3 | 3 |
| Alpha-2B adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 0.4975 | 21 | 26 |
| Alpha-2C adrenergic receptor | Homo sapiens (human) | IC50 | 0.6630 | 2 | 4 |
| Alpha-2C adrenergic receptor | Homo sapiens (human) | Ki | 0.0985 | 23 | 29 |
| Alpha-2C adrenergic receptor | Mus musculus (house mouse) | Ki | 0.0913 | 3 | 3 |
| Alpha-2C adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 0.4958 | 17 | 22 |
| ATP-binding cassette sub-family C member 3 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 1 |
| ATP-dependent translocase ABCB1 | Homo sapiens (human) | Ki | 56.5750 | 2 | 2 |
| ATP-dependent translocase ABCB1 | Mus musculus (house mouse) | Ki | 103.4000 | 2 | 2 |
| Beta-1 adrenergic receptor | Homo sapiens (human) | IC50 | 4.1420 | 1 | 1 |
| Beta-1 adrenergic receptor | Homo sapiens (human) | Ki | 2.3920 | 1 | 1 |
| Beta-1 adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 13.0000 | 1 | 1 |
| Beta-2 adrenergic receptor | Homo sapiens (human) | IC50 | 2.7610 | 1 | 1 |
| Beta-2 adrenergic receptor | Homo sapiens (human) | Ki | 1.8980 | 1 | 1 |
| Bile salt export pump | Homo sapiens (human) | IC50 | 807.5556 | 4 | 9 |
| Bile salt export pump | Rattus norvegicus (Norway rat) | IC50 | 1,000.0000 | 1 | 1 |
| Canalicular multispecific organic anion transporter 1 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 1 |
| Cystathionine gamma-lyase | Homo sapiens (human) | IC50 | 3,000.0000 | 1 | 1 |
| Cytochrome P450 2D6 | Homo sapiens (human) | IC50 | 0.2000 | 1 | 1 |
| Cytochrome P450 3A4 | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
| D | Rattus norvegicus (Norway rat) | Ki | 0.0030 | 1 | 1 |
| D(1A) dopamine receptor | Homo sapiens (human) | IC50 | 1.7280 | 1 | 1 |
| D(1A) dopamine receptor | Homo sapiens (human) | Ki | 0.3147 | 2 | 3 |
| D(2) dopamine receptor | Bos taurus (cattle) | IC50 | 1.5800 | 1 | 2 |
| D(2) dopamine receptor | Homo sapiens (human) | IC50 | 0.0043 | 1 | 1 |
| D(2) dopamine receptor | Bos taurus (cattle) | Ki | 0.7900 | 1 | 1 |
| D(2) dopamine receptor | Homo sapiens (human) | Ki | 0.4057 | 2 | 2 |
| D(3) dopamine receptor | Homo sapiens (human) | IC50 | 0.0043 | 1 | 1 |
| D(3) dopamine receptor | Homo sapiens (human) | Ki | 0.0015 | 1 | 1 |
| Epidermal growth factor receptor | Homo sapiens (human) | IC50 | 5.2280 | 1 | 1 |
| estrogen receptor beta isoform 1 | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| Lysine-specific demethylase 4E | Homo sapiens (human) | Ki | 1.9200 | 1 | 1 |
| Macrophage migration inhibitory factor | Homo sapiens (human) | IC50 | 98.1000 | 1 | 1 |
| Macrophage migration inhibitory factor | Homo sapiens (human) | Ki | 77.1000 | 1 | 1 |
| MPI protein | Homo sapiens (human) | IC50 | 50.0000 | 1 | 2 |
| Multidrug resistance-associated protein 4 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 1 |
| Muscarinic acetylcholine receptor M4 | Homo sapiens (human) | IC50 | 3.2610 | 1 | 1 |
| Muscarinic acetylcholine receptor M4 | Homo sapiens (human) | Ki | 0.4550 | 1 | 1 |
| Muscarinic acetylcholine receptor M5 | Homo sapiens (human) | IC50 | 1.3320 | 1 | 1 |
| Muscarinic acetylcholine receptor M5 | Homo sapiens (human) | Ki | 0.9570 | 1 | 1 |
| Nischarin | Homo sapiens (human) | Ki | 0.0173 | 1 | 4 |
| Nischarin | Rattus norvegicus (Norway rat) | Ki | 0.0056 | 1 | 1 |
| Polyunsaturated fatty acid lipoxygenase ALOX15 | Oryctolagus cuniculus (rabbit) | IC50 | 2.1260 | 1 | 1 |
| Sodium-dependent dopamine transporter | Rattus norvegicus (Norway rat) | Ki | 0.0400 | 1 | 1 |
| Solute carrier family 15 member 1 | Homo sapiens (human) | IC50 | 151,600.0000 | 1 | 1 |
| Thromboxane-A synthase | Homo sapiens (human) | IC50 | 3.0640 | 1 | 1 |
| Tyrosine-protein kinase Fyn | Homo sapiens (human) | IC50 | 4.1680 | 1 | 2 |
| Tyrosine-protein kinase Lck | Homo sapiens (human) | IC50 | 6.4990 | 1 | 1 |
Activation Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 1A | Homo sapiens (human) | EC50 | 0.0700 | 1 | 1 |
| 5-hydroxytryptamine receptor 1A | Rattus norvegicus (Norway rat) | EC50 | 12.5694 | 2 | 2 |
| 5-hydroxytryptamine receptor 1B | Rattus norvegicus (Norway rat) | EC50 | 0.0200 | 1 | 1 |
| 5-hydroxytryptamine receptor 1D | Rattus norvegicus (Norway rat) | EC50 | 0.0200 | 1 | 1 |
| 5-hydroxytryptamine receptor 1F | Rattus norvegicus (Norway rat) | EC50 | 0.0200 | 1 | 1 |
| Adenosine receptor A2a | Rattus norvegicus (Norway rat) | EC50 | 0.0019 | 1 | 1 |
| Adenosine receptor A2b | Rattus norvegicus (Norway rat) | EC50 | 0.0019 | 1 | 1 |
| Alpha-1A adrenergic receptor | Bos taurus (cattle) | EC50 | 0.4452 | 1 | 4 |
| Alpha-1A adrenergic receptor | Homo sapiens (human) | EC50 | 0.7836 | 8 | 10 |
| Alpha-1A adrenergic receptor | Rattus norvegicus (Norway rat) | EC50 | 0.7760 | 1 | 1 |
| Alpha-1B adrenergic receptor | Homo sapiens (human) | EC50 | 5.0766 | 7 | 9 |
| Alpha-1B adrenergic receptor | Rattus norvegicus (Norway rat) | EC50 | 0.7760 | 1 | 1 |
| Alpha-1B adrenergic receptor | Cricetulus griseus (Chinese hamster) | EC50 | 0.4098 | 1 | 4 |
| Alpha-1D adrenergic receptor | Homo sapiens (human) | EC50 | 6.5261 | 5 | 7 |
| Alpha-1D adrenergic receptor | Rattus norvegicus (Norway rat) | EC50 | 0.7760 | 1 | 1 |
| Alpha-2A adrenergic receptor | Homo sapiens (human) | EC50 | 2.5548 | 10 | 13 |
| Alpha-2A adrenergic receptor | Rattus norvegicus (Norway rat) | EC50 | 25.1189 | 1 | 1 |
| Alpha-2B adrenergic receptor | Homo sapiens (human) | EC50 | 5.4256 | 5 | 5 |
| Alpha-2B adrenergic receptor | Rattus norvegicus (Norway rat) | EC50 | 12.5870 | 2 | 2 |
| Alpha-2C adrenergic receptor | Homo sapiens (human) | EC50 | 2.7096 | 6 | 9 |
| Alpha-2C adrenergic receptor | Rattus norvegicus (Norway rat) | EC50 | 25.1189 | 1 | 1 |
| alternatively spliced Trp4 | Mus musculus (house mouse) | EC50 | 3.3500 | 1 | 1 |
| Beta-1 adrenergic receptor | Homo sapiens (human) | EC50 | 6.0000 | 1 | 1 |
| Beta-2 adrenergic receptor | Homo sapiens (human) | EC50 | 6.0000 | 1 | 1 |
| Beta-3 adrenergic receptor | Homo sapiens (human) | EC50 | 6.0000 | 1 | 1 |
| D | Rattus norvegicus (Norway rat) | EC50 | 0.0570 | 1 | 1 |
| D(1A) dopamine receptor | Homo sapiens (human) | EC50 | 0.0172 | 2 | 2 |
| D(1A) dopamine receptor | Homo sapiens (human) | Kd | 0.0280 | 1 | 1 |
| D(2) dopamine receptor | Rattus norvegicus (Norway rat) | Kd | 4.0400 | 4 | 5 |
| G protein-activated inward rectifier potassium channel 1 | Rattus norvegicus (Norway rat) | EC50 | 0.0820 | 1 | 1 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | EC50 | 0.0700 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | EC50 | 0.0700 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | EC50 | 0.0700 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | EC50 | 0.0700 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | EC50 | 0.0700 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | EC50 | 0.0700 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | EC50 | 0.0700 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | EC50 | 0.0700 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | EC50 | 0.0700 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | EC50 | 0.0700 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | EC50 | 0.0700 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | EC50 | 0.0700 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | EC50 | 0.0700 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | EC50 | 0.0700 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | EC50 | 0.0700 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | EC50 | 0.0700 | 1 | 2 |
| Neuromedin-U receptor 2 | Homo sapiens (human) | EC50 | 6.6000 | 1 | 1 |
Other Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Alpha-1A adrenergic receptor | Homo sapiens (human) | Kb | 0.0110 | 1 | 2 |
| Alpha-1B adrenergic receptor | Homo sapiens (human) | Kb | 0.0110 | 1 | 2 |
| Alpha-1D adrenergic receptor | Homo sapiens (human) | Kb | 0.0110 | 1 | 2 |
| Alpha-2A adrenergic receptor | Mus musculus (house mouse) | IC40 | 0.0780 | 1 | 1 |
| Alpha-2B adrenergic receptor | Mus musculus (house mouse) | IC40 | 0.0780 | 1 | 1 |
| Alpha-2C adrenergic receptor | Mus musculus (house mouse) | IC40 | 0.0780 | 1 | 1 |
| Caspase 6, apoptosis-related cysteine peptidase | Homo sapiens (human) | AC50 | 39.2300 | 1 | 1 |
| D | Rattus norvegicus (Norway rat) | KL | 0.0210 | 1 | 1 |
| D(2) dopamine receptor | Rattus norvegicus (Norway rat) | KL | 1.0000 | 1 | 1 |
| POU domain, class 2, transcription factor 1 | Homo sapiens (human) | Km | 221.2000 | 1 | 1 |