Page last updated: 2024-08-05 15:22:43
G-protein-coupled receptor agonist
An agonist that binds to and activates G-protein-coupled receptors
ChEBI ID: 70998
Members (4)
| Member | Definition | Class |
|---|---|---|
| 3-methoxycatechol | A member of the class of catechols that is catechol in which a hydrogen that is ortho to one of the hydroxy groups has been replaced by a methoxy group. It displays agonistic activity against G protein-coupled receptor 35 (GPR35). | 3-methoxycatechol |
| diphenyleneiodium chloride | An organic chloride salt having dibenziodolium as the counterion. | dibenziodolium chloride |
| kynurenic acid | A quinolinemonocarboxylic acid that is quinoline-2-carboxylic acid substituted by a hydroxy group at C-4. | kynurenic acid |
| medica 16 | An alpha,omega-dicarboxylic acid that is hexadecanedioic acid carrying methyl groups at positions 3 and 14. It is a free fatty acid 1 (FFA1/GPR40) receptor agonist and an ATP citrate lyase inhibitor, and exhibits hypolipidemic and antidiabetogenic properties. | MEDICA 16 |
Research
Studies (2,584)
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 455 (17.61) | 18.7374 |
| 1990's | 792 (30.65) | 18.2507 |
| 2000's | 535 (20.70) | 29.6817 |
| 2010's | 555 (21.48) | 24.3611 |
| 2020's | 247 (9.56) | 2.80 |
Study Types
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 28 (1.05%) | 5.53% |
| Reviews | 121 (4.54%) | 6.00% |
| Case Studies | 4 (0.15%) | 4.05% |
| Observational | 4 (0.15%) | 0.25% |
| Other | 2,511 (94.12%) | 84.16% |
Protein Targets (135)
Potency Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1 | Homo sapiens (human) | Potency | 17.2168 | 1 | 3 |
| 15-lipoxygenase, partial | Homo sapiens (human) | Potency | 0.7943 | 1 | 1 |
| 67.9K protein | Vaccinia virus | Potency | 11.2698 | 2 | 3 |
| activating transcription factor 6 | Homo sapiens (human) | Potency | 57.1125 | 1 | 1 |
| aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 13.9473 | 2 | 3 |
| alpha-galactosidase | Homo sapiens (human) | Potency | 8.9125 | 1 | 1 |
| AR protein | Homo sapiens (human) | Potency | 30.9091 | 5 | 5 |
| aryl hydrocarbon receptor | Homo sapiens (human) | Potency | 35.9458 | 2 | 2 |
| Ataxin-2 | Homo sapiens (human) | Potency | 56.5948 | 1 | 1 |
| ATP-dependent phosphofructokinase | Trypanosoma brucei brucei TREU927 | Potency | 0.7569 | 1 | 1 |
| ATPase family AAA domain-containing protein 5 | Homo sapiens (human) | Potency | 57.7018 | 2 | 2 |
| Bloom syndrome protein isoform 1 | Homo sapiens (human) | Potency | 15.8489 | 1 | 1 |
| bromodomain adjacent to zinc finger domain 2B | Homo sapiens (human) | Potency | 89.1251 | 1 | 1 |
| cellular tumor antigen p53 isoform a | Homo sapiens (human) | Potency | 5.6608 | 2 | 2 |
| Chain A, 2-oxoglutarate Oxygenase | Homo sapiens (human) | Potency | 21.0494 | 1 | 4 |
| Chain A, HADH2 protein | Homo sapiens (human) | Potency | 21.1490 | 2 | 4 |
| Chain A, JmjC domain-containing histone demethylation protein 3A | Homo sapiens (human) | Potency | 89.1251 | 1 | 1 |
| Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE | Homo sapiens (human) | Potency | 22.4394 | 3 | 6 |
| Chain A, Putative fructose-1,6-bisphosphate aldolase | Giardia intestinalis | Potency | 17.7407 | 1 | 2 |
| Chain A, TYROSYL-DNA PHOSPHODIESTERASE | Homo sapiens (human) | Potency | 63.0957 | 1 | 1 |
| Chain B, HADH2 protein | Homo sapiens (human) | Potency | 21.1490 | 2 | 4 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 0.0474 | 1 | 1 |
| cytochrome P450 2C19 precursor | Homo sapiens (human) | Potency | 19.9526 | 1 | 1 |
| cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 19.9526 | 2 | 2 |
| cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a | Homo sapiens (human) | Potency | 35.7089 | 1 | 1 |
| DNA polymerase beta | Homo sapiens (human) | Potency | 28.1838 | 1 | 1 |
| DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 32.1220 | 1 | 2 |
| DNA polymerase kappa isoform 1 | Homo sapiens (human) | Potency | 13.6190 | 1 | 3 |
| endonuclease IV | Escherichia coli | Potency | 44.6684 | 1 | 1 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 31.1213 | 4 | 4 |
| estrogen receptor 2 (ER beta) | Homo sapiens (human) | Potency | 23.2677 | 3 | 3 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 26.0915 | 9 | 9 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 3.6675 | 1 | 3 |
| farnesoid X nuclear receptor | Homo sapiens (human) | Potency | 50.9016 | 1 | 1 |
| flap endonuclease 1 | Homo sapiens (human) | Potency | 50.1187 | 1 | 1 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 19.9526 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 19.9526 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 19.9526 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 19.9526 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 19.9526 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 19.9526 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 19.9526 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 19.9526 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 19.9526 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 19.9526 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 19.9526 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 19.9526 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 19.9526 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 19.9526 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 19.9526 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 19.9526 | 1 | 1 |
| geminin | Homo sapiens (human) | Potency | 2.4291 | 3 | 3 |
| GLI family zinc finger 3 | Homo sapiens (human) | Potency | 30.8038 | 3 | 3 |
| Glutamate receptor 1 | Rattus norvegicus (Norway rat) | Potency | 39.8107 | 1 | 1 |
| Glutamate receptor 2 | Rattus norvegicus (Norway rat) | Potency | 39.8107 | 1 | 1 |
| Glutamate receptor 3 | Rattus norvegicus (Norway rat) | Potency | 39.8107 | 1 | 1 |
| Glutamate receptor 4 | Rattus norvegicus (Norway rat) | Potency | 39.8107 | 1 | 1 |
| heat shock protein beta-1 | Homo sapiens (human) | Potency | 52.1267 | 2 | 2 |
| Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 1.2589 | 1 | 2 |
| histone acetyltransferase KAT2A isoform 1 | Homo sapiens (human) | Potency | 39.8107 | 1 | 1 |
| Histone H2A.x | Cricetulus griseus (Chinese hamster) | Potency | 95.5763 | 2 | 2 |
| histone-lysine N-methyltransferase 2A isoform 2 precursor | Homo sapiens (human) | Potency | 50.1187 | 1 | 1 |
| Inositol monophosphatase 1 | Rattus norvegicus (Norway rat) | Potency | 10.0000 | 1 | 1 |
| Integrin alpha-IIb | Homo sapiens (human) | Potency | 5.0119 | 1 | 1 |
| Integrin beta-3 | Homo sapiens (human) | Potency | 5.0119 | 1 | 1 |
| lamin isoform A-delta10 | Homo sapiens (human) | Potency | 5.2884 | 2 | 3 |
| lethal factor (plasmid) | Bacillus anthracis str. A2012 | Potency | 12.5893 | 1 | 1 |
| lysosomal alpha-glucosidase preproprotein | Homo sapiens (human) | Potency | 0.2512 | 1 | 1 |
| Microtubule-associated protein tau | Homo sapiens (human) | Potency | 19.6222 | 2 | 2 |
| mitogen-activated protein kinase 1 | Homo sapiens (human) | Potency | 24.7028 | 2 | 2 |
| muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | Potency | 0.0178 | 1 | 1 |
| nonstructural protein 1 | Influenza A virus (A/WSN/1933(H1N1)) | Potency | 6.3096 | 1 | 1 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 3.0453 | 2 | 2 |
| nuclear factor erythroid 2-related factor 2 isoform 2 | Homo sapiens (human) | Potency | 0.2060 | 1 | 1 |
| nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 23.3507 | 2 | 2 |
| nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 63.9218 | 2 | 2 |
| Parkin | Homo sapiens (human) | Potency | 1.8356 | 1 | 1 |
| peripheral myelin protein 22 isoform 1 | Homo sapiens (human) | Potency | 0.2133 | 1 | 1 |
| peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 20.8647 | 3 | 3 |
| phosphopantetheinyl transferase | Bacillus subtilis | Potency | 19.9526 | 1 | 1 |
| polyunsaturated fatty acid lipoxygenase ALOX12 | Homo sapiens (human) | Potency | 39.8107 | 1 | 1 |
| Polyunsaturated fatty acid lipoxygenase ALOX15B | Homo sapiens (human) | Potency | 1.2589 | 1 | 1 |
| potassium voltage-gated channel subfamily H member 2 isoform d | Homo sapiens (human) | Potency | 35.4813 | 1 | 1 |
| pregnane X nuclear receptor | Homo sapiens (human) | Potency | 25.2800 | 1 | 1 |
| RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 60.0476 | 2 | 2 |
| retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 65.4951 | 3 | 3 |
| retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 53.9177 | 1 | 1 |
| Smad3 | Homo sapiens (human) | Potency | 4.4668 | 1 | 1 |
| survival motor neuron protein isoform d | Homo sapiens (human) | Potency | 0.1122 | 1 | 1 |
| TDP1 protein | Homo sapiens (human) | Potency | 1.7074 | 2 | 5 |
| thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 22.9833 | 1 | 2 |
| thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 40.0145 | 2 | 2 |
| v-jun sarcoma virus 17 oncogene homolog (avian) | Homo sapiens (human) | Potency | 44.0972 | 2 | 2 |
| vitamin D3 receptor isoform VDRA | Homo sapiens (human) | Potency | 42.8000 | 1 | 2 |
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| ATP-citrate synthase | Rattus norvegicus (Norway rat) | Ki | 11.6667 | 3 | 3 |
| Dihydroorotate dehydrogenase | Plasmodium falciparum (malaria parasite P. falciparum) | IC50 | 10.0000 | 1 | 1 |
| Dihydroorotate dehydrogenase (fumarate) | Saccharomyces cerevisiae S288C | IC50 | 10.0000 | 1 | 1 |
| G-protein coupled receptor 35 | Homo sapiens (human) | IC50 | 39.0000 | 1 | 1 |
| G-protein coupled receptor 35 | Homo sapiens (human) | Ki | 137.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Homo sapiens (human) | IC50 | 2,900.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Homo sapiens (human) | IC50 | 2,900.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Homo sapiens (human) | IC50 | 2,900.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Homo sapiens (human) | IC50 | 2,900.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Homo sapiens (human) | IC50 | 2,900.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Homo sapiens (human) | IC50 | 2,900.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Homo sapiens (human) | IC50 | 2,900.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Homo sapiens (human) | IC50 | 2,900.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Homo sapiens (human) | IC50 | 2,900.0000 | 1 | 1 |
| Glutamate receptor 1 | Rattus norvegicus (Norway rat) | IC50 | 101.0000 | 1 | 1 |
| Glutamate receptor 2 | Rattus norvegicus (Norway rat) | IC50 | 101.0000 | 1 | 1 |
| Glutamate receptor 3 | Rattus norvegicus (Norway rat) | IC50 | 101.0000 | 1 | 1 |
| Glutamate receptor 4 | Rattus norvegicus (Norway rat) | IC50 | 101.0000 | 1 | 1 |
| Glutamate receptor ionotropic, kainate 1 | Rattus norvegicus (Norway rat) | IC50 | 1,000.0000 | 1 | 2 |
| Glutamate receptor ionotropic, kainate 2 | Rattus norvegicus (Norway rat) | IC50 | 1,000.0000 | 1 | 2 |
| Glutamate receptor ionotropic, kainate 3 | Rattus norvegicus (Norway rat) | IC50 | 1,000.0000 | 1 | 2 |
| Glutamate receptor ionotropic, kainate 4 | Rattus norvegicus (Norway rat) | IC50 | 1,000.0000 | 1 | 2 |
| Glutamate receptor ionotropic, kainate 5 | Rattus norvegicus (Norway rat) | IC50 | 1,000.0000 | 1 | 2 |
| Glutamate receptor ionotropic, NMDA 1 | Homo sapiens (human) | IC50 | 15.0000 | 1 | 1 |
| Glutamate receptor ionotropic, NMDA 1 | Rattus norvegicus (Norway rat) | IC50 | 98.0400 | 4 | 5 |
| Glutamate receptor ionotropic, NMDA 1 | Rattus norvegicus (Norway rat) | Ki | 5.4000 | 1 | 1 |
| Glutamate receptor ionotropic, NMDA 2A | Homo sapiens (human) | IC50 | 15.0000 | 1 | 1 |
| Glutamate receptor ionotropic, NMDA 2A | Rattus norvegicus (Norway rat) | IC50 | 112.5000 | 3 | 4 |
| Glutamate receptor ionotropic, NMDA 2B | Homo sapiens (human) | IC50 | 15.0000 | 1 | 1 |
| Glutamate receptor ionotropic, NMDA 2B | Rattus norvegicus (Norway rat) | IC50 | 112.5000 | 3 | 4 |
| Glutamate receptor ionotropic, NMDA 2C | Homo sapiens (human) | IC50 | 15.0000 | 1 | 1 |
| Glutamate receptor ionotropic, NMDA 2C | Rattus norvegicus (Norway rat) | IC50 | 112.5000 | 3 | 4 |
| Glutamate receptor ionotropic, NMDA 2D | Homo sapiens (human) | IC50 | 15.0000 | 1 | 1 |
| Glutamate receptor ionotropic, NMDA 2D | Rattus norvegicus (Norway rat) | IC50 | 112.5000 | 3 | 4 |
| Glutamate receptor ionotropic, NMDA 3A | Homo sapiens (human) | IC50 | 15.0000 | 1 | 1 |
| Glutamate receptor ionotropic, NMDA 3A | Rattus norvegicus (Norway rat) | IC50 | 112.5000 | 3 | 4 |
| Glutamate receptor ionotropic, NMDA 3B | Homo sapiens (human) | IC50 | 15.0000 | 1 | 1 |
| Glutamate receptor ionotropic, NMDA 3B | Rattus norvegicus (Norway rat) | IC50 | 112.5000 | 3 | 4 |
| Mitogen-activated protein kinase 11 | Homo sapiens (human) | Ki | 1,300.0000 | 1 | 1 |
| Mitogen-activated protein kinase 12 | Homo sapiens (human) | Ki | 1,300.0000 | 1 | 1 |
| Mitogen-activated protein kinase 13 | Homo sapiens (human) | Ki | 1,300.0000 | 1 | 1 |
| Mitogen-activated protein kinase 14 | Homo sapiens (human) | Ki | 1,300.0000 | 1 | 1 |
| Neuronal acetylcholine receptor subunit alpha-7 | Homo sapiens (human) | IC50 | 7.0000 | 1 | 1 |
| Vesicular glutamate transporter 3 | Rattus norvegicus (Norway rat) | Ki | 1,300.0000 | 1 | 1 |
Activation Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Aryl hydrocarbon receptor | Homo sapiens (human) | EC50 | 0.3000 | 1 | 1 |
| G protein-coupled receptor GPR35 | Rattus norvegicus (Norway rat) | EC50 | 66.0000 | 1 | 1 |
| G-protein coupled receptor 35 | Homo sapiens (human) | EC50 | 199.8000 | 9 | 9 |
| Histamine H3 receptor | Rattus norvegicus (Norway rat) | EC50 | 500.0000 | 1 | 1 |
Other Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Glutamate receptor 1 | Rattus norvegicus (Norway rat) | Kb | 137.0000 | 2 | 2 |
| Glutamate receptor 2 | Rattus norvegicus (Norway rat) | Kb | 137.0000 | 2 | 2 |
| Glutamate receptor 3 | Rattus norvegicus (Norway rat) | Kb | 137.0000 | 2 | 2 |
| Glutamate receptor 4 | Rattus norvegicus (Norway rat) | Kb | 137.0000 | 2 | 2 |
| Glutamate receptor ionotropic, kainate 1 | Rattus norvegicus (Norway rat) | Kb | 89.0000 | 1 | 1 |
| Glutamate receptor ionotropic, kainate 2 | Rattus norvegicus (Norway rat) | Kb | 89.0000 | 1 | 1 |
| Glutamate receptor ionotropic, kainate 3 | Rattus norvegicus (Norway rat) | Kb | 89.0000 | 1 | 1 |
| Glutamate receptor ionotropic, kainate 4 | Rattus norvegicus (Norway rat) | Kb | 89.0000 | 1 | 1 |
| Glutamate receptor ionotropic, kainate 5 | Rattus norvegicus (Norway rat) | Kb | 89.0000 | 1 | 1 |
| Glutamate receptor ionotropic, NMDA 1 | Rattus norvegicus (Norway rat) | Kb | 154.0000 | 3 | 3 |
| Glutamate receptor ionotropic, NMDA 2A | Rattus norvegicus (Norway rat) | Kb | 154.0000 | 3 | 3 |
| Glutamate receptor ionotropic, NMDA 2B | Rattus norvegicus (Norway rat) | Kb | 154.0000 | 3 | 3 |
| Glutamate receptor ionotropic, NMDA 2C | Rattus norvegicus (Norway rat) | Kb | 154.0000 | 3 | 3 |
| Glutamate receptor ionotropic, NMDA 2D | Rattus norvegicus (Norway rat) | Kb | 154.0000 | 3 | 3 |
| Glutamate receptor ionotropic, NMDA 3A | Rattus norvegicus (Norway rat) | Kb | 154.0000 | 3 | 3 |
| Glutamate receptor ionotropic, NMDA 3B | Rattus norvegicus (Norway rat) | Kb | 154.0000 | 3 | 3 |