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)

MemberDefinitionClass
3-methoxycatecholA member of the class of catechols that is catechol in which a hydrogen that is ortho to one of the hydroxy groups has been replaced by a methoxy group.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 chlorideAn organic chloride salt having dibenziodolium as the counterion.dibenziodolium chloride
kynurenic acidA quinolinemonocarboxylic acid that is quinoline-2-carboxylic acid substituted by a hydroxy group at C-4.kynurenic acid
medica 16An 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)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-1990455 (17.61)18.7374
1990's792 (30.65)18.2507
2000's535 (20.70)29.6817
2010's555 (21.48)24.3611
2020's247 (9.56)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials28 (1.05%)5.53%
Reviews121 (4.54%)6.00%
Case Studies4 (0.15%)4.05%
Observational4 (0.15%)0.25%
Other2,511 (94.12%)84.16%

Protein Targets (135)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency17.216813
15-lipoxygenase, partialHomo sapiens (human)Potency0.794311
67.9K proteinVaccinia virusPotency11.269823
activating transcription factor 6Homo sapiens (human)Potency57.112511
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency13.947323
alpha-galactosidaseHomo sapiens (human)Potency8.912511
AR proteinHomo sapiens (human)Potency30.909155
aryl hydrocarbon receptorHomo sapiens (human)Potency35.945822
Ataxin-2Homo sapiens (human)Potency56.594811
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency0.756911
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency57.701822
Bloom syndrome protein isoform 1Homo sapiens (human)Potency15.848911
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency89.125111
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency5.660822
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency21.049414
Chain A, HADH2 proteinHomo sapiens (human)Potency21.149024
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency89.125111
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency22.439436
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency17.740712
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency63.095711
Chain B, HADH2 proteinHomo sapiens (human)Potency21.149024
chromobox protein homolog 1Homo sapiens (human)Potency0.047411
cytochrome P450 2C19 precursorHomo sapiens (human)Potency19.952611
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency19.952622
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency35.708911
DNA polymerase betaHomo sapiens (human)Potency28.183811
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency32.122012
DNA polymerase kappa isoform 1Homo sapiens (human)Potency13.619013
endonuclease IVEscherichia coliPotency44.668411
estrogen nuclear receptor alphaHomo sapiens (human)Potency31.121344
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency23.267733
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency26.091599
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency3.667513
farnesoid X nuclear receptorHomo sapiens (human)Potency50.901611
flap endonuclease 1Homo sapiens (human)Potency50.118711
GABA theta subunitRattus norvegicus (Norway rat)Potency19.952611
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency19.952611
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency19.952611
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency19.952611
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency19.952611
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency19.952611
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency19.952611
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency19.952611
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency19.952611
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency19.952611
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency19.952611
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency19.952611
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency19.952611
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency19.952611
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency19.952611
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency19.952611
gemininHomo sapiens (human)Potency2.429133
GLI family zinc finger 3Homo sapiens (human)Potency30.803833
Glutamate receptor 1Rattus norvegicus (Norway rat)Potency39.810711
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency39.810711
Glutamate receptor 3Rattus norvegicus (Norway rat)Potency39.810711
Glutamate receptor 4Rattus norvegicus (Norway rat)Potency39.810711
heat shock protein beta-1Homo sapiens (human)Potency52.126722
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency1.258912
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency39.810711
Histone H2A.xCricetulus griseus (Chinese hamster)Potency95.576322
histone-lysine N-methyltransferase 2A isoform 2 precursorHomo sapiens (human)Potency50.118711
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency10.000011
Integrin alpha-IIbHomo sapiens (human)Potency5.011911
Integrin beta-3Homo sapiens (human)Potency5.011911
lamin isoform A-delta10Homo sapiens (human)Potency5.288423
lethal factor (plasmid)Bacillus anthracis str. A2012Potency12.589311
lysosomal alpha-glucosidase preproproteinHomo sapiens (human)Potency0.251211
Microtubule-associated protein tauHomo sapiens (human)Potency19.622222
mitogen-activated protein kinase 1Homo sapiens (human)Potency24.702822
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency0.017811
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency6.309611
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency3.045322
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency0.206011
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency23.350722
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency63.921822
ParkinHomo sapiens (human)Potency1.835611
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency0.213311
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency20.864733
phosphopantetheinyl transferaseBacillus subtilisPotency19.952611
polyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)Potency39.810711
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency1.258911
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency35.481311
pregnane X nuclear receptorHomo sapiens (human)Potency25.280011
RAR-related orphan receptor gammaMus musculus (house mouse)Potency60.047622
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency65.495133
retinoid X nuclear receptor alphaHomo sapiens (human)Potency53.917711
Smad3Homo sapiens (human)Potency4.466811
survival motor neuron protein isoform dHomo sapiens (human)Potency0.112211
TDP1 proteinHomo sapiens (human)Potency1.707425
thioredoxin reductaseRattus norvegicus (Norway rat)Potency22.983312
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency40.014522
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency44.097222
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency42.800012

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
ATP-citrate synthase Rattus norvegicus (Norway rat)Ki11.666733
Dihydroorotate dehydrogenase Plasmodium falciparum (malaria parasite P. falciparum)IC5010.000011
Dihydroorotate dehydrogenase (fumarate)Saccharomyces cerevisiae S288CIC5010.000011
G-protein coupled receptor 35Homo sapiens (human)IC5039.000011
G-protein coupled receptor 35Homo sapiens (human)Ki137.000011
Gamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)IC502,900.000011
Gamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)IC502,900.000011
Gamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)IC502,900.000011
Gamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)IC502,900.000011
Gamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)IC502,900.000011
Gamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)IC502,900.000011
Gamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)IC502,900.000011
Gamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)IC502,900.000011
Gamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)IC502,900.000011
Glutamate receptor 1Rattus norvegicus (Norway rat)IC50101.000011
Glutamate receptor 2Rattus norvegicus (Norway rat)IC50101.000011
Glutamate receptor 3Rattus norvegicus (Norway rat)IC50101.000011
Glutamate receptor 4Rattus norvegicus (Norway rat)IC50101.000011
Glutamate receptor ionotropic, kainate 1Rattus norvegicus (Norway rat)IC501,000.000012
Glutamate receptor ionotropic, kainate 2Rattus norvegicus (Norway rat)IC501,000.000012
Glutamate receptor ionotropic, kainate 3Rattus norvegicus (Norway rat)IC501,000.000012
Glutamate receptor ionotropic, kainate 4Rattus norvegicus (Norway rat)IC501,000.000012
Glutamate receptor ionotropic, kainate 5Rattus norvegicus (Norway rat)IC501,000.000012
Glutamate receptor ionotropic, NMDA 1Homo sapiens (human)IC5015.000011
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)IC5098.040045
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)Ki5.400011
Glutamate receptor ionotropic, NMDA 2AHomo sapiens (human)IC5015.000011
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)IC50112.500034
Glutamate receptor ionotropic, NMDA 2BHomo sapiens (human)IC5015.000011
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)IC50112.500034
Glutamate receptor ionotropic, NMDA 2CHomo sapiens (human)IC5015.000011
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)IC50112.500034
Glutamate receptor ionotropic, NMDA 2DHomo sapiens (human)IC5015.000011
Glutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)IC50112.500034
Glutamate receptor ionotropic, NMDA 3AHomo sapiens (human)IC5015.000011
Glutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)IC50112.500034
Glutamate receptor ionotropic, NMDA 3BHomo sapiens (human)IC5015.000011
Glutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)IC50112.500034
Mitogen-activated protein kinase 11Homo sapiens (human)Ki1,300.000011
Mitogen-activated protein kinase 12Homo sapiens (human)Ki1,300.000011
Mitogen-activated protein kinase 13Homo sapiens (human)Ki1,300.000011
Mitogen-activated protein kinase 14Homo sapiens (human)Ki1,300.000011
Neuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)IC507.000011
Vesicular glutamate transporter 3Rattus norvegicus (Norway rat)Ki1,300.000011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Aryl hydrocarbon receptorHomo sapiens (human)EC500.300011
G protein-coupled receptor GPR35Rattus norvegicus (Norway rat)EC5066.000011
G-protein coupled receptor 35Homo sapiens (human)EC50199.800099
Histamine H3 receptorRattus norvegicus (Norway rat)EC50500.000011

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Glutamate receptor 1Rattus norvegicus (Norway rat)Kb137.000022
Glutamate receptor 2Rattus norvegicus (Norway rat)Kb137.000022
Glutamate receptor 3Rattus norvegicus (Norway rat)Kb137.000022
Glutamate receptor 4Rattus norvegicus (Norway rat)Kb137.000022
Glutamate receptor ionotropic, kainate 1Rattus norvegicus (Norway rat)Kb89.000011
Glutamate receptor ionotropic, kainate 2Rattus norvegicus (Norway rat)Kb89.000011
Glutamate receptor ionotropic, kainate 3Rattus norvegicus (Norway rat)Kb89.000011
Glutamate receptor ionotropic, kainate 4Rattus norvegicus (Norway rat)Kb89.000011
Glutamate receptor ionotropic, kainate 5Rattus norvegicus (Norway rat)Kb89.000011
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)Kb154.000033
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)Kb154.000033
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)Kb154.000033
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)Kb154.000033
Glutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)Kb154.000033
Glutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)Kb154.000033
Glutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)Kb154.000033