Page last updated: 2024-11-12

amg 009

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth

Description

AMG 009: an anti-inflammatory agent; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID10483360
CHEMBL ID589973
SCHEMBL ID6951622
MeSH IDM0572119

Synonyms (23)

Synonym
amg-009
CHEMBL589973 ,
2-(4-(4-(butylcarbamoyl)-2-(2,4-dichlorophenylsulfonamido)phenoxy)-3-methoxyphenyl)acetic acid
bdbm50302828
1027847-67-1
83262trk3s ,
unii-83262trk3s
benzeneacetic acid, 4-(4-((butylamino)carbonyl)-2-(((2,4-dichlorophenyl)sulfonyl)amino)phenoxy)-3-methoxy-
amg 009
721947-97-3
SCHEMBL6951622
CS-6808
HY-19499
amg009
benzeneacetic acid, 4-[4-[(butylamino)carbonyl]-2-[[(2,4-dichlorophenyl)sulfonyl]amino]phenoxy]-3-methoxy-;benzeneacetic acid, 4-[4-[(butylamino)carbonyl]-2-[[(2,4-dichlorophenyl)sulfonyl]amino]phenoxy]-3-methoxy-
Q27269380
2-[4-[4-(butylcarbamoyl)-2-[(2,4-dichlorophenyl)sulfonylamino]phenoxy]-3-methoxyphenyl]acetic acid
EX-A4582
2-(4-(4-(butylcarbamoyl)-2-((2,4-dichlorophenyl)sulfonamido)phenoxy)-3-methoxyphenyl)acetic acid
GLXC-25371
4-[4-[(butylamino)carbonyl]-2-[[(2,4-dichlorophenyl)sulfonyl]amino]phenoxy]-3-methoxy-benzeneaceticacid
CRB84767
AKOS040741101

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" The objective of this study is to investigate whether similar dissolution enhancement of AMG 009 can be achieved from a bilayer dosage form, where AMG 009 and sodium carbonate are placed in a separate layer with or without the addition of HPMC K100 LV in each layer."( Enhancing and sustaining AMG 009 dissolution from a bilayer oral solid dosage form via microenvironmental pH modulation and supersaturation.
Alvarez, F; Alvarez-Nunez, F; Bi, M; Kyad, A, 2011
)
0.89
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (10)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)1.10000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)13.50000.20005.677410.0000AID1473741
Bile salt export pumpHomo sapiens (human)IC50 (µMol)11.50000.11007.190310.0000AID1473738
Thromboxane A2 receptor Homo sapiens (human)IC50 (µMol)30.00000.00110.71065.2000AID444132
Prostaglandin G/H synthase 2Homo sapiens (human)IC50 (µMol)0.01200.00010.995010.0000AID648029
Prostaglandin E2 receptor EP4 subtypeHomo sapiens (human)Ki44.00000.00010.47443.1623AID444134
Prostaglandin E2 receptor EP2 subtypeHomo sapiens (human)Ki44.00000.00100.54483.0000AID444133
Prostaglandin D2 receptorHomo sapiens (human)IC50 (µMol)0.00940.00011.15837.3000AID1153218; AID1153220; AID444116; AID638302; AID648027; AID648029
Prostaglandin D2 receptorHomo sapiens (human)Ki0.14800.00060.49131.4000AID444131
Chemoattractant receptor-homologous molecule expressed on Th2 cells Cavia porcellus (domestic guinea pig)IC50 (µMol)0.00300.00300.00300.0030AID444137
Prostaglandin D2 receptor 2Homo sapiens (human)IC50 (µMol)0.00600.00040.10090.9600AID1153218; AID444115; AID638301; AID638302; AID648027; AID648029
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Prostaglandin D2 receptor 2Homo sapiens (human)Kb0.00040.00000.00030.0010AID638306; AID645364; AID648031
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (135)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
smooth muscle contractionThromboxane A2 receptor Homo sapiens (human)
G protein-coupled receptor signaling pathwayThromboxane A2 receptor Homo sapiens (human)
response to nutrientThromboxane A2 receptor Homo sapiens (human)
response to xenobiotic stimulusThromboxane A2 receptor Homo sapiens (human)
positive regulation of blood coagulationThromboxane A2 receptor Homo sapiens (human)
response to testosteroneThromboxane A2 receptor Homo sapiens (human)
thromboxane A2 signaling pathwayThromboxane A2 receptor Homo sapiens (human)
response to ethanolThromboxane A2 receptor Homo sapiens (human)
positive regulation of angiogenesisThromboxane A2 receptor Homo sapiens (human)
positive regulation of smooth muscle contractionThromboxane A2 receptor Homo sapiens (human)
cellular response to lipopolysaccharideThromboxane A2 receptor Homo sapiens (human)
negative regulation of cell migration involved in sprouting angiogenesisThromboxane A2 receptor Homo sapiens (human)
inflammatory responseThromboxane A2 receptor Homo sapiens (human)
positive regulation of blood pressureThromboxane A2 receptor Homo sapiens (human)
positive regulation of vasoconstrictionThromboxane A2 receptor Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationThromboxane A2 receptor Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayThromboxane A2 receptor Homo sapiens (human)
prostaglandin biosynthetic processProstaglandin G/H synthase 2Homo sapiens (human)
angiogenesisProstaglandin G/H synthase 2Homo sapiens (human)
response to oxidative stressProstaglandin G/H synthase 2Homo sapiens (human)
embryo implantationProstaglandin G/H synthase 2Homo sapiens (human)
learningProstaglandin G/H synthase 2Homo sapiens (human)
memoryProstaglandin G/H synthase 2Homo sapiens (human)
regulation of blood pressureProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of cell population proliferationProstaglandin G/H synthase 2Homo sapiens (human)
response to xenobiotic stimulusProstaglandin G/H synthase 2Homo sapiens (human)
response to nematodeProstaglandin G/H synthase 2Homo sapiens (human)
response to fructoseProstaglandin G/H synthase 2Homo sapiens (human)
response to manganese ionProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of vascular endothelial growth factor productionProstaglandin G/H synthase 2Homo sapiens (human)
cyclooxygenase pathwayProstaglandin G/H synthase 2Homo sapiens (human)
bone mineralizationProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of prostaglandin biosynthetic processProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of fever generationProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of synaptic plasticityProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of synaptic transmission, dopaminergicProstaglandin G/H synthase 2Homo sapiens (human)
prostaglandin secretionProstaglandin G/H synthase 2Homo sapiens (human)
response to estradiolProstaglandin G/H synthase 2Homo sapiens (human)
response to lipopolysaccharideProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylationProstaglandin G/H synthase 2Homo sapiens (human)
response to vitamin DProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to heatProstaglandin G/H synthase 2Homo sapiens (human)
response to tumor necrosis factorProstaglandin G/H synthase 2Homo sapiens (human)
maintenance of blood-brain barrierProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of protein import into nucleusProstaglandin G/H synthase 2Homo sapiens (human)
hair cycleProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of apoptotic processProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of nitric oxide biosynthetic processProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of cell cycleProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of vasoconstrictionProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of smooth muscle contractionProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of smooth muscle contractionProstaglandin G/H synthase 2Homo sapiens (human)
decidualizationProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of smooth muscle cell proliferationProstaglandin G/H synthase 2Homo sapiens (human)
regulation of inflammatory responseProstaglandin G/H synthase 2Homo sapiens (human)
brown fat cell differentiationProstaglandin G/H synthase 2Homo sapiens (human)
response to glucocorticoidProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of calcium ion transportProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of synaptic transmission, glutamatergicProstaglandin G/H synthase 2Homo sapiens (human)
response to fatty acidProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to mechanical stimulusProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to lead ionProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to ATPProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to hypoxiaProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to non-ionic osmotic stressProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to fluid shear stressProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of transforming growth factor beta productionProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of cell migration involved in sprouting angiogenesisProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of fibroblast growth factor productionProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of brown fat cell differentiationProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of platelet-derived growth factor productionProstaglandin G/H synthase 2Homo sapiens (human)
cellular oxidant detoxificationProstaglandin G/H synthase 2Homo sapiens (human)
regulation of neuroinflammatory responseProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to osmotic stressProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to homocysteineProstaglandin G/H synthase 2Homo sapiens (human)
response to angiotensinProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of cytokine productionProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
positive regulation of cytokine productionProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
immune responseProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
JNK cascadeProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
response to mechanical stimulusProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
response to nematodeProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
regulation of ossificationProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
response to lipopolysaccharideProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
negative regulation of integrin activationProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
T-helper cell differentiationProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
negative regulation of inflammatory responseProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
positive regulation of inflammatory responseProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
regulation of stress fiber assemblyProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
bone developmentProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
ERK1 and ERK2 cascadeProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
cellular response to mechanical stimulusProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
negative regulation of eosinophil extravasationProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
cellular response to prostaglandin E stimulusProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
inflammatory responseProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
G protein-coupled receptor signaling pathwayProstaglandin E2 receptor EP2 subtypeHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayProstaglandin E2 receptor EP2 subtypeHomo sapiens (human)
response to nematodeProstaglandin E2 receptor EP2 subtypeHomo sapiens (human)
response to lipopolysaccharideProstaglandin E2 receptor EP2 subtypeHomo sapiens (human)
response to progesteroneProstaglandin E2 receptor EP2 subtypeHomo sapiens (human)
regulation of cell population proliferationProstaglandin E2 receptor EP2 subtypeHomo sapiens (human)
cellular response to prostaglandin E stimulusProstaglandin E2 receptor EP2 subtypeHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationProstaglandin E2 receptor EP2 subtypeHomo sapiens (human)
inflammatory responseProstaglandin E2 receptor EP2 subtypeHomo sapiens (human)
G protein-coupled receptor signaling pathwayProstaglandin D2 receptorHomo sapiens (human)
male sex determinationProstaglandin D2 receptorHomo sapiens (human)
sleepProstaglandin D2 receptorHomo sapiens (human)
mast cell degranulationProstaglandin D2 receptorHomo sapiens (human)
adenosine metabolic processProstaglandin D2 receptorHomo sapiens (human)
cellular response to prostaglandin D stimulusProstaglandin D2 receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationProstaglandin D2 receptorHomo sapiens (human)
inflammatory responseProstaglandin D2 receptorHomo sapiens (human)
chemotaxisProstaglandin D2 receptor 2Homo sapiens (human)
immune responseProstaglandin D2 receptor 2Homo sapiens (human)
G protein-coupled receptor signaling pathwayProstaglandin D2 receptor 2Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayProstaglandin D2 receptor 2Homo sapiens (human)
calcium-mediated signalingProstaglandin D2 receptor 2Homo sapiens (human)
positive regulation of G protein-coupled receptor signaling pathwayProstaglandin D2 receptor 2Homo sapiens (human)
negative regulation of male germ cell proliferationProstaglandin D2 receptor 2Homo sapiens (human)
neuropeptide signaling pathwayProstaglandin D2 receptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (37)

Processvia Protein(s)Taxonomy
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
thromboxane A2 receptor activityThromboxane A2 receptor Homo sapiens (human)
guanyl-nucleotide exchange factor activityThromboxane A2 receptor Homo sapiens (human)
protein bindingThromboxane A2 receptor Homo sapiens (human)
peroxidase activityProstaglandin G/H synthase 2Homo sapiens (human)
prostaglandin-endoperoxide synthase activityProstaglandin G/H synthase 2Homo sapiens (human)
protein bindingProstaglandin G/H synthase 2Homo sapiens (human)
enzyme bindingProstaglandin G/H synthase 2Homo sapiens (human)
heme bindingProstaglandin G/H synthase 2Homo sapiens (human)
protein homodimerization activityProstaglandin G/H synthase 2Homo sapiens (human)
metal ion bindingProstaglandin G/H synthase 2Homo sapiens (human)
oxidoreductase activity, acting on single donors with incorporation of molecular oxygen, incorporation of two atoms of oxygenProstaglandin G/H synthase 2Homo sapiens (human)
prostaglandin E receptor activityProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
protein bindingProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
prostaglandin E receptor activityProstaglandin E2 receptor EP2 subtypeHomo sapiens (human)
prostaglandin J receptor activityProstaglandin D2 receptorHomo sapiens (human)
prostaglandin D receptor activityProstaglandin D2 receptorHomo sapiens (human)
protein bindingProstaglandin D2 receptorHomo sapiens (human)
prostaglandin J receptor activityProstaglandin D2 receptor 2Homo sapiens (human)
G protein-coupled receptor activityProstaglandin D2 receptor 2Homo sapiens (human)
prostaglandin D receptor activityProstaglandin D2 receptor 2Homo sapiens (human)
prostaglandin F receptor activityProstaglandin D2 receptor 2Homo sapiens (human)
neuropeptide bindingProstaglandin D2 receptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (28)

Processvia Protein(s)Taxonomy
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
acrosomal vesicleThromboxane A2 receptor Homo sapiens (human)
plasma membraneThromboxane A2 receptor Homo sapiens (human)
nuclear speckThromboxane A2 receptor Homo sapiens (human)
plasma membraneThromboxane A2 receptor Homo sapiens (human)
nuclear inner membraneProstaglandin G/H synthase 2Homo sapiens (human)
nuclear outer membraneProstaglandin G/H synthase 2Homo sapiens (human)
cytoplasmProstaglandin G/H synthase 2Homo sapiens (human)
endoplasmic reticulumProstaglandin G/H synthase 2Homo sapiens (human)
endoplasmic reticulum lumenProstaglandin G/H synthase 2Homo sapiens (human)
endoplasmic reticulum membraneProstaglandin G/H synthase 2Homo sapiens (human)
caveolaProstaglandin G/H synthase 2Homo sapiens (human)
neuron projectionProstaglandin G/H synthase 2Homo sapiens (human)
protein-containing complexProstaglandin G/H synthase 2Homo sapiens (human)
neuron projectionProstaglandin G/H synthase 2Homo sapiens (human)
cytoplasmProstaglandin G/H synthase 2Homo sapiens (human)
plasma membraneProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
membraneProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
plasma membraneProstaglandin E2 receptor EP4 subtypeHomo sapiens (human)
plasma membraneProstaglandin E2 receptor EP2 subtypeHomo sapiens (human)
plasma membraneProstaglandin E2 receptor EP2 subtypeHomo sapiens (human)
plasma membraneProstaglandin D2 receptorHomo sapiens (human)
membraneProstaglandin D2 receptorHomo sapiens (human)
plasma membraneProstaglandin D2 receptorHomo sapiens (human)
plasma membraneProstaglandin D2 receptor 2Homo sapiens (human)
plasma membraneProstaglandin D2 receptor 2Homo sapiens (human)
neuron projectionProstaglandin D2 receptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (58)

Assay IDTitleYearJournalArticle
AID444138Inhibition of guinea pig DP receptor expressed in HEK 293 cells assessed as inhibition of PGD2-induced cAMP production by competitive ELISA2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Discovery and optimization of CRTH2 and DP dual antagonists.
AID444118Clearance in rat at 0.5 mg/kg, iv2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Discovery and optimization of CRTH2 and DP dual antagonists.
AID444131Antagonist activity at DP receptor in human platelets assessed as inhibition of PGD2-induced cAMP production by competitive ELISA2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Discovery and optimization of CRTH2 and DP dual antagonists.
AID444116Displacement of [3H]-PGD2 from human DP receptor expressed in HEK 293 cells in presence of 0.5% BSA by scintillation counting2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Discovery and optimization of CRTH2 and DP dual antagonists.
AID645056Antagonist activity at guinea pig Prostanoid DP receptor in whole blood by cAMP assay2011ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
Discovery of AMG 853, a CRTH2 and DP Dual Antagonist.
AID648027Displacement of [3H]-PGD2 from human CRTH2 receptor expressed in human HEK293 cells by scintillation counter in presence of 0.5% bovine serum albumin2011ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
Discovery of AMG 853, a CRTH2 and DP Dual Antagonist.
AID648030Displacement of [3H]-PGD2 from human Prostanoid DP receptor expressed in human HEK293 cells by scintillation counter in presence of 50% human plasma2011ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
Discovery of AMG 853, a CRTH2 and DP Dual Antagonist.
AID645364Antagonist activity at CRTH2 receptor in human eosinophol assessed as inhibition of PGD2-induced eosinophol shape change preincubated for 10 mins prior PGD2 stimulation measured after 10 mins by FACS flow cytometry2012Bioorganic & medicinal chemistry letters, Feb-15, Volume: 22, Issue:4
Optimization of phenylacetic acid derivatives for balanced CRTH2 and DP dual antagonists.
AID444125Oral bioavailability in dog at 2 mg/kg2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Discovery and optimization of CRTH2 and DP dual antagonists.
AID1473736Ratio of AUC in liver to plasma in Sprague-Dawley rat at 1500 mg/kg, po administered as single oral gavage measured after 24 hrs by Liquid chromatography/tandem mass spectrometry2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID645051Plasma concentration in guinea pig at 10 mg/kg, sc after 4 hrs2011ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
Discovery of AMG 853, a CRTH2 and DP Dual Antagonist.
AID645053Plasma concentration in guinea pig at 1 mg/kg, sc after 4 hrs2011ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
Discovery of AMG 853, a CRTH2 and DP Dual Antagonist.
AID444130Inhibition of PGD2-induced CRTH2 receptor internalization of CD16 negative granulocytes in human whole blood by flow cytometry2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Discovery and optimization of CRTH2 and DP dual antagonists.
AID1153220Displacement of [3H]-PGD2 from human DP receptor expressed in HEK293 cells in buffer solution with 0.5% bovine serum albumin by scintillation counting2014Bioorganic & medicinal chemistry letters, Jul-01, Volume: 24, Issue:13
Solving time-dependent CYP3A4 inhibition for a series of indole-phenylacetic acid dual antagonists of the PGD(2) receptors CRTH2 and DP.
AID638306Antagonist activity at CRTH2 receptor in human eosinophil assessed as inhibition of PGD2-induced cell shape change preincubated for 10 mins before PGD2 challenge by FACS analysis2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
Optimization of phenylacetic acid derivatives for CRTH2 and DP selective antagonism.
AID1474160Drug concentration at steady state in human at 100 mg, po BID2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1474163Ratio of drug concentration at steady state in human at 100 mg, po BID to IC50 for human MRP4 overexpressed in Sf9 insect cells2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID444120Volume of distribution at steady state in rat at 0.5 mg/kg, iv and 2 mg/kg, po2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Discovery and optimization of CRTH2 and DP dual antagonists.
AID1474159AUC in human at 100 mg, po BID2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID648028Displacement of [3H]-PGD2 from human CRTH2 receptor expressed in human HEK293 cells by scintillation counter in presence of 50% human plasma2011ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
Discovery of AMG 853, a CRTH2 and DP Dual Antagonist.
AID648031Inhibition of PGD2-induced CRTH2 internalization in human CD16 negative granulocytes by flow cytometry2011ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
Discovery of AMG 853, a CRTH2 and DP Dual Antagonist.
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID645362Displacement of [3H]PGD2 from human CRTH2 receptor expressed in HEK293 cells by scintillation counting in presence of 50% plasma2012Bioorganic & medicinal chemistry letters, Feb-15, Volume: 22, Issue:4
Optimization of phenylacetic acid derivatives for balanced CRTH2 and DP dual antagonists.
AID645054Plasma concentration in guinea pig at 0.3 mg/kg, sc after 4 hrs2011ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
Discovery of AMG 853, a CRTH2 and DP Dual Antagonist.
AID645365Antagonist activity at DP receptor in PGD2-stimulated human platelets in 80% whole blood assessed as inhibition of IBMX-stimulated cAMP production preincubated for 30 mins prior PGD2 stimulation measured after 60 mins by immunoassay2012Bioorganic & medicinal chemistry letters, Feb-15, Volume: 22, Issue:4
Optimization of phenylacetic acid derivatives for balanced CRTH2 and DP dual antagonists.
AID1153217Time dependent inhibition of human liver microsome CYP3A4 activity assessed as percentage remaining activity by measuring 6-beta-OH-testosterone formation at 15 uM for 15 mins using 200 uM testosterone as a substrate by LC/MS/MS analysis2014Bioorganic & medicinal chemistry letters, Jul-01, Volume: 24, Issue:13
Solving time-dependent CYP3A4 inhibition for a series of indole-phenylacetic acid dual antagonists of the PGD(2) receptors CRTH2 and DP.
AID645052Plasma concentration in guinea pig at 3 mg/kg, sc after 4 hrs2011ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
Discovery of AMG 853, a CRTH2 and DP Dual Antagonist.
AID648032Antagonist activity at human CRTH2 receptor in human whole blood cells assessed as inhibition of PGD2-induced cAMP formation by ELISA2011ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
Discovery of AMG 853, a CRTH2 and DP Dual Antagonist.
AID638303Displacement of [3H]PGD2 from human CRTh2 receptor expressed in 293 cells by scintillation counting in presence of 50 % human plasma2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
Optimization of phenylacetic acid derivatives for CRTH2 and DP selective antagonism.
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID645050Inhibition of PGD2-induced airway constriction in guinea pig model at 0.3 to 10 mg/kg, sc administered 4 hrs prior to aerosolized PGD2 challenge2011ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
Discovery of AMG 853, a CRTH2 and DP Dual Antagonist.
AID1153218Displacement of [3H]-PGD2 from human CRTH2 expressed in HEK293 cells in buffer solution with 0.5% bovine serum albumin by scintillation counting2014Bioorganic & medicinal chemistry letters, Jul-01, Volume: 24, Issue:13
Solving time-dependent CYP3A4 inhibition for a series of indole-phenylacetic acid dual antagonists of the PGD(2) receptors CRTH2 and DP.
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID444122Clearance in dog at 0.5 mg/kg, iv2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Discovery and optimization of CRTH2 and DP dual antagonists.
AID444127Mean residence time in cynomolgus monkey at 0.5 mg/kg, iv and 2 mg/kg, po2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Discovery and optimization of CRTH2 and DP dual antagonists.
AID638305Antagonist activity at DP receptor in human whole blood assessed as inhibition of PGD2-induced cAMP accumulation preincubated for 30 mins before PGD2 challenge measured after 60 mins by direct immunoassay2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
Optimization of phenylacetic acid derivatives for CRTH2 and DP selective antagonism.
AID645363Displacement of [3H]PGD2 from human DP receptor expressed in HEK293 cells by scintillation counting in presence of 50% plasma2012Bioorganic & medicinal chemistry letters, Feb-15, Volume: 22, Issue:4
Optimization of phenylacetic acid derivatives for balanced CRTH2 and DP dual antagonists.
AID1474161Ratio of drug concentration at steady state in human at 100 mg, po BID to IC50 for human MRP3 overexpressed in Sf9 insect cells2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID444132Displacement of [3H]SQ29548 from human TP receptor transfected in HEK 293 EBNA cells2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Discovery and optimization of CRTH2 and DP dual antagonists.
AID1474162Ratio of drug concentration at steady state in human at 100 mg, po BID to IC50 for human BSEP overexpressed in Sf9 insect cells2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID444133Inhibition of EP2 expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP production2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Discovery and optimization of CRTH2 and DP dual antagonists.
AID444124Volume of distribution at steady state in dog at 0.5 mg/kg, iv and 2 mg/kg, po2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Discovery and optimization of CRTH2 and DP dual antagonists.
AID444134Inhibition of EP4 expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP production2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Discovery and optimization of CRTH2 and DP dual antagonists.
AID444119Mean residence time in rat at 0.5 mg/kg, iv and 2 mg/kg, po2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Discovery and optimization of CRTH2 and DP dual antagonists.
AID1473835Stimulation of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID638302Displacement of [3H]PGD2 from human DP receptor expressed in 293 cells by scintillation counting in presence of 0.5 % BSA2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
Optimization of phenylacetic acid derivatives for CRTH2 and DP selective antagonism.
AID638304Displacement of [3H]PGD2 from human DP receptor expressed in 293 cells by scintillation counting in presence of 50 % human plasma2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
Optimization of phenylacetic acid derivatives for CRTH2 and DP selective antagonism.
AID444137Displacement of [3H]-PGD2 from guinea pig CRTH2 receptor expressed in HEK293 cells2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Discovery and optimization of CRTH2 and DP dual antagonists.
AID638301Displacement of [3H]PGD2 from human CRTH2 receptor expressed in 293 cells by scintillation counting in presence of 0.5 % BSA2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
Optimization of phenylacetic acid derivatives for CRTH2 and DP selective antagonism.
AID444135Antiallergic activity in Dunkin-Hartley guinea pig assessed as decrease in airway resistance against PGD2-induced airflow obstruction at 3 to 30 mg/kg, sc dosed 15 mins before PGD2 challenge by whole body plethysmography2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Discovery and optimization of CRTH2 and DP dual antagonists.
AID444128Volume of distribution at steady state in cynomolgus monkey at 0.5 mg/kg, iv and 2 mg/kg, po2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Discovery and optimization of CRTH2 and DP dual antagonists.
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID444115Displacement of [3H]-PGD2 from human CRTH2 expressed in HEK 293 cells in presence of 0.5% BSA by scintillation counting2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Discovery and optimization of CRTH2 and DP dual antagonists.
AID444123Mean residence time in dog at 0.5 mg/kg, iv and 2 mg/kg, po2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Discovery and optimization of CRTH2 and DP dual antagonists.
AID648029Displacement of [3H]-PGD2 from human Prostanoid DP receptor expressed in human HEK293 cells by scintillation counter in presence of 0.5% bovine serum albumin2011ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
Discovery of AMG 853, a CRTH2 and DP Dual Antagonist.
AID444129Oral bioavailability in cynomolgus monkey at 2 mg/kg2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Discovery and optimization of CRTH2 and DP dual antagonists.
AID444121Oral bioavailability in rat at 2 mg/kg2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Discovery and optimization of CRTH2 and DP dual antagonists.
AID444126Clearance in cynomolgus monkey at 0.5 mg/kg, iv2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Discovery and optimization of CRTH2 and DP dual antagonists.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (11)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (9.09)29.6817
2010's9 (81.82)24.3611
2020's1 (9.09)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other11 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]