Proteins > Prostaglandin E2 receptor EP1 subtype
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Prostaglandin E2 receptor EP1 subtype
A prostaglandin E2 receptor EP1 subtype that is encoded in the genome of human. [PRO:WCB, UniProtKB:P34995]
Synonyms
PGE receptor EP1 subtype;
PGE2 receptor EP1 subtype;
Prostanoid EP1 receptor
Research
Bioassay Publications (19)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 12 (63.16) | 29.6817 |
| 2010's | 6 (31.58) | 24.3611 |
| 2020's | 1 (5.26) | 2.80 |
Compounds (21)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| ah 6809 | Homo sapiens (human) | Ki | 1.2000 | 1 | 1 |
| dinoprostone | Homo sapiens (human) | IC50 | 0.0156 | 2 | 2 |
| dinoprostone | Homo sapiens (human) | Ki | 0.0121 | 3 | 3 |
| dinoprost | Homo sapiens (human) | IC50 | 0.3000 | 2 | 2 |
| butaprost | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| cloprostenol | Homo sapiens (human) | IC50 | 0.4960 | 1 | 1 |
| mk-0524 | Homo sapiens (human) | Ki | 1.1600 | 1 | 1 |
| cp533536 | Homo sapiens (human) | Ki | 2.8000 | 1 | 1 |
| dg 041 | Homo sapiens (human) | IC50 | 20.0000 | 1 | 1 |
| cj-042794 | Homo sapiens (human) | IC50 | 20.0000 | 1 | 1 |
| gw9508 | Homo sapiens (human) | Ki | 1.5849 | 1 | 1 |
| cj-023,423 | Homo sapiens (human) | Ki | 5.0000 | 1 | 1 |
| l-798106 | Homo sapiens (human) | Ki | 39.0000 | 1 | 1 |
| cp 544326 | Homo sapiens (human) | Ki | 3.2000 | 1 | 1 |
| fr181157 | Homo sapiens (human) | Ki | 1.0000 | 3 | 3 |
| cay 10580 | Homo sapiens (human) | Ki | 13.0000 | 1 | 1 |
Drugs with Activation Measurements
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| tg4-155 | Homo sapiens (human) | Kb | 2.1000 | 1 | 1 |
| pf-04418948 | Homo sapiens (human) | Kb | 100.0000 | 1 | 1 |
| tg6-10-1 | Homo sapiens (human) | Kb | 1.7000 | 1 | 1 |
Identification of a Selective, Non-Prostanoid EP2 Receptor Agonist for the Treatment of Glaucoma: Omidenepag and its Prodrug Omidenepag Isopropyl.Journal of medicinal chemistry, , 08-09, Volume: 61, Issue:15, 2018
Discovery of G Protein-Biased EP2 Receptor Agonists.ACS medicinal chemistry letters, , Mar-10, Volume: 7, Issue:3, 2016
Prostanoid receptor EP2 as a therapeutic target.Journal of medicinal chemistry, , Jun-12, Volume: 57, Issue:11, 2014
Emerging targets in osteoporosis disease modification.Journal of medicinal chemistry, , Jun-10, Volume: 53, Issue:11, 2010
Synthesis and evaluation of a gamma-lactam as a highly selective EP2 and EP4 receptor agonist.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 18, Issue:2, 2008
Discovery of novel prostaglandin analogs of PGE2 as potent and selective EP2 and EP4 receptor agonists.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 17, Issue:15, 2007
Synthesis and biological evaluation of prostaglandin-F alkylphosphinic acid derivatives as bone anabolic agents for the treatment of osteoporosis.Journal of medicinal chemistry, , Nov-22, Volume: 44, Issue:24, 2001
Design and synthesis of 13,14-dihydro prostaglandin F(1alpha) analogues as potent and selective ligands for the human FP receptor.Journal of medicinal chemistry, , Mar-09, Volume: 43, Issue:5, 2000
Synthesis and in vitro evaluation of human FP-receptor selective prostaglandin analogues.Bioorganic & medicinal chemistry letters, , Jul-17, Volume: 10, Issue:14, 2000
Design and synthesis of 13,14-dihydro prostaglandin F(1alpha) analogues as potent and selective ligands for the human FP receptor.Journal of medicinal chemistry, , Mar-09, Volume: 43, Issue:5, 2000
Synthesis and in vitro evaluation of human FP-receptor selective prostaglandin analogues.Bioorganic & medicinal chemistry letters, , Jul-17, Volume: 10, Issue:14, 2000
Discovery of diphenyloxazole and Ndelta-Z-ornithine derivatives as highly potent and selective human prostaglandin EP(4) receptor antagonists.Journal of medicinal chemistry, , May-05, Volume: 48, Issue:9, 2005
Discovery of diphenylcarbamate derivatives as highly potent and selective IP receptor agonists: orally active prostacyclin mimetics. Part 3.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 15, Issue:12, 2005
Metabolism investigation leading to novel drug design: orally active prostacyclin mimetics. Part 4.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 15, Issue:13, 2005
Enables
This protein enables 2 target(s):
| Target | Category | Definition |
|---|
| D1 dopamine receptor binding | molecular function | Binding to a D1 dopamine receptor. [GOC:mah, GOC:nln] |
| prostaglandin E receptor activity | molecular function | Combining with prostaglandin E (PGE(2)) to initiate a change in cell activity. [ISBN:0198506732] |
Located In
This protein is located in 1 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
Active In
This protein is active in 1 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
Involved In
This protein is involved in 6 target(s):
| Target | Category | Definition |
|---|
| G protein-coupled receptor signaling pathway | biological process | The series of molecular signals initiated by a ligand binding to its receptor, in which the activated receptor promotes the exchange of GDP for GTP on the alpha-subunit of an associated heterotrimeric G-protein complex. The GTP-bound activated alpha-G-protein then dissociates from the beta- and gamma-subunits to further transmit the signal within the cell. The pathway begins with receptor-ligand interaction, and ends with regulation of a downstream cellular process. The pathway can start from the plasma membrane, Golgi or nuclear membrane. [GOC:bf, GOC:mah, PMID:16902576, PMID:24568158, Wikipedia:G_protein-coupled_receptor] |
| adenylate cyclase-activating dopamine receptor signaling pathway | biological process | An adenylate cyclase-activating G protein-coupled receptor signaling pathway initiated by dopamine binding to its receptor, and ending with the regulation of a downstream cellular process. [GOC:mah, GOC:signaling] |
| response to lipopolysaccharide | biological process | Any process that results in a change in state or activity of an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a lipopolysaccharide stimulus; lipopolysaccharide is a major component of the cell wall of gram-negative bacteria. [GOC:add, ISBN:0721601464] |
| positive regulation of cytosolic calcium ion concentration | biological process | Any process that increases the concentration of calcium ions in the cytosol. [GOC:ai] |
| inflammatory response | biological process | The immediate defensive reaction (by vertebrate tissue) to infection or injury caused by chemical or physical agents. The process is characterized by local vasodilation, extravasation of plasma into intercellular spaces and accumulation of white blood cells and macrophages. [GO_REF:0000022, ISBN:0198506732] |
| adenylate cyclase-activating G protein-coupled receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation of adenylyl cyclase activity which results in an increase in the intracellular concentration of cyclic AMP (cAMP). This pathway is negatively regulated by phosphodiesterase, which cleaves cAMP and terminates the signaling. [GOC:dph, GOC:mah, GOC:signaling, GOC:tb, ISBN:0815316194] |