Proteins > Sphingosine 1-phosphate receptor 3
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Sphingosine 1-phosphate receptor 3
A sphingosine 1-phosphate receptor 3 that is encoded in the genome of human. [PRO:WCB, UniProtKB:Q99500]
Synonyms
S1P receptor 3;
S1P3;
Endothelial differentiation G-protein coupled receptor 3;
Sphingosine 1-phosphate receptor Edg-3;
S1P receptor Edg-3
Research
Bioassay Publications (44)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 11 (25.00) | 29.6817 |
| 2010's | 28 (63.64) | 24.3611 |
| 2020's | 5 (11.36) | 2.80 |
Compounds (14)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| fingolimod | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| bml 241 | Homo sapiens (human) | IC50 | 11.6000 | 1 | 1 |
| sew2871 | Homo sapiens (human) | IC50 | 5.0050 | 2 | 2 |
| sphingosine 1-phosphate | Homo sapiens (human) | IC50 | 0.0004 | 6 | 6 |
| fty 720p | Homo sapiens (human) | IC50 | 0.0063 | 2 | 2 |
| fty 720p | Homo sapiens (human) | Ki | 0.2117 | 1 | 5 |
| jte 013 | Homo sapiens (human) | IC50 | 1.0000 | 2 | 2 |
| fty 720p | Homo sapiens (human) | IC50 | 0.0146 | 2 | 2 |
| fty 720p | Homo sapiens (human) | Ki | 0.2066 | 1 | 5 |
Drugs with Activation Measurements
Spiro-1-benzofuranpiperidinylalkanoic acids as a novel and selective sphingosine S1PBioorganic & medicinal chemistry letters, , 02-01, Volume: 28, Issue:3, 2018
Late-stage optimization of a tercyclic class of S1P3-sparing, S1P1 receptor agonists.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 26, Issue:2, 2016
Modulators of the Sphingosine 1-phosphate receptor 1.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 23, Issue:23, 2013
Novel immunomodulator FTY720 is phosphorylated in rats and humans to form a single stereoisomer. Identification, chemical proof, and biological characterization of the biologically active species and its enantiomer.Journal of medicinal chemistry, , Aug-11, Volume: 48, Issue:16, 2005
A rational utilization of high-throughput screening affords selective, orally bioavailable 1-benzyl-3-carboxyazetidine sphingosine-1-phosphate-1 receptor agonists.Journal of medicinal chemistry, , Dec-30, Volume: 47, Issue:27, 2004
Quinolinone-based agonists of S1P₁: use of a N-scan SAR strategy to optimize in vitro and in vivo activity.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 22, Issue:1, 2012
Benzofuran Derivatives as Potent, Orally Active S1P1 Receptor Agonists: A Preclinical Lead Molecule for MS.ACS medicinal chemistry letters, , Feb-10, Volume: 2, Issue:2, 2011
A rational utilization of high-throughput screening affords selective, orally bioavailable 1-benzyl-3-carboxyazetidine sphingosine-1-phosphate-1 receptor agonists.Journal of medicinal chemistry, , Dec-30, Volume: 47, Issue:27, 2004
Synthesis and evaluation of highly selective quinazoline-2,4-dione ligands for sphingosine-1-phosphate receptor 2.RSC medicinal chemistry, , Feb-23, Volume: 13, Issue:2, 2022
Design and synthesis of pyrazolopyridine derivatives as sphingosine 1-phosphate receptor 2 ligands.Bioorganic & medicinal chemistry letters, , 02-01, Volume: 28, Issue:3, 2018
Late-stage optimization of a tercyclic class of S1P3-sparing, S1P1 receptor agonists.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 26, Issue:2, 2016
Exploring amino acids derivatives as potent, selective, and direct agonists of sphingosine-1-phosphate receptor subtype-1.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 23, Issue:2, 2013
Discovery of Clinical Candidate GSK1842799 As a Selective S1P1 Receptor Agonist (Prodrug) for Multiple Sclerosis.ACS medicinal chemistry letters, , Oct-10, Volume: 4, Issue:10, 2013
2-imino-thiazolidin-4-one derivatives as potent, orally active S1P1 receptor agonists.Journal of medicinal chemistry, , May-27, Volume: 53, Issue:10, 2010
Exploration of amino alcohol derivatives as novel, potent, and highly selective sphingosine-1-phosphate receptor subtype-1 agonists.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 20, Issue:8, 2010
Stereochemistry-activity relationship of orally active tetralin S1P agonist prodrugs.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 20, Issue:7, 2010
Synthesis and evaluation of alkoxy-phenylamides and alkoxy-phenylimidazoles as potent sphingosine-1-phosphate receptor subtype-1 agonists.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 19, Issue:2, 2009
Constrained azacyclic analogues of the immunomodulatory agent FTY720 as molecular probes for sphingosine 1-phosphate receptors.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 17, Issue:2, 2007
Synthesis of 4(5)-phenylimidazole-based analogues of sphingosine-1-phosphate and FTY720: discovery of potent S1P1 receptor agonists.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 15, Issue:15, 2005
Synthesis of benzimidazole based analogues of sphingosine-1-phosphate: discovery of potent, subtype-selective S1P4 receptor agonists.Bioorganic & medicinal chemistry letters, , Oct-04, Volume: 14, Issue:19, 2004
A rational utilization of high-throughput screening affords selective, orally bioavailable 1-benzyl-3-carboxyazetidine sphingosine-1-phosphate-1 receptor agonists.Journal of medicinal chemistry, , Dec-30, Volume: 47, Issue:27, 2004
Potent S1P receptor agonists replicate the pharmacologic actions of the novel immune modulator FTY720.Bioorganic & medicinal chemistry letters, , Jun-21, Volume: 14, Issue:12, 2004
Synthesis of para-alkyl aryl amide analogues of sphingosine-1-phosphate: discovery of potent S1P receptor agonists.Bioorganic & medicinal chemistry letters, , Oct-20, Volume: 13, Issue:20, 2003
Discovery of Novel Sphingosine-1-Phosphate-1 Receptor Agonists for the Treatment of Multiple Sclerosis.Journal of medicinal chemistry, , 02-24, Volume: 65, Issue:4, 2022
Bicyclic Ligand-Biased Agonists of S1PJournal of medicinal chemistry, , 02-11, Volume: 64, Issue:3, 2021
S1PBioorganic & medicinal chemistry letters, , 06-01, Volume: 30, Issue:11, 2020
Identification and Preclinical Pharmacology of BMS-986104: A Differentiated S1P1 Receptor Modulator in Clinical Trials.ACS medicinal chemistry letters, , Mar-10, Volume: 7, Issue:3, 2016
Discovery of oxazole and triazole derivatives as potent and selective S1P(1) agonists through pharmacophore-guided design.European journal of medicinal chemistry, , Oct-06, Volume: 85, 2014
Removal of sphingosine 1-phosphate receptor-3 (S1P(3)) agonism is essential, but inadequate to obtain immunomodulating 2-aminopropane-1,3-diol S1P(1) agonists with reduced effect on heart rate.Journal of medicinal chemistry, , Apr-22, Volume: 53, Issue:8, 2010
Synthesis and biological evaluation of gamma-aminophosphonates as potent, subtype-selective sphingosine 1-phosphate receptor agonists and antagonists.Bioorganic & medicinal chemistry, , Jan-15, Volume: 15, Issue:2, 2007
Asymmetric synthesis and biological evaluation of the enantiomeric isomers of the immunosuppressive FTY720-phosphate.Bioorganic & medicinal chemistry, , Jan-17, Volume: 13, Issue:2, 2005
Synthesis of 4(5)-phenylimidazole-based analogues of sphingosine-1-phosphate and FTY720: discovery of potent S1P1 receptor agonists.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 15, Issue:15, 2005
Novel immunomodulator FTY720 is phosphorylated in rats and humans to form a single stereoisomer. Identification, chemical proof, and biological characterization of the biologically active species and its enantiomer.Journal of medicinal chemistry, , Aug-11, Volume: 48, Issue:16, 2005
Potent S1P receptor agonists replicate the pharmacologic actions of the novel immune modulator FTY720.Bioorganic & medicinal chemistry letters, , Jun-21, Volume: 14, Issue:12, 2004
A rational utilization of high-throughput screening affords selective, orally bioavailable 1-benzyl-3-carboxyazetidine sphingosine-1-phosphate-1 receptor agonists.Journal of medicinal chemistry, , Dec-30, Volume: 47, Issue:27, 2004
Design, synthesis, and in vitro bioactivity evaluation of fluorine-containing analogues for sphingosine-1-phosphate 2 receptor.Bioorganic & medicinal chemistry, , 08-15, Volume: 27, Issue:16, 2019
Design and synthesis of pyrazolopyridine derivatives as sphingosine 1-phosphate receptor 2 ligands.Bioorganic & medicinal chemistry letters, , 02-01, Volume: 28, Issue:3, 2018
Novel Potent Selective Orally Active S1P5 Receptor Antagonists.ACS medicinal chemistry letters, , Mar-11, Volume: 12, Issue:3, 2021
Identification and Preclinical Pharmacology of ((1 R,3 S)-1-Amino-3-(( S)-6-(2-methoxyphenethyl)-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopentyl)methanol (BMS-986166): A Differentiated Sphingosine-1-phosphate Receptor 1 (S1PJournal of medicinal chemistry, , 03-14, Volume: 62, Issue:5, 2019
Kinase-independent phosphoramidate S1PBioorganic & medicinal chemistry letters, , 03-15, Volume: 27, Issue:6, 2017
Discovery of Tetrahydropyrazolopyridine as Sphingosine 1-Phosphate Receptor 3 (S1P3)-Sparing S1P1 Agonists Active at Low Oral Doses.Journal of medicinal chemistry, , Feb-11, Volume: 59, Issue:3, 2016
Late-stage optimization of a tercyclic class of S1P3-sparing, S1P1 receptor agonists.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 26, Issue:2, 2016
Synthesis and SAR studies of benzyl ether derivatives as potent orally active S1P₁ agonists.Bioorganic & medicinal chemistry, , Aug-01, Volume: 22, Issue:15, 2014
Novel immunomodulators based on an oxazolin-2-one-4-carboxamide scaffold.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 22, Issue:1, 2012
Identification of benzoxazole analogs as novel, S1P(3) sparing S1P(1) agonists.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 22, Issue:12, 2012
Synthesis and evaluation of CS-2100, a potent, orally active and S1P(3)- sparing S1P(1) agonist.European journal of medicinal chemistry, , Volume: 51, 2012
Quinolinone-based agonists of S1P₁: use of a N-scan SAR strategy to optimize in vitro and in vivo activity.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 22, Issue:1, 2012
Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist.ACS medicinal chemistry letters, , May-12, Volume: 2, Issue:5, 2011
Benzofuran Derivatives as Potent, Orally Active S1P1 Receptor Agonists: A Preclinical Lead Molecule for MS.ACS medicinal chemistry letters, , Feb-10, Volume: 2, Issue:2, 2011
Discovery of a brain-penetrant S1P₃-sparing direct agonist of the S1P₁ and S1P₅ receptors efficacious at low oral dose.Journal of medicinal chemistry, , Oct-13, Volume: 54, Issue:19, 2011
Stereochemistry-activity relationship of orally active tetralin S1P agonist prodrugs.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 20, Issue:7, 2010
Asymmetric synthesis and biological evaluation of the enantiomeric isomers of the immunosuppressive FTY720-phosphate.Bioorganic & medicinal chemistry, , Jan-17, Volume: 13, Issue:2, 2005
Novel immunomodulator FTY720 is phosphorylated in rats and humans to form a single stereoisomer. Identification, chemical proof, and biological characterization of the biologically active species and its enantiomer.Journal of medicinal chemistry, , Aug-11, Volume: 48, Issue:16, 2005
Synthesis and SAR of 1,3-thiazolyl thiophene and pyridine derivatives as potent, orally active and S1P₃-sparing S1P₁ agonists.Bioorganic & medicinal chemistry letters, , May-01, Volume: 22, Issue:9, 2012
Discovery of CS-2100, a potent, orally active and S1P3-sparing S1P1 agonist.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 22, Issue:4, 2012
Synthesis and evaluation of CS-2100, a potent, orally active and S1P(3)- sparing S1P(1) agonist.European journal of medicinal chemistry, , Volume: 51, 2012
Enables
This protein enables 5 target(s):
| Target | Category | Definition |
|---|
| integrin binding | molecular function | Binding to an integrin. [GOC:ceb] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| lipid binding | molecular function | Binding to a lipid. [GOC:ai] |
| sphingosine-1-phosphate receptor activity | molecular function | Combining with the sphingolipid sphingosine-1-phosphate (S1P), and transmitting the signal across the membrane by activating an associated G-protein. [GOC:bf, PMID:12728273, Wikipedia:S1PR1] |
| G protein-coupled receptor activity | molecular function | Combining with an extracellular signal and transmitting the signal across the membrane by activating an associated G-protein; promotes the exchange of GDP for GTP on the alpha subunit of a heterotrimeric G-protein complex. [GOC:bf, http://www.iuphar-db.org, Wikipedia:GPCR] |
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 2 target(s):
| Target | Category | Definition |
|---|
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
| 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 12 target(s):
| Target | Category | Definition |
|---|
| sphingosine-1-phosphate receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway initiated by sphingosine-1-phosphate binding to its receptor on the surface of a cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:ascb_2009, GOC:signaling, PMID:14592418, PMID:22001186, Reactome:R-HSA-419428] |
| 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] |
| 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-inhibiting G protein-coupled receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the inhibition of adenylyl cyclase activity and a subsequent decrease in the intracellular concentration of cyclic AMP (cAMP). [GOC:dph, GOC:mah, GOC:signaling, GOC:tb, ISBN:0815316194] |
| positive regulation of cytosolic calcium ion concentration | biological process | Any process that increases the concentration of calcium ions in the cytosol. [GOC:ai] |
| Notch signaling pathway | biological process | The series of molecular signals initiated by an extracellular ligand binding to the receptor Notch on the surface of a target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:go_curators, GOC:signaling] |
| positive regulation of cell population proliferation | biological process | Any process that activates or increases the rate or extent of cell proliferation. [GOC:go_curators] |
| anatomical structure morphogenesis | biological process | The process in which anatomical structures are generated and organized. Morphogenesis pertains to the creation of form. [GOC:go_curators, ISBN:0521436125] |
| regulation of interleukin-1 beta production | biological process | Any process that modulates the frequency, rate, or extent of interleukin-1 beta production. [GOC:mah] |
| negative regulation of establishment of endothelial barrier | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of establishment of endothelial barrier. [GO_REF:0000058, GOC:als, GOC:TermGenie, PMID:24851274] |
| 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] |
| regulation of metabolic process | biological process | Any process that modulates the frequency, rate or extent of the chemical reactions and pathways within a cell or an organism. [GOC:go_curators] |