Proteins > Sphingosine 1-phosphate receptor 5
Page last updated: 2024-08-07 17:25:58
Sphingosine 1-phosphate receptor 5
A sphingosine 1-phosphate receptor 5 that is encoded in the genome of human. [PRO:WCB, UniProtKB:Q9H228]
Synonyms
S1P receptor 5;
S1P5;
Endothelial differentiation G-protein-coupled receptor 8;
Sphingosine 1-phosphate receptor Edg-8;
S1P receptor Edg-8
Research
Bioassay Publications (26)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 9 (34.62) | 29.6817 |
| 2010's | 14 (53.85) | 24.3611 |
| 2020's | 3 (11.54) | 2.80 |
Compounds (10)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| fingolimod | Homo sapiens (human) | IC50 | 2.1000 | 1 | 1 |
| sew2871 | Homo sapiens (human) | IC50 | 4.6000 | 1 | 1 |
| sphingosine 1-phosphate | Homo sapiens (human) | IC50 | 0.0020 | 5 | 5 |
| fty 720p | Homo sapiens (human) | IC50 | 0.0008 | 1 | 1 |
| fty 720p | Homo sapiens (human) | Ki | 0.2117 | 1 | 5 |
| jte 013 | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
| 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
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
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
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
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
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 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
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
Bicyclic Ligand-Biased Agonists of S1PJournal of medicinal chemistry, , 02-11, Volume: 64, Issue:3, 2021
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 A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders.Journal of medicinal chemistry, , Dec-10, Volume: 58, Issue:23, 2015
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
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
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
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
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
Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist.ACS medicinal chemistry letters, , May-12, Volume: 2, Issue:5, 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
Enables
This protein enables 3 target(s):
| Target | Category | Definition |
|---|
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| 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 4 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] |
| regulation of neuron differentiation | biological process | Any process that modulates the frequency, rate or extent of neuron differentiation. [GOC:go_curators] |
| 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] |
| 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] |