Proteins > Sphingosine 1-phosphate receptor 2
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Sphingosine 1-phosphate receptor 2
A sphingosine 1-phosphate receptor 2 that is encoded in the genome of human. [PRO:WCB, UniProtKB:O95136]
Synonyms
S1P receptor 2;
S1P2;
Endothelial differentiation G-protein coupled receptor 5;
Sphingosine 1-phosphate receptor Edg-5;
S1P receptor Edg-5
Research
Bioassay Publications (22)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 7 (31.82) | 29.6817 |
| 2010's | 10 (45.45) | 24.3611 |
| 2020's | 5 (22.73) | 2.80 |
Compounds (12)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| fingolimod | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| sew2871 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| sphingosine 1-phosphate | Homo sapiens (human) | IC50 | 0.0019 | 4 | 4 |
| fty 720p | Homo sapiens (human) | IC50 | 0.5504 | 2 | 2 |
| fty 720p | Homo sapiens (human) | Ki | 0.2117 | 1 | 5 |
| jte 013 | Homo sapiens (human) | IC50 | 0.0401 | 6 | 6 |
| fty 720p | Homo sapiens (human) | IC50 | 0.0059 | 1 | 1 |
| fty 720p | Homo sapiens (human) | Ki | 0.2066 | 1 | 5 |
Drugs with Activation Measurements
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| jte 013 | Homo sapiens (human) | Activity | 1.7500 | 1 | 1 |
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
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
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
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
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
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
[no title available]European journal of medicinal chemistry, , Jan-05, Volume: 227, 2022
[no title available]Journal of medicinal chemistry, , 10-14, Volume: 64, Issue:19, 2021
The Repertoire of Small-Molecule PET Probes for Neuroinflammation Imaging: Challenges and Opportunities beyond TSPO.Journal of medicinal chemistry, , 12-23, Volume: 64, Issue:24, 2021
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
Fibrogenic Disorders in Human Diseases: From Inflammation to Organ Dysfunction.Journal of medicinal chemistry, , 11-21, Volume: 61, Issue:22, 2018
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 novel S1P2 antagonists. Part 1: discovery of 1,3-bis(aryloxy)benzene derivatives.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 25, Issue:7, 2015
Novel Potent Selective Orally Active S1P5 Receptor Antagonists.ACS medicinal chemistry letters, , Mar-11, Volume: 12, Issue:3, 2021
Novel immunomodulators based on an oxazolin-2-one-4-carboxamide scaffold.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 22, Issue:1, 2012
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 7 target(s):
| Target | Category | Definition |
|---|
| G protein-coupled receptor binding | molecular function | Binding to a G protein-coupled receptor. [GOC:ceb, GOC:dph] |
| 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] |
| 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] |
| G protein-coupled peptide receptor activity | molecular function | Combining with a peptide 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:dph, GOC:tb] |
| 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] |
Located In
This protein is located in 2 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] |
| postsynapse | cellular component | The part of a synapse that is part of the post-synaptic cell. [GOC:dos] |
Active In
This protein is active in 2 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] |
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
Involved In
This protein is involved in 10 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] |
| positive regulation of cell population proliferation | biological process | Any process that activates or increases the rate or extent of cell proliferation. [GOC:go_curators] |
| positive regulation of peptidyl-threonine phosphorylation | biological process | Any process that increases the frequency, rate or extent of peptidyl-threonine phosphorylation. Peptidyl-threonine phosphorylation is the phosphorylation of peptidyl-threonine to form peptidyl-O-phospho-L-threonine. [GOC:dph, GOC:tb] |
| actin cytoskeleton organization | biological process | A process that is carried out at the cellular level which results in the assembly, arrangement of constituent parts, or disassembly of cytoskeletal structures comprising actin filaments and their associated proteins. [GOC:dph, GOC:jl, GOC:mah] |
| filopodium assembly | biological process | The assembly of a filopodium, a thin, stiff protrusion extended by the leading edge of a motile cell such as a crawling fibroblast or amoeba, or an axonal growth cone. [GOC:dph, GOC:mah, GOC:tb, PMID:16337369, PMID:18464790] |
| excitatory postsynaptic potential | biological process | A process that leads to a temporary increase in postsynaptic potential due to the flow of positively charged ions into the postsynaptic cell. The flow of ions that causes an EPSP is an excitatory postsynaptic current (EPSC) and makes it easier for the neuron to fire an action potential. [GOC:dph, GOC:ef] |
| negative regulation of excitatory postsynaptic potential | biological process | Any process that prevents the establishment or decreases the extent of the excitatory postsynaptic potential (EPSP) which is a temporary increase in postsynaptic potential due to the flow of positively charged ions into the postsynaptic cell. The flow of ions that causes an EPSP is an excitatory postsynaptic current (EPSC) and makes it easier for the neuron to fire an action potential. [GOC:BHF] |
| positive regulation of establishment of endothelial barrier | biological process | Any process that activates or increases the frequency, rate or extent of establishment of endothelial barrier. [GO_REF:0000058, GOC:als, GOC:TermGenie, PMID:24851274] |
| 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] |