Page last updated: 2024-08-07 12:47:30
Sphingosine 1-phosphate receptor 4
A sphingosine 1-phosphate receptor 4 that is encoded in the genome of human. [PRO:WCB, UniProtKB:O95977]
Synonyms
S1P receptor 4;
S1P4;
Endothelial differentiation G-protein coupled receptor 6;
Sphingosine 1-phosphate receptor Edg-6;
S1P receptor Edg-6
Research
Bioassay Publications (28)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 10 (35.71) | 29.6817 |
| 2010's | 15 (53.57) | 24.3611 |
| 2020's | 3 (10.71) | 2.80 |
Compounds (17)
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 | 0.0522 | 7 | 7 |
| fty 720p | Homo sapiens (human) | IC50 | 0.0150 | 2 | 2 |
| 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) | IC50 | 0.0022 | 1 | 1 |
| fty 720p | Homo sapiens (human) | Ki | 0.2066 | 1 | 5 |
| 5-(2,5-difluorophenyl)-N-(2,6-dimethylphenyl)-2-furancarboxamide | Homo sapiens (human) | IC50 | 0.3080 | 1 | 1 |
| 5-(2,5-dichlorophenyl)-N-(2,6-dimethoxyphenyl)-2-furancarboxamide | Homo sapiens (human) | IC50 | 0.4170 | 1 | 1 |
| 5-(2,5-dichlorophenyl)-N-[2,6-di(propan-2-yl)phenyl]-2-furancarboxamide | Homo sapiens (human) | IC50 | 0.1050 | 1 | 1 |
| 5-(2,5-dichlorophenyl)-N-(2,6-diethylphenyl)-2-furancarboxamide | Homo sapiens (human) | IC50 | 0.0890 | 1 | 1 |
| N-(2,6-dimethylphenyl)-5-(4-methyl-3-thiophenyl)-2-furancarboxamide | Homo sapiens (human) | IC50 | 0.2860 | 1 | 1 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|---|---|---|---|---|
| fingolimod | Homo sapiens (human) | EC50 | 5.0002 | 2 | 2 |
| 3-[2-(2,4-dichlorophenoxy)ethoxy]-6-methyl-2-nitropyridine | Homo sapiens (human) | EC50 | 0.1620 | 1 | 1 |
| sphingosine 1-phosphate | Homo sapiens (human) | EC50 | 0.1270 | 6 | 6 |
| N,N-dicyclohexyl-5-propyl-3-isoxazolecarboxamide | Homo sapiens (human) | EC50 | 50.0000 | 1 | 1 |
| fty 720p | Homo sapiens (human) | EC50 | 0.0098 | 5 | 5 |
| fty 720p | Homo sapiens (human) | EC50 | 0.0492 | 5 | 5 |
| VPC 23019 | Homo sapiens (human) | EC50 | 0.5000 | 1 | 1 |
| cs-2100 | Homo sapiens (human) | EC50 | 0.0580 | 1 | 1 |
| cym-5442 | Homo sapiens (human) | EC50 | 3.2500 | 1 | 0 |
| siponimod | Homo sapiens (human) | EC50 | 0.7500 | 1 | 1 |
Enables
This protein enables 4 target(s):
| Target | Category | Definition |
|---|---|---|
| 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 2 target(s):
| Target | Category | Definition |
|---|---|---|
| mitochondrion | cellular component | A semiautonomous, self replicating organelle that occurs in varying numbers, shapes, and sizes in the cytoplasm of virtually all eukaryotic cells. It is notably the site of tissue respiration. [GOC:giardia, ISBN:0198506732] |
| 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 |
|---|---|---|
| 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 7 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] |
| immune response | biological process | Any immune system process that functions in the calibrated response of an organism to a potential internal or invasive threat. [GO_REF:0000022, GOC:add] |
| 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] |
| activation of phospholipase C activity | biological process | The initiation of the activity of the inactive enzyme phospolipase C as the result of The series of molecular signals generated as a consequence of a G protein-coupled receptor binding to its physiological ligand. [GOC:dph, GOC:mah, GOC:tb, PMID:8280098] |
| positive regulation of cytosolic calcium ion concentration | biological process | Any process that increases the concentration of calcium ions in the cytosol. [GOC:ai] |
| 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] |