Page last updated: 2024-11-10

sphingosine 1-phosphate

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

sphingosine 1-phosphate: RN given refers to (R-(R*,S*-(E)))-isomer; RN for cpd without isomeric designation not available 8/89 [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

sphingosine 1-phosphate : A phosphosphingolipid that consists of sphingosine having a phospho group attached at position 1 [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID5283560
CHEMBL ID225155
CHEBI ID37550
SCHEMBL ID3886
SCHEMBL ID2559423
MeSH IDM0168077

Synonyms (55)

Synonym
gtpl911
(2s,3r,e)-2-amino-3-hydroxyoctadec-4-enyl dihydrogen phosphate
LMSP01050001
sphingosine-1-phosphate
sphing-4-enine-1-phosphate
HSCI1_000397
4-octadecene-1,3-diol, 2-amino-, 1-(dihydrogen phosphate), [r-[r*,s*-(e)]]-
4-octadecene-1,3-diol, 2-amino-, 1-(dihydrogen phosphate),(r-(r*,s*-(e)))-
c18-sphingosine 1-phosphate
d-erythro-sphingosine-1-phosphate
sphingosine, d-erythro-1-phosphate
4-octadecene-1,3-diol, 2-amino-, 1-(dihydrogen phosphate), (2s,3r,4e)-
sphing-4-enine 1-phosphate
sphingosine 1-phosphate
S1P ,
26993-30-6
C06124
sphingosine 1 phosphate
sphingosine 1-phosphate, >=95%, powder
NCGC00161364-02
CHEBI:37550 ,
NCGC00161364-01
(2s,3r,4e)-2-amino-4-octadecene-1,3-diol 1-(dihydrogen phosphate)
(2-amino-3-hydroxy-octadec-4-enoxy)phosphonic acid
(2s,3r,4e)-2-amino-3-hydroxyoctadec-4-en-1-yl dihydrogen phosphate
sphingosine 1-phosphic acid
d-erythro-sphingosine 1-phosphate
4-octadecene-1,3-diol, 2-amino-, 1-(dihydrogen phosphate), (r-(r*,s*-(e)))-
s1p compound
sphingosine-1-phosphate (d18:1)
yp-005
CHEMBL225155 ,
BML3-D06
bdbm50158348
[(2s,3r)-2-amino-3-hydroxyoctadec-4-enyl] dihydrogen phosphate
(2s,3r,e)-2-amino-3-hydroxyoctadec-4-en-1-yl dihydrogen phosphate
unii-yve187nj1u
yve187nj1u ,
EPITOPE ID:161059
(2s,3r,4e)-2-amino-4-octadecene-1,3-diol 1-(dihydrogen phosphate)
SCHEMBL3886
(e)-d-erythro-2-amino-1-(dihydrogenphosphate)-4-octadecene-1,3-diol
SCHEMBL2559423
AKOS024456554
DTXSID4037166
mfcd00270077
sphingosine 1-phosphate, >=98.0% (tlc)
sphingosin-1-phosphat
(2s,3r,4e)-1-(dihydrogen phosphate)2-amino-4-octadecene-1,3-diol
Q418267
HY-108496
CS-0028986
AMY3353
c18-sphingosine 1-phosphate; d-erythro-sphingosine-1-phosphate
BP-29640

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" In our previous study, FB1 was confirmed to be toxic to both liver and kidneys, coupled with simultaneous elevation of sphinganine 1-phosphate."( Elevation of sphingoid base 1-phosphate as a potential contributor to hepatotoxicity in fumonisin B1-exposed mice.
Kim, DH; Lee, YM; Lee, YS; Oh, S; Yoo, HS; Yun, YP, 2007
)
0.34
" In clinical trials, fingolimod was generally safe and well tolerated."( Mechanisms of fingolimod's efficacy and adverse effects in multiple sclerosis.
Chun, J; Cohen, JA, 2011
)
0.37
"We studied the role of two powerful molecular signalling mechanisms involved in the cardioprotective effect of sphingosine-1-phosphate (S1P), a major component of high density lipoprotein (HDL) against myocardial ischaemic-reperfusion injury, namely the RISK pathway (Akt/Erk), including its downstream target FOXO-1 and, the SAFE pathway (TNF/STAT-3)."( Interplay between SAFE and RISK pathways in sphingosine-1-phosphate-induced cardioprotection.
Frias, M; Lacerda, L; Lecour, S; Opie, LH; Somers, SJ, 2012
)
0.38
"In conclusion, S1P activates both the SAFE and RISK pathways, therefore suggesting a dual protective signalling in S1P-induced cardioprotection."( Interplay between SAFE and RISK pathways in sphingosine-1-phosphate-induced cardioprotection.
Frias, M; Lacerda, L; Lecour, S; Opie, LH; Somers, SJ, 2012
)
0.38
" We also demonstrated that sphingosine is safe to use for inhalation up to high doses, at least in mice."( Clinical Development of Sphingosine as Anti-Bacterial Drug: Inhalation of Sphingosine in Mini Pigs has no Adverse Side Effects.
Becker, KA; Carpinteiro, A; Carstens, H; Dubicanac, M; Edwards, MJ; Gulbins, E; Herrmann, D; Hilken, G; Kamler, M; Keitsch, S; Kleuser, B; Kramer, M; Kühn, C; Schumacher, F; Sehl, C; Soddemann, M; Swaidan, A; Verhaegh, R; Wilker, B; Wissmann, A, 2019
)
0.51
"A major dose-limiting side effect of docetaxel chemotherapy is peripheral neuropathy."( Role of 1-Deoxysphingolipids in docetaxel neurotoxicity.
Becker, KA; Bieberich, E; Bielawski, J; Doolen, S; Goins, L; Gulbins, E; McQuerry, KJ; Spassieva, SD; Sure, U; Taylor, BK; Uerschels, AK, 2020
)
0.56

Pharmacokinetics

ExcerptReferenceRelevance
"The pharmacokinetic (PK) and pharmacodynamic (PD) parameters of ONO-4641 in humans were estimated using preclinical data in order to provide essential information to better design future clinical studies."( The prediction of human response to ONO-4641, a sphingosine 1-phosphate receptor modulator, from preclinical data based on pharmacokinetic-pharmacodynamic modeling.
Hasegawa, C; Honda, N; Kitagawa, J; Nakade, S; Ogawa, M; Ohno, T, 2010
)
0.62
" In this investigation, we present a semimechanistic pharmacokinetic model for the interconversion of S1PHK substrates and their respective phosphates in rats and humans with the aim of investigating whether characterization of the rate of phosphorylation in blood platelets constitutes a basis for interspecies scaling using fingolimod as a model compound."( Translational pharmacokinetic modeling of fingolimod (FTY720) as a paradigm compound subject to sphingosine kinase-mediated phosphorylation.
Danhof, M; Luttringer, O; Ploeger, BA; Snelder, N; Stanski, DR, 2014
)
0.4
" Therefore, S1P can also be potentially used as a pharmacodynamic marker to study adjuvant arthritis (AA) rats."( UHPLC-MS/MS analysis of sphingosine 1-phosphate in joint cavity dialysate and hemodialysis solution of adjuvant arthritis rats: Application to geniposide pharmacodynamic study.
Feng, L; Hong, W; Jun, F; Li, D; Ran, D; Wenyu, W; Xiang, Z; Xuejing, D; Yan, W; Zhengrong, Z, 2019
)
0.82

Compound-Compound Interactions

ExcerptReferenceRelevance
" We conducted a phase I trial of safingol (S) alone and in combination with cisplatin (C)."( A phase I clinical trial of safingol in combination with cisplatin in advanced solid tumors.
Cane, LM; Carvajal, RD; Dickson, MA; Gonen, M; Merrill, AH; Schwartz, GK, 2011
)
0.37
"Safingol, the first putative SphK inhibitor to enter clinical trials, can be safely administered in combination with cisplatin."( A phase I clinical trial of safingol in combination with cisplatin in advanced solid tumors.
Cane, LM; Carvajal, RD; Dickson, MA; Gonen, M; Merrill, AH; Schwartz, GK, 2011
)
0.37

Bioavailability

ExcerptReferenceRelevance
" It has been proposed that the lipid phosphate phosphatases exhibit ecto activity that may function to limit bioavailability of these lipid agonists at their receptors."( G-protein-coupled receptor stimulation of the p42/p44 mitogen-activated protein kinase pathway is attenuated by lipid phosphate phosphatases 1, 1a, and 2 in human embryonic kidney 293 cells.
Ahmed, IS; Alderton, F; Darroch, P; McKie, A; Pyne, N; Pyne, S; Sambi, B, 2001
)
0.31
" From a clinical perspective, the present study identifies new potential therapeutic targets for the treatment of vascular-based, "stroke-like" inner ear pathologies: the enzymes responsible for S1P bioavailability and the S1P receptors."( Sphingosine-1-phosphate modulates spiral modiolar artery tone: A potential role in vascular-based inner ear pathologies?
Arnold, W; Bolz, SS; Lidington, D; Oestreicher, E; Pohl, U; Scherer, EQ, 2006
)
0.33
" This review focuses on the role S1P plays in endothelial function, its receptors and signalling pathways, and the role its major carrier high-density lipoproteins (HDL) play in its bioavailability and transport."( Endothelial functions of sphingosine-1-phosphate.
Levkau, B; Lucke, S, 2010
)
0.36
" Inhibition of 1) S1P formation with SK-I, a sphingosine kinase inhibitor, 2) S1P bioavailability with the S1P blocking antibody Sphingomab, LT1002 (but not its negative control, LT1017) or 3) S1P actions through S1PR(1) with the selective S1PR(1) antagonist, W146 (but not its inactive enantiomer, W140) blocked thermal hyperalgesia and infiltration of neutrophils."( Sphingosine 1-phosphate mediates hyperalgesia via a neutrophil-dependent mechanism.
Chen, Z; Cuzzocrea, S; Esposito, E; Finley, A; Sabbadini, R; Salvemini, D, 2013
)
1.83
" The alcohol 10 demonstrated good oral bioavailability and rapid in vivo conversion to 10-P."( Discovery of Clinical Candidate GSK1842799 As a Selective S1P1 Receptor Agonist (Prodrug) for Multiple Sclerosis.
Bernier, SG; Deng, H; Doyle, E; Evindar, G; Lorusso, J; Morgan, BA; Westlin, WF, 2013
)
0.39
" Most notably, fingolimod (FTY720, Gilenya, Novartis), an S1P receptor modulator, became the first FDA-approved medicine as an orally bioavailable drug for treating relapsing forms of multiple sclerosis."( Lysophospholipid receptors in drug discovery.
Chun, J; Kihara, Y; Mizuno, H, 2015
)
0.42
" Therefore, in the present review, based on available literatures we highlight the present knowledge on the production and bioavailability of these molecules, the mechanism of their regulation of hypertension, and patho-physiological role in malaria."( Malaria link of hypertension: a hidden syndicate of angiotensin II, bradykinin and sphingosine 1-phosphate.
Dhangadamajhi, G; Singh, S, 2021
)
0.85

Dosage Studied

ExcerptRelevanceReference
" Sph-1-P induced intracellular Ca2+ mobilization and the dose-response for Ca2+ release correlated closely with the concentration required for induction of shape change."( Sphingosine-1-phosphate: a platelet-activating sphingolipid released from agonist-stimulated human platelets.
Hakomori, S; Igarashi, Y; Ruan, F; Yatomi, Y, 1995
)
0.29
" The dose-response for calcium release induced by sphingosine-1-phosphate correlated closely with the concentration required for stimulation of DNA synthesis."( Sphingosine-1-phosphate, a putative second messenger, mobilizes calcium from internal stores via an inositol trisphosphate-independent pathway.
Brooker, G; Mattie, M; Spiegel, S, 1994
)
0.29
" S1P did not affect PDGF-stimulated tyrosine phosphorylation of PDGF-beta receptor, but strongly inhibited PDGF-induced Rac activation, with a dose-response relationship similar to that for inhibition of PDGF-elicited chemotaxis."( Sphingosine-1-phosphate, a platelet-derived lysophospholipid mediator, negatively regulates cellular Rac activity and cell migration in vascular smooth muscle cells.
Matsui, O; Okamoto, H; Ryu, Y; Sakurada, S; Sugimoto, N; Takuwa, N; Takuwa, Y; Usui, S, 2002
)
0.31
" In addition, we found that LPA has no effect on neutrophil chemotaxis; however, it has stimulatory effects on neutrophil respiratory burst in a dose-response manner."( Lysophosphatidic acid triggers calcium entry through a non-store-operated pathway in human neutrophils.
Hauser, CJ; Itagaki, K; Kannan, KB, 2005
)
0.33
" This ligand-induced, receptor-mediated cell motility follows a typical bell-shaped dose-response curve, that is, stimulation with low concentrations of S1P enhances cell motility, whereas excess ligand stimulation does not enhance it."( Attenuation of cell motility observed with high doses of sphingosine 1-phosphate or phosphorylated FTY720 involves RGS2 through its interactions with the receptor S1P.
Igarashi, Y; Kohno, T, 2008
)
0.59
" Subsequently, simulations were utilized to design a multiple ascending dose study with adaptive dosing regimens that would meet targeted pharmacodynamic (PD) response thresholds (eg, minimum 40% reduction in lymphocytes) while maintaining CD4 counts above a reasonable safety threshold."( Use of an exposure-response model to aid early drug development of an oral sphingosine 1-phosphate receptor modulator.
Carrothers, TJ; Inaba, S; Moberly, JB; Rohatagi, S; Shimozato, T; Truitt, KE; Zahir, H, 2009
)
0.58
" When cells were treated with 1 microM S1P simultaneously with OGD and recovery, cell viability increases in a dose-response manner."( Involvement of mitochondria on neuroprotective effect of sphingosine-1-phosphate in cell death in an in vitro model of brain ischemia.
Agudo-López, A; Fernández, I; Martínez, AM; Miguel, BG, 2010
)
0.36
" Pharmacokinetic investigation of 8bo in beagle dogs suggests that the compound is suitable for once daily dosing in humans."( 2-imino-thiazolidin-4-one derivatives as potent, orally active S1P1 receptor agonists.
Abele, S; Binkert, C; Bolli, MH; Bravo, R; Buchmann, S; Bur, D; Gatfield, J; Hess, P; Kohl, C; Mangold, C; Mathys, B; Menyhart, K; Müller, C; Nayler, O; Scherz, M; Schmidt, G; Sippel, V; Steiner, B; Strasser, D; Treiber, A; Weller, T, 2010
)
0.36
"Responses were evaluated from dose-response curves of the metabolites and metabolic inhibitors in which growth of HeLa cells, apoptosis based on DAPI fluorescence and cytosolic NADH levels were correlated with sphingomyelinase and spingosine kinase activities and levels of ceramide and sphingosine1-phosphate."( Metabolite modulation of HeLa cell response to ENOX2 inhibitors EGCG and phenoxodiol.
De Luca, T; Morré, DJ; Morré, DM; Watanabe, T; Wu, LY, 2011
)
0.37
"The frequency of LT1009 dosage was determined initially using an enzyme-linked immunosorbent assay assay measuring LT1009 eye tissue retention in 6 New Zealand White rabbits."( Prevention of ocular scarring after glaucoma filtering surgery using the monoclonal antibody LT1009 (Sonepcizumab) in a rabbit model.
Beattie, AR; Levine, MA; Lukowski, ZL; Meyers, CA; Min, J; Samuelson, DA; Schultz, GS; Sherwood, MB; Stoller, G, 2013
)
0.39
"001) and increased in a dose-response manner as the number of VF increased (P for the trend<0."( Plasma sphingosine 1-phosphate levels and the risk of vertebral fracture in postmenopausal women.
Cho, EH; Kim, BJ; Kim, GS; Kim, SW; Kim, SY; Kim, TH; Koh, JM; Lee, SH; Lee, SY; Lee, YS; Lim, KH, 2012
)
0.83
" Rats were administered an S1P1 inhibitor once daily for 4 weeks and necropsies were conducted at the end of the dosing phase, and clinical pathology and histopathologic examination were performed."( Gastric parietal cell atrophy and depletion after administration of a sphingosine-1-phosphate 1 inhibitor.
Radi, ZA; Vogel, MW, 2014
)
0.4
" Repeated oral dosing of the S1PL inhibitor in telemeterized, conscious rats resulted in significant bradycardia within 48 hours of drug treatment, comparable in magnitude to the bradycardia induced by 3 mg/kg fingolimod."( Sphingosine-1-Phosphate (S1P) Lyase Inhibition Causes Increased Cardiac S1P Levels and Bradycardia in Rats.
Banfor, P; Bousquet, P; Duignan, DB; Gintant, G; Harris, CM; Hart, M; Kim, Y; Mittelstadt, S; Segreti, J, 2016
)
0.43
" Defining the best drug dosing regimens to control the extent and duration of lymphopenia is critical to achieve the desired effects."( Selective Sphingosine 1-Phosphate Receptor 1 Agonist Is Protective Against Ischemia/Reperfusion in Mice.
Brait, VH; Gavaldà, A; Godessart, N; Planas, AM; Tarrasón, G, 2016
)
0.84
" Two weeks of NIBR-0213 oral dosing at 30, 100 and 300 mg/kg QD induced moderate pulmonary changes, characterized by alveolar wall thickening, macrophage accumulation, fibrosis, micro-hemorrhage, edema and necrosis."( Pathophysiological Consequences of a Break in S1P1-Dependent Homeostasis of Vascular Permeability Revealed by S1P1 Competitive Antagonism.
Angst, D; Beckmann, N; Beerli, C; Bigaud, M; Bollbuck, B; Bruns, C; Dawson, J; Dincer, Z; Fishli-Cavelti, G; Hersperger, R; Janser, P; Nahler, M; Otto, H; Quancard, J; Rosner, E, 2016
)
0.43
" Here, we showed that valproic acid (VPA), a histone deacetylase inhibitor, enforced the priming effect of S1P at a low dosage for human umbilical cord-derived MSCs (UC-MSCs)."( Valproic acid enforces the priming effect of sphingosine-1 phosphate on human mesenchymal stem cells.
Choi, KC; Heo, J; Ju, H; Kim, IG; Kim, Y; Lee, HY; Lee, S; Lim, J; Oh, YM; Shin, DM; Son, J, 2017
)
0.46
" The localized release dosage of effectors could be controlled by the change of environmental temperature."( Temperature-Gating Titania Nanotubes Regulate Migration of Endothelial Cells.
Bai, J; Du, W; Duan, Y; Gao, C; Liu, Y; Ouyang, H; Wu, S; Zhang, D; Zou, X, 2019
)
0.51
" The latest researches showed that S1P can alleviate acute lung injury (ALI) and the inflammation caused by ALI, while the dosage of S1P is still needed to be considered."( [Research advances of the roles of sphingosine-1-phosphate in acute lung injury].
Cui, P; Wang, MY; Xin, HM, 2022
)
0.72
" S1P was administered at a dosage of 200 μg/kg body weight per day by intraperitoneal injection."( S1P/S1PR2 promote pancreatic stellate cell activation and pancreatic fibrosis in chronic pancreatitis by regulating autophagy and the NLRP3 inflammasome.
Cui, L; Cui, N; Li, C; Yao, G; Zhang, G; Zhang, L; Zhang, S; Zhuo, Y, 2023
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (5)

RoleDescription
vasodilator agentA drug used to cause dilation of the blood vessels.
sphingosine-1-phosphate receptor agonistAn agonist that binds to and activates sphingosine 1-phosphate receptors.
signalling moleculeA molecular messenger in which the molecule is specifically involved in transmitting information between cells. Such molecules are released from the cell sending the signal, cross over the gap between cells by diffusion, and interact with specific receptors in another cell, triggering a response in that cell by activating a series of enzyme controlled reactions which lead to changes inside the cell.
T-cell proliferation inhibitorAn inhibitor that interferes with the process of T-cell proliferation.
mouse metaboliteAny mammalian metabolite produced during a metabolic reaction in a mouse (Mus musculus).
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (1)

ClassDescription
sphingoid 1-phosphateA generic class of phosphosphingolipids, encompassing monophosphorylated derivatives of sphinganine, its homologues and stereoisomers, as well as the hydroxy and unsaturated derivatives of these compounds.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Pathways (15)

PathwayProteinsCompounds
Sphingolipid Metabolism2335
Gaucher Disease2335
Globoid Cell Leukodystrophy2335
Metachromatic Leukodystrophy (MLD)2335
Fabry Disease2335
Krabbe Disease2335
Sphingolipid metabolism (integrated pathway)1167
Sphingolipid metabolism overview415
Sphingolipid metabolism: integrated pathway163
Sphingolipid metabolism in senescence97
GDNF signaling1338
Modulation of PI3K-Akt-mTOR signaling by bioactive sphingolipids43
Synthesis of ceramides and 1-deoxyceramides115
Clock-controlled autophagy in bone metabolism01
Sphingolipid pathway315

Protein Targets (7)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency44.66840.011212.4002100.0000AID1030
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Sphingosine 1-phosphate receptor 2Homo sapiens (human)IC50 (µMol)0.00190.00020.10421.1000AID1370457; AID1853948; AID204174; AID282268
Sphingosine 1-phosphate receptor 4Homo sapiens (human)IC50 (µMol)0.05220.00100.10680.4170AID1370460; AID1853951; AID204055; AID282270; AID392391; AID476459; AID481652
Sphingosine 1-phosphate receptor 1Homo sapiens (human)IC50 (µMol)0.00080.00000.08550.8400AID1370458; AID1853949; AID204037; AID282267; AID392389; AID476457
Sodium-dependent serotonin transporterHomo sapiens (human)IC50 (µMol)0.02300.00010.86458.7096AID204055
Sphingosine 1-phosphate receptor 3Homo sapiens (human)IC50 (µMol)0.00040.00000.00450.0230AID1370459; AID1853950; AID204054; AID282269; AID392390; AID476458
Sphingosine 1-phosphate receptor 5Homo sapiens (human)IC50 (µMol)0.00200.00050.83884.6000AID1370461; AID1853952; AID282271; AID392392; AID476460
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Sphingosine 1-phosphate receptor 2Homo sapiens (human)EC50 (µMol)0.00970.00070.36512.8530AID1062165; AID204039; AID204040; AID240212; AID240301; AID481645; AID481650
Sphingosine 1-phosphate receptor 4Homo sapiens (human)EC50 (µMol)0.12700.00010.26263.2500AID1062163; AID204165; AID240214; AID240303; AID305222; AID481647
Sphingosine 1-phosphate receptor 1Homo sapiens (human)EC50 (µMol)0.00670.00000.17597.8700AID1062166; AID1176592; AID1271835; AID204032; AID204033; AID240202; AID240300; AID305220; AID392394; AID473717; AID476463; AID481644; AID481649; AID642403; AID721982
Sodium-dependent serotonin transporterHomo sapiens (human)EC50 (µMol)0.00110.00112.38838.7000AID204047
Sphingosine 1-phosphate receptor 3Homo sapiens (human)EC50 (µMol)0.00870.00010.30925.0000AID1062164; AID1271836; AID204047; AID204048; AID240213; AID240302; AID305221; AID392395; AID473718; AID476464; AID481646; AID481651; AID721983
Sphingosine 1-phosphate receptor 5Homo sapiens (human)EC50 (µMol)0.02350.00020.13653.1623AID1062162; AID204176; AID204177; AID240215; AID240304; AID305223; AID481648; AID481653
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (76)

Processvia Protein(s)Taxonomy
G protein-coupled receptor signaling pathwaySphingosine 1-phosphate receptor 2Homo sapiens (human)
sphingosine-1-phosphate receptor signaling pathwaySphingosine 1-phosphate receptor 2Homo sapiens (human)
positive regulation of cell population proliferationSphingosine 1-phosphate receptor 2Homo sapiens (human)
positive regulation of peptidyl-threonine phosphorylationSphingosine 1-phosphate receptor 2Homo sapiens (human)
actin cytoskeleton organizationSphingosine 1-phosphate receptor 2Homo sapiens (human)
filopodium assemblySphingosine 1-phosphate receptor 2Homo sapiens (human)
excitatory postsynaptic potentialSphingosine 1-phosphate receptor 2Homo sapiens (human)
negative regulation of excitatory postsynaptic potentialSphingosine 1-phosphate receptor 2Homo sapiens (human)
positive regulation of establishment of endothelial barrierSphingosine 1-phosphate receptor 2Homo sapiens (human)
regulation of metabolic processSphingosine 1-phosphate receptor 2Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwaySphingosine 1-phosphate receptor 2Homo sapiens (human)
sphingosine-1-phosphate receptor signaling pathwaySphingosine 1-phosphate receptor 4Homo sapiens (human)
immune responseSphingosine 1-phosphate receptor 4Homo sapiens (human)
G protein-coupled receptor signaling pathwaySphingosine 1-phosphate receptor 4Homo sapiens (human)
activation of phospholipase C activitySphingosine 1-phosphate receptor 4Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationSphingosine 1-phosphate receptor 4Homo sapiens (human)
regulation of metabolic processSphingosine 1-phosphate receptor 4Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwaySphingosine 1-phosphate receptor 4Homo sapiens (human)
blood vessel maturationSphingosine 1-phosphate receptor 1Homo sapiens (human)
cardiac muscle tissue growth involved in heart morphogenesisSphingosine 1-phosphate receptor 1Homo sapiens (human)
sphingosine-1-phosphate receptor signaling pathwaySphingosine 1-phosphate receptor 1Homo sapiens (human)
chemotaxisSphingosine 1-phosphate receptor 1Homo sapiens (human)
cell adhesionSphingosine 1-phosphate receptor 1Homo sapiens (human)
G protein-coupled receptor signaling pathwaySphingosine 1-phosphate receptor 1Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwaySphingosine 1-phosphate receptor 1Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwaySphingosine 1-phosphate receptor 1Homo sapiens (human)
brain developmentSphingosine 1-phosphate receptor 1Homo sapiens (human)
cell population proliferationSphingosine 1-phosphate receptor 1Homo sapiens (human)
cell migrationSphingosine 1-phosphate receptor 1Homo sapiens (human)
transmission of nerve impulseSphingosine 1-phosphate receptor 1Homo sapiens (human)
lamellipodium assemblySphingosine 1-phosphate receptor 1Homo sapiens (human)
actin cytoskeleton organizationSphingosine 1-phosphate receptor 1Homo sapiens (human)
regulation of cell adhesionSphingosine 1-phosphate receptor 1Homo sapiens (human)
neuron differentiationSphingosine 1-phosphate receptor 1Homo sapiens (human)
positive regulation of cell migrationSphingosine 1-phosphate receptor 1Homo sapiens (human)
regulation of bone mineralizationSphingosine 1-phosphate receptor 1Homo sapiens (human)
leukocyte chemotaxisSphingosine 1-phosphate receptor 1Homo sapiens (human)
regulation of bone resorptionSphingosine 1-phosphate receptor 1Homo sapiens (human)
endothelial cell differentiationSphingosine 1-phosphate receptor 1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IISphingosine 1-phosphate receptor 1Homo sapiens (human)
positive regulation of smooth muscle cell proliferationSphingosine 1-phosphate receptor 1Homo sapiens (human)
positive regulation of positive chemotaxisSphingosine 1-phosphate receptor 1Homo sapiens (human)
negative regulation of stress fiber assemblySphingosine 1-phosphate receptor 1Homo sapiens (human)
heart trabecula morphogenesisSphingosine 1-phosphate receptor 1Homo sapiens (human)
T cell migrationSphingosine 1-phosphate receptor 1Homo sapiens (human)
angiogenesisSphingosine 1-phosphate receptor 1Homo sapiens (human)
regulation of metabolic processSphingosine 1-phosphate receptor 1Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwaySphingosine 1-phosphate receptor 1Homo sapiens (human)
monoamine transportSodium-dependent serotonin transporterHomo sapiens (human)
response to hypoxiaSodium-dependent serotonin transporterHomo sapiens (human)
neurotransmitter transportSodium-dependent serotonin transporterHomo sapiens (human)
response to nutrientSodium-dependent serotonin transporterHomo sapiens (human)
memorySodium-dependent serotonin transporterHomo sapiens (human)
circadian rhythmSodium-dependent serotonin transporterHomo sapiens (human)
response to xenobiotic stimulusSodium-dependent serotonin transporterHomo sapiens (human)
response to toxic substanceSodium-dependent serotonin transporterHomo sapiens (human)
positive regulation of gene expressionSodium-dependent serotonin transporterHomo sapiens (human)
positive regulation of serotonin secretionSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of cerebellar granule cell precursor proliferationSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of synaptic transmission, dopaminergicSodium-dependent serotonin transporterHomo sapiens (human)
response to estradiolSodium-dependent serotonin transporterHomo sapiens (human)
social behaviorSodium-dependent serotonin transporterHomo sapiens (human)
vasoconstrictionSodium-dependent serotonin transporterHomo sapiens (human)
sperm ejaculationSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of neuron differentiationSodium-dependent serotonin transporterHomo sapiens (human)
positive regulation of cell cycleSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of organ growthSodium-dependent serotonin transporterHomo sapiens (human)
behavioral response to cocaineSodium-dependent serotonin transporterHomo sapiens (human)
enteric nervous system developmentSodium-dependent serotonin transporterHomo sapiens (human)
brain morphogenesisSodium-dependent serotonin transporterHomo sapiens (human)
serotonin uptakeSodium-dependent serotonin transporterHomo sapiens (human)
membrane depolarizationSodium-dependent serotonin transporterHomo sapiens (human)
platelet aggregationSodium-dependent serotonin transporterHomo sapiens (human)
cellular response to retinoic acidSodium-dependent serotonin transporterHomo sapiens (human)
cellular response to cGMPSodium-dependent serotonin transporterHomo sapiens (human)
regulation of thalamus sizeSodium-dependent serotonin transporterHomo sapiens (human)
conditioned place preferenceSodium-dependent serotonin transporterHomo sapiens (human)
sodium ion transmembrane transportSodium-dependent serotonin transporterHomo sapiens (human)
amino acid transportSodium-dependent serotonin transporterHomo sapiens (human)
sphingosine-1-phosphate receptor signaling pathwaySphingosine 1-phosphate receptor 3Homo sapiens (human)
inflammatory responseSphingosine 1-phosphate receptor 3Homo sapiens (human)
G protein-coupled receptor signaling pathwaySphingosine 1-phosphate receptor 3Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwaySphingosine 1-phosphate receptor 3Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationSphingosine 1-phosphate receptor 3Homo sapiens (human)
Notch signaling pathwaySphingosine 1-phosphate receptor 3Homo sapiens (human)
positive regulation of cell population proliferationSphingosine 1-phosphate receptor 3Homo sapiens (human)
anatomical structure morphogenesisSphingosine 1-phosphate receptor 3Homo sapiens (human)
regulation of interleukin-1 beta productionSphingosine 1-phosphate receptor 3Homo sapiens (human)
negative regulation of establishment of endothelial barrierSphingosine 1-phosphate receptor 3Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwaySphingosine 1-phosphate receptor 3Homo sapiens (human)
regulation of metabolic processSphingosine 1-phosphate receptor 3Homo sapiens (human)
sphingosine-1-phosphate receptor signaling pathwaySphingosine 1-phosphate receptor 5Homo sapiens (human)
regulation of neuron differentiationSphingosine 1-phosphate receptor 5Homo sapiens (human)
regulation of metabolic processSphingosine 1-phosphate receptor 5Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwaySphingosine 1-phosphate receptor 5Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (20)

Processvia Protein(s)Taxonomy
G protein-coupled receptor bindingSphingosine 1-phosphate receptor 2Homo sapiens (human)
G protein-coupled receptor activitySphingosine 1-phosphate receptor 2Homo sapiens (human)
integrin bindingSphingosine 1-phosphate receptor 2Homo sapiens (human)
protein bindingSphingosine 1-phosphate receptor 2Homo sapiens (human)
lipid bindingSphingosine 1-phosphate receptor 2Homo sapiens (human)
G protein-coupled peptide receptor activitySphingosine 1-phosphate receptor 2Homo sapiens (human)
sphingosine-1-phosphate receptor activitySphingosine 1-phosphate receptor 2Homo sapiens (human)
protein bindingSphingosine 1-phosphate receptor 4Homo sapiens (human)
lipid bindingSphingosine 1-phosphate receptor 4Homo sapiens (human)
sphingosine-1-phosphate receptor activitySphingosine 1-phosphate receptor 4Homo sapiens (human)
G protein-coupled receptor activitySphingosine 1-phosphate receptor 4Homo sapiens (human)
G protein-coupled receptor bindingSphingosine 1-phosphate receptor 1Homo sapiens (human)
G protein-coupled receptor activitySphingosine 1-phosphate receptor 1Homo sapiens (human)
protein bindingSphingosine 1-phosphate receptor 1Homo sapiens (human)
sphingosine-1-phosphate receptor activitySphingosine 1-phosphate receptor 1Homo sapiens (human)
sphingolipid bindingSphingosine 1-phosphate receptor 1Homo sapiens (human)
integrin bindingSodium-dependent serotonin transporterHomo sapiens (human)
monoatomic cation channel activitySodium-dependent serotonin transporterHomo sapiens (human)
neurotransmitter transmembrane transporter activitySodium-dependent serotonin transporterHomo sapiens (human)
serotonin:sodium:chloride symporter activitySodium-dependent serotonin transporterHomo sapiens (human)
protein bindingSodium-dependent serotonin transporterHomo sapiens (human)
monoamine transmembrane transporter activitySodium-dependent serotonin transporterHomo sapiens (human)
antiporter activitySodium-dependent serotonin transporterHomo sapiens (human)
syntaxin-1 bindingSodium-dependent serotonin transporterHomo sapiens (human)
cocaine bindingSodium-dependent serotonin transporterHomo sapiens (human)
sodium ion bindingSodium-dependent serotonin transporterHomo sapiens (human)
identical protein bindingSodium-dependent serotonin transporterHomo sapiens (human)
nitric-oxide synthase bindingSodium-dependent serotonin transporterHomo sapiens (human)
actin filament bindingSodium-dependent serotonin transporterHomo sapiens (human)
serotonin bindingSodium-dependent serotonin transporterHomo sapiens (human)
integrin bindingSphingosine 1-phosphate receptor 3Homo sapiens (human)
protein bindingSphingosine 1-phosphate receptor 3Homo sapiens (human)
lipid bindingSphingosine 1-phosphate receptor 3Homo sapiens (human)
sphingosine-1-phosphate receptor activitySphingosine 1-phosphate receptor 3Homo sapiens (human)
G protein-coupled receptor activitySphingosine 1-phosphate receptor 3Homo sapiens (human)
protein bindingSphingosine 1-phosphate receptor 5Homo sapiens (human)
sphingosine-1-phosphate receptor activitySphingosine 1-phosphate receptor 5Homo sapiens (human)
G protein-coupled receptor activitySphingosine 1-phosphate receptor 5Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (17)

Processvia Protein(s)Taxonomy
plasma membraneSphingosine 1-phosphate receptor 2Homo sapiens (human)
postsynapseSphingosine 1-phosphate receptor 2Homo sapiens (human)
plasma membraneSphingosine 1-phosphate receptor 2Homo sapiens (human)
cytoplasmSphingosine 1-phosphate receptor 2Homo sapiens (human)
mitochondrionSphingosine 1-phosphate receptor 4Homo sapiens (human)
plasma membraneSphingosine 1-phosphate receptor 4Homo sapiens (human)
plasma membraneSphingosine 1-phosphate receptor 4Homo sapiens (human)
cytoplasmSphingosine 1-phosphate receptor 4Homo sapiens (human)
nucleoplasmSphingosine 1-phosphate receptor 1Homo sapiens (human)
endosomeSphingosine 1-phosphate receptor 1Homo sapiens (human)
plasma membraneSphingosine 1-phosphate receptor 1Homo sapiens (human)
external side of plasma membraneSphingosine 1-phosphate receptor 1Homo sapiens (human)
intracellular membrane-bounded organelleSphingosine 1-phosphate receptor 1Homo sapiens (human)
membrane raftSphingosine 1-phosphate receptor 1Homo sapiens (human)
plasma membraneSphingosine 1-phosphate receptor 1Homo sapiens (human)
cytoplasmSphingosine 1-phosphate receptor 1Homo sapiens (human)
plasma membraneSodium-dependent serotonin transporterHomo sapiens (human)
focal adhesionSodium-dependent serotonin transporterHomo sapiens (human)
endosome membraneSodium-dependent serotonin transporterHomo sapiens (human)
endomembrane systemSodium-dependent serotonin transporterHomo sapiens (human)
presynaptic membraneSodium-dependent serotonin transporterHomo sapiens (human)
membrane raftSodium-dependent serotonin transporterHomo sapiens (human)
synapseSodium-dependent serotonin transporterHomo sapiens (human)
postsynaptic membraneSodium-dependent serotonin transporterHomo sapiens (human)
serotonergic synapseSodium-dependent serotonin transporterHomo sapiens (human)
synapseSodium-dependent serotonin transporterHomo sapiens (human)
plasma membraneSodium-dependent serotonin transporterHomo sapiens (human)
neuron projectionSodium-dependent serotonin transporterHomo sapiens (human)
plasma membraneSphingosine 1-phosphate receptor 3Homo sapiens (human)
cytoplasmSphingosine 1-phosphate receptor 3Homo sapiens (human)
plasma membraneSphingosine 1-phosphate receptor 3Homo sapiens (human)
plasma membraneSphingosine 1-phosphate receptor 5Homo sapiens (human)
cytoplasmSphingosine 1-phosphate receptor 5Homo sapiens (human)
plasma membraneSphingosine 1-phosphate receptor 5Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (142)

Assay IDTitleYearJournalArticle
AID1346242Human S1P5 receptor (Lysophospholipid (S1P) receptors)2004The Journal of biological chemistry, Apr-02, Volume: 279, Issue:14
Sphingosine 1-phosphate (S1P) receptor subtypes S1P1 and S1P3, respectively, regulate lymphocyte recirculation and heart rate.
AID1346170Human S1P1 receptor (Lysophospholipid (S1P) receptors)2001Biochemistry, Nov-20, Volume: 40, Issue:46
Characterization of the human and mouse sphingosine 1-phosphate receptor, S1P5 (Edg-8): structure-activity relationship of sphingosine1-phosphate receptors.
AID1346205Human S1P3 receptor (Lysophospholipid (S1P) receptors)2002The Journal of biological chemistry, Jun-14, Volume: 277, Issue:24
The immune modulator FTY720 targets sphingosine 1-phosphate receptors.
AID1346242Human S1P5 receptor (Lysophospholipid (S1P) receptors)2006Chemistry & biology, Nov, Volume: 13, Issue:11
A monoselective sphingosine-1-phosphate receptor-1 agonist prevents allograft rejection in a stringent rat heart transplantation model.
AID1346170Human S1P1 receptor (Lysophospholipid (S1P) receptors)2006Chemistry & biology, Nov, Volume: 13, Issue:11
A monoselective sphingosine-1-phosphate receptor-1 agonist prevents allograft rejection in a stringent rat heart transplantation model.
AID1346234Mouse S1P5 receptor (Lysophospholipid (S1P) receptors)2004The Journal of biological chemistry, Apr-02, Volume: 279, Issue:14
Sphingosine 1-phosphate (S1P) receptor subtypes S1P1 and S1P3, respectively, regulate lymphocyte recirculation and heart rate.
AID1346242Human S1P5 receptor (Lysophospholipid (S1P) receptors)2001Biochemistry, Nov-20, Volume: 40, Issue:46
Characterization of the human and mouse sphingosine 1-phosphate receptor, S1P5 (Edg-8): structure-activity relationship of sphingosine1-phosphate receptors.
AID1346870Human GPR3 (Class A Orphans)2002Cellular signalling, Nov, Volume: 14, Issue:11
Sphingosine 1-phosphate is a ligand of the human gpr3, gpr6 and gpr12 family of constitutively active G protein-coupled receptors.
AID1346236Human S1P2 receptor (Lysophospholipid (S1P) receptors)2006Chemistry & biology, Nov, Volume: 13, Issue:11
A monoselective sphingosine-1-phosphate receptor-1 agonist prevents allograft rejection in a stringent rat heart transplantation model.
AID1346236Human S1P2 receptor (Lysophospholipid (S1P) receptors)1999The Journal of biological chemistry, Feb-19, Volume: 274, Issue:8
Sphingosine 1-phosphate-induced cell rounding and neurite retraction are mediated by the G protein-coupled receptor H218.
AID1346162Human S1P4 receptor (Lysophospholipid (S1P) receptors)2002The Journal of biological chemistry, Jun-14, Volume: 277, Issue:24
The immune modulator FTY720 targets sphingosine 1-phosphate receptors.
AID1346234Mouse S1P5 receptor (Lysophospholipid (S1P) receptors)2001Biochemistry, Nov-20, Volume: 40, Issue:46
Characterization of the human and mouse sphingosine 1-phosphate receptor, S1P5 (Edg-8): structure-activity relationship of sphingosine1-phosphate receptors.
AID1346162Human S1P4 receptor (Lysophospholipid (S1P) receptors)2004The Journal of biological chemistry, Apr-02, Volume: 279, Issue:14
Sphingosine 1-phosphate (S1P) receptor subtypes S1P1 and S1P3, respectively, regulate lymphocyte recirculation and heart rate.
AID1346229Rat S1P5 receptor (Lysophospholipid (S1P) receptors)2000The Journal of biological chemistry, May-12, Volume: 275, Issue:19
Characterization of a novel sphingosine 1-phosphate receptor, Edg-8.
AID1346205Human S1P3 receptor (Lysophospholipid (S1P) receptors)2007Molecular pharmacology, Mar, Volume: 71, Issue:3
Identification of Leu276 of the S1P1 receptor and Phe263 of the S1P3 receptor in interaction with receptor specific agonists by molecular modeling, site-directed mutagenesis, and affinity studies.
AID1346190Mouse S1P1 receptor (Lysophospholipid (S1P) receptors)2006Chemistry & biology, Nov, Volume: 13, Issue:11
A monoselective sphingosine-1-phosphate receptor-1 agonist prevents allograft rejection in a stringent rat heart transplantation model.
AID1346199Mouse S1P3 receptor (Lysophospholipid (S1P) receptors)2004The Journal of biological chemistry, Apr-02, Volume: 279, Issue:14
Sphingosine 1-phosphate (S1P) receptor subtypes S1P1 and S1P3, respectively, regulate lymphocyte recirculation and heart rate.
AID1346907Mouse GPR6 (Class A Orphans)2002Cellular signalling, Nov, Volume: 14, Issue:11
Sphingosine 1-phosphate is a ligand of the human gpr3, gpr6 and gpr12 family of constitutively active G protein-coupled receptors.
AID1346162Human S1P4 receptor (Lysophospholipid (S1P) receptors)2002Biochemical and biophysical research communications, Sep-27, Volume: 297, Issue:3
Phytosphingosine 1-phosphate: a high affinity ligand for the S1P(4)/Edg-6 receptor.
AID1346170Human S1P1 receptor (Lysophospholipid (S1P) receptors)2007Molecular pharmacology, Mar, Volume: 71, Issue:3
Identification of Leu276 of the S1P1 receptor and Phe263 of the S1P3 receptor in interaction with receptor specific agonists by molecular modeling, site-directed mutagenesis, and affinity studies.
AID1345173Human GPR63 (Class A Orphans)2003Cellular signalling, Apr, Volume: 15, Issue:4
Sphingosine 1-phosphate and dioleoylphosphatidic acid are low affinity agonists for the orphan receptor GPR63.
AID1346170Human S1P1 receptor (Lysophospholipid (S1P) receptors)2002The Journal of biological chemistry, Jun-14, Volume: 277, Issue:24
The immune modulator FTY720 targets sphingosine 1-phosphate receptors.
AID1346205Human S1P3 receptor (Lysophospholipid (S1P) receptors)1999The Journal of biological chemistry, Aug-20, Volume: 274, Issue:34
Comparison of intrinsic activities of the putative sphingosine 1-phosphate receptor subtypes to regulate several signaling pathways in their cDNA-transfected Chinese hamster ovary cells.
AID1346142Mouse S1P2 receptor (Lysophospholipid (S1P) receptors)2004The Journal of biological chemistry, Apr-02, Volume: 279, Issue:14
Sphingosine 1-phosphate (S1P) receptor subtypes S1P1 and S1P3, respectively, regulate lymphocyte recirculation and heart rate.
AID1345463Human P2RY10 (Class A Orphans)2008Biochemical and biophysical research communications, Jul-11, Volume: 371, Issue:4
Identification of the orphan GPCR, P2Y(10) receptor as the sphingosine-1-phosphate and lysophosphatidic acid receptor.
AID1346170Human S1P1 receptor (Lysophospholipid (S1P) receptors)1998The Journal of biological chemistry, Oct-16, Volume: 273, Issue:42
EDG1 is a functional sphingosine-1-phosphate receptor that is linked via a Gi/o to multiple signaling pathways, including phospholipase C activation, Ca2+ mobilization, Ras-mitogen-activated protein kinase activation, and adenylate cyclase inhibition.
AID1346236Human S1P2 receptor (Lysophospholipid (S1P) receptors)2001Biochemistry, Nov-20, Volume: 40, Issue:46
Characterization of the human and mouse sphingosine 1-phosphate receptor, S1P5 (Edg-8): structure-activity relationship of sphingosine1-phosphate receptors.
AID1346205Human S1P3 receptor (Lysophospholipid (S1P) receptors)2001Biochemistry, Nov-20, Volume: 40, Issue:46
Characterization of the human and mouse sphingosine 1-phosphate receptor, S1P5 (Edg-8): structure-activity relationship of sphingosine1-phosphate receptors.
AID1346170Human S1P1 receptor (Lysophospholipid (S1P) receptors)1999The Journal of biological chemistry, Aug-20, Volume: 274, Issue:34
Comparison of intrinsic activities of the putative sphingosine 1-phosphate receptor subtypes to regulate several signaling pathways in their cDNA-transfected Chinese hamster ovary cells.
AID1346236Human S1P2 receptor (Lysophospholipid (S1P) receptors)1999The Journal of biological chemistry, Aug-20, Volume: 274, Issue:34
Comparison of intrinsic activities of the putative sphingosine 1-phosphate receptor subtypes to regulate several signaling pathways in their cDNA-transfected Chinese hamster ovary cells.
AID1346185Mouse S1P4 receptor (Lysophospholipid (S1P) receptors)2004The Journal of biological chemistry, Apr-02, Volume: 279, Issue:14
Sphingosine 1-phosphate (S1P) receptor subtypes S1P1 and S1P3, respectively, regulate lymphocyte recirculation and heart rate.
AID1346190Mouse S1P1 receptor (Lysophospholipid (S1P) receptors)2004The Journal of biological chemistry, Apr-02, Volume: 279, Issue:14
Sphingosine 1-phosphate (S1P) receptor subtypes S1P1 and S1P3, respectively, regulate lymphocyte recirculation and heart rate.
AID1346242Human S1P5 receptor (Lysophospholipid (S1P) receptors)2002The Journal of biological chemistry, Jun-14, Volume: 277, Issue:24
The immune modulator FTY720 targets sphingosine 1-phosphate receptors.
AID1346205Human S1P3 receptor (Lysophospholipid (S1P) receptors)1999The Journal of biological chemistry, Feb-19, Volume: 274, Issue:8
Sphingosine 1-phosphate-induced cell rounding and neurite retraction are mediated by the G protein-coupled receptor H218.
AID1346205Human S1P3 receptor (Lysophospholipid (S1P) receptors)2006Chemistry & biology, Nov, Volume: 13, Issue:11
A monoselective sphingosine-1-phosphate receptor-1 agonist prevents allograft rejection in a stringent rat heart transplantation model.
AID1346170Human S1P1 receptor (Lysophospholipid (S1P) receptors)2004The Journal of biological chemistry, Apr-02, Volume: 279, Issue:14
Sphingosine 1-phosphate (S1P) receptor subtypes S1P1 and S1P3, respectively, regulate lymphocyte recirculation and heart rate.
AID1346907Mouse GPR6 (Class A Orphans)2003Biochemical and biophysical research communications, Nov-14, Volume: 311, Issue:2
Sphingosine-1-phosphate is a high-affinity ligand for the G protein-coupled receptor GPR6 from mouse and induces intracellular Ca2+ release by activating the sphingosine-kinase pathway.
AID1346162Human S1P4 receptor (Lysophospholipid (S1P) receptors)2006Chemistry & biology, Nov, Volume: 13, Issue:11
A monoselective sphingosine-1-phosphate receptor-1 agonist prevents allograft rejection in a stringent rat heart transplantation model.
AID1346904Human GPR12 (Class A Orphans)2002Cellular signalling, Nov, Volume: 14, Issue:11
Sphingosine 1-phosphate is a ligand of the human gpr3, gpr6 and gpr12 family of constitutively active G protein-coupled receptors.
AID1370457Displacement of [32P]S1P from recombinant human S1PR2 expressed in Chem1 cell membranes co-expressing Galpha15 pretreated for 30 mins followed by [32P]S1P addition measured after 60 mins by scintillation counting method2018Bioorganic & medicinal chemistry letters, 02-01, Volume: 28, Issue:3
Design and synthesis of pyrazolopyridine derivatives as sphingosine 1-phosphate receptor 2 ligands.
AID240300In vitro binding affinity towards human Sphingosine 1-phosphate receptor 1 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand2004Bioorganic & medicinal chemistry letters, Oct-04, Volume: 14, Issue:19
Synthesis of benzimidazole based analogues of sphingosine-1-phosphate: discovery of potent, subtype-selective S1P4 receptor agonists.
AID204167In vitro binding affinity towards human Sphingosine 1-phosphate receptor 4 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand; Not determined (Experiment 1)2003Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20
Synthesis of para-alkyl aryl amide analogues of sphingosine-1-phosphate: discovery of potent S1P receptor agonists.
AID498736Induction of human S1P1 receptor internalization expressed in CHO cells pretreated at 1 uM for 1 hr measured after 5 hrs washout period2009Nature chemical biology, Jun, Volume: 5, Issue:6
Persistent signaling induced by FTY720-phosphate is mediated by internalized S1P1 receptors.
AID476457Displacement of [33P]sphingosine-1-phosphate from human S1P1 receptor expressed in HEK293T cells after 60 mins by scintillation counting2010Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8
Exploration of amino alcohol derivatives as novel, potent, and highly selective sphingosine-1-phosphate receptor subtype-1 agonists.
AID1062161Selectivity ratio of EC50 for S1P3R (unknown origin) to EC50 for S1P1R (unknown origin)2013ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
Discovery of Clinical Candidate GSK1842799 As a Selective S1P1 Receptor Agonist (Prodrug) for Multiple Sclerosis.
AID240301In vitro binding affinity towards human Sphingosine 1-phosphate receptor 2 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand2004Bioorganic & medicinal chemistry letters, Oct-04, Volume: 14, Issue:19
Synthesis of benzimidazole based analogues of sphingosine-1-phosphate: discovery of potent, subtype-selective S1P4 receptor agonists.
AID240452Maximal efficacy against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay2005Bioorganic & medicinal chemistry letters, Aug-01, Volume: 15, Issue:15
Synthesis of 4(5)-phenylimidazole-based analogues of sphingosine-1-phosphate and FTY720: discovery of potent S1P1 receptor agonists.
AID721983Agonist activity at human S1P3 receptor expressed in HEK293T cells assessed as stimulation of [35S]GTPgammaS binding2013Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2
Exploring amino acids derivatives as potent, selective, and direct agonists of sphingosine-1-phosphate receptor subtype-1.
AID204054Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 3 expressed on CHO cell membranes2004Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
Potent S1P receptor agonists replicate the pharmacologic actions of the novel immune modulator FTY720.
AID481646Agonist activity at human recombinant S1P3 receptor expressed in HEK cells by GTPgammaS binding assay2010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
2-imino-thiazolidin-4-one derivatives as potent, orally active S1P1 receptor agonists.
AID1257230Agonist activity at human sphingosin-1-phosphate receptor 1 expressed in CHO cells assessed as phosphorylation status of p44/42 MAPK after 2.5 to 5 mins by Western blotting2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
New fluorinated agonists for targeting the sphingosin-1-phosphate receptor 1 (S1P(1)).
AID204032In vitro binding affinity towards human Sphingosine 1-phosphate receptor 1 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 1)2003Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20
Synthesis of para-alkyl aryl amide analogues of sphingosine-1-phosphate: discovery of potent S1P receptor agonists.
AID1203735Agonist activity at human S1P3 receptor overexpressed in CHO cells assessed as p44/42 MAPK phosphorylation at 1 uM by Western blot analysis2015Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8
Synthesis and evaluation of fluorinated fingolimod (FTY720) analogues for sphingosine-1-phosphate receptor molecular imaging by positron emission tomography.
AID240212Effective concentration against sphingosine 1-phosphate receptor 2 determined by a [c-35S]-GTP binding assay2005Bioorganic & medicinal chemistry letters, Aug-01, Volume: 15, Issue:15
Synthesis of 4(5)-phenylimidazole-based analogues of sphingosine-1-phosphate and FTY720: discovery of potent S1P1 receptor agonists.
AID240449Maximal efficacy against sphingosine 1-phosphate receptor 2 determined by a [c-35S]-GTP binding assay2005Bioorganic & medicinal chemistry letters, Aug-01, Volume: 15, Issue:15
Synthesis of 4(5)-phenylimidazole-based analogues of sphingosine-1-phosphate and FTY720: discovery of potent S1P1 receptor agonists.
AID1184690Agonist activity at S1P receptor in human PC3 cells assessed as increase in proliferation at 100 nM after 24 hrs by [3H]-thymidine incorporation assay2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Synthesis of fluorinated agonist of sphingosine-1-phosphate receptor 1.
AID240447Maximal efficacy against sphingosine-1-phosphate receptor 1 determined by a [c-35S]-GTP binding assay2005Bioorganic & medicinal chemistry letters, Aug-01, Volume: 15, Issue:15
Synthesis of 4(5)-phenylimidazole-based analogues of sphingosine-1-phosphate and FTY720: discovery of potent S1P1 receptor agonists.
AID498735Agonist activity at human S1P1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP formation at 1 uM after 60 mins2009Nature chemical biology, Jun, Volume: 5, Issue:6
Persistent signaling induced by FTY720-phosphate is mediated by internalized S1P1 receptors.
AID1271836Agonist activity at human S1P3 receptor expressed in EDG3-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assay2016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Late-stage optimization of a tercyclic class of S1P3-sparing, S1P1 receptor agonists.
AID476459Displacement of [33P]sphingosine-1-phosphate from human S1P4 receptor expressed in HEK293T cells after 60 mins by scintillation counting2010Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8
Exploration of amino alcohol derivatives as novel, potent, and highly selective sphingosine-1-phosphate receptor subtype-1 agonists.
AID305223Activity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay2007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
Constrained azacyclic analogues of the immunomodulatory agent FTY720 as molecular probes for sphingosine 1-phosphate receptors.
AID204047In vitro binding affinity towards human Sphingosine 1-phosphate receptor 3 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 1)2003Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20
Synthesis of para-alkyl aryl amide analogues of sphingosine-1-phosphate: discovery of potent S1P receptor agonists.
AID305220Activity at human recombinant S1P1 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay2007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
Constrained azacyclic analogues of the immunomodulatory agent FTY720 as molecular probes for sphingosine 1-phosphate receptors.
AID1370459Displacement of [32P]S1P from recombinant human S1PR3 expressed in Chem1 cell membranes co-expressing Galpha15 pretreated for 30 mins followed by [32P]S1P addition measured after 60 mins by scintillation counting method2018Bioorganic & medicinal chemistry letters, 02-01, Volume: 28, Issue:3
Design and synthesis of pyrazolopyridine derivatives as sphingosine 1-phosphate receptor 2 ligands.
AID282269Displacement of [33P]sphingosine 1 phosphate from human S1P3 receptor expressed in CHO cells2004Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27
A rational utilization of high-throughput screening affords selective, orally bioavailable 1-benzyl-3-carboxyazetidine sphingosine-1-phosphate-1 receptor agonists.
AID481650Displacement of [33P]S1P from human recombinant S1P2 receptor expressed in HEK cells by scintillation counting2010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
2-imino-thiazolidin-4-one derivatives as potent, orally active S1P1 receptor agonists.
AID282270Displacement of [33P]sphingosine 1 phosphate from human S1P4 receptor expressed in CHO cells2004Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27
A rational utilization of high-throughput screening affords selective, orally bioavailable 1-benzyl-3-carboxyazetidine sphingosine-1-phosphate-1 receptor agonists.
AID240213Effective concentration against sphingosine 1-phosphate receptor 3 determined by a [c-35S]-GTP binding assay2005Bioorganic & medicinal chemistry letters, Aug-01, Volume: 15, Issue:15
Synthesis of 4(5)-phenylimidazole-based analogues of sphingosine-1-phosphate and FTY720: discovery of potent S1P1 receptor agonists.
AID498734Agonist activity at human S1P1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP formation at 1 uM after 20 mins2009Nature chemical biology, Jun, Volume: 5, Issue:6
Persistent signaling induced by FTY720-phosphate is mediated by internalized S1P1 receptors.
AID204165In vitro binding affinity towards human Sphingosine 1-phosphate receptor 4 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 2)2003Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20
Synthesis of para-alkyl aryl amide analogues of sphingosine-1-phosphate: discovery of potent S1P receptor agonists.
AID1062165Agonist activity at human S1P2R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation counting2013ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
Discovery of Clinical Candidate GSK1842799 As a Selective S1P1 Receptor Agonist (Prodrug) for Multiple Sclerosis.
AID204048In vitro binding affinity towards human Sphingosine 1-phosphate receptor 3 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 2)2003Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20
Synthesis of para-alkyl aryl amide analogues of sphingosine-1-phosphate: discovery of potent S1P receptor agonists.
AID476460Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation counting2010Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8
Exploration of amino alcohol derivatives as novel, potent, and highly selective sphingosine-1-phosphate receptor subtype-1 agonists.
AID1271835Agonist activity at human S1P1 receptor expressed in EDG1-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assay2016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Late-stage optimization of a tercyclic class of S1P3-sparing, S1P1 receptor agonists.
AID476464Antagonist activity at human S1P3 receptor expressed in HEK293T cells assessed as inhibition of sphingosine-1-phosphate-induced gamma-[35S]GTP binding after 30 mins by scintillation counting2010Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8
Exploration of amino alcohol derivatives as novel, potent, and highly selective sphingosine-1-phosphate receptor subtype-1 agonists.
AID1203734Agonist activity at human S1P1 receptor overexpressed in CHO cells assessed as p44/42 MAPK phosphorylation at 1 uM by Western blot analysis2015Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8
Synthesis and evaluation of fluorinated fingolimod (FTY720) analogues for sphingosine-1-phosphate receptor molecular imaging by positron emission tomography.
AID392394Agonist activity at human S1P1 receptor assessed as stimulation of [35S]GTPgammaS binding2009Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2
Synthesis and evaluation of alkoxy-phenylamides and alkoxy-phenylimidazoles as potent sphingosine-1-phosphate receptor subtype-1 agonists.
AID255662Effective concentration required for [35S]GTP-gamma-S binding towards Sphingosine 1-phosphate receptor G-protein complex expressed in HEK293T cells2005Bioorganic & medicinal chemistry letters, Oct-15, Volume: 15, Issue:20
Synthesis, stability, and implications of phosphothioate agonists of sphingosine-1-phosphate receptors.
AID481645Agonist activity at human recombinant S1P2 receptor expressed in HEK cells by GTPgammaS binding assay2010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
2-imino-thiazolidin-4-one derivatives as potent, orally active S1P1 receptor agonists.
AID204176In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 1)2003Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20
Synthesis of para-alkyl aryl amide analogues of sphingosine-1-phosphate: discovery of potent S1P receptor agonists.
AID240302In vitro binding affinity towards human Sphingosine 1-phosphate receptor 3 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand2004Bioorganic & medicinal chemistry letters, Oct-04, Volume: 14, Issue:19
Synthesis of benzimidazole based analogues of sphingosine-1-phosphate: discovery of potent, subtype-selective S1P4 receptor agonists.
AID1062162Agonist activity at human S1P5R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation counting2013ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
Discovery of Clinical Candidate GSK1842799 As a Selective S1P1 Receptor Agonist (Prodrug) for Multiple Sclerosis.
AID240450Maximal efficacy against sphingosine 1-phosphate receptor 3 determined by a [c-35S]-GTP binding assay2005Bioorganic & medicinal chemistry letters, Aug-01, Volume: 15, Issue:15
Synthesis of 4(5)-phenylimidazole-based analogues of sphingosine-1-phosphate and FTY720: discovery of potent S1P1 receptor agonists.
AID476463Antagonist activity at human S1P1 receptor expressed in HEK293T cells assessed as inhibition of sphingosine-1-phosphate-induced gamma-[35S]GTP binding after 30 mins by scintillation counting2010Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8
Exploration of amino alcohol derivatives as novel, potent, and highly selective sphingosine-1-phosphate receptor subtype-1 agonists.
AID481644Agonist activity at human recombinant S1P1 receptor expressed in HEK cells by GTPgammaS binding assay2010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
2-imino-thiazolidin-4-one derivatives as potent, orally active S1P1 receptor agonists.
AID392390Displacement of [33P]sphingosine-1-phosphate from human S1P3 receptor2009Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2
Synthesis and evaluation of alkoxy-phenylamides and alkoxy-phenylimidazoles as potent sphingosine-1-phosphate receptor subtype-1 agonists.
AID240451Maximal efficacy against sphingosine 1-phosphate receptor 4 determined by a [c-35S]-GTP binding assay2005Bioorganic & medicinal chemistry letters, Aug-01, Volume: 15, Issue:15
Synthesis of 4(5)-phenylimidazole-based analogues of sphingosine-1-phosphate and FTY720: discovery of potent S1P1 receptor agonists.
AID1176771Activation of Inward rectifier potassium channel in human atrial myocytes2014ACS medicinal chemistry letters, Dec-11, Volume: 5, Issue:12
(7-Benzyloxy-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetic Acids as S1P1 Functional Antagonists.
AID481651Displacement of [33P]S1P from human recombinant S1P3 receptor expressed in HEK cells by scintillation counting2010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
2-imino-thiazolidin-4-one derivatives as potent, orally active S1P1 receptor agonists.
AID1062166Agonist activity at human S1P1R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation counting2013ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
Discovery of Clinical Candidate GSK1842799 As a Selective S1P1 Receptor Agonist (Prodrug) for Multiple Sclerosis.
AID240214Effective concentration against sphingosine 1-phosphate receptor 4 determined by a [c-35S]-GTP binding assay2005Bioorganic & medicinal chemistry letters, Aug-01, Volume: 15, Issue:15
Synthesis of 4(5)-phenylimidazole-based analogues of sphingosine-1-phosphate and FTY720: discovery of potent S1P1 receptor agonists.
AID1165186Agonist activity at S1P2/3 receptor in HEK293 cells assessed as inhibition of forskolin-induced cAMP level after 1 hr by alphascreen immunoassay2014Bioorganic & medicinal chemistry letters, Oct-15, Volume: 24, Issue:20
The design and implementation of a generic lipopeptide scanning platform to enable the identification of 'locally acting' agonists for the apelin receptor.
AID473717Agonist activity at human S1P1 receptor assessed as effect on calcium mobilization by Gi dependent whole cell assay2010Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7
Stereochemistry-activity relationship of orally active tetralin S1P agonist prodrugs.
AID1370460Displacement of [32P]S1P from recombinant human S1PR4 expressed in cell membranes pretreated for 30 mins followed by [32P]S1P addition measured after 60 mins by scintillation counting method2018Bioorganic & medicinal chemistry letters, 02-01, Volume: 28, Issue:3
Design and synthesis of pyrazolopyridine derivatives as sphingosine 1-phosphate receptor 2 ligands.
AID392389Displacement of [33P]sphingosine-1-phosphate from human S1P1 receptor2009Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2
Synthesis and evaluation of alkoxy-phenylamides and alkoxy-phenylimidazoles as potent sphingosine-1-phosphate receptor subtype-1 agonists.
AID642403Agonist activity at human S1P1 receptor expressed in human U2OS cells co-expressing eGFP assessed as receptor internalization into cytoplasm using Hoechst dye staining2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
Quinolinone-based agonists of S1P₁: use of a N-scan SAR strategy to optimize in vitro and in vivo activity.
AID481647Agonist activity at human recombinant S1P4 receptor expressed in CHO cells by GTPgammaS binding assay2010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
2-imino-thiazolidin-4-one derivatives as potent, orally active S1P1 receptor agonists.
AID204039In vitro binding affinity towards human Sphingosine 1-phosphate receptor 2 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 1)2003Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20
Synthesis of para-alkyl aryl amide analogues of sphingosine-1-phosphate: discovery of potent S1P receptor agonists.
AID1853952Displacement of [32P]S1P from human recombinant S1PR5 incubated for 60 mins by competitive binding assay based scintillation counter2022RSC medicinal chemistry, Feb-23, Volume: 13, Issue:2
Synthesis and evaluation of highly selective quinazoline-2,4-dione ligands for sphingosine-1-phosphate receptor 2.
AID204174Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes2004Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
Potent S1P receptor agonists replicate the pharmacologic actions of the novel immune modulator FTY720.
AID240304In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand2004Bioorganic & medicinal chemistry letters, Oct-04, Volume: 14, Issue:19
Synthesis of benzimidazole based analogues of sphingosine-1-phosphate: discovery of potent, subtype-selective S1P4 receptor agonists.
AID1296151Induction of internalization of C-terminal GFP-fused human S1P1 receptor expressed in CHO cell membranes assessed as remaining receptor level in cell membrane at 1.2 uM preincubated for 50 mins followed by compound washout measured at 4 hrs relative to co2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Potent and Selective Agonists of Sphingosine 1-Phosphate 1 (S1P1): Discovery and SAR of a Novel Isoxazole Based Series.
AID305221Activity at human recombinant S1P3 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay2007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
Constrained azacyclic analogues of the immunomodulatory agent FTY720 as molecular probes for sphingosine 1-phosphate receptors.
AID498737Agonist activity at human S1P1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP formation pretreated at 1 uM for 1 hr measured after 5 hrs washout peroid2009Nature chemical biology, Jun, Volume: 5, Issue:6
Persistent signaling induced by FTY720-phosphate is mediated by internalized S1P1 receptors.
AID481652Displacement of [33P]S1P from human recombinant S1P4 receptor expressed in CHO cells by scintillation counting2010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
2-imino-thiazolidin-4-one derivatives as potent, orally active S1P1 receptor agonists.
AID721982Agonist activity at human S1P1 receptor expressed in HEK293T cells assessed as stimulation of [35S]GTPgammaS binding2013Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2
Exploring amino acids derivatives as potent, selective, and direct agonists of sphingosine-1-phosphate receptor subtype-1.
AID240202Effective concentration against sphingosine-1-phosphate receptor 1 determined by a [c-35S]-GTP binding assay2005Bioorganic & medicinal chemistry letters, Aug-01, Volume: 15, Issue:15
Synthesis of 4(5)-phenylimidazole-based analogues of sphingosine-1-phosphate and FTY720: discovery of potent S1P1 receptor agonists.
AID481648Agonist activity at human recombinant S1P5 receptor expressed in CHO cells by GTPgammaS binding assay2010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
2-imino-thiazolidin-4-one derivatives as potent, orally active S1P1 receptor agonists.
AID282267Displacement of [33P]sphingosine 1 phosphate from human S1P1 receptor expressed in CHO cells2004Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27
A rational utilization of high-throughput screening affords selective, orally bioavailable 1-benzyl-3-carboxyazetidine sphingosine-1-phosphate-1 receptor agonists.
AID1184691Agonist activity at S1P receptor in human C4-2B cells assessed as increase in proliferation at 100 nM after 24 hrs by [3H]-thymidine incorporation assay2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Synthesis of fluorinated agonist of sphingosine-1-phosphate receptor 1.
AID481649Displacement of [33P]S1P from human recombinant S1P1 receptor expressed in HEK cells by scintillation counting2010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
2-imino-thiazolidin-4-one derivatives as potent, orally active S1P1 receptor agonists.
AID282271Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells2004Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27
A rational utilization of high-throughput screening affords selective, orally bioavailable 1-benzyl-3-carboxyazetidine sphingosine-1-phosphate-1 receptor agonists.
AID204040In vitro binding affinity towards human Sphingosine 1-phosphate receptor 2 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 2)2003Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20
Synthesis of para-alkyl aryl amide analogues of sphingosine-1-phosphate: discovery of potent S1P receptor agonists.
AID1853951Displacement of [32P]S1P from human recombinant S1PR4 incubated for 60 mins by competitive binding assay based scintillation counter2022RSC medicinal chemistry, Feb-23, Volume: 13, Issue:2
Synthesis and evaluation of highly selective quinazoline-2,4-dione ligands for sphingosine-1-phosphate receptor 2.
AID1062164Agonist activity at human S1P3R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation counting2013ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
Discovery of Clinical Candidate GSK1842799 As a Selective S1P1 Receptor Agonist (Prodrug) for Multiple Sclerosis.
AID1062163Agonist activity at human S1P4R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation counting2013ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
Discovery of Clinical Candidate GSK1842799 As a Selective S1P1 Receptor Agonist (Prodrug) for Multiple Sclerosis.
AID305222Activity at human recombinant S1P4 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay2007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
Constrained azacyclic analogues of the immunomodulatory agent FTY720 as molecular probes for sphingosine 1-phosphate receptors.
AID1370461Displacement of [32P]S1P from recombinant human S1PR5 expressed in cell membranes pretreated for 30 mins followed by [32P]S1P addition measured after 60 mins by scintillation counting method2018Bioorganic & medicinal chemistry letters, 02-01, Volume: 28, Issue:3
Design and synthesis of pyrazolopyridine derivatives as sphingosine 1-phosphate receptor 2 ligands.
AID204033In vitro binding affinity towards human Sphingosine 1-phosphate receptor 1 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand. (Experiment 2)2003Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20
Synthesis of para-alkyl aryl amide analogues of sphingosine-1-phosphate: discovery of potent S1P receptor agonists.
AID204177In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 2)2003Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20
Synthesis of para-alkyl aryl amide analogues of sphingosine-1-phosphate: discovery of potent S1P receptor agonists.
AID1176678Activation of Inward rectifier potassium channel in human atrial myocytes2014ACS medicinal chemistry letters, Dec-11, Volume: 5, Issue:12
Discovery of APD334: Design of a Clinical Stage Functional Antagonist of the Sphingosine-1-phosphate-1 Receptor.
AID204037Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 1 expressed on CHO cell membranes2004Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
Potent S1P receptor agonists replicate the pharmacologic actions of the novel immune modulator FTY720.
AID481653Displacement of [33P]S1P from human recombinant S1P5 receptor expressed in CHO cells by scintillation counting2010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
2-imino-thiazolidin-4-one derivatives as potent, orally active S1P1 receptor agonists.
AID473718Agonist activity at human S1P3 receptor assessed as effect on calcium mobilization by Gi dependent whole cell assay2010Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7
Stereochemistry-activity relationship of orally active tetralin S1P agonist prodrugs.
AID240215Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay2005Bioorganic & medicinal chemistry letters, Aug-01, Volume: 15, Issue:15
Synthesis of 4(5)-phenylimidazole-based analogues of sphingosine-1-phosphate and FTY720: discovery of potent S1P1 receptor agonists.
AID392395Agonist activity at human S1P3 receptor assessed as stimulation of [35S]GTPgammaS binding2009Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2
Synthesis and evaluation of alkoxy-phenylamides and alkoxy-phenylimidazoles as potent sphingosine-1-phosphate receptor subtype-1 agonists.
AID282268Displacement of [33P]sphingosine 1 phosphate from human S1P2 receptor expressed in CHO cells2004Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27
A rational utilization of high-throughput screening affords selective, orally bioavailable 1-benzyl-3-carboxyazetidine sphingosine-1-phosphate-1 receptor agonists.
AID1296152Induction of internalization of C-terminal GFP-fused human S1P1 receptor expressed in CHO cell membranes assessed as remaining receptor level in cell membrane at 1.2 uM preincubated for 50 mins followed by compound washout measured at 16 hrs relative to c2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Potent and Selective Agonists of Sphingosine 1-Phosphate 1 (S1P1): Discovery and SAR of a Novel Isoxazole Based Series.
AID1853949Displacement of [32P]S1P from human recombinant S1PR1 incubated for 60 mins by competitive binding assay based scintillation counter2022RSC medicinal chemistry, Feb-23, Volume: 13, Issue:2
Synthesis and evaluation of highly selective quinazoline-2,4-dione ligands for sphingosine-1-phosphate receptor 2.
AID1296150Induction of internalization of C-terminal GFP-fused human S1P1 receptor expressed in CHO cell membranes at 1.2 uM after 50 mins relative to control2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Potent and Selective Agonists of Sphingosine 1-Phosphate 1 (S1P1): Discovery and SAR of a Novel Isoxazole Based Series.
AID642478Agonist activity at human S1P1 receptor expressed in human U2OS cells co-expressing eGFP assessed as receptor internalization into cytoplasm using Hoechst dye staining relative to 1-(4-(6-benzylbenzofuran-2-yl)-3- fluorobenzyl)azetidine-3-carboxylic acid2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
Quinolinone-based agonists of S1P₁: use of a N-scan SAR strategy to optimize in vitro and in vivo activity.
AID476458Displacement of [33P]sphingosine-1-phosphate from human S1P3 receptor expressed in HEK293T cells after 60 mins by scintillation counting2010Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8
Exploration of amino alcohol derivatives as novel, potent, and highly selective sphingosine-1-phosphate receptor subtype-1 agonists.
AID392391Displacement of [33P]sphingosine-1-phosphate from human S1P4 receptor2009Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2
Synthesis and evaluation of alkoxy-phenylamides and alkoxy-phenylimidazoles as potent sphingosine-1-phosphate receptor subtype-1 agonists.
AID204055Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 4 expressed on CHO cell membranes2004Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
Potent S1P receptor agonists replicate the pharmacologic actions of the novel immune modulator FTY720.
AID1853950Displacement of [32P]S1P from human recombinant S1PR3 incubated for 60 mins by competitive binding assay based scintillation counter2022RSC medicinal chemistry, Feb-23, Volume: 13, Issue:2
Synthesis and evaluation of highly selective quinazoline-2,4-dione ligands for sphingosine-1-phosphate receptor 2.
AID1176592Agonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assay2014ACS medicinal chemistry letters, Dec-11, Volume: 5, Issue:12
Discovery of APD334: Design of a Clinical Stage Functional Antagonist of the Sphingosine-1-phosphate-1 Receptor.
AID240303In vitro binding affinity towards human Sphingosine 1-phosphate receptor 4 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand2004Bioorganic & medicinal chemistry letters, Oct-04, Volume: 14, Issue:19
Synthesis of benzimidazole based analogues of sphingosine-1-phosphate: discovery of potent, subtype-selective S1P4 receptor agonists.
AID1370458Displacement of [32P]S1P from recombinant human S1PR1 expressed in CHOK1 cell membranes pretreated for 30 mins followed by [32P]S1P addition measured after 60 mins by scintillation counting method2018Bioorganic & medicinal chemistry letters, 02-01, Volume: 28, Issue:3
Design and synthesis of pyrazolopyridine derivatives as sphingosine 1-phosphate receptor 2 ligands.
AID392396Ratio of EC50 for human S1P3 receptor to EC50 for human S1P1 receptor2009Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2
Synthesis and evaluation of alkoxy-phenylamides and alkoxy-phenylimidazoles as potent sphingosine-1-phosphate receptor subtype-1 agonists.
AID498733Induction of human S1P1 receptor internalization expressed in CHO cells at 1 uM after 60 mins2009Nature chemical biology, Jun, Volume: 5, Issue:6
Persistent signaling induced by FTY720-phosphate is mediated by internalized S1P1 receptors.
AID1853948Displacement of [32P]S1P from human recombinant S1PR2 incubated for 60 mins by competitive binding assay based scintillation counter2022RSC medicinal chemistry, Feb-23, Volume: 13, Issue:2
Synthesis and evaluation of highly selective quinazoline-2,4-dione ligands for sphingosine-1-phosphate receptor 2.
AID392392Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptor2009Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2
Synthesis and evaluation of alkoxy-phenylamides and alkoxy-phenylimidazoles as potent sphingosine-1-phosphate receptor subtype-1 agonists.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (3,743)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901 (0.03)18.7374
1990's180 (4.81)18.2507
2000's1241 (33.16)29.6817
2010's1799 (48.06)24.3611
2020's522 (13.95)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 43.54

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index43.54 (24.57)
Research Supply Index8.25 (2.92)
Research Growth Index6.91 (4.65)
Search Engine Demand Index124.52 (26.88)
Search Engine Supply Index3.70 (0.95)

This Compound (43.54)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials23 (0.61%)5.53%
Reviews744 (19.60%)6.00%
Case Studies2 (0.05%)4.05%
Observational10 (0.26%)0.25%
Other3,017 (79.48%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]