fty 720p profile

fingolimod phosphate : A primary amino compound that is fingolimod in which one on the hydroxy groups has been converted into its dihydrogen phosphate derivative. It is the active metabolite of fingolimod. [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]

ID Source	ID
PubMed CID	11452022
CHEMBL ID	366208
SCHEMBL ID	4267565
MeSH ID	M0516545
PubMed CID	9908268
CHEMBL ID	114606
CHEBI ID	73420
SCHEMBL ID	80475
MeSH ID	M0516545

Synonym
(s)-fty720p
[(2s)-2-amino-3-hydroxy-2-[2-(4-octylphenyl)ethyl]propoxy]phosphonic acid
chembl366208 ,
bdbm23165
fty720-phosphate, (s)-2
fty-720p
402616-26-6
(s) fty720 phosphate
(s)-fty720-phosphate
[(2s)-2-amino-2-(hydroxymethyl)-4-(4-octylphenyl)butyl] dihydrogen phosphate
gtpl6996
SCHEMBL4267565
fingolimod p
(s)-fty 720p
aml629
(+)-(s)-fty 720 phosphate
fty720 (s)-phosphate
1,3-propanediol, 2-amino-2-(2-(4-octylphenyl)ethyl)-, 1-(dihydrogen phosphate), (2s)-
92YDM6122J ,
fingolimod phosphate ester, (s)-
1,3-propanediol, 2-amino-2-(2-(4-octylphenyl)ethyl)-, mono(dihydrogen phosphate) (ester), (2s)-
unii-92ydm6122j
(s)-2-amino-2-(hydroxymethyl)-4-(4-octylphenyl)butyl dihydrogen phosphate
s-fingolimod phosphate ester
Q27088789
AS-16872
fingolimod phosphate ester, s-
CS-0006041
HY-15382
(s)-fty720p;(s)-fty720 phosphate
C90298
(2s)- amino-2-[2-(4-octylphenyl)ethyl]-1-(dihydrogen phosphate)-1,3-propanediol
AKOS037643556
J89 ,
(s)-2-amino-2-(hydroxymethyl)-4-(4-octylphenyl)butyldihydrogenphosphate
1,3-propanediol, 2-amino-2-[2-(4-octylphenyl)ethyl]-, 1-(dihydrogen phosphate), (2s)-
DTXSID801127241
fingolimod-phosphate
fty-p
[2-amino-2-(hydroxymethyl)-4-(4-octylphenyl)butyl] dihydrogen phosphate
gtpl2924
fingolimod phosphate
chembl114606 ,
fty720-phosphate, rac-2
{2-amino-3-hydroxy-2-[2-(4-octylphenyl)ethyl]propoxy}phosphonic acid
bdbm23163
fty-720-p
chebi:73420 ,
2-amino-2-({[dihydroxy(oxido)-$l^{5}-phosphanyl]oxy}methyl)-4-(4-octylphenyl)butan-1-ol
bdbm50152337
fty720-p
fty720-phosphate
FT-0668885
FT-0668884
2-amino-2-(hydroxymethyl)-4-(4-octylphenyl)butyl dihydrogen phosphate
fingolimod-p
fty720 phosphate
402616-23-3
fty720 (r)-phosphate
402615-91-2
rac fty720 phosphate
SCHEMBL80475
DTXSID20432703
rac fty 720 phosphate
2-adamantylacrylate
phosphoric acid mono-[2-amino-2-hydroxymethyl-4-(4-octyl-phenyl)-butyl] ester
phosphoric acid mono-[(r/s)-2-amino-2-hydroxymethyl-4-(4-octyl-phenyl)-butyl]ester
phosphoric acid mono-[2-amino-2-hydroxymethyl-4-(4-octyl-phenyl)-butyl]ester
Q27077754
BCP10789
ES-2595
2- amino- 2[2- (4- octylphenyl)ethyl]- 1, 3- propanediol, mono dihydrogen phosphate ester
AKOS037652817
HY-15381
CS-0006040
(2~{s})-2-azanyl-4-(4-octylphenyl)-2-[[oxidanyl-bis(oxidanylidene)-$l^{6}-phosphanyl]oxymethyl]butan-1-ol

Excerpt	Reference	Relevance
" It demonstrated a good in vitro ADME profile and excellent oral bioavailability across species."	( Benzofuran Derivatives as Potent, Orally Active S1P1 Receptor Agonists: A Preclinical Lead Molecule for MS. Bürli, RW; Buys, J; Chereku, S; Horner, M; Lin, J; Lobera, M; Marantz, Y; McCauley, D; McElvain, M; Middleton, S; Saha, AK; Salyers, K; Schrag, M; Schutz, N; Segal, D; Sharadendu, A; Siu, J; Vargas, HM; Xu, H; Xu, Y; Yu, X, 2011)	0.37
" 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

Excerpt	Relevance	Reference
" Herein we describe the development of a series of selective S1P5 agonists that led to the identification of compound 29, which is highly selective for S1P5 and has excellent plasma and CNS exposure after oral dosing in preclinical species."	( Discovery of A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders. Abibi, A; Aguirre, AL; Bousquet, P; Gintant, G; Harris, CM; Hobson, AD; Kebede, T; Kim, Y; Konopacki, DB; Larson, K; Maull, JW; Moore, NS; Sarris, KK; Shi, D; Shrestha, A; Tang, X; Turner, SC; van der Kam, EL; Zhang, P, 2015)	0.42

Role	Description
antineoplastic agent	A substance that inhibits or prevents the proliferation of neoplasms.
immunosuppressive agent	An agent that suppresses immune function by one of several mechanisms of action. Classical cytotoxic immunosuppressants act by inhibiting DNA synthesis. Others may act through activation of T-cells or by inhibiting the activation of helper cells. In addition, an immunosuppressive agent is a role played by a compound which is exhibited by a capability to diminish the extent and/or voracity of an immune response.
sphingosine-1-phosphate receptor agonist	An agonist that binds to and activates sphingosine 1-phosphate receptors.
[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]

Class	Description
monoalkyl phosphate
primary amino compound	A compound formally derived from ammonia by replacing one hydrogen atom by an organyl group.
primary alcohol	A primary alcohol is a compound in which a hydroxy group, -OH, is attached to a saturated carbon atom which has either three hydrogen atoms attached to it or only one other carbon atom and two hydrogen atoms attached to it.
[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]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Sphingosine 1-phosphate receptor 2	Homo sapiens (human)	IC50 (µMol)	0.0059	0.0002	0.1042	1.1000	AID639282
Sphingosine 1-phosphate receptor 2	Homo sapiens (human)	Ki	0.2066	0.0021	0.0114	0.0370	AID1798300
Sphingosine 1-phosphate receptor 4	Homo sapiens (human)	IC50 (µMol)	0.0022	0.0010	0.1068	0.4170	AID639284
Sphingosine 1-phosphate receptor 4	Homo sapiens (human)	Ki	0.2066	0.0021	0.0114	0.0370	AID1798300
Sphingosine 1-phosphate receptor 1	Homo sapiens (human)	IC50 (µMol)	0.0008	0.0000	0.0855	0.8400	AID1735816; AID553425; AID639281
Sphingosine 1-phosphate receptor 1	Homo sapiens (human)	Ki	0.2066	0.0021	0.0114	0.0370	AID1798300
Sphingosine 1-phosphate receptor 3	Homo sapiens (human)	IC50 (µMol)	0.0147	0.0000	0.0045	0.0230	AID553426; AID639283
Sphingosine 1-phosphate receptor 3	Homo sapiens (human)	Ki	0.2066	0.0021	0.0114	0.0370	AID1798300
Sphingosine 1-phosphate receptor 5	Homo sapiens (human)	Ki	0.2066	0.0021	0.0114	0.0370	AID1798300
Sphingosine 1-phosphate receptor 2	Homo sapiens (human)	IC50 (µMol)	0.5504	0.0002	0.1042	1.1000	AID204174; AID282268
Sphingosine 1-phosphate receptor 2	Homo sapiens (human)	Ki	0.2117	0.0021	0.0114	0.0370	AID1798300
Sphingosine 1-phosphate receptor 4	Homo sapiens (human)	IC50 (µMol)	0.0150	0.0010	0.1068	0.4170	AID204055; AID282270
Sphingosine 1-phosphate receptor 4	Homo sapiens (human)	Ki	0.2117	0.0021	0.0114	0.0370	AID1798300
Sphingosine 1-phosphate receptor 1	Homo sapiens (human)	IC50 (µMol)	0.0001	0.0000	0.0855	0.8400	AID1300062; AID1730770; AID204037; AID282267
Sphingosine 1-phosphate receptor 1	Homo sapiens (human)	Ki	0.2117	0.0021	0.0114	0.0370	AID1798300
Sodium-dependent serotonin transporter	Homo sapiens (human)	IC50 (µMol)	0.0150	0.0001	0.8645	8.7096	AID204055
Sphingosine 1-phosphate receptor 3	Homo sapiens (human)	IC50 (µMol)	0.0063	0.0000	0.0045	0.0230	AID204054; AID282269
Sphingosine 1-phosphate receptor 3	Homo sapiens (human)	Ki	0.2117	0.0021	0.0114	0.0370	AID1798300
Sphingosine 1-phosphate receptor 5	Homo sapiens (human)	IC50 (µMol)	0.0008	0.0005	0.8388	4.6000	AID282271
Sphingosine 1-phosphate receptor 5	Homo sapiens (human)	Ki	0.2117	0.0021	0.0114	0.0370	AID1798300
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Sphingosine 1-phosphate receptor 2	Homo sapiens (human)	EC50 (µMol)	11.6570	0.0007	0.3651	2.8530	AID1719746; AID240248; AID473720; AID620822
Sphingosine 1-phosphate receptor 4	Homo sapiens (human)	EC50 (µMol)	0.0492	0.0001	0.2626	3.2500	AID1719748; AID1735827; AID240250; AID473722; AID620521
Sphingosine 1-phosphate receptor 1	Homo sapiens (human)	EC50 (µMol)	0.0035	0.0000	0.1759	7.8700	AID1176592; AID1179536; AID1271835; AID1280938; AID1280940; AID1296149; AID1432802; AID1719745; AID1735818; AID1735820; AID1735822; AID1735824; AID240247; AID473717; AID473719; AID620821; AID645085; AID648581; AID662677
Type-1 angiotensin II receptor	Oryctolagus cuniculus (rabbit)	EC50 (µMol)	0.0003	0.0003	0.0003	0.0003	AID645091
Sphingosine 1-phosphate receptor 1	Rattus norvegicus (Norway rat)	EC50 (µMol)	0.0003	0.0003	0.0007	0.0015	AID645087; AID648579
Sphingosine 1-phosphate receptor 3	Homo sapiens (human)	EC50 (µMol)	0.0147	0.0001	0.3092	5.0000	AID1179537; AID1271836; AID1280939; AID1432803; AID1719747; AID1735826; AID240249; AID473718; AID473721; AID620823; AID642466; AID645086; AID648582; AID662676
Sphingosine 1-phosphate receptor 5	Homo sapiens (human)	EC50 (µMol)	0.0109	0.0002	0.1365	3.1623	AID1719749; AID1735828; AID240251; AID473723; AID620490; AID645091
Sphingosine 1-phosphate receptor 2	Homo sapiens (human)	EC50 (µMol)	10.0000	0.0007	0.3651	2.8530	AID240248
Sphingosine 1-phosphate receptor 4	Homo sapiens (human)	EC50 (µMol)	0.0098	0.0001	0.2626	3.2500	AID1300069; AID1730779; AID240214; AID240250; AID284812
Cytochrome P450 3A4	Homo sapiens (human)	EC50 (µMol)	0.0001	0.0001	0.2328	3.2000	AID1300069
Sphingosine 1-phosphate receptor 1	Homo sapiens (human)	EC50 (µMol)	0.0013	0.0000	0.1759	7.8700	AID1185979; AID1300063; AID1300064; AID1300065; AID1300066; AID1668168; AID1730772; AID1730774; AID1730776; AID1901408; AID1901409; AID240202; AID240247; AID282274; AID284809; AID475240
Sphingosine 1-phosphate receptor 3	Homo sapiens (human)	EC50 (µMol)	0.0188	0.0001	0.3092	5.0000	AID1185980; AID1300068; AID1668169; AID1730778; AID1901410; AID240213; AID240249; AID284811; AID475241
Sphingosine 1-phosphate receptor 5	Homo sapiens (human)	EC50 (µMol)	0.0092	0.0002	0.1365	3.1623	AID1264633; AID1264634; AID1300070; AID1730780; AID240215; AID240251; AID284813
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Sphingosine 1-phosphate receptor 1	Homo sapiens (human)	Activity	0.0072	0.0012	0.0072	0.0133	AID1062172; AID1062173
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
G protein-coupled receptor signaling pathway	Sphingosine 1-phosphate receptor 2	Homo sapiens (human)
sphingosine-1-phosphate receptor signaling pathway	Sphingosine 1-phosphate receptor 2	Homo sapiens (human)
positive regulation of cell population proliferation	Sphingosine 1-phosphate receptor 2	Homo sapiens (human)
positive regulation of peptidyl-threonine phosphorylation	Sphingosine 1-phosphate receptor 2	Homo sapiens (human)
actin cytoskeleton organization	Sphingosine 1-phosphate receptor 2	Homo sapiens (human)
filopodium assembly	Sphingosine 1-phosphate receptor 2	Homo sapiens (human)
excitatory postsynaptic potential	Sphingosine 1-phosphate receptor 2	Homo sapiens (human)
negative regulation of excitatory postsynaptic potential	Sphingosine 1-phosphate receptor 2	Homo sapiens (human)
positive regulation of establishment of endothelial barrier	Sphingosine 1-phosphate receptor 2	Homo sapiens (human)
regulation of metabolic process	Sphingosine 1-phosphate receptor 2	Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathway	Sphingosine 1-phosphate receptor 2	Homo sapiens (human)
sphingosine-1-phosphate receptor signaling pathway	Sphingosine 1-phosphate receptor 4	Homo sapiens (human)
immune response	Sphingosine 1-phosphate receptor 4	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Sphingosine 1-phosphate receptor 4	Homo sapiens (human)
activation of phospholipase C activity	Sphingosine 1-phosphate receptor 4	Homo sapiens (human)
positive regulation of cytosolic calcium ion concentration	Sphingosine 1-phosphate receptor 4	Homo sapiens (human)
regulation of metabolic process	Sphingosine 1-phosphate receptor 4	Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathway	Sphingosine 1-phosphate receptor 4	Homo sapiens (human)
blood vessel maturation	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
cardiac muscle tissue growth involved in heart morphogenesis	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
sphingosine-1-phosphate receptor signaling pathway	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
chemotaxis	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
cell adhesion	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
brain development	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
cell population proliferation	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
cell migration	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
transmission of nerve impulse	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
lamellipodium assembly	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
actin cytoskeleton organization	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
regulation of cell adhesion	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
neuron differentiation	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
positive regulation of cell migration	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
regulation of bone mineralization	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
leukocyte chemotaxis	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
regulation of bone resorption	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
endothelial cell differentiation	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
positive regulation of smooth muscle cell proliferation	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
positive regulation of positive chemotaxis	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
negative regulation of stress fiber assembly	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
heart trabecula morphogenesis	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
T cell migration	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
angiogenesis	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
regulation of metabolic process	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathway	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
sphingosine-1-phosphate receptor signaling pathway	Sphingosine 1-phosphate receptor 3	Homo sapiens (human)
inflammatory response	Sphingosine 1-phosphate receptor 3	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Sphingosine 1-phosphate receptor 3	Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway	Sphingosine 1-phosphate receptor 3	Homo sapiens (human)
positive regulation of cytosolic calcium ion concentration	Sphingosine 1-phosphate receptor 3	Homo sapiens (human)
Notch signaling pathway	Sphingosine 1-phosphate receptor 3	Homo sapiens (human)
positive regulation of cell population proliferation	Sphingosine 1-phosphate receptor 3	Homo sapiens (human)
anatomical structure morphogenesis	Sphingosine 1-phosphate receptor 3	Homo sapiens (human)
regulation of interleukin-1 beta production	Sphingosine 1-phosphate receptor 3	Homo sapiens (human)
negative regulation of establishment of endothelial barrier	Sphingosine 1-phosphate receptor 3	Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathway	Sphingosine 1-phosphate receptor 3	Homo sapiens (human)
regulation of metabolic process	Sphingosine 1-phosphate receptor 3	Homo sapiens (human)
sphingosine-1-phosphate receptor signaling pathway	Sphingosine 1-phosphate receptor 5	Homo sapiens (human)
regulation of neuron differentiation	Sphingosine 1-phosphate receptor 5	Homo sapiens (human)
regulation of metabolic process	Sphingosine 1-phosphate receptor 5	Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathway	Sphingosine 1-phosphate receptor 5	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Sphingosine 1-phosphate receptor 2	Homo sapiens (human)
sphingosine-1-phosphate receptor signaling pathway	Sphingosine 1-phosphate receptor 2	Homo sapiens (human)
positive regulation of cell population proliferation	Sphingosine 1-phosphate receptor 2	Homo sapiens (human)
positive regulation of peptidyl-threonine phosphorylation	Sphingosine 1-phosphate receptor 2	Homo sapiens (human)
actin cytoskeleton organization	Sphingosine 1-phosphate receptor 2	Homo sapiens (human)
filopodium assembly	Sphingosine 1-phosphate receptor 2	Homo sapiens (human)
excitatory postsynaptic potential	Sphingosine 1-phosphate receptor 2	Homo sapiens (human)
negative regulation of excitatory postsynaptic potential	Sphingosine 1-phosphate receptor 2	Homo sapiens (human)
positive regulation of establishment of endothelial barrier	Sphingosine 1-phosphate receptor 2	Homo sapiens (human)
regulation of metabolic process	Sphingosine 1-phosphate receptor 2	Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathway	Sphingosine 1-phosphate receptor 2	Homo sapiens (human)
sphingosine-1-phosphate receptor signaling pathway	Sphingosine 1-phosphate receptor 4	Homo sapiens (human)
immune response	Sphingosine 1-phosphate receptor 4	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Sphingosine 1-phosphate receptor 4	Homo sapiens (human)
activation of phospholipase C activity	Sphingosine 1-phosphate receptor 4	Homo sapiens (human)
positive regulation of cytosolic calcium ion concentration	Sphingosine 1-phosphate receptor 4	Homo sapiens (human)
regulation of metabolic process	Sphingosine 1-phosphate receptor 4	Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathway	Sphingosine 1-phosphate receptor 4	Homo sapiens (human)
lipid hydroxylation	Cytochrome P450 3A4	Homo sapiens (human)
lipid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
steroid catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
androgen metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
alkaloid catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
calcitriol biosynthetic process from calciol	Cytochrome P450 3A4	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
retinol metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
retinoic acid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
long-chain fatty acid biosynthetic process	Cytochrome P450 3A4	Homo sapiens (human)
aflatoxin metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 3A4	Homo sapiens (human)
blood vessel maturation	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
cardiac muscle tissue growth involved in heart morphogenesis	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
sphingosine-1-phosphate receptor signaling pathway	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
chemotaxis	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
cell adhesion	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
brain development	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
cell population proliferation	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
cell migration	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
transmission of nerve impulse	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
lamellipodium assembly	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
actin cytoskeleton organization	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
regulation of cell adhesion	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
neuron differentiation	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
positive regulation of cell migration	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
regulation of bone mineralization	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
leukocyte chemotaxis	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
regulation of bone resorption	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
endothelial cell differentiation	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
positive regulation of smooth muscle cell proliferation	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
positive regulation of positive chemotaxis	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
negative regulation of stress fiber assembly	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
heart trabecula morphogenesis	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
T cell migration	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
angiogenesis	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
regulation of metabolic process	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathway	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
monoamine transport	Sodium-dependent serotonin transporter	Homo sapiens (human)
response to hypoxia	Sodium-dependent serotonin transporter	Homo sapiens (human)
neurotransmitter transport	Sodium-dependent serotonin transporter	Homo sapiens (human)
response to nutrient	Sodium-dependent serotonin transporter	Homo sapiens (human)
memory	Sodium-dependent serotonin transporter	Homo sapiens (human)
circadian rhythm	Sodium-dependent serotonin transporter	Homo sapiens (human)
response to xenobiotic stimulus	Sodium-dependent serotonin transporter	Homo sapiens (human)
response to toxic substance	Sodium-dependent serotonin transporter	Homo sapiens (human)
positive regulation of gene expression	Sodium-dependent serotonin transporter	Homo sapiens (human)
positive regulation of serotonin secretion	Sodium-dependent serotonin transporter	Homo sapiens (human)
negative regulation of cerebellar granule cell precursor proliferation	Sodium-dependent serotonin transporter	Homo sapiens (human)
negative regulation of synaptic transmission, dopaminergic	Sodium-dependent serotonin transporter	Homo sapiens (human)
response to estradiol	Sodium-dependent serotonin transporter	Homo sapiens (human)
social behavior	Sodium-dependent serotonin transporter	Homo sapiens (human)
vasoconstriction	Sodium-dependent serotonin transporter	Homo sapiens (human)
sperm ejaculation	Sodium-dependent serotonin transporter	Homo sapiens (human)
negative regulation of neuron differentiation	Sodium-dependent serotonin transporter	Homo sapiens (human)
positive regulation of cell cycle	Sodium-dependent serotonin transporter	Homo sapiens (human)
negative regulation of organ growth	Sodium-dependent serotonin transporter	Homo sapiens (human)
behavioral response to cocaine	Sodium-dependent serotonin transporter	Homo sapiens (human)
enteric nervous system development	Sodium-dependent serotonin transporter	Homo sapiens (human)
brain morphogenesis	Sodium-dependent serotonin transporter	Homo sapiens (human)
serotonin uptake	Sodium-dependent serotonin transporter	Homo sapiens (human)
membrane depolarization	Sodium-dependent serotonin transporter	Homo sapiens (human)
platelet aggregation	Sodium-dependent serotonin transporter	Homo sapiens (human)
cellular response to retinoic acid	Sodium-dependent serotonin transporter	Homo sapiens (human)
cellular response to cGMP	Sodium-dependent serotonin transporter	Homo sapiens (human)
regulation of thalamus size	Sodium-dependent serotonin transporter	Homo sapiens (human)
conditioned place preference	Sodium-dependent serotonin transporter	Homo sapiens (human)
sodium ion transmembrane transport	Sodium-dependent serotonin transporter	Homo sapiens (human)
amino acid transport	Sodium-dependent serotonin transporter	Homo sapiens (human)
sphingosine-1-phosphate receptor signaling pathway	Sphingosine 1-phosphate receptor 3	Homo sapiens (human)
inflammatory response	Sphingosine 1-phosphate receptor 3	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Sphingosine 1-phosphate receptor 3	Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway	Sphingosine 1-phosphate receptor 3	Homo sapiens (human)
positive regulation of cytosolic calcium ion concentration	Sphingosine 1-phosphate receptor 3	Homo sapiens (human)
Notch signaling pathway	Sphingosine 1-phosphate receptor 3	Homo sapiens (human)
positive regulation of cell population proliferation	Sphingosine 1-phosphate receptor 3	Homo sapiens (human)
anatomical structure morphogenesis	Sphingosine 1-phosphate receptor 3	Homo sapiens (human)
regulation of interleukin-1 beta production	Sphingosine 1-phosphate receptor 3	Homo sapiens (human)
negative regulation of establishment of endothelial barrier	Sphingosine 1-phosphate receptor 3	Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathway	Sphingosine 1-phosphate receptor 3	Homo sapiens (human)
regulation of metabolic process	Sphingosine 1-phosphate receptor 3	Homo sapiens (human)
sphingosine-1-phosphate receptor signaling pathway	Sphingosine 1-phosphate receptor 5	Homo sapiens (human)
regulation of neuron differentiation	Sphingosine 1-phosphate receptor 5	Homo sapiens (human)
regulation of metabolic process	Sphingosine 1-phosphate receptor 5	Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathway	Sphingosine 1-phosphate receptor 5	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
G protein-coupled receptor binding	Sphingosine 1-phosphate receptor 2	Homo sapiens (human)
G protein-coupled receptor activity	Sphingosine 1-phosphate receptor 2	Homo sapiens (human)
integrin binding	Sphingosine 1-phosphate receptor 2	Homo sapiens (human)
protein binding	Sphingosine 1-phosphate receptor 2	Homo sapiens (human)
lipid binding	Sphingosine 1-phosphate receptor 2	Homo sapiens (human)
G protein-coupled peptide receptor activity	Sphingosine 1-phosphate receptor 2	Homo sapiens (human)
sphingosine-1-phosphate receptor activity	Sphingosine 1-phosphate receptor 2	Homo sapiens (human)
protein binding	Sphingosine 1-phosphate receptor 4	Homo sapiens (human)
lipid binding	Sphingosine 1-phosphate receptor 4	Homo sapiens (human)
sphingosine-1-phosphate receptor activity	Sphingosine 1-phosphate receptor 4	Homo sapiens (human)
G protein-coupled receptor activity	Sphingosine 1-phosphate receptor 4	Homo sapiens (human)
G protein-coupled receptor binding	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
G protein-coupled receptor activity	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
protein binding	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
sphingosine-1-phosphate receptor activity	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
sphingolipid binding	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
integrin binding	Sphingosine 1-phosphate receptor 3	Homo sapiens (human)
protein binding	Sphingosine 1-phosphate receptor 3	Homo sapiens (human)
lipid binding	Sphingosine 1-phosphate receptor 3	Homo sapiens (human)
sphingosine-1-phosphate receptor activity	Sphingosine 1-phosphate receptor 3	Homo sapiens (human)
G protein-coupled receptor activity	Sphingosine 1-phosphate receptor 3	Homo sapiens (human)
protein binding	Sphingosine 1-phosphate receptor 5	Homo sapiens (human)
sphingosine-1-phosphate receptor activity	Sphingosine 1-phosphate receptor 5	Homo sapiens (human)
G protein-coupled receptor activity	Sphingosine 1-phosphate receptor 5	Homo sapiens (human)
G protein-coupled receptor binding	Sphingosine 1-phosphate receptor 2	Homo sapiens (human)
G protein-coupled receptor activity	Sphingosine 1-phosphate receptor 2	Homo sapiens (human)
integrin binding	Sphingosine 1-phosphate receptor 2	Homo sapiens (human)
protein binding	Sphingosine 1-phosphate receptor 2	Homo sapiens (human)
lipid binding	Sphingosine 1-phosphate receptor 2	Homo sapiens (human)
G protein-coupled peptide receptor activity	Sphingosine 1-phosphate receptor 2	Homo sapiens (human)
sphingosine-1-phosphate receptor activity	Sphingosine 1-phosphate receptor 2	Homo sapiens (human)
protein binding	Sphingosine 1-phosphate receptor 4	Homo sapiens (human)
lipid binding	Sphingosine 1-phosphate receptor 4	Homo sapiens (human)
sphingosine-1-phosphate receptor activity	Sphingosine 1-phosphate receptor 4	Homo sapiens (human)
G protein-coupled receptor activity	Sphingosine 1-phosphate receptor 4	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 3A4	Homo sapiens (human)
steroid binding	Cytochrome P450 3A4	Homo sapiens (human)
iron ion binding	Cytochrome P450 3A4	Homo sapiens (human)
protein binding	Cytochrome P450 3A4	Homo sapiens (human)
steroid hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
retinoic acid 4-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 3A4	Homo sapiens (human)
oxygen binding	Cytochrome P450 3A4	Homo sapiens (human)
enzyme binding	Cytochrome P450 3A4	Homo sapiens (human)
heme binding	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D3 25-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
caffeine oxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
quinine 3-monooxygenase activity	Cytochrome P450 3A4	Homo sapiens (human)
testosterone 6-beta-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
anandamide 8,9 epoxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
anandamide 11,12 epoxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
anandamide 14,15 epoxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
aromatase activity	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D 24-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
estrogen 16-alpha-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
estrogen 2-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activity	Cytochrome P450 3A4	Homo sapiens (human)
G protein-coupled receptor binding	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
G protein-coupled receptor activity	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
protein binding	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
sphingosine-1-phosphate receptor activity	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
sphingolipid binding	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
integrin binding	Sodium-dependent serotonin transporter	Homo sapiens (human)
monoatomic cation channel activity	Sodium-dependent serotonin transporter	Homo sapiens (human)
neurotransmitter transmembrane transporter activity	Sodium-dependent serotonin transporter	Homo sapiens (human)
serotonin:sodium:chloride symporter activity	Sodium-dependent serotonin transporter	Homo sapiens (human)
protein binding	Sodium-dependent serotonin transporter	Homo sapiens (human)
monoamine transmembrane transporter activity	Sodium-dependent serotonin transporter	Homo sapiens (human)
antiporter activity	Sodium-dependent serotonin transporter	Homo sapiens (human)
syntaxin-1 binding	Sodium-dependent serotonin transporter	Homo sapiens (human)
cocaine binding	Sodium-dependent serotonin transporter	Homo sapiens (human)
sodium ion binding	Sodium-dependent serotonin transporter	Homo sapiens (human)
identical protein binding	Sodium-dependent serotonin transporter	Homo sapiens (human)
nitric-oxide synthase binding	Sodium-dependent serotonin transporter	Homo sapiens (human)
actin filament binding	Sodium-dependent serotonin transporter	Homo sapiens (human)
serotonin binding	Sodium-dependent serotonin transporter	Homo sapiens (human)
integrin binding	Sphingosine 1-phosphate receptor 3	Homo sapiens (human)
protein binding	Sphingosine 1-phosphate receptor 3	Homo sapiens (human)
lipid binding	Sphingosine 1-phosphate receptor 3	Homo sapiens (human)
sphingosine-1-phosphate receptor activity	Sphingosine 1-phosphate receptor 3	Homo sapiens (human)
G protein-coupled receptor activity	Sphingosine 1-phosphate receptor 3	Homo sapiens (human)
protein binding	Sphingosine 1-phosphate receptor 5	Homo sapiens (human)
sphingosine-1-phosphate receptor activity	Sphingosine 1-phosphate receptor 5	Homo sapiens (human)
G protein-coupled receptor activity	Sphingosine 1-phosphate receptor 5	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
plasma membrane	Sphingosine 1-phosphate receptor 2	Homo sapiens (human)
postsynapse	Sphingosine 1-phosphate receptor 2	Homo sapiens (human)
plasma membrane	Sphingosine 1-phosphate receptor 2	Homo sapiens (human)
cytoplasm	Sphingosine 1-phosphate receptor 2	Homo sapiens (human)
mitochondrion	Sphingosine 1-phosphate receptor 4	Homo sapiens (human)
plasma membrane	Sphingosine 1-phosphate receptor 4	Homo sapiens (human)
plasma membrane	Sphingosine 1-phosphate receptor 4	Homo sapiens (human)
cytoplasm	Sphingosine 1-phosphate receptor 4	Homo sapiens (human)
nucleoplasm	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
endosome	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
plasma membrane	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
external side of plasma membrane	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
intracellular membrane-bounded organelle	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
membrane raft	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
plasma membrane	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
cytoplasm	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
plasma membrane	Sphingosine 1-phosphate receptor 3	Homo sapiens (human)
cytoplasm	Sphingosine 1-phosphate receptor 3	Homo sapiens (human)
plasma membrane	Sphingosine 1-phosphate receptor 3	Homo sapiens (human)
plasma membrane	Sphingosine 1-phosphate receptor 5	Homo sapiens (human)
cytoplasm	Sphingosine 1-phosphate receptor 5	Homo sapiens (human)
plasma membrane	Sphingosine 1-phosphate receptor 5	Homo sapiens (human)
plasma membrane	Sphingosine 1-phosphate receptor 2	Homo sapiens (human)
postsynapse	Sphingosine 1-phosphate receptor 2	Homo sapiens (human)
plasma membrane	Sphingosine 1-phosphate receptor 2	Homo sapiens (human)
cytoplasm	Sphingosine 1-phosphate receptor 2	Homo sapiens (human)
mitochondrion	Sphingosine 1-phosphate receptor 4	Homo sapiens (human)
plasma membrane	Sphingosine 1-phosphate receptor 4	Homo sapiens (human)
plasma membrane	Sphingosine 1-phosphate receptor 4	Homo sapiens (human)
cytoplasm	Sphingosine 1-phosphate receptor 4	Homo sapiens (human)
cytoplasm	Cytochrome P450 3A4	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 3A4	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 3A4	Homo sapiens (human)
nucleoplasm	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
endosome	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
plasma membrane	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
external side of plasma membrane	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
intracellular membrane-bounded organelle	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
membrane raft	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
plasma membrane	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
cytoplasm	Sphingosine 1-phosphate receptor 1	Homo sapiens (human)
plasma membrane	Sodium-dependent serotonin transporter	Homo sapiens (human)
focal adhesion	Sodium-dependent serotonin transporter	Homo sapiens (human)
endosome membrane	Sodium-dependent serotonin transporter	Homo sapiens (human)
endomembrane system	Sodium-dependent serotonin transporter	Homo sapiens (human)
presynaptic membrane	Sodium-dependent serotonin transporter	Homo sapiens (human)
membrane raft	Sodium-dependent serotonin transporter	Homo sapiens (human)
synapse	Sodium-dependent serotonin transporter	Homo sapiens (human)
postsynaptic membrane	Sodium-dependent serotonin transporter	Homo sapiens (human)
serotonergic synapse	Sodium-dependent serotonin transporter	Homo sapiens (human)
synapse	Sodium-dependent serotonin transporter	Homo sapiens (human)
plasma membrane	Sodium-dependent serotonin transporter	Homo sapiens (human)
neuron projection	Sodium-dependent serotonin transporter	Homo sapiens (human)
plasma membrane	Sphingosine 1-phosphate receptor 3	Homo sapiens (human)
cytoplasm	Sphingosine 1-phosphate receptor 3	Homo sapiens (human)
plasma membrane	Sphingosine 1-phosphate receptor 3	Homo sapiens (human)
plasma membrane	Sphingosine 1-phosphate receptor 5	Homo sapiens (human)
cytoplasm	Sphingosine 1-phosphate receptor 5	Homo sapiens (human)
plasma membrane	Sphingosine 1-phosphate receptor 5	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (222)

Assay ID	Title	Year	Journal	Article
AID1798300	[32P] S1P Binding Assay from Article 10.1016/j.bmc.2004.10.008: \\Asymmetric synthesis and biological evaluation of the enantiomeric isomers of the immunosuppressive FTY720-phosphate.\\	2005	Bioorganic & medicinal chemistry, Jan-17, Volume: 13, Issue:2	Asymmetric synthesis and biological evaluation of the enantiomeric isomers of the immunosuppressive FTY720-phosphate.
AID642466	Agonist activity at human S1P3 receptor expressed in CHO-K1 cells co-expressing Gq/i5 G-protein assessed as calcium mobilization by FLIPR assay	2012	Bioorganic & 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.
AID1735818	Agonist activity at human recombinant S1P1 expressed in CHO cell membranes assessed as stimulation of cAMP accumulation incubated for 10 mins by HTRF assay	2019	Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5	Identification and Preclinical Pharmacology of ((1 R,3 S)-1-Amino-3-(( S)-6-(2-methoxyphenethyl)-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopentyl)methanol (BMS-986166): A Differentiated Sphingosine-1-phosphate Receptor 1 (S1P
AID1735824	Agonist activity at human recombinant S1P1 expressed in CHO cells assessed as stimulation of ERK phosphorylation incubated for 7 mins by microplate reader analysis	2019	Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5	Identification and Preclinical Pharmacology of ((1 R,3 S)-1-Amino-3-(( S)-6-(2-methoxyphenethyl)-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopentyl)methanol (BMS-986166): A Differentiated Sphingosine-1-phosphate Receptor 1 (S1P
AID1280939	Agonist activity at human S1P3 receptor expressed in RBL cells by [35S]GTP-gammaS accumulation assay	2016	Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3	Discovery of Tetrahydropyrazolopyridine as Sphingosine 1-Phosphate Receptor 3 (S1P3)-Sparing S1P1 Agonists Active at Low Oral Doses.
AID1719746	Agonist activity at recombinant human S1P2 receptor expressed in Chem-1 cells assessed as calcium flux measured for 180 secs by FLIPR assay	2021	ACS medicinal chemistry letters, Mar-11, Volume: 12, Issue:3	Novel Potent Selective Orally Active S1P5 Receptor Antagonists.
AID648579	Agonist activity at rat S1P1 receptor expressed in CHO-K1 cells assessed as induction of GTPgammaS binding	2012	European journal of medicinal chemistry, May, Volume: 51	Synthesis and evaluation of CS-2100, a potent, orally active and S1P(3)- sparing S1P(1) agonist.
AID1179547	Cmax in rat at 1 mg/kg, po	2014	Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15	Synthesis and SAR studies of benzyl ether derivatives as potent orally active S1P₁ agonists.
AID1719749	Agonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as calcium flux measured for 180 secs by FLIPR assay	2021	ACS medicinal chemistry letters, Mar-11, Volume: 12, Issue:3	Novel Potent Selective Orally Active S1P5 Receptor Antagonists.
AID1432803	Agonist activity at human S1P3 receptor expressed in CHOK1 cell membranes by [35S]-GTPgammaS binding assay	2017	Bioorganic & medicinal chemistry letters, 03-15, Volume: 27, Issue:6	Kinase-independent phosphoramidate S1P
AID596410	Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition after 78 hrs by WST-1 assay	2011	Journal of natural products, Apr-25, Volume: 74, Issue:4	Fingolimod (FTY720): a recently approved multiple sclerosis drug based on a fungal secondary metabolite.
AID1271835	Agonist activity at human S1P1 receptor expressed in EDG1-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assay	2016	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2	Late-stage optimization of a tercyclic class of S1P3-sparing, S1P1 receptor agonists.
AID648582	Agonist activity at human S1P3 receptor expressed in CHO-K1 cells assessed as induction of GTPgammaS binding	2012	European journal of medicinal chemistry, May, Volume: 51	Synthesis and evaluation of CS-2100, a potent, orally active and S1P(3)- sparing S1P(1) agonist.
AID645092	Binding affinity to human S1P2R	2011	ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5	Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist.
AID1735826	Agonist activity at human recombinant S1P3 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting assay	2019	Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5	Identification and Preclinical Pharmacology of ((1 R,3 S)-1-Amino-3-(( S)-6-(2-methoxyphenethyl)-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopentyl)methanol (BMS-986166): A Differentiated Sphingosine-1-phosphate Receptor 1 (S1P
AID240251	Agonism of human S1P-5 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand	2005	Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16	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.
AID639283	Agonist activity at human S1P3 expressed in CHO cells after 60 mins by [35S]GTPgammaS binding assay	2012	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1	Novel immunomodulators based on an oxazolin-2-one-4-carboxamide scaffold.
AID1735817	Displacement of [33P]-SIP from human recombinant S1P1 expressed in CHO cell membranes measured after 45 mins by radioligand competitive binding analysis relative to control	2019	Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5	Identification and Preclinical Pharmacology of ((1 R,3 S)-1-Amino-3-(( S)-6-(2-methoxyphenethyl)-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopentyl)methanol (BMS-986166): A Differentiated Sphingosine-1-phosphate Receptor 1 (S1P
AID1719748	Agonist activity at recombinant human S1P4 receptor expressed in Chem-1 cells assessed as calcium flux measured for 180 secs by FLIPR assay	2021	ACS medicinal chemistry letters, Mar-11, Volume: 12, Issue:3	Novel Potent Selective Orally Active S1P5 Receptor Antagonists.
AID553426	Displacement of [33P]S1P from human S1P3R expressed in CHO cell membranes	2011	ACS medicinal chemistry letters, Feb-10, Volume: 2, Issue:2	Benzofuran Derivatives as Potent, Orally Active S1P1 Receptor Agonists: A Preclinical Lead Molecule for MS.
AID240249	Agonism of human S1P-3 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand	2005	Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16	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.
AID648583	Selectivity ratio of EC50 for human S1P3 receptor to EC50 for human S1P1 receptor	2012	European journal of medicinal chemistry, May, Volume: 51	Synthesis and evaluation of CS-2100, a potent, orally active and S1P(3)- sparing S1P(1) agonist.
AID648580	Agonist activity at rat S1P3 receptor expressed in CHO-K1 cells assessed as induction of GTPgammaS binding	2012	European journal of medicinal chemistry, May, Volume: 51	Synthesis and evaluation of CS-2100, a potent, orally active and S1P(3)- sparing S1P(1) agonist.
AID473719	Agonist activity at human S1P1 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assay	2010	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7	Stereochemistry-activity relationship of orally active tetralin S1P agonist prodrugs.
AID596409	Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 78 hrs by WST-1 assay	2011	Journal of natural products, Apr-25, Volume: 74, Issue:4	Fingolimod (FTY720): a recently approved multiple sclerosis drug based on a fungal secondary metabolite.
AID473723	Agonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assay	2010	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7	Stereochemistry-activity relationship of orally active tetralin S1P agonist prodrugs.
AID639282	Agonist activity at human S1P2 expressed in CHO cells after 60 mins by [35S]GTPgammaS binding assay	2012	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1	Novel immunomodulators based on an oxazolin-2-one-4-carboxamide scaffold.
AID473720	Agonist activity at human S1P2 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assay	2010	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7	Stereochemistry-activity relationship of orally active tetralin S1P agonist prodrugs.
AID473721	Agonist activity at human S1P3 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assay	2010	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7	Stereochemistry-activity relationship of orally active tetralin S1P agonist prodrugs.
AID620822	Agonist activity at human S1P2 receptor expressed in yeast MMY24 assessed as conversion of FDGlu to fluorescein after 24 hrs	2011	Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19	Discovery of a brain-penetrant S1P₃-sparing direct agonist of the S1P₁ and S1P₅ receptors efficacious at low oral dose.
AID1432804	Selectivity ratio of EC50 for human S1P3 receptor to EC50 for human S1P1 receptor	2017	Bioorganic & medicinal chemistry letters, 03-15, Volume: 27, Issue:6	Kinase-independent phosphoramidate S1P
AID620530	Agonist activity at human S1P5 receptor expressed in CHO-K1 aequorin cells assessed as calcium accumulation of by luminescence assay in presence of cofactor coelenterazine relative to control	2011	Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19	Discovery of a brain-penetrant S1P₃-sparing direct agonist of the S1P₁ and S1P₅ receptors efficacious at low oral dose.
AID1735816	Displacement of [33P]-SIP from human recombinant S1P1 expressed in CHO cell membranes measured after 45 mins by radioligand competitive binding analysis	2019	Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5	Identification and Preclinical Pharmacology of ((1 R,3 S)-1-Amino-3-(( S)-6-(2-methoxyphenethyl)-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopentyl)methanol (BMS-986166): A Differentiated Sphingosine-1-phosphate Receptor 1 (S1P
AID1735821	Agonist activity at human recombinant S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting assay relative to control	2019	Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5	Identification and Preclinical Pharmacology of ((1 R,3 S)-1-Amino-3-(( S)-6-(2-methoxyphenethyl)-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopentyl)methanol (BMS-986166): A Differentiated Sphingosine-1-phosphate Receptor 1 (S1P
AID1735820	Agonist activity at human recombinant S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting assay	2019	Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5	Identification and Preclinical Pharmacology of ((1 R,3 S)-1-Amino-3-(( S)-6-(2-methoxyphenethyl)-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopentyl)methanol (BMS-986166): A Differentiated Sphingosine-1-phosphate Receptor 1 (S1P
AID473722	Agonist activity at human S1P4 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assay	2010	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7	Stereochemistry-activity relationship of orally active tetralin S1P agonist prodrugs.
AID1735829	Antimigratory activity against human T cells assessed as inhibition of S1P-induced T cell migration preincubated for 10 mins followed by addition of S1P measured after 120 mins by calcein-AM dye based fluorescence analysis	2019	Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5	Identification and Preclinical Pharmacology of ((1 R,3 S)-1-Amino-3-(( S)-6-(2-methoxyphenethyl)-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopentyl)methanol (BMS-986166): A Differentiated Sphingosine-1-phosphate Receptor 1 (S1P
AID645090	Selectivity ratio of EC50 for rat S1P3R to EC50 for rat S1P1R	2011	ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5	Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist.
AID596412	Antiproliferative activity against human HCT116 cells assessed as growth inhibition after 78 hrs by WST-1 assay	2011	Journal of natural products, Apr-25, Volume: 74, Issue:4	Fingolimod (FTY720): a recently approved multiple sclerosis drug based on a fungal secondary metabolite.
AID645088	Agonist activity at rat S1P3R expressed in CHO-K1 cells by [35S]GTPgammaS binding assay	2011	ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5	Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist.
AID1179548	AUC (0 to 48 hrs) in rat at 1 mg/kg, po	2014	Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15	Synthesis and SAR studies of benzyl ether derivatives as potent orally active S1P₁ agonists.
AID620824	Agonist activity at human S1P4 expressed in CHO-K1 aequorin cells assessed as calcium accumulation of by luminescence assay in presence of cofactor coelenterazine relative to control	2011	Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19	Discovery of a brain-penetrant S1P₃-sparing direct agonist of the S1P₁ and S1P₅ receptors efficacious at low oral dose.
AID1735827	Agonist activity at human recombinant S1P4 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting assay	2019	Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5	Identification and Preclinical Pharmacology of ((1 R,3 S)-1-Amino-3-(( S)-6-(2-methoxyphenethyl)-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopentyl)methanol (BMS-986166): A Differentiated Sphingosine-1-phosphate Receptor 1 (S1P
AID473717	Agonist activity at human S1P1 receptor assessed as effect on calcium mobilization by Gi dependent whole cell assay	2010	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7	Stereochemistry-activity relationship of orally active tetralin S1P agonist prodrugs.
AID1735814	Cardiotoxicity in human iPSC derived cardiomyocytes assessed as reduction in beating rate at 1 nM measured over 2 hrs by multi-electrode array relative to control	2019	Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5	Identification and Preclinical Pharmacology of ((1 R,3 S)-1-Amino-3-(( S)-6-(2-methoxyphenethyl)-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopentyl)methanol (BMS-986166): A Differentiated Sphingosine-1-phosphate Receptor 1 (S1P
AID620529	Agonist activity at human S1P3 receptor expressed in RBL cells assessed as [35S]GTPgammaS binding after 3 hrs by radiometric assay relative to control	2011	Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19	Discovery of a brain-penetrant S1P₃-sparing direct agonist of the S1P₁ and S1P₅ receptors efficacious at low oral dose.
AID1179550	Metabolic stability in rat hepatic microsomes assessed as parent compound remaining after 30 mins at 37 degC	2014	Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15	Synthesis and SAR studies of benzyl ether derivatives as potent orally active S1P₁ agonists.
AID1735828	Agonist activity at human recombinant S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting assay	2019	Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5	Identification and Preclinical Pharmacology of ((1 R,3 S)-1-Amino-3-(( S)-6-(2-methoxyphenethyl)-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopentyl)methanol (BMS-986166): A Differentiated Sphingosine-1-phosphate Receptor 1 (S1P
AID1280940	Agonist activity at human S1P1 receptor expressed in CHO-K1 EDG1 cells by beta-arrestin recruitment assay	2016	Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3	Discovery of Tetrahydropyrazolopyridine as Sphingosine 1-Phosphate Receptor 3 (S1P3)-Sparing S1P1 Agonists Active at Low Oral Doses.
AID620490	Agonist activity at human S1P5 receptor expressed in CHO-K1 aequorin cells assessed as calcium accumulation of by luminescence assay in presence of cofactor coelenterazine	2011	Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19	Discovery of a brain-penetrant S1P₃-sparing direct agonist of the S1P₁ and S1P₅ receptors efficacious at low oral dose.
AID645086	Agonist activity at human S1P3R expressed in CHO-K1 cells by [35S]GTPgammaS binding assay	2011	ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5	Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist.
AID639281	Agonist activity at human S1P1 expressed in CHO cells after 60 mins by [35S]GTPgammaS binding assay	2012	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1	Novel immunomodulators based on an oxazolin-2-one-4-carboxamide scaffold.
AID639284	Agonist activity at human S1P4 expressed in CHO cells after 60 mins by [35S]GTPgammaS binding assay	2012	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1	Novel immunomodulators based on an oxazolin-2-one-4-carboxamide scaffold.
AID662676	Agonist activity at SIP3 receptor	2012	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12	Identification of benzoxazole analogs as novel, S1P(3) sparing S1P(1) agonists.
AID645091	Agonist activity at human S1P5R	2011	ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5	Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist.
AID1735825	Agonist activity at human recombinant S1P1 expressed in CHO cells assessed as stimulation of ERK phosphorylation incubated for 7 mins by microplate reader analysis relative to S1P	2019	Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5	Identification and Preclinical Pharmacology of ((1 R,3 S)-1-Amino-3-(( S)-6-(2-methoxyphenethyl)-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopentyl)methanol (BMS-986166): A Differentiated Sphingosine-1-phosphate Receptor 1 (S1P
AID645085	Agonist activity at human S1P1 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay	2011	ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5	Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist.
AID1735819	Agonist activity at human recombinant S1P1 expressed in CHO cell membranes assessed as stimulation of cAMP accumulation incubated for 10 mins by HTRF assay relative to control	2019	Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5	Identification and Preclinical Pharmacology of ((1 R,3 S)-1-Amino-3-(( S)-6-(2-methoxyphenethyl)-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopentyl)methanol (BMS-986166): A Differentiated Sphingosine-1-phosphate Receptor 1 (S1P
AID596413	Antiproliferative activity against human SW620 cells assessed as growth inhibition after 78 hrs by WST-1 assay	2011	Journal of natural products, Apr-25, Volume: 74, Issue:4	Fingolimod (FTY720): a recently approved multiple sclerosis drug based on a fungal secondary metabolite.
AID240250	Agonism of human S1P-4 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand	2005	Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16	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.
AID620821	Agonist activity at human S1P1 receptor expressed in CHO-K1 EDG1 cells expressing beta-arrestin 2 after 105 mins by chemi-luminescence assay	2011	Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19	Discovery of a brain-penetrant S1P₃-sparing direct agonist of the S1P₁ and S1P₅ receptors efficacious at low oral dose.
AID1735822	Agonist activity at human recombinant C-terminal GFP-fused S1P1 expressed in CHO cells assessed as induction of receptor internalization incubated for 50 mins by fluorescence based confocal laser scanning microscopic analysis	2019	Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5	Identification and Preclinical Pharmacology of ((1 R,3 S)-1-Amino-3-(( S)-6-(2-methoxyphenethyl)-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopentyl)methanol (BMS-986166): A Differentiated Sphingosine-1-phosphate Receptor 1 (S1P
AID1719747	Agonist activity at recombinant human S1P3 receptor expressed in Chem-1 cells assessed as calcium flux measured for 180 secs by FLIPR assay	2021	ACS medicinal chemistry letters, Mar-11, Volume: 12, Issue:3	Novel Potent Selective Orally Active S1P5 Receptor Antagonists.
AID620527	Agonist activity at human S1P1 receptor expressed in CHO-K1 EDG1 cells expressing beta-arrestin 2 after 105 mins by chemi-luminescence assay relative to control	2011	Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19	Discovery of a brain-penetrant S1P₃-sparing direct agonist of the S1P₁ and S1P₅ receptors efficacious at low oral dose.
AID473718	Agonist activity at human S1P3 receptor assessed as effect on calcium mobilization by Gi dependent whole cell assay	2010	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7	Stereochemistry-activity relationship of orally active tetralin S1P agonist prodrugs.
AID662677	Agonist activity at SIP1 receptor	2012	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12	Identification of benzoxazole analogs as novel, S1P(3) sparing S1P(1) agonists.
AID1296149	Induction of internalization of C-terminal GFP-fused human S1P1 receptor expressed in CHO cell membranes after 50 mins	2016	Journal 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.
AID642479	Agonist activity at human S1P3 receptor expressed in CHO-K1 cells co-expressing Gq/i5 G-protein assessed as calcium mobilization by FLIPR assay relative to S1P	2012	Bioorganic & 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.
AID620823	Agonist activity at human S1P3 receptor expressed in RBL cells assessed as [35S]GTPgammaS binding after 3 hrs by radiometric assay	2011	Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19	Discovery of a brain-penetrant S1P₃-sparing direct agonist of the S1P₁ and S1P₅ receptors efficacious at low oral dose.
AID1735823	Agonist activity at human recombinant C-terminal GFP-fused S1P1 expressed in CHO cells assessed as induction of receptor internalization incubated for 50 mins by fluorescence based confocal laser scanning microscopic analysis relative to control	2019	Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5	Identification and Preclinical Pharmacology of ((1 R,3 S)-1-Amino-3-(( S)-6-(2-methoxyphenethyl)-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopentyl)methanol (BMS-986166): A Differentiated Sphingosine-1-phosphate Receptor 1 (S1P
AID620521	Agonist activity at human S1P4 expressed in CHO-K1 aequorin cells assessed as calcium accumulation of by luminescence assay in presence of cofactor coelenterazine	2011	Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19	Discovery of a brain-penetrant S1P₃-sparing direct agonist of the S1P₁ and S1P₅ receptors efficacious at low oral dose.
AID240247	Agonism of human S1P-1 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand	2005	Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16	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.
AID1176592	Agonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assay	2014	ACS 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.
AID1271836	Agonist activity at human S1P3 receptor expressed in EDG3-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assay	2016	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2	Late-stage optimization of a tercyclic class of S1P3-sparing, S1P1 receptor agonists.
AID645089	Selectivity ratio of EC50 for human S1P3R to EC50 for human S1P1R	2011	ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5	Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist.
AID1179538	Selectivity index, ratio of EC50 for human S1P3 receptor to EC50 for human S1P1 receptor	2014	Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15	Synthesis and SAR studies of benzyl ether derivatives as potent orally active S1P₁ agonists.
AID240248	Agonism of human S1P-2 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand	2005	Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16	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.
AID1735872	Induction of remyelination in lysophosphatidylcholine-induced demyelination in wild-type CD1 mouse organotypic cerebellar slice at 0.01 to 10 nM incubated for 7 days by immunohistochemistry based three-dimensional brain cell culture assay	2019	Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5	Identification and Preclinical Pharmacology of ((1 R,3 S)-1-Amino-3-(( S)-6-(2-methoxyphenethyl)-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopentyl)methanol (BMS-986166): A Differentiated Sphingosine-1-phosphate Receptor 1 (S1P
AID1179537	Agonist activity at human S1P3 receptor expressed in CHOK1 cell membranes by [35S]GTPgammaS binding assay	2014	Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15	Synthesis and SAR studies of benzyl ether derivatives as potent orally active S1P₁ agonists.
AID648581	Agonist activity at human S1P1 receptor expressed in CHO-K1 cells assessed as induction of GTPgammaS binding	2012	European journal of medicinal chemistry, May, Volume: 51	Synthesis and evaluation of CS-2100, a potent, orally active and S1P(3)- sparing S1P(1) agonist.
AID1735873	Induction of remyelination in lysophosphatidylcholine-induced demyelination in wild-type CD1 mouse organotypic cerebellar slice assessed as myelination index at 0.01 to 10 nM incubated for 7 days by immunohistochemistry based three-dimensional brain cell	2019	Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5	Identification and Preclinical Pharmacology of ((1 R,3 S)-1-Amino-3-(( S)-6-(2-methoxyphenethyl)-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopentyl)methanol (BMS-986166): A Differentiated Sphingosine-1-phosphate Receptor 1 (S1P
AID1176593	Agonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assay relative to S1P	2014	ACS 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.
AID553425	Displacement of [33P]S1P from human S1P1R expressed in CHO cell membranes	2011	ACS medicinal chemistry letters, Feb-10, Volume: 2, Issue:2	Benzofuran Derivatives as Potent, Orally Active S1P1 Receptor Agonists: A Preclinical Lead Molecule for MS.
AID1719745	Agonist activity at recombinant human S1P1 receptor expressed in Chem-1 cells assessed as calcium flux measured for 180 secs by FLIPR assay	2021	ACS medicinal chemistry letters, Mar-11, Volume: 12, Issue:3	Novel Potent Selective Orally Active S1P5 Receptor Antagonists.
AID392388	Immunomodulatory activity in C57BL/6 mouse assessed as lymphopenia at 1 mg/kg, po after 6 hrs by complete blood count analysis	2009	Bioorganic & 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.
AID645087	Agonist activity at rat S1P1 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay	2011	ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5	Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist.
AID1735815	Cardiotoxicity in human iPSC derived cardiomyocytes assessed as reduction in beating rate at 10 nM measured over 2 hrs by multi-electrode array relative to control	2019	Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5	Identification and Preclinical Pharmacology of ((1 R,3 S)-1-Amino-3-(( S)-6-(2-methoxyphenethyl)-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopentyl)methanol (BMS-986166): A Differentiated Sphingosine-1-phosphate Receptor 1 (S1P
AID1432802	Agonist activity at human S1P1 receptor expressed in CHOK1 cell membranes by [35S]-GTPgammaS binding assay	2017	Bioorganic & medicinal chemistry letters, 03-15, Volume: 27, Issue:6	Kinase-independent phosphoramidate S1P
AID596411	Antiproliferative activity against human SK-BR-3 cells assessed as growth inhibition after 78 hrs by WST-1 assay	2011	Journal of natural products, Apr-25, Volume: 74, Issue:4	Fingolimod (FTY720): a recently approved multiple sclerosis drug based on a fungal secondary metabolite.
AID1179549	Half life in rat at 1 mg/kg, po	2014	Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15	Synthesis and SAR studies of benzyl ether derivatives as potent orally active S1P₁ agonists.
AID1280938	Agonist activity at human S1P1 receptor expressed in RH7777 cells by [35S]GTP-gammaS accumulation assay	2016	Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3	Discovery of Tetrahydropyrazolopyridine as Sphingosine 1-Phosphate Receptor 3 (S1P3)-Sparing S1P1 Agonists Active at Low Oral Doses.
AID1179536	Agonist activity at human S1P1 receptor expressed in CHOK1 cell membranes by [35S]GTPgammaS binding assay	2014	Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15	Synthesis and SAR studies of benzyl ether derivatives as potent orally active S1P₁ agonists.
AID1346205	Human S1P3 receptor (Lysophospholipid (S1P) receptors)	2006	Chemistry & biology, Nov, Volume: 13, Issue:11	A monoselective sphingosine-1-phosphate receptor-1 agonist prevents allograft rejection in a stringent rat heart transplantation model.
AID1346170	Human S1P1 receptor (Lysophospholipid (S1P) receptors)	2006	Chemistry & biology, Nov, Volume: 13, Issue:11	A monoselective sphingosine-1-phosphate receptor-1 agonist prevents allograft rejection in a stringent rat heart transplantation model.
AID1346236	Human S1P2 receptor (Lysophospholipid (S1P) receptors)	2015	Molecular pharmacology, Jun, Volume: 87, Issue:6	FTY720 Phosphate Activates Sphingosine-1-Phosphate Receptor 2 and Selectively Couples to Gα12/13/Rho/ROCK to Induce Myofibroblast Contraction.
AID1346242	Human S1P5 receptor (Lysophospholipid (S1P) receptors)	2004	The Journal of pharmacology and experimental therapeutics, May, Volume: 309, Issue:2	Immune cell regulation and cardiovascular effects of sphingosine 1-phosphate receptor agonists in rodents are mediated via distinct receptor subtypes.
AID1346185	Mouse S1P4 receptor (Lysophospholipid (S1P) receptors)	2008	The Journal of pharmacology and experimental therapeutics, Jan, Volume: 324, Issue:1	A novel sphingosine 1-phosphate receptor agonist, 2-amino-2-propanediol hydrochloride (KRP-203), regulates chronic colitis in interleukin-10 gene-deficient mice.
AID1346162	Human S1P4 receptor (Lysophospholipid (S1P) receptors)	2004	The Journal of pharmacology and experimental therapeutics, May, Volume: 309, Issue:2	Immune cell regulation and cardiovascular effects of sphingosine 1-phosphate receptor agonists in rodents are mediated via distinct receptor subtypes.
AID1346162	Human S1P4 receptor (Lysophospholipid (S1P) receptors)	2014	PloS one, , Volume: 9, Issue:10	ASP4058, a novel agonist for sphingosine 1-phosphate receptors 1 and 5, ameliorates rodent experimental autoimmune encephalomyelitis with a favorable safety profile.
AID1346190	Mouse S1P1 receptor (Lysophospholipid (S1P) receptors)	2008	The Journal of pharmacology and experimental therapeutics, Jan, Volume: 324, Issue:1	A novel sphingosine 1-phosphate receptor agonist, 2-amino-2-propanediol hydrochloride (KRP-203), regulates chronic colitis in interleukin-10 gene-deficient mice.
AID1346242	Human S1P5 receptor (Lysophospholipid (S1P) receptors)	2006	Chemistry & biology, Nov, Volume: 13, Issue:11	A monoselective sphingosine-1-phosphate receptor-1 agonist prevents allograft rejection in a stringent rat heart transplantation model.
AID1346162	Human S1P4 receptor (Lysophospholipid (S1P) receptors)	2006	Chemistry & biology, Nov, Volume: 13, Issue:11	A monoselective sphingosine-1-phosphate receptor-1 agonist prevents allograft rejection in a stringent rat heart transplantation model.
AID1346170	Human S1P1 receptor (Lysophospholipid (S1P) receptors)	2007	Regulatory peptides, Feb-01, Volume: 138, Issue:2-3	Neither intravenous nor intracerebroventricular administration of obestatin affects the secretion of GH, PRL, TSH and ACTH in rats.
AID1346242	Human S1P5 receptor (Lysophospholipid (S1P) receptors)	2002	The Journal of biological chemistry, Jun-14, Volume: 277, Issue:24	The immune modulator FTY720 targets sphingosine 1-phosphate receptors.
AID1346205	Human S1P3 receptor (Lysophospholipid (S1P) receptors)	2004	The Journal of pharmacology and experimental therapeutics, May, Volume: 309, Issue:2	Immune cell regulation and cardiovascular effects of sphingosine 1-phosphate receptor agonists in rodents are mediated via distinct receptor subtypes.
AID1346170	Human S1P1 receptor (Lysophospholipid (S1P) receptors)	2004	The Journal of pharmacology and experimental therapeutics, May, Volume: 309, Issue:2	Immune cell regulation and cardiovascular effects of sphingosine 1-phosphate receptor agonists in rodents are mediated via distinct receptor subtypes.
AID1346185	Mouse S1P4 receptor (Lysophospholipid (S1P) receptors)	2002	The Journal of biological chemistry, Jun-14, Volume: 277, Issue:24	The immune modulator FTY720 targets sphingosine 1-phosphate receptors.
AID1346162	Human S1P4 receptor (Lysophospholipid (S1P) receptors)	2004	The 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.
AID1346190	Mouse S1P1 receptor (Lysophospholipid (S1P) receptors)	2002	The Journal of biological chemistry, Jun-14, Volume: 277, Issue:24	The immune modulator FTY720 targets sphingosine 1-phosphate receptors.
AID1346205	Human S1P3 receptor (Lysophospholipid (S1P) receptors)	2002	The Journal of biological chemistry, Jun-14, Volume: 277, Issue:24	The immune modulator FTY720 targets sphingosine 1-phosphate receptors.
AID1346170	Human S1P1 receptor (Lysophospholipid (S1P) receptors)	2002	The Journal of biological chemistry, Jun-14, Volume: 277, Issue:24	The immune modulator FTY720 targets sphingosine 1-phosphate receptors.
AID1901410	Agonist activity at S1P3 receptor (unknown origin) expressed in PathHunter CHO-K1 EDG1 beta-arrestin cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by measuring chemiluminescence signal by microplate reader method	2022	Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4	Discovery of Novel Sphingosine-1-Phosphate-1 Receptor Agonists for the Treatment of Multiple Sclerosis.
AID1300066	Agonist activity at human S1P1 receptor by GTPgammaS binding assay	2016	ACS medicinal chemistry letters, Mar-10, Volume: 7, Issue:3	Identification and Preclinical Pharmacology of BMS-986104: A Differentiated S1P1 Receptor Modulator in Clinical Trials.
AID1062172	Agonist activity at S1P3R (unknown origin) assessed as [33P] binding activity	2013	ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10	Discovery of Clinical Candidate GSK1842799 As a Selective S1P1 Receptor Agonist (Prodrug) for Multiple Sclerosis.
AID1730771	Displacement of [33P]-SIP from human recombinant S1P1 expressed in CHO cell membranes measured after 45 mins by TopCount scintillation counting method relative to control	2021	Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3	Bicyclic Ligand-Biased Agonists of S1P
AID11287	Volume of distribution was determined in rat at a dose of 1 mpk i.v.	2004	Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12	Potent S1P receptor agonists replicate the pharmacologic actions of the novel immune modulator FTY720.
AID1300102	Agonist activity at human S1P1 receptor expressed in CHO cells assessed as cAMP accumulation after 30 mins by HTRF analysis relative to S1P	2016	ACS medicinal chemistry letters, Mar-10, Volume: 7, Issue:3	Identification and Preclinical Pharmacology of BMS-986104: A Differentiated S1P1 Receptor Modulator in Clinical Trials.
AID1730777	Agonist activity at human recombinant S1P1 expressed in CHO cells assessed as stimulation of ERK phosphorylation incubated for 7 mins by microplate reader analysis relative to S1P	2021	Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3	Bicyclic Ligand-Biased Agonists of S1P
AID1300068	Agonist activity at human S1P3 receptor by GTPgammaS binding assay	2016	ACS medicinal chemistry letters, Mar-10, Volume: 7, Issue:3	Identification and Preclinical Pharmacology of BMS-986104: A Differentiated S1P1 Receptor Modulator in Clinical Trials.
AID284811	Activity at human S1P3 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay	2007	Bioorganic & medicinal chemistry, Jan-15, Volume: 15, Issue:2	Synthesis and biological evaluation of gamma-aminophosphonates as potent, subtype-selective sphingosine 1-phosphate receptor agonists and antagonists.
AID1300103	Agonist activity at human S1P1 receptor expressed in CHO cells assessed as ERK phosphorylation after 7 mins by alphaLISA relative to S1P	2016	ACS medicinal chemistry letters, Mar-10, Volume: 7, Issue:3	Identification and Preclinical Pharmacology of BMS-986104: A Differentiated S1P1 Receptor Modulator in Clinical Trials.
AID1422499	Inhibition of HDAC in MEF assessed as increase in histone H3 acetylation at 10 to 20 uM after 6 hrs by Western blot analysis	2018	European journal of medicinal chemistry, Nov-05, Volume: 159	In search of constrained FTY720 and phytosphingosine analogs as dual acting anticancer agents targeting metabolic and epigenetic pathways.
AID282271	Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells	2004	Journal 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.
AID1185979	Agonist activity at human S1P1 receptor expressed in CHO cells preincubated for 2 hrs before IP1 addition by IP1-HTRF assay	2014	European journal of medicinal chemistry, Oct-06, Volume: 85	Discovery of oxazole and triazole derivatives as potent and selective S1P(1) agonists through pharmacophore-guided design.
AID1300070	Agonist activity at human S1P5 receptor by GTPgammaS binding assay	2016	ACS medicinal chemistry letters, Mar-10, Volume: 7, Issue:3	Identification and Preclinical Pharmacology of BMS-986104: A Differentiated S1P1 Receptor Modulator in Clinical Trials.
AID240213	Effective concentration against sphingosine 1-phosphate receptor 3 determined by a [c-35S]-GTP binding assay	2005	Bioorganic & 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.
AID1203749	In vivo inhibition of S1P1 receptor in mouse assessed as peripheral blood B cells at 1.25 mg/kg, ip after 24 hrs by flow cytometric analysis (Rvb = 4.72 +/- 0.53 10'6/ml)	2015	Journal 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.
AID240247	Agonism of human S1P-1 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand	2005	Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16	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.
AID1422502	Inhibition of HDAC in MEF assessed as increase in histone H3K18 acetylation at 5 uM after 6 hrs by Western blot analysis	2018	European journal of medicinal chemistry, Nov-05, Volume: 159	In search of constrained FTY720 and phytosphingosine analogs as dual acting anticancer agents targeting metabolic and epigenetic pathways.
AID475241	Agonist activity at human S1P3 receptor expressed in CHO cells assessed as intracellular calcium mobilization	2010	Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8	Removal of sphingosine 1-phosphate receptor-3 (S1P(3)) agonism is essential, but inadequate to obtain immunomodulating 2-aminopropane-1,3-diol S1P(1) agonists with reduced effect on heart rate.
AID240451	Maximal efficacy against sphingosine 1-phosphate receptor 4 determined by a [c-35S]-GTP binding assay	2005	Bioorganic & 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.
AID1185982	Cmax in Sprague-Dawley rat at 3 mg/kg, po	2014	European journal of medicinal chemistry, Oct-06, Volume: 85	Discovery of oxazole and triazole derivatives as potent and selective S1P(1) agonists through pharmacophore-guided design.
AID1300063	Agonist activity at human S1P1 receptor expressed in CHO cells assessed as cAMP accumulation after 30 mins by HTRF analysis	2016	ACS medicinal chemistry letters, Mar-10, Volume: 7, Issue:3	Identification and Preclinical Pharmacology of BMS-986104: A Differentiated S1P1 Receptor Modulator in Clinical Trials.
AID1730773	Agonist activity at recombinant human S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting method relative to control	2021	Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3	Bicyclic Ligand-Biased Agonists of S1P
AID284809	Activity at human S1P1 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay	2007	Bioorganic & medicinal chemistry, Jan-15, Volume: 15, Issue:2	Synthesis and biological evaluation of gamma-aminophosphonates as potent, subtype-selective sphingosine 1-phosphate receptor agonists and antagonists.
AID1300104	Agonist activity at human S1P1 receptor expressed in CHO cells co-expressing GFP assessed as cellular internalization after 45 mins by Hoechst assay relative to 2-((3R)-1-(2-hydroxy-2-(4-(5-(3-phenyl-4-(trifluoromethyl)isoxazol-5-yl)-1,2,4-oxadiazol-3-yl)	2016	ACS medicinal chemistry letters, Mar-10, Volume: 7, Issue:3	Identification and Preclinical Pharmacology of BMS-986104: A Differentiated S1P1 Receptor Modulator in Clinical Trials.
AID282268	Displacement of [33P]sphingosine 1 phosphate from human S1P2 receptor expressed in CHO cells	2004	Journal 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.
AID284818	Efficacy at human S1P5 receptor expressed in HEK293T cells relative to S1P	2007	Bioorganic & medicinal chemistry, Jan-15, Volume: 15, Issue:2	Synthesis and biological evaluation of gamma-aminophosphonates as potent, subtype-selective sphingosine 1-phosphate receptor agonists and antagonists.
AID1422504	Inhibition of HDAC in MEF assessed as increase in histone H4K5 acetylation at 5 uM after 6 hrs by Western blot analysis	2018	European journal of medicinal chemistry, Nov-05, Volume: 159	In search of constrained FTY720 and phytosphingosine analogs as dual acting anticancer agents targeting metabolic and epigenetic pathways.
AID11210	Clearance rate was determined in rat at a dose of 1 mpk i.v.	2004	Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12	Potent S1P receptor agonists replicate the pharmacologic actions of the novel immune modulator FTY720.
AID1300116	Reduction of blood lymphocyte level in BALB/c mouse administered through oral gavage after 24 hrs by hematology analysis	2016	ACS medicinal chemistry letters, Mar-10, Volume: 7, Issue:3	Identification and Preclinical Pharmacology of BMS-986104: A Differentiated S1P1 Receptor Modulator in Clinical Trials.
AID1901409	Agonist activity at S1P1 receptor (unknown origin) expressed in PathHunter HEK 293 EDG1 Total GPCR Internalization cells assessed as receptor internalization incubated for 90 mins by measuring chemiluminescence signal by microplate reader method	2022	Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4	Discovery of Novel Sphingosine-1-Phosphate-1 Receptor Agonists for the Treatment of Multiple Sclerosis.
AID282269	Displacement of [33P]sphingosine 1 phosphate from human S1P3 receptor expressed in CHO cells	2004	Journal 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.
AID1062173	Agonist activity at S1P1R (unknown origin) assessed as [33P] binding activity	2013	ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10	Discovery of Clinical Candidate GSK1842799 As a Selective S1P1 Receptor Agonist (Prodrug) for Multiple Sclerosis.
AID204174	Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes	2004	Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12	Potent S1P receptor agonists replicate the pharmacologic actions of the novel immune modulator FTY720.
AID1300100	Toxicity in human-inducible pluripotent stem cell-derived Cardiomyocyte assessed as reduction in cardiomyocyte beating at 0.1 nM after 2 hrs	2016	ACS medicinal chemistry letters, Mar-10, Volume: 7, Issue:3	Identification and Preclinical Pharmacology of BMS-986104: A Differentiated S1P1 Receptor Modulator in Clinical Trials.
AID240287	Effective concentration against sphingosine 1-phosphate receptor 2 determined by a [c-35S]-GTP binding assay; no agonist activity	2005	Bioorganic & 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.
AID1422510	Inhibition of HDAC in MEF assessed as increase in histone H4K5 acetylation at 10 uM after 6 hrs by Western blot analysis	2018	European journal of medicinal chemistry, Nov-05, Volume: 159	In search of constrained FTY720 and phytosphingosine analogs as dual acting anticancer agents targeting metabolic and epigenetic pathways.
AID475240	Agonist activity at human S1P1 receptor expressed in human Chem1 cells assessed as intracellular calcium mobilization	2010	Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8	Removal of sphingosine 1-phosphate receptor-3 (S1P(3)) agonism is essential, but inadequate to obtain immunomodulating 2-aminopropane-1,3-diol S1P(1) agonists with reduced effect on heart rate.
AID284812	Activity at human S1P4 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay	2007	Bioorganic & medicinal chemistry, Jan-15, Volume: 15, Issue:2	Synthesis and biological evaluation of gamma-aminophosphonates as potent, subtype-selective sphingosine 1-phosphate receptor agonists and antagonists.
AID1422509	Inhibition of HDAC in MEF assessed as increase in histone H3 acetylation at 6.1 uM after 24 hrs by Western blot analysis	2018	European journal of medicinal chemistry, Nov-05, Volume: 159	In search of constrained FTY720 and phytosphingosine analogs as dual acting anticancer agents targeting metabolic and epigenetic pathways.
AID284815	Efficacy at human S1P2 receptor expressed in HEK293T cells relative to S1P	2007	Bioorganic & medicinal chemistry, Jan-15, Volume: 15, Issue:2	Synthesis and biological evaluation of gamma-aminophosphonates as potent, subtype-selective sphingosine 1-phosphate receptor agonists and antagonists.
AID284813	Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay	2007	Bioorganic & medicinal chemistry, Jan-15, Volume: 15, Issue:2	Synthesis and biological evaluation of gamma-aminophosphonates as potent, subtype-selective sphingosine 1-phosphate receptor agonists and antagonists.
AID1422505	Inhibition of HDAC in MEF assessed as increase in histone H4K8 acetylation at 5 uM after 6 hrs by Western blot analysis	2018	European journal of medicinal chemistry, Nov-05, Volume: 159	In search of constrained FTY720 and phytosphingosine analogs as dual acting anticancer agents targeting metabolic and epigenetic pathways.
AID1300064	Agonist activity at human S1P1 receptor expressed in CHO cells assessed as ERK phosphorylation after 7 mins by alphaLISA	2016	ACS medicinal chemistry letters, Mar-10, Volume: 7, Issue:3	Identification and Preclinical Pharmacology of BMS-986104: A Differentiated S1P1 Receptor Modulator in Clinical Trials.
AID240215	Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay	2005	Bioorganic & 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.
AID1730781	Antimigratory activity against human T cells assessed as inhibition of S1P-induced T cell migration preincubated for 10 mins followed by addition of S1P measured after 120 mins by calcein-AM dye based fluorescence analysis	2021	Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3	Bicyclic Ligand-Biased Agonists of S1P
AID1422506	Inhibition of HDAC in MEF assessed as increase in histone H4 acetylation at 5 uM after 6 hrs by Western blot analysis	2018	European journal of medicinal chemistry, Nov-05, Volume: 159	In search of constrained FTY720 and phytosphingosine analogs as dual acting anticancer agents targeting metabolic and epigenetic pathways.
AID282274	Activity at human S1P1 receptor expressed in CHO cells by [35S]GTPgammaS binding assay	2004	Journal 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.
AID1203750	In vivo inhibition of S1P1 receptor in mouse assessed as reduction of peripheral blood CD8+ cells at 1.25 mg/kg, ip after 24 hrs by flow cytometric analysis relative to control	2015	Journal 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.
AID1264634	Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding assay	2015	Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23	Discovery of A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders.
AID284814	Efficacy at human S1P1 receptor expressed in HEK293T cells relative to S1P	2007	Bioorganic & medicinal chemistry, Jan-15, Volume: 15, Issue:2	Synthesis and biological evaluation of gamma-aminophosphonates as potent, subtype-selective sphingosine 1-phosphate receptor agonists and antagonists.
AID1203748	In vivo inhibition of S1P1 receptor in mouse assessed as peripheral blood CD8+ cells at 1.25 mg/kg, ip after 24 hrs by flow cytometric analysis (Rvb = 0.48 +/- 0.05 10'6/ml)	2015	Journal 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.
AID284817	Efficacy at human S1P4 receptor expressed in HEK293T cells relative to S1P	2007	Bioorganic & medicinal chemistry, Jan-15, Volume: 15, Issue:2	Synthesis and biological evaluation of gamma-aminophosphonates as potent, subtype-selective sphingosine 1-phosphate receptor agonists and antagonists.
AID240449	Maximal efficacy against sphingosine 1-phosphate receptor 2 determined by a [c-35S]-GTP binding assay	2005	Bioorganic & 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.
AID1185983	Tmax in Sprague-Dawley rat at 3 mg/kg, po	2014	European journal of medicinal chemistry, Oct-06, Volume: 85	Discovery of oxazole and triazole derivatives as potent and selective S1P(1) agonists through pharmacophore-guided design.
AID1668169	Agonist activity at S1PR3 (unknown origin) by HTRF assay	2020	Bioorganic & medicinal chemistry letters, 06-01, Volume: 30, Issue:11	S1P
AID204037	Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 1 expressed on CHO cell membranes	2004	Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12	Potent S1P receptor agonists replicate the pharmacologic actions of the novel immune modulator FTY720.
AID284810	Activity at human S1P2 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay	2007	Bioorganic & medicinal chemistry, Jan-15, Volume: 15, Issue:2	Synthesis and biological evaluation of gamma-aminophosphonates as potent, subtype-selective sphingosine 1-phosphate receptor agonists and antagonists.
AID1730776	Agonist activity at human recombinant S1P1 expressed in CHO cells assessed as stimulation of ERK phosphorylation incubated for 7 mins by microplate reader analysis	2021	Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3	Bicyclic Ligand-Biased Agonists of S1P
AID1422498	Inhibition of HDAC in mouse FL5.12 cells assessed as increase in histone H3 acetylation at 10 uM after 6 hrs by Western blot analysis	2018	European journal of medicinal chemistry, Nov-05, Volume: 159	In search of constrained FTY720 and phytosphingosine analogs as dual acting anticancer agents targeting metabolic and epigenetic pathways.
AID1668170	Ratio of EC50 for S1PR3 (unknown origin) to EC50 for S1PR1 (unknown origin)	2020	Bioorganic & medicinal chemistry letters, 06-01, Volume: 30, Issue:11	S1P
AID1203747	In vivo inhibition of S1P1 receptor in mouse assessed as peripheral blood WBC at 1.25 mg/kg, ip after 24 hrs by flow cytometric analysis (Rvb = 8.94 +/- 0.59 10'6/ml)	2015	Journal 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.
AID1300062	Displacement of 33-P-S1P from from human S1P receptor expressed in CHO cell membranes after 50 mins by scintillation counting	2016	ACS medicinal chemistry letters, Mar-10, Volume: 7, Issue:3	Identification and Preclinical Pharmacology of BMS-986104: A Differentiated S1P1 Receptor Modulator in Clinical Trials.
AID1185984	Half life in Sprague-Dawley rat at 3 mg/kg, po	2014	European journal of medicinal chemistry, Oct-06, Volume: 85	Discovery of oxazole and triazole derivatives as potent and selective S1P(1) agonists through pharmacophore-guided design.
AID240450	Maximal efficacy against sphingosine 1-phosphate receptor 3 determined by a [c-35S]-GTP binding assay	2005	Bioorganic & 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.
AID1184691	Agonist activity at S1P receptor in human C4-2B cells assessed as increase in proliferation at 100 nM after 24 hrs by [3H]-thymidine incorporation assay	2014	Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17	Synthesis of fluorinated agonist of sphingosine-1-phosphate receptor 1.
AID1300065	Agonist activity at human S1P1 receptor expressed in CHO cells co-expressing GFP assessed as cellular internalization after 45 mins by Hoechst assay	2016	ACS medicinal chemistry letters, Mar-10, Volume: 7, Issue:3	Identification and Preclinical Pharmacology of BMS-986104: A Differentiated S1P1 Receptor Modulator in Clinical Trials.
AID282267	Displacement of [33P]sphingosine 1 phosphate from human S1P1 receptor expressed in CHO cells	2004	Journal 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.
AID1730772	Agonist activity at recombinant human S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting method	2021	Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3	Bicyclic Ligand-Biased Agonists of S1P
AID240452	Maximal efficacy against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay	2005	Bioorganic & 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.
AID132579	Immunosuppressive efficacy for peripheral blood lymphocyte lowering (PLL) in mouse expressed intravenous ED50	2004	Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12	Potent S1P receptor agonists replicate the pharmacologic actions of the novel immune modulator FTY720.
AID282270	Displacement of [33P]sphingosine 1 phosphate from human S1P4 receptor expressed in CHO cells	2004	Journal 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.
AID1185986	Apparent oral clearance in Sprague-Dawley rat at 3 mg/kg, po	2014	European journal of medicinal chemistry, Oct-06, Volume: 85	Discovery of oxazole and triazole derivatives as potent and selective S1P(1) agonists through pharmacophore-guided design.
AID1300099	Toxicity in human-inducible pluripotent stem cell-derived Cardiomyocyte assessed as reduction in cardiomyocyte beating after 2 hrs	2016	ACS medicinal chemistry letters, Mar-10, Volume: 7, Issue:3	Identification and Preclinical Pharmacology of BMS-986104: A Differentiated S1P1 Receptor Modulator in Clinical Trials.
AID1185987	Apparent volume of distribution in steady state in Sprague-Dawley rat at 3 mg/kg, po	2014	European journal of medicinal chemistry, Oct-06, Volume: 85	Discovery of oxazole and triazole derivatives as potent and selective S1P(1) agonists through pharmacophore-guided design.
AID1184690	Agonist activity at S1P receptor in human PC3 cells assessed as increase in proliferation at 100 nM after 24 hrs by [3H]-thymidine incorporation assay	2014	Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17	Synthesis of fluorinated agonist of sphingosine-1-phosphate receptor 1.
AID1422507	Inhibition of HDAC in MEF assessed as increase in histone H3K9 acetylation at 6.1 uM after 24 hrs by Western blot analysis	2018	European journal of medicinal chemistry, Nov-05, Volume: 159	In search of constrained FTY720 and phytosphingosine analogs as dual acting anticancer agents targeting metabolic and epigenetic pathways.
AID1422508	Inhibition of HDAC in MEF assessed as increase in histone H3K18 acetylation at 6.1 uM after 24 hrs by Western blot analysis	2018	European journal of medicinal chemistry, Nov-05, Volume: 159	In search of constrained FTY720 and phytosphingosine analogs as dual acting anticancer agents targeting metabolic and epigenetic pathways.
AID12879	Half-life was determined in rat at a dose of 1 mpk i.v.	2004	Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12	Potent S1P receptor agonists replicate the pharmacologic actions of the novel immune modulator FTY720.
AID240202	Effective concentration against sphingosine-1-phosphate receptor 1 determined by a [c-35S]-GTP binding assay	2005	Bioorganic & 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.
AID204055	Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 4 expressed on CHO cell membranes	2004	Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12	Potent S1P receptor agonists replicate the pharmacologic actions of the novel immune modulator FTY720.
AID1901408	Agonist activity at S1P1 receptor (unknown origin) expressed in PathHunter CHO-K1 EDG1 beta-arrestin cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by measuring chemiluminescence signal by microplate reader method	2022	Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4	Discovery of Novel Sphingosine-1-Phosphate-1 Receptor Agonists for the Treatment of Multiple Sclerosis.
AID1730770	Displacement of [33P]-SIP from human recombinant S1P1 expressed in CHO cell membranes measured after 45 mins by TopCount scintillation counting method	2021	Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3	Bicyclic Ligand-Biased Agonists of S1P
AID1730779	Agonist activity at recombinant human S1P4 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting method	2021	Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3	Bicyclic Ligand-Biased Agonists of S1P
AID1300092	Toxicity in guinea pig heart assessed as reduction in ventricular rate at 1 nM after 10 mins by ECG analysis	2016	ACS medicinal chemistry letters, Mar-10, Volume: 7, Issue:3	Identification and Preclinical Pharmacology of BMS-986104: A Differentiated S1P1 Receptor Modulator in Clinical Trials.
AID1422511	Inhibition of HDAC in MEF assessed as increase in histone H4 acetylation at 10 uM after 6 hrs by Western blot analysis	2018	European journal of medicinal chemistry, Nov-05, Volume: 159	In search of constrained FTY720 and phytosphingosine analogs as dual acting anticancer agents targeting metabolic and epigenetic pathways.
AID1422522	Inhibition of HDAC (unknown origin) at 5 uM	2018	European journal of medicinal chemistry, Nov-05, Volume: 159	In search of constrained FTY720 and phytosphingosine analogs as dual acting anticancer agents targeting metabolic and epigenetic pathways.
AID240447	Maximal efficacy against sphingosine-1-phosphate receptor 1 determined by a [c-35S]-GTP binding assay	2005	Bioorganic & 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.
AID1422501	Inhibition of HDAC in MEF assessed as increase in histone H3K9 acetylation at 5 uM after 6 hrs by Western blot analysis	2018	European journal of medicinal chemistry, Nov-05, Volume: 159	In search of constrained FTY720 and phytosphingosine analogs as dual acting anticancer agents targeting metabolic and epigenetic pathways.
AID1300093	Toxicity in guinea pig heart assessed as third degree AV block at 1 nM after 10 mins by ECG analysis	2016	ACS medicinal chemistry letters, Mar-10, Volume: 7, Issue:3	Identification and Preclinical Pharmacology of BMS-986104: A Differentiated S1P1 Receptor Modulator in Clinical Trials.
AID240249	Agonism of human S1P-3 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand	2005	Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16	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.
AID1730778	Agonist activity at recombinant human S1P3 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting method	2021	Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3	Bicyclic Ligand-Biased Agonists of S1P
AID1422503	Inhibition of HDAC in MEF assessed as increase in histone H3 acetylation at 5 uM after 6 hrs by Western blot analysis	2018	European journal of medicinal chemistry, Nov-05, Volume: 159	In search of constrained FTY720 and phytosphingosine analogs as dual acting anticancer agents targeting metabolic and epigenetic pathways.
AID1264633	Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by GTPgammaS binding assay	2015	Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23	Discovery of A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders.
AID1730774	Agonist activity at human recombinant C-terminal GFP-fused S1P1 expressed in CHO cells assessed as induction of receptor internalization incubated for 50 mins by fluorescence based confocal laser scanning microscopic analysis	2021	Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3	Bicyclic Ligand-Biased Agonists of S1P
AID1730780	Agonist activity at recombinant human S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting method	2021	Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3	Bicyclic Ligand-Biased Agonists of S1P
AID1062171	Selectivity ratio for S1P3R (unknown origin) to S1P1R (unknown origin)	2013	ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10	Discovery of Clinical Candidate GSK1842799 As a Selective S1P1 Receptor Agonist (Prodrug) for Multiple Sclerosis.
AID240251	Agonism of human S1P-5 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand	2005	Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16	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.
AID240248	Agonism of human S1P-2 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand	2005	Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16	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.
AID240214	Effective concentration against sphingosine 1-phosphate receptor 4 determined by a [c-35S]-GTP binding assay	2005	Bioorganic & 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.
AID1185980	Agonist activity at human S1P3 receptor expressed in CHO cells preincubated for 2 hrs before IP1 addition by IP1-HTRF assay	2014	European journal of medicinal chemistry, Oct-06, Volume: 85	Discovery of oxazole and triazole derivatives as potent and selective S1P(1) agonists through pharmacophore-guided design.
AID1300101	Toxicity in human-inducible pluripotent stem cell-derived Cardiomyocyte assessed as reduction in cardiomyocyte beating at 1 nM after 2 hrs	2016	ACS medicinal chemistry letters, Mar-10, Volume: 7, Issue:3	Identification and Preclinical Pharmacology of BMS-986104: A Differentiated S1P1 Receptor Modulator in Clinical Trials.
AID1668168	Agonist activity at S1P1 (unknown origin) by HTRF assay	2020	Bioorganic & medicinal chemistry letters, 06-01, Volume: 30, Issue:11	S1P
AID1185985	AUC (0 to t) in Sprague-Dawley rat at 3 mg/kg, po	2014	European journal of medicinal chemistry, Oct-06, Volume: 85	Discovery of oxazole and triazole derivatives as potent and selective S1P(1) agonists through pharmacophore-guided design.
AID1300069	Agonist activity at human S1P4 receptor by GTPgammaS binding assay	2016	ACS medicinal chemistry letters, Mar-10, Volume: 7, Issue:3	Identification and Preclinical Pharmacology of BMS-986104: A Differentiated S1P1 Receptor Modulator in Clinical Trials.
AID475243	Toxicity in iv dosed Sprague-Dawley rat assessed as reduction in heart rate	2010	Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8	Removal of sphingosine 1-phosphate receptor-3 (S1P(3)) agonism is essential, but inadequate to obtain immunomodulating 2-aminopropane-1,3-diol S1P(1) agonists with reduced effect on heart rate.
AID284816	Efficacy at human S1P3 receptor expressed in HEK293T cells relative to S1P	2007	Bioorganic & medicinal chemistry, Jan-15, Volume: 15, Issue:2	Synthesis and biological evaluation of gamma-aminophosphonates as potent, subtype-selective sphingosine 1-phosphate receptor agonists and antagonists.
AID240250	Agonism of human S1P-4 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand	2005	Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16	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.
AID204054	Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 3 expressed on CHO cell membranes	2004	Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12	Potent S1P receptor agonists replicate the pharmacologic actions of the novel immune modulator FTY720.
AID1730775	Agonist activity at human recombinant C-terminal GFP-fused S1P1 expressed in CHO cells assessed as induction of receptor internalization incubated for 50 mins by fluorescence based confocal laser scanning microscopic analysis relative to control	2021	Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3	Bicyclic Ligand-Biased Agonists of S1P
AID1798300	[32P] S1P Binding Assay from Article 10.1016/j.bmc.2004.10.008: \\Asymmetric synthesis and biological evaluation of the enantiomeric isomers of the immunosuppressive FTY720-phosphate.\\	2005	Bioorganic & medicinal chemistry, Jan-17, Volume: 13, Issue:2	Asymmetric synthesis and biological evaluation of the enantiomeric isomers of the immunosuppressive FTY720-phosphate.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	13 (30.23)	29.6817
2010's	26 (60.47)	24.3611
2020's	4 (9.30)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	0 (0.00%)	5.53%
Trials	0 (0.00%)	5.53%
Reviews	1 (4.76%)	6.00%
Reviews	0 (0.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Observational	0 (0.00%)	0.25%
Other	20 (95.24%)	84.16%
Other	25 (100.00%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
fingolimod hydrochloride Fingolimod Hydrochloride: A sphingosine-derivative and IMMUNOSUPPRESSIVE AGENT that blocks the migration and homing of LYMPHOCYTES to the CENTRAL NERVOUS SYSTEM through its action on SPHINGOSINE 1-PHOSPHATE RECEPTORS. It is used in the treatment of MULTIPLE SCLEROSIS.. fingolimod hydrochloride : The hydrochloride salt of 2-amino-2-[2-(4-octylphenyl) ethyl]-1,3-propanediol (fingolimod).	2.48	2	hydrochloride	immunosuppressive agent; prodrug; sphingosine-1-phosphate receptor agonist
fingolimod fingolimod : An aminodiol that consists of propane-1,3-diol having amino and 2-(4-octylphenyl)ethyl substituents at the 2-position. It is a sphingosine 1-phosphate receptor modulator used for the treatment of relapsing-remitting multiple sclerosis. A prodrug, fingolimod is phosphorylated by sphingosine kinase to active metabolite fingolimod-phosphate, a structural analogue of sphingosine 1-phosphate.	4.89	10	aminodiol; primary amino compound	antineoplastic agent; CB1 receptor antagonist; immunosuppressive agent; prodrug; sphingosine-1-phosphate receptor agonist
methotrexate [no description available]	2.1	1	dicarboxylic acid; monocarboxylic acid amide; pteridines	abortifacient; antimetabolite; antineoplastic agent; antirheumatic drug; dermatologic drug; DNA synthesis inhibitor; EC 1.5.1.3 (dihydrofolate reductase) inhibitor; immunosuppressive agent
sew2871 SEW2871: structure in first source	2.47	2	oxadiazole; ring assembly
sphingosine 1-phosphate sphingosine 1-phosphate: RN given refers to (R-(R,S-(E)))-isomer; RN for cpd without isomeric designation not available 8/89. sphingosine 1-phosphate : A phosphosphingolipid that consists of sphingosine having a phospho group attached at position 1	3.46	7	sphingoid 1-phosphate	mouse metabolite; signalling molecule; sphingosine-1-phosphate receptor agonist; T-cell proliferation inhibitor; vasodilator agent
cyclosporine ramihyphin A: one of the metabolites produced by Fusarium sp. S-435; RN given refers to cpd with unknown MF	3.16	1	homodetic cyclic peptide	anti-asthmatic drug; anticoronaviral agent; antifungal agent; antirheumatic drug; carcinogenic agent; dermatologic drug; EC 3.1.3.16 (phosphoprotein phosphatase) inhibitor; geroprotector; immunosuppressive agent; metabolite
thermozymocidin thermozymocidin: a serine palmitoyltransferase inhibitor; FTY720 is an analog	3.16	1	alpha-amino fatty acid; hydroxy monocarboxylic acid; non-proteinogenic alpha-amino acid; sphingoid	antifungal agent; antimicrobial agent; antineoplastic agent; apoptosis inducer; EC 2.3.1.50 (serine C-palmitoyltransferase) inhibitor; fungal metabolite; immunosuppressive agent
auy 954 AUY 954: an S1P(1) receptor agonist; structure in first source	2.03	1
cs 0777 CS 0777: a sphingosine-1-phosphate receptor modulator	2.06	1
cs-2100 [no description available]	2.07	1
vorinostat Vorinostat: A hydroxamic acid and anilide derivative that acts as a HISTONE DEACETYLASE inhibitor. It is used in the treatment of CUTANEOUS T-CELL LYMPHOMA and SEZARY SYNDROME.. vorinostat : A dicarboxylic acid diamide comprising suberic (octanedioic) acid coupled to aniline and hydroxylamine. A histone deacetylase inhibitor, it is marketed under the name Zolinza for the treatment of cutaneous T cell lymphoma (CTCL).	2.17	1	dicarboxylic acid diamide; hydroxamic acid	antineoplastic agent; apoptosis inducer; EC 3.5.1.98 (histone deacetylase) inhibitor
fingolimod fingolimod : An aminodiol that consists of propane-1,3-diol having amino and 2-(4-octylphenyl)ethyl substituents at the 2-position. It is a sphingosine 1-phosphate receptor modulator used for the treatment of relapsing-remitting multiple sclerosis. A prodrug, fingolimod is phosphorylated by sphingosine kinase to active metabolite fingolimod-phosphate, a structural analogue of sphingosine 1-phosphate.	3.78	10	aminodiol; primary amino compound	antineoplastic agent; CB1 receptor antagonist; immunosuppressive agent; prodrug; sphingosine-1-phosphate receptor agonist
sew2871 SEW2871: structure in first source	2.42	2	oxadiazole; ring assembly
sphingosine 1-phosphate sphingosine 1-phosphate: RN given refers to (R-(R,S-(E)))-isomer; RN for cpd without isomeric designation not available 8/89. sphingosine 1-phosphate : A phosphosphingolipid that consists of sphingosine having a phospho group attached at position 1	3.64	9	sphingoid 1-phosphate	mouse metabolite; signalling molecule; sphingosine-1-phosphate receptor agonist; T-cell proliferation inhibitor; vasodilator agent
auy 954 AUY 954: an S1P(1) receptor agonist; structure in first source	2.44	2
VPC 23019 VPC23019: inhibits S1P3 receptor; structure in first source. VPC 23019 : A secondary carboxamide resulting from the formal condensation of the carboxy group of O-phospho-D-serine with the amino group of m-octylaniline. An analogue of sphingosine-1-phosphate (S1P), it is a potent antagonist for both S1P1 and S1P3 receptors. It can inhibit S1P-induced migration of thyroid cancer cells, ovarian cancer cells, and neural stem cells.	2.03	1	aromatic amide; D-serine derivative; organic phosphate; phosphoric ester; secondary carboxamide	sphingosine-1-phosphate receptor 1 antagonist; sphingosine-1-phosphate receptor 3 antagonist
siponimod siponimod: S1P receptor modulator	2.13	1

Condition	Relationship Strength	Studies
Lymphocytopenia [description not available]	2.94	4
MS (Multiple Sclerosis) [description not available]	3.92	4
Lymphopenia Reduction in the number of lymphocytes.	2.94	4
Multiple Sclerosis An autoimmune disorder mainly affecting young adults and characterized by destruction of myelin in the central nervous system. Pathologic findings include multiple sharply demarcated areas of demyelination throughout the white matter of the central nervous system. Clinical manifestations include visual loss, extra-ocular movement disorders, paresthesias, loss of sensation, weakness, dysarthria, spasticity, ataxia, and bladder dysfunction. The usual pattern is one of recurrent attacks followed by partial recovery (see MULTIPLE SCLEROSIS, RELAPSING-REMITTING), but acute fulminating and chronic progressive forms (see MULTIPLE SCLEROSIS, CHRONIC PROGRESSIVE) also occur. (Adams et al., Principles of Neurology, 6th ed, p903)	3.92	4
Acute Relapsing Multiple Sclerosis [description not available]	2.06	1
Multiple Sclerosis, Relapsing-Remitting The most common clinical variant of MULTIPLE SCLEROSIS, characterized by recurrent acute exacerbations of neurologic dysfunction followed by partial or complete recovery. Common clinical manifestations include loss of visual (see OPTIC NEURITIS), motor, sensory, or bladder function. Acute episodes of demyelination may occur at any site in the central nervous system, and commonly involve the optic nerves, spinal cord, brain stem, and cerebellum. (Adams et al., Principles of Neurology, 6th ed, pp903-914)	2.06	1
Cardiovascular Diseases Pathological conditions involving the CARDIOVASCULAR SYSTEM including the HEART; the BLOOD VESSELS; or the PERICARDIUM.	2.07	1
Sensitivity and Specificity Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)	2.07	1
Adjuvant Arthritis [description not available]	2.59	2
Allergic Encephalomyelitis [description not available]	3.01	4
Anesthesia A state characterized by loss of feeling or sensation. This depression of nerve function is usually the result of pharmacologic action and is induced to allow performance of surgery or other painful procedures.	2.02	1
Bradyarrhythmia [description not available]	2.02	1
Bradycardia Cardiac arrhythmias that are characterized by excessively slow HEART RATE, usually below 50 beats per minute in human adults. They can be classified broadly into SINOATRIAL NODE dysfunction and ATRIOVENTRICULAR BLOCK.	2.02	1
Chronic Illness [description not available]	2.04	1
Chronic Disease Diseases which have one or more of the following characteristics: they are permanent, leave residual disability, are caused by nonreversible pathological alteration, require special training of the patient for rehabilitation, or may be expected to require a long period of supervision, observation, or care (Dictionary of Health Services Management, 2d ed). For epidemiological studies chronic disease often includes HEART DISEASES; STROKE; CANCER; and diabetes (DIABETES MELLITUS, TYPE 2).	2.04	1
Colitis Inflammation of the COLON section of the large intestine (INTESTINE, LARGE), usually with symptoms such as DIARRHEA (often with blood and mucus), ABDOMINAL PAIN, and FEVER.	2.04	1
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	2.1	1
Degenerative Diseases, Central Nervous System [description not available]	2.11	1
Neurodegenerative Diseases Hereditary and sporadic conditions which are characterized by progressive nervous system dysfunction. These disorders are often associated with atrophy of the affected central or peripheral nervous system structures.	2.11	1
Autoimmune Disease [description not available]	2.31	1
Disease, Pulmonary [description not available]	2.31	1
Autoimmune Diseases Disorders that are characterized by the production of antibodies that react with host tissues or immune effector cells that are autoreactive to endogenous peptides.	2.31	1
Lung Diseases Pathological processes involving any part of the LUNG.	2.31	1

fty 720p

Description

Cross-References

Synonyms (76)

Research Excerpts

Bioavailability

Dosage Studied

Roles (3)

Drug Classes (3)

Protein Targets (9)

Inhibition Measurements

Activation Measurements

Other Measurements

Biological Processes (95)

Molecular Functions (42)

Ceullar Components (18)

Bioassays (222)

Research

Studies (43)

Study Types

fty 720p

Description

Cross-References

Synonyms (76)

Research Excerpts

Bioavailability

Dosage Studied

Roles (3)

Drug Classes (3)

Protein Targets (9)

Inhibition Measurements

Activation Measurements

Other Measurements

Biological Processes (95)

Molecular Functions (42)

Ceullar Components (18)

Bioassays (222)

Research

Studies (43)

Study Types

Related Drugs (17)

Related Conditions (23)