Target family: Lysophospholipid (S1P) receptors (type: gpcr)
Target: S1P<sub>3</sub> receptor

Ligand: AFD(R) (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): The immune modulator FTY720 targets sphingosine 1-phosphate receptors.
Published in: J Biol Chem

Ligand: ASP4058 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.039999961853027 pEC50
Reference (Journal): ASP4058, a novel agonist for sphingosine 1-phosphate receptors 1 and 5, ameliorates rodent experimental autoimmune encephalomyelitis with a favorable safety profile.
Published in: PLoS ONE

Ligand: AUY954 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): A monoselective sphingosine-1-phosphate receptor-1 agonist prevents allograft rejection in a stringent rat heart transplantation model.
Published in: Chem Biol

Ligand: AUY954 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Synthesis and biological evaluation of gamma-aminophosphonates as potent, subtype-selective sphingosine 1-phosphate receptor agonists and antagonists.
Published in: Bioorg Med Chem

Ligand: compound 26 [PMID: 16190743] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 4.9 pIC50
Reference (Journal): Discovery of potent 3,5-diphenyl-1,2,4-oxadiazole sphingosine-1-phosphate-1 (S1P1) receptor agonists with exceptional selectivity against S1P2 and S1P3.
Published in: J Med Chem

Ligand: compound 43 [PMID: 26751273] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.099999904632568 pEC50
Reference (Journal): Discovery of Tetrahydropyrazolopyridine as Sphingosine 1-Phosphate Receptor 3 (S1P3)-Sparing S1P1 Agonists Active at Low Oral Doses.
Published in: J Med Chem

Ligand: CYM-5541 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 8.5 pA2
Reference (Journal): Bitopic Sphingosine 1-Phosphate Receptor 3 (S1P3) Antagonist Rescue from Complete Heart Block: Pharmacological and Genetic Evidence for Direct S1P3 Regulation of Mouse Cardiac Conduction.
Published in: Mol Pharmacol

Ligand: CYM-5541 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Novel selective allosteric and bitopic ligands for the S1P(3) receptor.
Published in: ACS Chem Biol

Ligand: fingolimod-phosphate (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pIC50
Reference (Journal): The immune modulator FTY720 targets sphingosine 1-phosphate receptors.
Published in: J Biol Chem

Ligand: fingolimod-phosphate (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): The immune modulator FTY720 targets sphingosine 1-phosphate receptors.
Published in: J Biol Chem

Ligand: fingolimod-phosphate (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pIC50
Reference (Journal): Immune cell regulation and cardiovascular effects of sphingosine 1-phosphate receptor agonists in rodents are mediated via distinct receptor subtypes.
Published in: J Pharmacol Exp Ther

Ligand: fingolimod-phosphate (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Immune cell regulation and cardiovascular effects of sphingosine 1-phosphate receptor agonists in rodents are mediated via distinct receptor subtypes.
Published in: J Pharmacol Exp Ther

Ligand: mocravimod-phosphate (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 6 pEC50
Reference (Journal): Use of sphingosine-1-phosphate 1 receptor agonist, KRP-203, in combination with a subtherapeutic dose of cyclosporine A for rat renal transplantation.
Published in: Transplantation

Ligand: ozanimod (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: EMA & FDA (2020)
Primary target: no
Median affinity: 5 pEC50
Reference (Journal): Ozanimod (RPC1063) is a potent sphingosine-1-phosphate receptor-1 (S1P1 ) and receptor-5 (S1P5 ) agonist with autoimmune disease-modifying activity.
Published in: Br J Pharmacol

Ligand: ponesimod (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: EMA & FDA (2021)
Primary target: no
Median affinity: 5.679999828338623 pIC50
Reference (Journal): 2-imino-thiazolidin-4-one derivatives as potent, orally active S1P1 receptor agonists.
Published in: J Med Chem

Ligand: (S)-FTY720-phosphate (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.510000228881836 pEC50
Reference (Journal): A monoselective sphingosine-1-phosphate receptor-1 agonist prevents allograft rejection in a stringent rat heart transplantation model.
Published in: Chem Biol

Ligand: siponimod (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2019), EMA (2020)
Primary target: no
Median affinity: 5.300000190734863 pEC50
Reference (Journal): Discovery of BAF312 (Siponimod), a Potent and Selective S1P Receptor Modulator.
Published in: ACS Med Chem Lett

Ligand: sphingosine 1-phosphate (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Comparison of intrinsic activities of the putative sphingosine 1-phosphate receptor subtypes to regulate several signaling pathways in their cDNA-transfected Chinese hamster ovary cells.
Published in: J Biol Chem

Ligand: sphingosine 1-phosphate (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Sphingosine 1-phosphate-induced cell rounding and neurite retraction are mediated by the G protein-coupled receptor H218.
Published in: J Biol Chem

Ligand: sphingosine 1-phosphate (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Identification of Leu276 of the S1P1 receptor and Phe263 of the S1P3 receptor in interaction with receptor specific agonists by molecular modeling, site-directed mutagenesis, and affinity studies.
Published in: Mol Pharmacol

Ligand: sphingosine 1-phosphate (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Characterization of the human and mouse sphingosine 1-phosphate receptor, S1P5 (Edg-8): structure-activity relationship of sphingosine1-phosphate receptors.
Published in: Biochemistry

Ligand: sphingosine 1-phosphate (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): The immune modulator FTY720 targets sphingosine 1-phosphate receptors.
Published in: J Biol Chem

Ligand: sphingosine 1-phosphate (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.640000343322754 pEC50
Reference (Journal): Sphingosine 1-phosphate (S1P) receptor subtypes S1P1 and S1P3, respectively, regulate lymphocyte recirculation and heart rate.
Published in: J Biol Chem

Ligand: sphingosine 1-phosphate (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): A monoselective sphingosine-1-phosphate receptor-1 agonist prevents allograft rejection in a stringent rat heart transplantation model.
Published in: Chem Biol