Target family: Lysophospholipid (S1P) receptors (type: gpcr)
Target: S1P<sub>2</sub> receptor

Ligand: AUY954 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: 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: compound 16 [PMID: 26794040] (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 8.09000015258789 pIC50
Reference (Journal): Discovery of novel S1P2 antagonists, part 3: Improving the oral bioavailability of a series of 1,3-bis(aryloxy)benzene derivatives.
Published in: Bioorg Med Chem Lett

Ligand: compound 43 [PMID: 26751273] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 4.5 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: CYM5520 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.320000171661377 pEC50
Reference (Journal): A sphingosine 1-phosphate receptor 2 selective allosteric agonist.
Published in: Bioorg Med Chem

Ligand: fingolimod-phosphate (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.460000038146973 pEC50
Reference (Journal): FTY720 Phosphate Activates Sphingosine-1-Phosphate Receptor 2 and Selectively Couples to Gα12/13/Rho/ROCK to Induce Myofibroblast Contraction.
Published in: Mol Pharmacol

Ligand: JTE-013 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Enhancement of sphingosine 1-phosphate-induced migration of vascular endothelial cells and smooth muscle cells by an EDG-5 antagonist.
Published in: Biochem Biophys Res Commun

Ligand: JTE-013 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.769999980926514 pIC50
Reference (Journal): Enhancement of sphingosine 1-phosphate-induced migration of vascular endothelial cells and smooth muscle cells by an EDG-5 antagonist.
Published in: Biochem Biophys Res Commun

Ligand: JTE-013 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Antiproliferative property of sphingosine 1-phosphate in rat hepatocytes involves activation of Rho via Edg-5.
Published in: Gastroenterology

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: S1P d20:1 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): S1P d20:1, an endogenous modulator of S1P d18:1/S1P<sub>2</sub> -dependent signaling.
Published in: FASEB J

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): 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:  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): A monoselective sphingosine-1-phosphate receptor-1 agonist prevents allograft rejection in a stringent rat heart transplantation model.
Published in: Chem Biol

Ligand: sphingosine 1-phosphate (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 pEC50
Reference (Journal): Sphingosine 1-phosphate (S1P) receptor subtypes S1P1 and S1P3, respectively, regulate lymphocyte recirculation and heart rate.
Published in: J Biol Chem