Target family: Lysophospholipid (S1P) receptors (type: gpcr)
Target: S1P<sub>4</sub> receptor

Ligand: VPC03090-P (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.760000228881836 pKd
Reference (Journal): Characterization of a sphingosine 1-phosphate receptor antagonist prodrug.
Published in: J Pharmacol Exp Ther

Ligand: VPC03090-P (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.75 pEC50
Reference (Journal): Characterization of a sphingosine 1-phosphate receptor antagonist prodrug.
Published in: J Pharmacol Exp Ther

Ligand: sphingosine 1-phosphate (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.119999885559082 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): 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

Ligand: sphingosine 1-phosphate (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pIC50
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:  pEC50
Reference (Journal): Phytosphingosine 1-phosphate: a high affinity ligand for the S1P(4)/Edg-6 receptor.
Published in: Biochem Biophys Res Commun

Ligand: sphingosine 1-phosphate (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Phytosphingosine 1-phosphate: a high affinity ligand for the S1P(4)/Edg-6 receptor.
Published in: Biochem Biophys Res Commun

Ligand: SLB736 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Sphingosine 1-Phosphate Receptor 4 Promotes Nonalcoholic Steatohepatitis by Activating NLRP3 Inflammasome.
Published in: Cell Mol Gastroenterol Hepatol

Ligand: siponimod (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2019), EMA (2020)
Primary target: no
Median affinity: 6.119999885559082 pEC50
Reference (Journal): Modulators of the Sphingosine 1-phosphate receptor 1.
Published in: Bioorg Med Chem Lett

Ligand: ponesimod (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: EMA & FDA (2021)
Primary target: no
Median affinity: 5.710000038146973 pIC50
Reference (Journal): 2-imino-thiazolidin-4-one derivatives as potent, orally active S1P1 receptor agonists.
Published in: J Med Chem

Ligand: phytosphingosine 1-phosphate (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8.8 pIC50
Reference (Journal): Phytosphingosine 1-phosphate: a high affinity ligand for the S1P(4)/Edg-6 receptor.
Published in: Biochem Biophys Res Commun

Ligand: ozanimod (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: EMA & FDA (2020)
Primary target: no
Median affinity: 5.099999904632568 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: mocravimod-phosphate (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8 pEC50
Reference (Journal): A novel sphingosine 1-phosphate receptor agonist, 2-amino-2-propanediol hydrochloride (KRP-203), regulates chronic colitis in interleukin-10 gene-deficient mice.
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): Sphingosine 1-phosphate (S1P) receptor subtypes S1P1 and S1P3, respectively, regulate lymphocyte recirculation and heart rate.
Published in: J Biol Chem

Ligand: fingolimod-phosphate (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.150000095367432 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:  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: 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:  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: fingolimod-phosphate (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.150000095367432 pEC50
Reference (Journal): A novel sphingosine 1-phosphate receptor agonist, 2-amino-2-propanediol hydrochloride (KRP-203), regulates chronic colitis in interleukin-10 gene-deficient mice.
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: etrasimod (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2023)
Primary target: no
Median affinity: 6.829999923706055 pEC50
Reference (Journal): P2Y(1) and P2Y(2) receptors are coupled to the NO/cGMP pathway to vasodilate the rat arterial mesenteric bed.
Published in: Br J Pharmacol

Ligand: etrasimod (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2023)
Primary target: no
Median affinity: 6.829999923706055 pEC50
Reference (Journal): Discovery of APD334: Design of a Clinical Stage Functional Antagonist of the Sphingosine-1-phosphate-1 Receptor.
Published in: ACS Med Chem Lett

Ligand: dihydrosphingosine 1-phosphate (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8 pIC50
Reference (Journal): Phytosphingosine 1-phosphate: a high affinity ligand for the S1P(4)/Edg-6 receptor.
Published in: Biochem Biophys Res Commun

Ligand: CYM-50358 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.599999904632568 pIC50
Reference (Journal): TGFβ1 evokes myoblast apoptotic response via a novel signaling pathway involving S1P4 transactivation upstream of Rho-kinase-2 activation.
Published in: FASEB J

Ligand: CYM-50358 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.599999904632568 pIC50
Reference (Journal): Discovery, design and synthesis of the first reported potent and selective sphingosine-1-phosphate 4 (S1P4) receptor antagonists.
Published in: Bioorg Med Chem Lett

Ligand: CYM-50308 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.25 pEC50
Reference (Journal): Discovery, synthesis and SAR analysis of novel selective small molecule S1P4-R agonists based on a (2Z,5Z)-5-((pyrrol-3-yl)methylene)-3-alkyl-2-(alkylimino)thiazolidin-4-one chemotype.
Published in: Bioorg Med Chem Lett

Ligand: compound 5c [PMID: 27894870] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 6.699999809265137 pEC50
Reference (Journal): A benzo[b]thiophene-based selective type 4 S1P receptor agonist.
Published in: Bioorg Med Chem Lett

Ligand: compound 5c [PMID: 27894870] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 6.809999942779541 pEC50
Reference (Journal): A benzo[b]thiophene-based selective type 4 S1P receptor agonist.
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: 4.400000095367432 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: compound 26 [PMID: 16190743] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 7.15 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: 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: ASP4058 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.639999866485596 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: AFD(R) (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  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: 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