Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T13852 Target Info
Target Name Sphingosine-1-phosphate receptor 1 (S1PR1)
Synonyms
Sphingosine 1-phosphate receptor Edg-1; S1P1; S1P receptor Edg-1; S1P receptor 1; Endothelial differentiation G-protein coupled receptor 1; CHEDG1; CD363
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Target Type Successful Target
Gene Name S1PR1
Biochemical Class GPCR rhodopsin
UniProt ID
S1PR1_HUMAN
Co-Targets of This Target  Top
Co-Target Name Sphingosine-1-phosphate receptor 5 (S1PR5) Clinical trial Target
UniProt ID S1PR5_HUMAN
Gene Name S1PR5
Synonyms
Sphingosine 1-phosphate receptor Edg-8; S1PR5; S1P5; S1P receptor Edg-8; S1P receptor 5; Endothelial differentiation G-protein-coupled receptor 8
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Representative Drug(s) Sphingosine-1-phosphate Drug Info EC50 = 0.2 nM Click to Show More [1]
2 Fingolimod Drug Info EC50 = 0.3 nM [2]
3 ONO-4641 Drug Info EC50 = 0.33 nM [3]
4 Siponimod Drug Info EC50 = 0.98 nM [2]
5 Ozanimod Drug Info EC50 = 4.3 nM [4]
6 Etrasimod Drug Info EC50 = 24.4 nM [5]
Co-Target Name Sphingosine-1-phosphate receptor 3 (S1PR3) Patented-recorded Target
UniProt ID S1PR3_HUMAN
Gene Name S1PR3
Synonyms
Sphingosine 1-phosphate receptor Edg-3; S1PR3; S1P3; S1P receptor Edg-3; S1P receptor 3; Endothelial differentiation G-protein coupled receptor 3
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Representative Drug(s) Sphingosine-1-phosphate Drug Info IC50 = 0.04 nM Click to Show More [6]
2 Fingolimod Drug Info EC50 = 3 nM [2]
3 Ponesimod Drug Info EC50 = 109 nM [1]
Co-Target Name Sphingosine-1-phosphate receptor 2 (S1PR2) Clinical trial Target
UniProt ID S1PR2_HUMAN
Gene Name S1PR2
Synonyms
Sphingosine 1-phosphate receptor Edg-5; S1PR2; S1P2; S1P receptor Edg-5; S1P receptor 2; Endothelial differentiation G-protein coupled receptor 5
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Representative Drug(s) Sphingosine-1-phosphate Drug Info IC50 = 0.23 nM [6]
Co-Target Name Sphingosine-1-phosphate receptor 4 (S1PR4) Literature-reported Target
UniProt ID S1PR4_HUMAN
Gene Name S1PR4
Synonyms
Sphingosine 1-phosphate receptor Edg-6; Sphingosine 1-phosphate receptor 4; S1P4; S1P receptor Edg-6; S1P receptor 4; Endothelial differentiation G-protein coupled receptor 6; EDG6
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Representative Drug(s) Fingolimod Drug Info EC50 = 0.3 nM Click to Show More [2]
2 Sphingosine-1-phosphate Drug Info IC50 = 1.04 nM [7]
3 ONO-4641 Drug Info Ki = 28.8 nM [3]
4 Etrasimod Drug Info EC50 = 147 nM [5]
5 Siponimod Drug Info EC50 = 750 nM [2]
References  Top
REF 1 2-imino-thiazolidin-4-one derivatives as potent, orally active S1P1 receptor agonists. J Med Chem. 2010 May 27;53(10):4198-211.
REF 2 Modulators of the Sphingosine 1-phosphate receptor 1. Bioorg Med Chem Lett. 2013 Dec 1;23(23):6377-89.
REF 3 Discovery of a 1-Methyl-3,4-dihydronaphthalene-Based Sphingosine-1-Phosphate (S1P) Receptor Agonist Ceralifimod (ONO-4641). A S1P. J Med Chem. 2017 Dec 14;60(23):9508-30.
REF 4 Small-molecule agents for the treatment of inflammatory bowel disease. Bioorg Med Chem Lett. 2019 Aug 15;29(16):2034-2041.
REF 5 Discovery of APD334: Design of a Clinical Stage Functional Antagonist of the Sphingosine-1-phosphate-1 Receptor. ACS Med Chem Lett. 2014 Nov 4;5(12):1313-7.
REF 6 Potent S1P receptor agonists replicate the pharmacologic actions of the novel immune modulator FTY720. Bioorg Med Chem Lett. 2004 Jun 21;14(12):3351-5.
REF 7 Exploration of amino alcohol derivatives as novel, potent, and highly selective sphingosine-1-phosphate receptor subtype-1 agonists. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2520-4.

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