SEW2871 [Ligand Id: 2926] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL224720 (SEW-2871)
  • S1P1 receptor/Sphingosine 1-phosphate receptor Edg-1 in Human [ChEMBL: CHEMBL4333] [GtoPdb: 275] [UniProtKB: P21453]
  • S1P1 receptor in Mouse [GtoPdb: 275] [UniProtKB: O08530]
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  • S1P3 receptor/Sphingosine 1-phosphate receptor Edg-3 in Human [ChEMBL: CHEMBL3892] [GtoPdb: 277] [UniProtKB: Q99500]
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  • S1P2 receptor/Sphingosine 1-phosphate receptor Edg-5 in Human [ChEMBL: CHEMBL2955] [GtoPdb: 276] [UniProtKB: O95136]
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  • S1P4 receptor/Sphingosine 1-phosphate receptor Edg-6 in Human [ChEMBL: CHEMBL3230] [GtoPdb: 278] [UniProtKB: O95977]
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  • S1P5 receptor/Sphingosine 1-phosphate receptor Edg-8 in Human [ChEMBL: CHEMBL2274] [GtoPdb: 279] [UniProtKB: Q9H228]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
S1P1 receptor/Sphingosine 1-phosphate receptor Edg-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4333] [GtoPdb: 275] [UniProtKB: P21453]
GtoPdb - - 7.7 pKi 18 nM Ki J Biol Chem (2004) 279: 13839-48 [PMID:14732717]
ChEMBL Displacement of [33P]sphingosine 1 phosphate from human S1P1 receptor expressed in CHO cells B 7.43 pIC50 37 nM IC50 J Med Chem (2004) 47: 6662-6665 [PMID:15615513]
ChEMBL Displacement of [33P]S1P from human S1P1R expressed in CHO cell membranes B 7.43 pIC50 37 nM IC50 ACS Med Chem Lett (2011) 2: 97-101 [PMID:24900286]
ChEMBL Agonist activity at human S1P1 receptor expressed in human U2OS cells co-expressing eGFP assessed as receptor internalization into cytoplasm using Hoechst dye staining F 6.57 pEC50 270 nM EC50 Bioorg Med Chem Lett (2012) 22: 527-531 [PMID:22104144]
ChEMBL Inhibition of S1P1 receptor (unknown origin) B 7.89 pEC50 13 nM EC50 Bioorg Med Chem Lett (2018) 28: 3585-3591 [PMID:30409535]
GtoPdb - - 7.9 pEC50 12.6 nM EC50 Mol Pharmacol (2008) 74: 1308-18 [PMID:18708635];
J Biol Chem (2004) 279: 13839-48 [PMID:14732717]
S1P1 receptor in Mouse [GtoPdb: 275] [UniProtKB: O08530]
GtoPdb - - 7.68 pEC50 20.7 nM EC50 J Biol Chem (2004) 279: 13839-48 [PMID:14732717]
S1P3 receptor/Sphingosine 1-phosphate receptor Edg-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3892] [GtoPdb: 277] [UniProtKB: Q99500]
ChEMBL Displacement of [33P]sphingosine 1 phosphate from human S1P3 receptor expressed in CHO cells B 5 pIC50 >10000 nM IC50 J Med Chem (2004) 47: 6662-6665 [PMID:15615513]
ChEMBL Displacement of [33P]S1P from human S1P3R expressed in CHO cell membranes B 8 pIC50 >10 nM IC50 ACS Med Chem Lett (2011) 2: 97-101 [PMID:24900286]
ChEMBL Agonist activity at human S1P3 receptor expressed in CHO-K1 cells co-expressing Gq/i5 G-protein assessed as calcium mobilization by FLIPR assay F 4.6 pEC50 >25000 nM EC50 Bioorg Med Chem Lett (2012) 22: 527-531 [PMID:22104144]
S1P2 receptor/Sphingosine 1-phosphate receptor Edg-5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2955] [GtoPdb: 276] [UniProtKB: O95136]
ChEMBL Displacement of [33P]sphingosine 1 phosphate from human S1P2 receptor expressed in CHO cells B 5 pIC50 >10000 nM IC50 J Med Chem (2004) 47: 6662-6665 [PMID:15615513]
S1P4 receptor/Sphingosine 1-phosphate receptor Edg-6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3230] [GtoPdb: 278] [UniProtKB: O95977]
ChEMBL Displacement of [33P]sphingosine 1 phosphate from human S1P4 receptor expressed in CHO cells B 5 pIC50 >10000 nM IC50 J Med Chem (2004) 47: 6662-6665 [PMID:15615513]
S1P5 receptor/Sphingosine 1-phosphate receptor Edg-8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2274] [GtoPdb: 279] [UniProtKB: Q9H228]
ChEMBL Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells B 5.34 pIC50 4600 nM IC50 J Med Chem (2004) 47: 6662-6665 [PMID:15615513]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]