(S)-FTY720-phosphate [Ligand Id: 6996] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL366208 (Fty720-p, FTY-720P)
  • S1P1 receptor/Sphingosine 1-phosphate receptor 1 in Rat [ChEMBL: CHEMBL1914263] [GtoPdb: 275] [UniProtKB: P48303]
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  • S1P1 receptor/Sphingosine 1-phosphate receptor Edg-1 in Human [ChEMBL: CHEMBL4333] [GtoPdb: 275] [UniProtKB: P21453]
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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 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1914263] [GtoPdb: 275] [UniProtKB: P48303]
ChEMBL Agonist activity at rat S1P1 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay F 9.54 pEC50 0.29 nM EC50 ACS Med. Chem. Lett. (2011) 2: 368-372 [PMID:24900318]
ChEMBL Agonist activity at rat S1P1 receptor expressed in CHO-K1 cells assessed as induction of GTPgammaS binding F 9.54 pEC50 0.29 nM EC50 Eur. J. Med. Chem. (2012) 51: 92-98 [PMID:22405291]
S1P1 receptor/Sphingosine 1-phosphate receptor Edg-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4333] [GtoPdb: 275] [UniProtKB: P21453]
ChEMBL Agonist activity at human S1P1 expressed in CHO cells after 60 mins by [35S]GTPgammaS binding assay F 8.68 pIC50 2.1 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 553-557 [PMID:22119341]
ChEMBL Displacement of [33P]S1P from human S1P1R expressed in CHO cell membranes B 9.55 pIC50 0.28 nM IC50 ACS Med. Chem. Lett. (2011) 2: 97-101 [PMID:24900286]
ChEMBL Agonist activity at human S1P1 receptor expressed in CHO-K1 EDG1 cells by beta-arrestin recruitment assay B 7.7 pEC50 19.95 nM EC50 J. Med. Chem. (2016) 59: 1003-1020 [PMID:26751273]
ChEMBL Agonist activity at human S1P1 receptor expressed in CHO-K1 EDG1 cells expressing beta-arrestin 2 after 105 mins by chemi-luminescence assay F 7.7 pEC50 19.95 nM EC50 J. Med. Chem. (2011) 54: 6724-6733 [PMID:21838322]
ChEMBL Agonist activity at human S1P1 receptor expressed in CHOK1 cell membranes by [35S]GTPgammaS binding assay F 8.15 pEC50 7 nM EC50 Bioorg. Med. Chem. (2014) 22: 4246-4256 [PMID:24909680]
ChEMBL Agonist activity at human S1P1 receptor expressed in CHOK1 cell membranes by [35S]-GTPgammaS binding assay F 8.15 pEC50 7 nM EC50 Bioorg Med Chem Lett (2017) 27: 1371-1378 [PMID:28236593]
ChEMBL Agonist activity at recombinant human S1P1 receptor expressed in Chem-1 cells assessed as calcium flux measured for 180 secs by FLIPR assay F 8.4 pEC50 4 nM EC50 ACS Med Chem Lett (2021) 12: 351-355 [PMID:33738061]
ChEMBL Agonist activity at human S1P1 receptor expressed in RH7777 cells by [35S]GTP-gammaS accumulation assay B 8.4 pEC50 3.98 nM EC50 J. Med. Chem. (2016) 59: 1003-1020 [PMID:26751273]
ChEMBL Agonist activity at human S1P1 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assay F 8.69 pEC50 2.02 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 2264-2269 [PMID:20188554]
ChEMBL Agonist activity at human recombinant S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting assay F 9.15 pEC50 0.7 nM EC50 J Med Chem (2019) 62: 2265-2285 [PMID:30785748]
ChEMBL Agonist activity at human S1P1 receptor expressed in EDG1-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assay B 9.4 pEC50 0.4 nM EC50 Bioorg. Med. Chem. Lett. (2016) 26: 466-471 [PMID:26687487]
ChEMBL Agonist activity at human S1P1 receptor expressed in CHO-K1 cells assessed as induction of GTPgammaS binding F 9.43 pEC50 0.37 nM EC50 Eur. J. Med. Chem. (2012) 51: 92-98 [PMID:22405291]
ChEMBL Agonist activity at human S1P1 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay F 9.43 pEC50 0.37 nM EC50 ACS Med. Chem. Lett. (2011) 2: 368-372 [PMID:24900318]
ChEMBL Agonism of human S1P-1 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand F 9.52 pEC50 0.3 nM EC50 J. Med. Chem. (2005) 48: 5373-5377 [PMID:16078855]
ChEMBL Agonist activity at SIP1 receptor F 9.52 pEC50 0.3 nM EC50 Bioorg. Med. Chem. Lett. (2012) 22: 3973-3977 [PMID:22583616]
ChEMBL Induction of internalization of C-terminal GFP-fused human S1P1 receptor expressed in CHO cell membranes after 50 mins B 9.55 pEC50 0.28 nM EC50 J. Med. Chem. (2016) 59: 2820-2840 [PMID:26924461]
ChEMBL Agonist activity at human recombinant C-terminal GFP-fused S1P1 expressed in CHO cells assessed as induction of receptor internalization incubated for 50 mins by fluorescence based confocal laser scanning microscopic analysis B 10.15 pEC50 0.07 nM EC50 J Med Chem (2019) 62: 2265-2285 [PMID:30785748]
ChEMBL Agonist activity at human recombinant S1P1 expressed in CHO cells assessed as stimulation of ERK phosphorylation incubated for 7 mins by microplate reader analysis B 10.7 pEC50 0.02 nM EC50 J Med Chem (2019) 62: 2265-2285 [PMID:30785748]
ChEMBL Agonist activity at human S1P1 receptor assessed as effect on calcium mobilization by Gi dependent whole cell assay F 10.92 pEC50 0.01 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 2264-2269 [PMID:20188554]
S1P3 receptor/Sphingosine 1-phosphate receptor Edg-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3892] [GtoPdb: 277] [UniProtKB: Q99500]
ChEMBL Agonist activity at human S1P3 expressed in CHO cells after 60 mins by [35S]GTPgammaS binding assay F 7.64 pIC50 23 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 553-557 [PMID:22119341]
ChEMBL Displacement of [33P]S1P from human S1P3R expressed in CHO cell membranes B 8.2 pIC50 6.3 nM IC50 ACS Med. Chem. Lett. (2011) 2: 97-101 [PMID:24900286]
ChEMBL Agonist activity at human S1P3 receptor expressed in EDG3-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assay B 7.03 pEC50 94 nM EC50 Bioorg. Med. Chem. Lett. (2016) 26: 466-471 [PMID:26687487]
ChEMBL Agonist activity at human S1P3 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assay F 7.56 pEC50 27.84 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 2264-2269 [PMID:20188554]
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 7.57 pEC50 27 nM EC50 Bioorg. Med. Chem. Lett. (2012) 22: 527-531 [PMID:22104144]
ChEMBL Agonist activity at recombinant human S1P3 receptor expressed in Chem-1 cells assessed as calcium flux measured for 180 secs by FLIPR assay F 7.57 pEC50 27 nM EC50 ACS Med Chem Lett (2021) 12: 351-355 [PMID:33738061]
ChEMBL Agonist activity at human S1P3 receptor expressed in RBL cells by [35S]GTP-gammaS accumulation assay B 8.3 pEC50 5.01 nM EC50 J. Med. Chem. (2016) 59: 1003-1020 [PMID:26751273]
ChEMBL Agonist activity at human S1P3 receptor expressed in RBL cells assessed as [35S]GTPgammaS binding after 3 hrs by radiometric assay F 8.3 pEC50 5.01 nM EC50 J. Med. Chem. (2011) 54: 6724-6733 [PMID:21838322]
ChEMBL Agonist activity at human S1P3 receptor expressed in CHO-K1 cells assessed as induction of GTPgammaS binding F 8.48 pEC50 3.3 nM EC50 Eur. J. Med. Chem. (2012) 51: 92-98 [PMID:22405291]
ChEMBL Agonist activity at human S1P3R expressed in CHO-K1 cells by [35S]GTPgammaS binding assay F 8.48 pEC50 3.3 nM EC50 ACS Med. Chem. Lett. (2011) 2: 368-372 [PMID:24900318]
ChEMBL Agonism of human S1P-3 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand F 8.51 pEC50 3.1 nM EC50 J. Med. Chem. (2005) 48: 5373-5377 [PMID:16078855]
GtoPdb - - 8.51 pEC50 3.1 nM EC50 Chem Biol (2006) 13: 1227-34 [PMID:17114004]
ChEMBL Agonist activity at SIP3 receptor F 8.52 pEC50 3 nM EC50 Bioorg. Med. Chem. Lett. (2012) 22: 3973-3977 [PMID:22583616]
ChEMBL Agonist activity at human S1P3 receptor expressed in CHOK1 cell membranes by [35S]GTPgammaS binding assay F 8.7 pEC50 2 nM EC50 Bioorg. Med. Chem. (2014) 22: 4246-4256 [PMID:24909680]
ChEMBL Agonist activity at human S1P3 receptor assessed as effect on calcium mobilization by Gi dependent whole cell assay F 9.87 pEC50 0.13 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 2264-2269 [PMID:20188554]
S1P2 receptor/Sphingosine 1-phosphate receptor Edg-5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2955] [GtoPdb: 276] [UniProtKB: O95136]
ChEMBL Agonist activity at human S1P2 expressed in CHO cells after 60 mins by [35S]GTPgammaS binding assay F 8.23 pIC50 5.9 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 553-557 [PMID:22119341]
ChEMBL Agonist activity at human S1P2 receptor expressed in yeast MMY24 assessed as conversion of FDGlu to fluorescein after 24 hrs F 4.5 pEC50 >31622.78 nM EC50 J. Med. Chem. (2011) 54: 6724-6733 [PMID:21838322]
ChEMBL Agonism of human S1P-2 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand F 5 pEC50 >10000 nM EC50 J. Med. Chem. (2005) 48: 5373-5377 [PMID:16078855]
ChEMBL Agonist activity at human S1P2 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assay F 5.3 pEC50 >5000 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 2264-2269 [PMID:20188554]
ChEMBL Agonist activity at recombinant human S1P2 receptor expressed in Chem-1 cells assessed as calcium flux measured for 180 secs by FLIPR assay F 8.3 pEC50 >5 nM EC50 ACS Med Chem Lett (2021) 12: 351-355 [PMID:33738061]
S1P4 receptor/Sphingosine 1-phosphate receptor Edg-6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3230] [GtoPdb: 278] [UniProtKB: O95977]
ChEMBL Agonist activity at human S1P4 expressed in CHO cells after 60 mins by [35S]GTPgammaS binding assay F 8.66 pIC50 2.2 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 553-557 [PMID:22119341]
ChEMBL Agonist activity at human S1P4 expressed in CHO-K1 aequorin cells assessed as calcium accumulation of by luminescence assay in presence of cofactor coelenterazine F 6.7 pEC50 199.53 nM EC50 J. Med. Chem. (2011) 54: 6724-6733 [PMID:21838322]
ChEMBL Agonist activity at human S1P4 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assay F 7.65 pEC50 22.16 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 2264-2269 [PMID:20188554]
ChEMBL Agonist activity at recombinant human S1P4 receptor expressed in Chem-1 cells assessed as calcium flux measured for 180 secs by FLIPR assay F 7.66 pEC50 22 nM EC50 ACS Med Chem Lett (2021) 12: 351-355 [PMID:33738061]
ChEMBL Agonist activity at human recombinant S1P4 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting assay F 8.8 pEC50 1.6 nM EC50 J Med Chem (2019) 62: 2265-2285 [PMID:30785748]
ChEMBL Agonism of human S1P-4 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand F 9.22 pEC50 0.6 nM EC50 J. Med. Chem. (2005) 48: 5373-5377 [PMID:16078855]
S1P5 receptor/Sphingosine 1-phosphate receptor Edg-8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2274] [GtoPdb: 279] [UniProtKB: Q9H228]
ChEMBL Agonist activity at human S1P5 receptor expressed in CHO-K1 aequorin cells assessed as calcium accumulation of by luminescence assay in presence of cofactor coelenterazine F 7.2 pEC50 63.1 nM EC50 J. Med. Chem. (2011) 54: 6724-6733 [PMID:21838322]
ChEMBL Agonist activity at human recombinant S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting assay F 9.17 pEC50 0.67 nM EC50 J Med Chem (2019) 62: 2265-2285 [PMID:30785748]
ChEMBL Agonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq dependent whole cell assay F 9.44 pEC50 0.36 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 2264-2269 [PMID:20188554]
ChEMBL Agonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as calcium flux measured for 180 secs by FLIPR assay F 9.44 pEC50 0.36 nM EC50 ACS Med Chem Lett (2021) 12: 351-355 [PMID:33738061]
ChEMBL Agonist activity at human S1P5R F 9.47 pEC50 0.34 nM EC50 ACS Med. Chem. Lett. (2011) 2: 368-372 [PMID:24900318]
ChEMBL Agonism of human S1P-5 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand F 9.52 pEC50 0.3 nM EC50 J. Med. Chem. (2005) 48: 5373-5377 [PMID:16078855]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]