(S)-FTY720-phosphate [Ligand Id: 6996] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL366208 (Fty720-p, FTY-720P) |
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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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
