(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 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 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 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 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 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 by [35S]GTPgammaS binding assay | F | 9.43 | pEC50 | 0.37 | nM | EC50 | ACS Med Chem Lett (2011) 2: 368-372 [PMID:24900318] |
| 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 | GPCR PRESTO-Tango dose-response in agonist mode with target: S1PR1 | F | 9.49 | pEC50 | 0.32 | nM | EC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| 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 | 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 | 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] |
| ChEMBL | Agonist activity at human recombinant S1P1 expressed in CHO cell membranes assessed as stimulation of cAMP accumulation incubated for 10 mins by HTRF assay | F | 11.15 | pEC50 | 0.01 | nM | EC50 | J Med Chem (2019) 62: 2265-2285 [PMID:30785748] |
| 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 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]
