fingolimod-phosphate [Ligand Id: 2924] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL114606
  • 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]
  • S1P4 receptor in Mouse [GtoPdb: 278] [UniProtKB: Q9Z0L1]
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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 - - 9.52 pIC50 0.3 nM IC50 J Pharmacol Exp Ther (2004) 309: 758-68 [PMID:14747617]
ChEMBL Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 1 expressed on CHO cell membranes B 9.55 pIC50 0.28 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 3351-3355 [PMID:15149705]
ChEMBL Displacement of [33P]sphingosine 1 phosphate from human S1P1 receptor expressed in CHO cells B 9.55 pIC50 0.28 nM IC50 J. Med. Chem. (2004) 47: 6662-6665 [PMID:15615513]
ChEMBL Displacement of 33-P-S1P from from human S1P receptor expressed in CHO cell membranes after 50 mins by scintillation counting B 10.85 pIC50 0.01 nM IC50 ACS Med. Chem. Lett. (2016) 7: 283-288 [PMID:26985316]
ChEMBL Agonist activity at S1P1 receptor (unknown origin) expressed in CHO cells preincubated for 2 hrs followed by D2-labeled IP1 and Ab-Cryp addition measured after 1 hr by fluorescence assay B 7.85 pEC50 14 nM EC50 MedChemComm (2013) 4: 1267-1274
ChEMBL Agonist activity at human S1P1 receptor expressed in CHO cells preincubated for 2 hrs before IP1 addition by IP1-HTRF assay B 8.04 pEC50 9.1 nM EC50 Eur. J. Med. Chem. (2014) 85: 1-15 [PMID:25072873]
ChEMBL Effective concentration against sphingosine-1-phosphate receptor 1 determined by a [c-35S]-GTP binding assay B 8.89 pEC50 1.3 nM EC50 Bioorg. Med. Chem. Lett. (2005) 15: 3568-3572 [PMID:15982878]
ChEMBL Activity at human S1P1 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay F 8.89 pEC50 1.3 nM EC50 Bioorg. Med. Chem. (2007) 15: 663-677 [PMID:17113298]
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 8.92 pEC50 1.2 nM EC50 J. Med. Chem. (2005) 48: 5373-5377 [PMID:16078855]
ChEMBL Agonist activity at human S1P1 receptor by GTPgammaS binding assay B 9.42 pEC50 0.38 nM EC50 ACS Med. Chem. Lett. (2016) 7: 283-288 [PMID:26985316]
ChEMBL Agonist activity at human S1P1 receptor expressed in human Chem1 cells assessed as intracellular calcium mobilization F 9.46 pEC50 0.35 nM EC50 J. Med. Chem. (2010) 53: 3154-3168 [PMID:20337461]
GtoPdb - - 9.5 pEC50 - - - J Biol Chem (2002) 277: 21453-7 [PMID:11967257];
J Pharmacol Exp Ther (2004) 309: 758-68 [PMID:14747617]
GtoPdb - - 9.52 pEC50 0.3 nM EC50 J Pharmacol Exp Ther (2004) 309: 758-68 [PMID:14747617]
ChEMBL Activity at human S1P1 receptor expressed in CHO cells by [35S]GTPgammaS binding assay F 9.52 pEC50 0.3 nM EC50 J. Med. Chem. (2004) 47: 6662-6665 [PMID:15615513]
ChEMBL Agonist activity at human S1P1 receptor expressed in CHO cells co-expressing GFP assessed as cellular internalization after 45 mins by Hoechst assay B 10.15 pEC50 0.07 nM EC50 ACS Med. Chem. Lett. (2016) 7: 283-288 [PMID:26985316]
S1P1 receptor in Mouse [GtoPdb: 275] [UniProtKB: O08530]
GtoPdb - - 9.5 pEC50 - - - J Pharmacol Exp Ther (2008) 324: 276-83 [PMID:17898319];
J Biol Chem (2002) 277: 21453-7 [PMID:11967257]
S1P3 receptor/Sphingosine 1-phosphate receptor Edg-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3892] [GtoPdb: 277] [UniProtKB: Q99500]
ChEMBL Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 3 expressed on CHO cell membranes B 8.2 pIC50 6.3 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 3351-3355 [PMID:15149705]
ChEMBL Displacement of [33P]sphingosine 1 phosphate from human S1P3 receptor expressed in CHO cells B 8.2 pIC50 6.3 nM IC50 J. Med. Chem. (2004) 47: 6662-6665 [PMID:15615513]
GtoPdb - - 8.3 pIC50 5 nM IC50 J Biol Chem (2002) 277: 21453-7 [PMID:11967257];
J Pharmacol Exp Ther (2004) 309: 758-68 [PMID:14747617]
ChEMBL Agonist activity at S1P3 receptor (unknown origin) expressed in CHO cells preincubated for 2 hrs followed by D2-labeled IP1 and Ab-Cryp addition measured after 1 hr by fluorescence assay B 7.36 pEC50 44 nM EC50 MedChemComm (2013) 4: 1267-1274
ChEMBL Agonist activity at human S1P3 receptor expressed in CHO cells preincubated for 2 hrs before IP1 addition by IP1-HTRF assay B 7.45 pEC50 35.1 nM EC50 Eur. J. Med. Chem. (2014) 85: 1-15 [PMID:25072873]
ChEMBL Agonist activity at human S1P3 receptor expressed in CHO cells assessed as intracellular calcium mobilization F 7.92 pEC50 12 nM EC50 J. Med. Chem. (2010) 53: 3154-3168 [PMID:20337461]
ChEMBL Agonist activity at human S1P3 receptor by GTPgammaS binding assay B 8.45 pEC50 3.57 nM EC50 ACS Med. Chem. Lett. (2016) 7: 283-288 [PMID:26985316]
ChEMBL Effective concentration against sphingosine 1-phosphate receptor 3 determined by a [c-35S]-GTP binding assay B 8.7 pEC50 2 nM EC50 Bioorg. Med. Chem. Lett. (2005) 15: 3568-3572 [PMID:15982878]
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 8.85 pEC50 1.4 nM EC50 J. Med. Chem. (2005) 48: 5373-5377 [PMID:16078855]
GtoPdb - - 9.4 pEC50 - - - J Biol Chem (2002) 277: 21453-7 [PMID:11967257];
J Pharmacol Exp Ther (2004) 309: 758-68 [PMID:14747617]
ChEMBL Activity at human S1P3 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay F 10 pEC50 0.1 nM EC50 Bioorg. Med. Chem. (2007) 15: 663-677 [PMID:17113298]
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 5.96 pIC50 1100 nM IC50 J. Med. Chem. (2004) 47: 6662-6665 [PMID:15615513]
ChEMBL Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes B 9.11 pIC50 0.77 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 3351-3355 [PMID:15149705]
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]
GtoPdb - - 7.46 pEC50 35 nM EC50 Mol Pharmacol (2015) 87: 916-27 [PMID:25762025]
S1P4 receptor/Sphingosine 1-phosphate receptor Edg-6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3230] [GtoPdb: 278] [UniProtKB: O95977]
ChEMBL Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 4 expressed on CHO cell membranes B 7.82 pIC50 15 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 3351-3355 [PMID:15149705]
ChEMBL Displacement of [33P]sphingosine 1 phosphate from human S1P4 receptor expressed in CHO cells B 7.82 pIC50 15 nM IC50 J. Med. Chem. (2004) 47: 6662-6665 [PMID:15615513]
ChEMBL Effective concentration against sphingosine 1-phosphate receptor 4 determined by a [c-35S]-GTP binding assay B 7.39 pEC50 41 nM EC50 Bioorg. Med. Chem. Lett. (2005) 15: 3568-3572 [PMID:15982878]
ChEMBL Activity at human S1P4 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay F 8.4 pEC50 4 nM EC50 Bioorg. Med. Chem. (2007) 15: 663-677 [PMID:17113298]
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 8.62 pEC50 2.4 nM EC50 J. Med. Chem. (2005) 48: 5373-5377 [PMID:16078855]
GtoPdb - - 9.22 pEC50 - - - Chem Biol (2006) 13: 1227-34 [PMID:17114004];
J Biol Chem (2002) 277: 21453-7 [PMID:11967257];
J Biol Chem (2004) 279: 13839-48 [PMID:14732717];
J Pharmacol Exp Ther (2004) 309: 758-68 [PMID:14747617];
PLoS ONE (2014) 9: e110819 [PMID:25347187]
ChEMBL Agonist activity at human S1P4 receptor by GTPgammaS binding assay B 10.05 pEC50 0.09 nM EC50 ACS Med. Chem. Lett. (2016) 7: 283-288 [PMID:26985316]
S1P4 receptor in Mouse [GtoPdb: 278] [UniProtKB: Q9Z0L1]
GtoPdb - - 7.15 pEC50 - - - J Pharmacol Exp Ther (2008) 324: 276-83 [PMID:17898319];
J Biol Chem (2002) 277: 21453-7 [PMID:11967257]
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 9.11 pIC50 0.77 nM IC50 J. Med. Chem. (2004) 47: 6662-6665 [PMID:15615513]
GtoPdb - - 9.22 pIC50 0.6 nM IC50 J Pharmacol Exp Ther (2004) 309: 758-68 [PMID:14747617]
ChEMBL Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay B 7.4 pEC50 40 nM EC50 Bioorg. Med. Chem. Lett. (2005) 15: 3568-3572 [PMID:15982878]
ChEMBL Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by GTPgammaS binding assay B 7.96 pEC50 11 nM EC50 J. Med. Chem. (2015) 58: 9154-9170 [PMID:26509640]
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 8.31 pEC50 4.9 nM EC50 J. Med. Chem. (2005) 48: 5373-5377 [PMID:16078855]
ChEMBL Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay F 8.4 pEC50 4 nM EC50 Bioorg. Med. Chem. (2007) 15: 663-677 [PMID:17113298]
ChEMBL Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding assay B 8.47 pEC50 3.4 nM EC50 J. Med. Chem. (2015) 58: 9154-9170 [PMID:26509640]
ChEMBL Agonist activity at human S1P5 receptor by GTPgammaS binding assay B 9.4 pEC50 0.4 nM EC50 ACS Med. Chem. Lett. (2016) 7: 283-288 [PMID:26985316]
GtoPdb - - 9.52 pEC50 - - - Chem Biol (2006) 13: 1227-34 [PMID:17114004];
J Biol Chem (2002) 277: 21453-7 [PMID:11967257];
J Pharmacol Exp Ther (2004) 309: 758-68 [PMID:14747617]

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]