fingolimod-phosphate [Ligand Id: 2924] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL114606 |
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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 | F | 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 | F | 8.04 | pEC50 | 9.1 | nM | EC50 | Eur J Med Chem (2014) 85: 1-15 [PMID:25072873] |
| ChEMBL | Agonist activity at S1P1 (unknown origin) by HTRF assay | B | 8.36 | pEC50 | 4.4 | nM | EC50 | Bioorg Med Chem Lett (2020) 30: 127141-127141 [PMID:32249117] |
| 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 recombinant human S1P1 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting method | F | 9.15 | pEC50 | 0.7 | nM | EC50 | J Med Chem (2021) 64: 1454-1480 [PMID:33492963] |
| ChEMBL | Agonist activity at human S1P1 receptor by GTPgammaS binding assay | F | 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] |
| 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 (2021) 64: 1454-1480 [PMID:33492963] |
| 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 (2021) 64: 1454-1480 [PMID:33492963] |
| 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 | F | 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 | F | 7.45 | pEC50 | 35.1 | nM | EC50 | Eur J Med Chem (2014) 85: 1-15 [PMID:25072873] |
| ChEMBL | Agonist activity at S1PR3 (unknown origin) by HTRF assay | B | 7.87 | pEC50 | 13.6 | nM | EC50 | Bioorg Med Chem Lett (2020) 30: 127141-127141 [PMID:32249117] |
| 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 recombinant human S1P3 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting method | F | 8.44 | pEC50 | 3.6 | nM | EC50 | J Med Chem (2021) 64: 1454-1480 [PMID:33492963] |
| ChEMBL | Agonist activity at human S1P3 receptor by GTPgammaS binding assay | F | 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] |
| ChEMBL | Agonist activity at recombinant human S1P4 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting method | F | 8.8 | pEC50 | 1.6 | nM | EC50 | J Med Chem (2021) 64: 1454-1480 [PMID:33492963] |
| 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 | F | 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 | F | 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 | F | 8.47 | pEC50 | 3.4 | nM | EC50 | J Med Chem (2015) 58: 9154-9170 [PMID:26509640] |
| ChEMBL | Agonist activity at recombinant human S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting method | F | 9.17 | pEC50 | 0.67 | nM | EC50 | J Med Chem (2021) 64: 1454-1480 [PMID:33492963] |
| ChEMBL | Agonist activity at human S1P5 receptor by GTPgammaS binding assay | F | 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 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]
