sphingosine 1-phosphate [Ligand Id: 911] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL225155
  • 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]
  • S1P3 receptor in Mouse [GtoPdb: 277] [UniProtKB: Q9Z0U9]
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  • S1P2 receptor/Sphingosine 1-phosphate receptor Edg-5 in Human [ChEMBL: CHEMBL2955] [GtoPdb: 276] [UniProtKB: O95136]
  • S1P2 receptor in Mouse [GtoPdb: 276] [UniProtKB: P52592]
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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]
  • S1P5 receptor in Mouse [GtoPdb: 279] [UniProtKB: Q91X56]
  • S1P5 receptor in Rat [GtoPdb: 279] [UniProtKB: Q9JKM5]
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  • GPR3 in Human [GtoPdb: 83] [UniProtKB: P46089]
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  • GPR6 in Mouse [GtoPdb: 85] [UniProtKB: Q6YNI2]
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  • GPR12 in Human [GtoPdb: 86] [UniProtKB: P47775]
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  • GPR63 in Human [GtoPdb: 112] [UniProtKB: Q9BZJ6]
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  • P2RY10 in Human [GtoPdb: 165] [UniProtKB: O00398]
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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 - - 9.41 pKd 0.39 nM Kd J Biol Chem (1999) 274: 23940-7 [PMID:10446161];
Mol Pharmacol (2007) 71: 724-35 [PMID:17170199]
ChEMBL Displacement of [32P]S1P from recombinant human S1PR1 expressed in CHOK1 cell membranes pretreated for 30 mins followed by [32P]S1P addition measured after 60 mins by scintillation counting method B 8.85 pIC50 1.4 nM IC50 Bioorg Med Chem Lett (2018) 28: 488-496
ChEMBL Displacement of [33P]sphingosine-1-phosphate from human S1P1 receptor expressed in HEK293T cells after 60 mins by scintillation counting B 9.11 pIC50 0.78 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 2520-2524 [PMID:20304639]
ChEMBL Displacement of [33P]sphingosine 1 phosphate from human S1P1 receptor expressed in CHO cells B 9.17 pIC50 0.67 nM IC50 J. Med. Chem. (2004) 47: 6662-6665 [PMID:15615513]
ChEMBL Displacement of [33P]sphingosine-1-phosphate from human S1P1 receptor B 9.33 pIC50 0.47 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 369-372 [PMID:19081720]
ChEMBL Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 1 expressed on CHO cell membranes B 9.8 pIC50 0.16 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 3351-3355 [PMID:15149705]
ChEMBL Agonist activity at human recombinant S1P1 receptor expressed in HEK cells by GTPgammaS binding assay B 7.6 pEC50 25.3 nM EC50 J. Med. Chem. (2010) 53: 4198-4211 [PMID:20446681]
ChEMBL In vitro binding affinity towards human Sphingosine 1-phosphate receptor 1 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand B 7.7 pEC50 20 nM EC50 Bioorg. Med. Chem. Lett. (2004) 14: 4903-4906 [PMID:15341948]
ChEMBL Agonist activity at human S1P1 receptor expressed in human U2OS cells co-expressing eGFP assessed as receptor internalization into cytoplasm using Hoechst dye staining F 7.74 pEC50 18 nM EC50 Bioorg. Med. Chem. Lett. (2012) 22: 527-531 [PMID:22104144]
ChEMBL Agonist activity at human S1P1 receptor assessed as stimulation of [35S]GTPgammaS binding F 8.1 pEC50 7.9 nM EC50 Bioorg. Med. Chem. Lett. (2009) 19: 369-372 [PMID:19081720]
ChEMBL Antagonist activity at human S1P1 receptor expressed in HEK293T cells assessed as inhibition of sphingosine-1-phosphate-induced gamma-[35S]GTP binding after 30 mins by scintillation counting F 8.25 pEC50 5.6 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 2520-2524 [PMID:20304639]
ChEMBL Agonist activity at human S1P1 receptor expressed in HEK293T cells assessed as stimulation of [35S]GTPgammaS binding F 8.25 pEC50 5.6 nM EC50 Bioorg. Med. Chem. Lett. (2013) 23: 472-475 [PMID:23245510]
ChEMBL Effective concentration against sphingosine-1-phosphate receptor 1 determined by a [c-35S]-GTP binding assay B 8.35 pEC50 4.5 nM EC50 Bioorg. Med. Chem. Lett. (2005) 15: 3568-3572 [PMID:15982878]
ChEMBL In vitro binding affinity towards human Sphingosine 1-phosphate receptor 1 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand. (Experiment 2) B 8.35 pEC50 4.5 nM EC50 Bioorg. Med. Chem. Lett. (2003) 13: 3401-3404 [PMID:14505636]
ChEMBL Agonist activity at human S1P1R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation counting F 8.37 pEC50 4.25 nM EC50 ACS Med. Chem. Lett. (2013) 4: 942-947 [PMID:24900589]
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 8.55 pEC50 2.8 nM EC50 Bioorg. Med. Chem. Lett. (2016) 26: 466-471 [PMID:26687487]
ChEMBL In vitro binding affinity towards human Sphingosine 1-phosphate receptor 1 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 1) B 9.05 pEC50 0.9 nM EC50 Bioorg. Med. Chem. Lett. (2003) 13: 3401-3404 [PMID:14505636]
ChEMBL Activity at human recombinant S1P1 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay F 9.26 pEC50 0.55 nM EC50 Bioorg. Med. Chem. Lett. (2007) 17: 491-494 [PMID:17070046]
GtoPdb - - 9.4 pEC50 0.4 nM EC50 Biochemistry (2001) 40: 14053-60 [PMID:11705398];
Chem Biol (2006) 13: 1227-34 [PMID:17114004];
J Biol Chem (1998) 273: 27104-10 [PMID:9765227];
J Biol Chem (2002) 277: 21453-7 [PMID:11967257];
J Biol Chem (2004) 279: 13839-48 [PMID:14732717]
GtoPdb - - 9.54 pEC50 0.29 nM EC50 PLoS One (2019) 14: e0226154 [PMID:31805144]
ChEMBL Displacement of [33P]S1P from human recombinant S1P1 receptor expressed in HEK cells by scintillation counting B 10 pEC50 0.1 nM EC50 J. Med. Chem. (2010) 53: 4198-4211 [PMID:20446681]
ChEMBL Agonist activity at human S1P1 receptor assessed as cAMP accumulation by HTRF assay F 10.21 pEC50 0.06 nM EC50 ACS Med. Chem. Lett. (2014) 5: 1313-1317 [PMID:25516790]
ChEMBL Agonist activity at human S1P1 receptor assessed as effect on calcium mobilization by Gi dependent whole cell assay F 10.57 pEC50 0.03 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 2264-2269 [PMID:20188554]
S1P1 receptor in Mouse [GtoPdb: 275] [UniProtKB: O08530]
GtoPdb - - 8.85 pEC50 1.4 nM EC50 Chem Biol (2006) 13: 1227-34 [PMID:17114004];
J Biol Chem (2004) 279: 13839-48 [PMID:14732717]
S1P3 receptor/Sphingosine 1-phosphate receptor Edg-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3892] [GtoPdb: 277] [UniProtKB: Q99500]
GtoPdb - - 9.64 pKd 0.23 nM Kd J Biol Chem (1999) 274: 23940-7 [PMID:10446161];
J Biol Chem (1999) 274: 4626-32 [PMID:9988698];
Mol Pharmacol (2007) 71: 724-35 [PMID:17170199]
ChEMBL Displacement of [33P]sphingosine-1-phosphate from human S1P3 receptor expressed in HEK293T cells after 60 mins by scintillation counting B 9.04 pIC50 0.92 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 2520-2524 [PMID:20304639]
ChEMBL Displacement of [33P]sphingosine-1-phosphate from human S1P3 receptor B 9.18 pIC50 0.66 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 369-372 [PMID:19081720]
ChEMBL Displacement of [32P]S1P from recombinant human S1PR3 expressed in Chem1 cell membranes co-expressing Galpha15 pretreated for 30 mins followed by [32P]S1P addition measured after 60 mins by scintillation counting method B 9.4 pIC50 0.4 nM IC50 Bioorg Med Chem Lett (2018) 28: 488-496
ChEMBL Displacement of [33P]sphingosine 1 phosphate from human S1P3 receptor expressed in CHO cells B 9.59 pIC50 0.26 nM IC50 J. Med. Chem. (2004) 47: 6662-6665 [PMID:15615513]
ChEMBL Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 3 expressed on CHO cell membranes B 10.4 pIC50 0.04 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 3351-3355 [PMID:15149705]
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 7.1 pEC50 79 nM EC50 Bioorg. Med. Chem. Lett. (2016) 26: 466-471 [PMID:26687487]
ChEMBL In vitro binding affinity towards human Sphingosine 1-phosphate receptor 3 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 2) B 8.06 pEC50 8.7 nM EC50 Bioorg. Med. Chem. Lett. (2003) 13: 3401-3404 [PMID:14505636]
ChEMBL Effective concentration against sphingosine 1-phosphate receptor 3 determined by a [c-35S]-GTP binding assay B 8.06 pEC50 8.7 nM EC50 Bioorg. Med. Chem. Lett. (2005) 15: 3568-3572 [PMID:15982878]
ChEMBL Agonist activity at human S1P3R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation counting F 8.4 pEC50 3.94 nM EC50 ACS Med. Chem. Lett. (2013) 4: 942-947 [PMID:24900589]
ChEMBL Agonist activity at human S1P3 receptor assessed as stimulation of [35S]GTPgammaS binding F 8.52 pEC50 3 nM EC50 Bioorg. Med. Chem. Lett. (2009) 19: 369-372 [PMID:19081720]
ChEMBL Antagonist activity at human S1P3 receptor expressed in HEK293T cells assessed as inhibition of sphingosine-1-phosphate-induced gamma-[35S]GTP binding after 30 mins by scintillation counting F 8.62 pEC50 2.4 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 2520-2524 [PMID:20304639]
ChEMBL Agonist activity at human S1P3 receptor expressed in HEK293T cells assessed as stimulation of [35S]GTPgammaS binding F 8.62 pEC50 2.4 nM EC50 Bioorg. Med. Chem. Lett. (2013) 23: 472-475 [PMID:23245510]
ChEMBL Activity at human recombinant S1P3 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay F 8.8 pEC50 1.6 nM EC50 Bioorg. Med. Chem. Lett. (2007) 17: 491-494 [PMID:17070046]
ChEMBL In vitro binding affinity towards human Sphingosine 1-phosphate receptor 3 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand B 8.92 pEC50 1.2 nM EC50 Bioorg. Med. Chem. Lett. (2004) 14: 4903-4906 [PMID:15341948]
ChEMBL In vitro binding affinity towards human Sphingosine 1-phosphate receptor 3 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 1) B 8.96 pEC50 1.1 nM EC50 Bioorg. Med. Chem. Lett. (2003) 13: 3401-3404 [PMID:14505636]
ChEMBL Agonist activity at human recombinant S1P3 receptor expressed in HEK cells by GTPgammaS binding assay B 9.15 pEC50 0.7 nM EC50 J. Med. Chem. (2010) 53: 4198-4211 [PMID:20446681]
ChEMBL Agonist activity at human S1P3 receptor assessed as effect on calcium mobilization by Gi dependent whole cell assay F 9.35 pEC50 0.45 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 2264-2269 [PMID:20188554]
ChEMBL Displacement of [33P]S1P from human recombinant S1P3 receptor expressed in HEK cells by scintillation counting B 9.7 pEC50 0.2 nM EC50 J. Med. Chem. (2010) 53: 4198-4211 [PMID:20446681]
GtoPdb - - 9.8 pEC50 - - - Biochemistry (2001) 40: 14053-60 [PMID:11705398];
Chem Biol (2006) 13: 1227-34 [PMID:17114004];
J Biol Chem (2002) 277: 21453-7 [PMID:11967257]
S1P3 receptor in Mouse [GtoPdb: 277] [UniProtKB: Q9Z0U9]
GtoPdb - - 8.64 pEC50 2.3 nM EC50 J Biol Chem (2004) 279: 13839-48 [PMID:14732717]
S1P2 receptor/Sphingosine 1-phosphate receptor Edg-5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2955] [GtoPdb: 276] [UniProtKB: O95136]
GtoPdb - - 7.69 pKd 20.4 nM Kd J Biol Chem (1999) 274: 23940-7 [PMID:10446161];
J Biol Chem (1999) 274: 4626-32 [PMID:9988698]
ChEMBL Displacement of [32P]S1P from recombinant human S1PR2 expressed in Chem1 cell membranes co-expressing Galpha15 pretreated for 30 mins followed by [32P]S1P addition measured after 60 mins by scintillation counting method B 8.44 pIC50 3.6 nM IC50 Bioorg Med Chem Lett (2018) 28: 488-496
ChEMBL Displacement of [33P]sphingosine 1 phosphate from human S1P2 receptor expressed in CHO cells B 9.46 pIC50 0.35 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 9.64 pIC50 0.23 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 3351-3355 [PMID:15149705]
ChEMBL Agonist activity at human recombinant S1P2 receptor expressed in HEK cells by GTPgammaS binding assay B 7.36 pEC50 43.9 nM EC50 J. Med. Chem. (2010) 53: 4198-4211 [PMID:20446681]
ChEMBL In vitro binding affinity towards human Sphingosine 1-phosphate receptor 2 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 2) B 8.08 pEC50 8.3 nM EC50 Bioorg. Med. Chem. Lett. (2003) 13: 3401-3404 [PMID:14505636]
ChEMBL Effective concentration against sphingosine 1-phosphate receptor 2 determined by a [c-35S]-GTP binding assay B 8.08 pEC50 8.3 nM EC50 Bioorg. Med. Chem. Lett. (2005) 15: 3568-3572 [PMID:15982878]
ChEMBL In vitro binding affinity towards human Sphingosine 1-phosphate receptor 2 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 1) B 8.54 pEC50 2.9 nM EC50 Bioorg. Med. Chem. Lett. (2003) 13: 3401-3404 [PMID:14505636]
GtoPdb - - 8.54 pEC50 - - - Biochemistry (2001) 40: 14053-60 [PMID:11705398];
Chem Biol (2006) 13: 1227-34 [PMID:17114004]
ChEMBL In vitro binding affinity towards human Sphingosine 1-phosphate receptor 2 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand B 8.66 pEC50 2.2 nM EC50 Bioorg. Med. Chem. Lett. (2004) 14: 4903-4906 [PMID:15341948]
ChEMBL Agonist activity at human S1P2R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation counting F 8.89 pEC50 1.3 nM EC50 ACS Med. Chem. Lett. (2013) 4: 942-947 [PMID:24900589]
ChEMBL Displacement of [33P]S1P from human recombinant S1P2 receptor expressed in HEK cells by scintillation counting B 9.15 pEC50 0.7 nM EC50 J. Med. Chem. (2010) 53: 4198-4211 [PMID:20446681]
S1P2 receptor in Mouse [GtoPdb: 276] [UniProtKB: P52592]
GtoPdb - - 8.7 pEC50 2 nM EC50 J Biol Chem (2004) 279: 13839-48 [PMID:14732717]
S1P4 receptor/Sphingosine 1-phosphate receptor Edg-6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3230] [GtoPdb: 278] [UniProtKB: O95977]
ChEMBL Displacement of [32P]S1P from recombinant human S1PR4 expressed in cell membranes pretreated for 30 mins followed by [32P]S1P addition measured after 60 mins by scintillation counting method B 6.82 pIC50 151 nM IC50 Bioorg Med Chem Lett (2018) 28: 488-496
GtoPdb - - 7 pIC50 - - - Biochem Biophys Res Commun (2002) 297: 600-6 [PMID:12270137];
J Biol Chem (2002) 277: 21453-7 [PMID:11967257]
ChEMBL Displacement of [33P]sphingosine 1 phosphate from human S1P4 receptor expressed in CHO cells B 7.47 pIC50 34 nM IC50 J. Med. Chem. (2004) 47: 6662-6665 [PMID:15615513]
ChEMBL Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 4 expressed on CHO cell membranes B 7.64 pIC50 23 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 3351-3355 [PMID:15149705]
ChEMBL Displacement of [33P]S1P from human recombinant S1P4 receptor expressed in CHO cells by scintillation counting B 8.54 pIC50 2.9 nM IC50 J. Med. Chem. (2010) 53: 4198-4211 [PMID:20446681]
ChEMBL Displacement of [33P]sphingosine-1-phosphate from human S1P4 receptor B 8.62 pIC50 2.4 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 369-372 [PMID:19081720]
ChEMBL Displacement of [33P]sphingosine-1-phosphate from human S1P4 receptor expressed in HEK293T cells after 60 mins by scintillation counting B 8.98 pIC50 1.04 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 2520-2524 [PMID:20304639]
ChEMBL In vitro binding affinity towards human Sphingosine 1-phosphate receptor 4 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 2) B 6.57 pEC50 270 nM EC50 Bioorg. Med. Chem. Lett. (2003) 13: 3401-3404 [PMID:14505636]
ChEMBL Effective concentration against sphingosine 1-phosphate receptor 4 determined by a [c-35S]-GTP binding assay B 6.57 pEC50 270 nM EC50 Bioorg. Med. Chem. Lett. (2005) 15: 3568-3572 [PMID:15982878]
ChEMBL Agonist activity at human recombinant S1P4 receptor expressed in CHO cells by GTPgammaS binding assay B 6.79 pEC50 164 nM EC50 J. Med. Chem. (2010) 53: 4198-4211 [PMID:20446681]
ChEMBL In vitro binding affinity towards human Sphingosine 1-phosphate receptor 4 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand B 7.43 pEC50 37 nM EC50 Bioorg. Med. Chem. Lett. (2004) 14: 4903-4906 [PMID:15341948]
ChEMBL Agonist activity at human S1P4R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation counting F 7.89 pEC50 13 nM EC50 ACS Med. Chem. Lett. (2013) 4: 942-947 [PMID:24900589]
GtoPdb - - 8.07 pEC50 67 nM EC50 Biochem Biophys Res Commun (2002) 297: 600-6 [PMID:12270137];
Chem Biol (2006) 13: 1227-34 [PMID:17114004];
J Biol Chem (2004) 279: 13839-48 [PMID:14732717]
ChEMBL Activity at human recombinant S1P4 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay F 8.1 pEC50 7.9 nM EC50 Bioorg. Med. Chem. Lett. (2007) 17: 491-494 [PMID:17070046]
S1P4 receptor in Mouse [GtoPdb: 278] [UniProtKB: Q9Z0L1]
GtoPdb - - 7.12 pEC50 75 nM EC50 J Biol Chem (2004) 279: 13839-48 [PMID:14732717]
S1P5 receptor/Sphingosine 1-phosphate receptor Edg-8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2274] [GtoPdb: 279] [UniProtKB: Q9H228]
ChEMBL Displacement of [32P]S1P from recombinant human S1PR5 expressed in cell membranes pretreated for 30 mins followed by [32P]S1P addition measured after 60 mins by scintillation counting method B 8.51 pIC50 3.1 nM IC50 Bioorg Med Chem Lett (2018) 28: 488-496
ChEMBL Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation counting B 8.7 pIC50 2 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 2520-2524 [PMID:20304639]
ChEMBL Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptor B 8.96 pIC50 1.1 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 369-372 [PMID:19081720]
ChEMBL Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells B 9.26 pIC50 0.55 nM IC50 J. Med. Chem. (2004) 47: 6662-6665 [PMID:15615513]
ChEMBL Agonist activity at human recombinant S1P5 receptor expressed in CHO cells by GTPgammaS binding assay B 6.92 pEC50 121 nM EC50 J. Med. Chem. (2010) 53: 4198-4211 [PMID:20446681]
ChEMBL In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 1) B 7.36 pEC50 43.9 nM EC50 Bioorg. Med. Chem. Lett. (2003) 13: 3401-3404 [PMID:14505636]
ChEMBL In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 2) B 8.04 pEC50 9.2 nM EC50 Bioorg. Med. Chem. Lett. (2003) 13: 3401-3404 [PMID:14505636]
ChEMBL Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay B 8.04 pEC50 9.2 nM EC50 Bioorg. Med. Chem. Lett. (2005) 15: 3568-3572 [PMID:15982878]
ChEMBL Agonist activity at human S1P5R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation counting F 8.74 pEC50 1.8 nM EC50 ACS Med. Chem. Lett. (2013) 4: 942-947 [PMID:24900589]
ChEMBL In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand B 8.77 pEC50 1.7 nM EC50 Bioorg. Med. Chem. Lett. (2004) 14: 4903-4906 [PMID:15341948]
GtoPdb - - 8.9 pEC50 - - - Biochemistry (2001) 40: 14053-60 [PMID:11705398];
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]
ChEMBL Activity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay F 9.04 pEC50 0.91 nM EC50 Bioorg. Med. Chem. Lett. (2007) 17: 491-494 [PMID:17070046]
ChEMBL Displacement of [33P]S1P from human recombinant S1P5 receptor expressed in CHO cells by scintillation counting B 9.7 pEC50 0.2 nM EC50 J. Med. Chem. (2010) 53: 4198-4211 [PMID:20446681]
S1P5 receptor in Mouse [GtoPdb: 279] [UniProtKB: Q91X56]
GtoPdb - - 7.9 pEC50 16 nM EC50 Biochemistry (2001) 40: 14053-60 [PMID:11705398];
J Biol Chem (2004) 279: 13839-48 [PMID:14732717]
S1P5 receptor in Rat [GtoPdb: 279] [UniProtKB: Q9JKM5]
GtoPdb - - 8.7 pKd - - - J Biol Chem (2000) 275: 14281-6 [PMID:10799507]
GPR3 in Human [GtoPdb: 83] [UniProtKB: P46089]
GtoPdb - - 7.7 pEC50 - - - Cell Signal (2002) 14: 941-953 [PMID:12220620]
GPR6 in Mouse [GtoPdb: 85] [UniProtKB: Q6YNI2]
GtoPdb - - 7.66 pEC50 22 nM EC50 Cell Signal (2002) 14: 941-953 [PMID:12220620];
Biochem Biophys Res Commun (2003) 311: 329-36 [PMID:14592418]
GPR12 in Human [GtoPdb: 86] [UniProtKB: P47775]
GtoPdb - - 6.97 pEC50 1200 nM EC50 Cell Signal (2002) 14: 941-953 [PMID:12220620]
GPR63 in Human [GtoPdb: 112] [UniProtKB: Q9BZJ6]
GtoPdb - - 6.18 pEC50 660 nM EC50 Cell Signal (2003) 15: 435-46 [PMID:12618218]
P2RY10 in Human [GtoPdb: 165] [UniProtKB: O00398]
GtoPdb - - 7.3 pEC50 - - - Biochem Biophys Res Commun (2008) 371: 707-12 [PMID:18466763]

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]