sphingosine 1-phosphate [Ligand Id: 911] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL225155 |
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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 [PMID:29249563] |
| 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 | F | 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 [PMID:29249563] |
| 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 | F | 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 [PMID:29249563] |
| 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 | F | 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 [PMID:29249563] |
| 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 | F | 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 [PMID:29249563] |
| 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 | F | 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 31:
Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]
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