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 [32P]S1P from human recombinant S1PR1 incubated for 60 mins by competitive binding assay based scintillation counter | B | 8.85 | pIC50 | 1.4 | nM | IC50 | RSC Med Chem (2022) 13: 202-207 [PMID:35308025] |
| 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 [32P]S1P from human recombinant S1PR3 incubated for 60 mins by competitive binding assay based scintillation counter | B | 9.4 | pIC50 | 0.4 | nM | IC50 | RSC Med Chem (2022) 13: 202-207 [PMID:35308025] |
| 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 [32P]S1P from human recombinant S1PR2 incubated for 60 mins by competitive binding assay based scintillation counter | B | 8.44 | pIC50 | 3.6 | nM | IC50 | RSC Med Chem (2022) 13: 202-207 [PMID:35308025] |
| 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 human recombinant S1PR4 incubated for 60 mins by competitive binding assay based scintillation counter | B | 6.82 | pIC50 | 151 | nM | IC50 | RSC Med Chem (2022) 13: 202-207 [PMID:35308025] |
| 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 [32P]S1P from human recombinant S1PR5 incubated for 60 mins by competitive binding assay based scintillation counter | B | 8.51 | pIC50 | 3.1 | nM | IC50 | RSC Med Chem (2022) 13: 202-207 [PMID:35308025] |
| 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 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]
