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 |
|---|---|---|---|---|---|---|---|---|
| σ2/Sigma intracellular receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105907] [GtoPdb: 2553] [UniProtKB: Q5BJF2] | ||||||||
| ChEMBL | PDSP Secondary Binding target: TMEM97 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 6.17 | pKi | 671.81 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| sigma non-opioid intracellular receptor 1/Sigma non-opioid intracellular receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720] | ||||||||
| ChEMBL | PDSP Secondary Binding target: SIGMAR1 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 5.22 | pKi | 5976.54 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| S1P1 receptor/Sphingosine 1-phosphate receptor 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 | In Vitro Binding Assay: Newly synthesized compounds were first evaluated for binding potency toward S1P1 by a [32P]S1P competitive binding assay following published procedure (J. Rosenberg, H. Liu, Z. Tu, A practical process for the preparation of [32P]S1P and binding assay for S1P receptor ligands, Appl. Radiat. Isot. 102 (2015) 5-9), and using S1P as a reference compound. [32P]S1P was first prepared by incubating sphingosine and [γ-32P]ATP with sphingosine kinase 1 as previously reported (J. Rosenberg, H. Liu, Z. Tu, A practical process for the preparation of [32P]S1P and binding assay for S1P receptor ligands, Appl. Radiat. Isot. 102 (2015) 5-9). [32P]S1P was dissolved in DMSO, and then diluted in the assay buffer (50 mM HEPES-Na with 5 mM MgCl2, 1 mM CaCl2, and 0.5% fatty acid-free bovine serum albumin, pH=7.5). Compounds were dissolved in DMSO and diluted to different concentrations with assay buffer, followed by adding commercial cell membranes expressing recombinant human S1P receptors (1, 2, 3, 4, and 5) in the assay buffer at room temperature in 96-well plate. [32P]S1P solution was then added to give a final volume of 150 μL containing 0.1 nM of [32P]S1P and 1 μg of membrane protein per well. Competitive binding was performed for 60 min at room temperature and terminated by collecting the membranes onto 96-well glass fiber (GF/B) filtration plates (Millipore, Billerica, Mass.). Each filter was washed with 200 μL of assay buffer for five times. The filter bound radionuclide was measured by a Beckman LS3801 scintillation counter using Cherenkov counting. The reported IC50 values were calculated using the 4 parameter equation, least-square non-linear regression curve-fit, with GraphPad Prism software (GraphPad Software, Inc). Each assay was repeated at least three times with duplicate wells for each compound; the reported values (mean±SD, nM) are calculated from the average of all assays. Assays for compounds which showed no activity (IC50>1000 nM) were only repeated twice. | B | 8.85 | pIC50 | 1.4 | nM | IC50 | US-10676467-B2. Compositions for binding sphingosine-1-phosphate receptor 1 (S1P1), imaging of S1P1, and methods of use thereof (2020) |
| 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 | In Vitro Binding Assay: Newly synthesized compounds were first evaluated for binding potency toward S1P1 by a [32P]S1P competitive binding assay following published procedure (J. Rosenberg, H. Liu, Z. Tu, A practical process for the preparation of [32P]S1P and binding assay for S1P receptor ligands, Appl. Radiat. Isot. 102 (2015) 5-9), and using S1P as a reference compound. [32P]S1P was first prepared by incubating sphingosine and [γ-32P]ATP with sphingosine kinase 1 as previously reported (J. Rosenberg, H. Liu, Z. Tu, A practical process for the preparation of [32P]S1P and binding assay for S1P receptor ligands, Appl. Radiat. Isot. 102 (2015) 5-9). [32P]S1P was dissolved in DMSO, and then diluted in the assay buffer (50 mM HEPES-Na with 5 mM MgCl2, 1 mM CaCl2, and 0.5% fatty acid-free bovine serum albumin, pH=7.5). Compounds were dissolved in DMSO and diluted to different concentrations with assay buffer, followed by adding commercial cell membranes expressing recombinant human S1P receptors (1, 2, 3, 4, and 5) in the assay buffer at room temperature in 96-well plate. [32P]S1P solution was then added to give a final volume of 150 μL containing 0.1 nM of [32P]S1P and 1 μg of membrane protein per well. Competitive binding was performed for 60 min at room temperature and terminated by collecting the membranes onto 96-well glass fiber (GF/B) filtration plates (Millipore, Billerica, Mass.). Each filter was washed with 200 μL of assay buffer for five times. The filter bound radionuclide was measured by a Beckman LS3801 scintillation counter using Cherenkov counting. The reported IC50 values were calculated using the 4 parameter equation, least-square non-linear regression curve-fit, with GraphPad Prism software (GraphPad Software, Inc). Each assay was repeated at least three times with duplicate wells for each compound; the reported values (mean±SD, nM) are calculated from the average of all assays. Assays for compounds which showed no activity (IC50>1000 nM) were only repeated twice. | B | 8.85 | pIC50 | 1.4 | nM | IC50 | US-10676467-B2. Compositions for binding sphingosine-1-phosphate receptor 1 (S1P1), imaging of S1P1, and methods of use thereof (2020) |
| 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 | Modulation of S1PR1 (unknown origin) | B | 7.9 | pEC50 | 12.59 | nM | EC50 | Eur J Med Chem (2023) 250: 115182-115182 [PMID:36758307] |
| 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 | 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 | 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 | 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] |
| S1P2 receptor/Sphingosine 1-phosphate receptor 2 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 | In Vitro Binding Assay: Newly synthesized compounds were first evaluated for binding potency toward S1P1 by a [32P]S1P competitive binding assay following published procedure (J. Rosenberg, H. Liu, Z. Tu, A practical process for the preparation of [32P]S1P and binding assay for S1P receptor ligands, Appl. Radiat. Isot. 102 (2015) 5-9), and using S1P as a reference compound. [32P]S1P was first prepared by incubating sphingosine and [γ-32P]ATP with sphingosine kinase 1 as previously reported (J. Rosenberg, H. Liu, Z. Tu, A practical process for the preparation of [32P]S1P and binding assay for S1P receptor ligands, Appl. Radiat. Isot. 102 (2015) 5-9). [32P]S1P was dissolved in DMSO, and then diluted in the assay buffer (50 mM HEPES-Na with 5 mM MgCl2, 1 mM CaCl2, and 0.5% fatty acid-free bovine serum albumin, pH=7.5). Compounds were dissolved in DMSO and diluted to different concentrations with assay buffer, followed by adding commercial cell membranes expressing recombinant human S1P receptors (1, 2, 3, 4, and 5) in the assay buffer at room temperature in 96-well plate. [32P]S1P solution was then added to give a final volume of 150 μL containing 0.1 nM of [32P]S1P and 1 μg of membrane protein per well. Competitive binding was performed for 60 min at room temperature and terminated by collecting the membranes onto 96-well glass fiber (GF/B) filtration plates (Millipore, Billerica, Mass.). Each filter was washed with 200 μL of assay buffer for five times. The filter bound radionuclide was measured by a Beckman LS3801 scintillation counter using Cherenkov counting. The reported IC50 values were calculated using the 4 parameter equation, least-square non-linear regression curve-fit, with GraphPad Prism software (GraphPad Software, Inc). Each assay was repeated at least three times with duplicate wells for each compound; the reported values (mean±SD, nM) are calculated from the average of all assays. Assays for compounds which showed no activity (IC50>1000 nM) were only repeated twice. | B | 8.44 | pIC50 | 3.6 | nM | IC50 | US-10676467-B2. Compositions for binding sphingosine-1-phosphate receptor 1 (S1P1), imaging of S1P1, and methods of use thereof (2020) |
| 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 | Agonist activity at S1P2 (unknown origin) expressed in PathHunter CHO-K1 EDG1 beta-arrestin cells assessed as beta-arrestin recruitment | F | 7.49 | pEC50 | 32 | nM | EC50 | J Med Chem (2023) 66: 10381-10412 [PMID:37489798] |
| ChEMBL | Agonist activity at S1P2 (unknown origin) expressed in CHO cells assessed as Ca2+ activation | F | 7.82 | pEC50 | 15 | nM | EC50 | J Med Chem (2023) 66: 10381-10412 [PMID:37489798] |
| 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 2) | B | 8.08 | pEC50 | 8.3 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 3401-3404 [PMID:14505636] |
| 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] |
| S1P3 receptor/Sphingosine 1-phosphate receptor 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 | In Vitro Binding Assay: Newly synthesized compounds were first evaluated for binding potency toward S1P1 by a [32P]S1P competitive binding assay following published procedure (J. Rosenberg, H. Liu, Z. Tu, A practical process for the preparation of [32P]S1P and binding assay for S1P receptor ligands, Appl. Radiat. Isot. 102 (2015) 5-9), and using S1P as a reference compound. [32P]S1P was first prepared by incubating sphingosine and [γ-32P]ATP with sphingosine kinase 1 as previously reported (J. Rosenberg, H. Liu, Z. Tu, A practical process for the preparation of [32P]S1P and binding assay for S1P receptor ligands, Appl. Radiat. Isot. 102 (2015) 5-9). [32P]S1P was dissolved in DMSO, and then diluted in the assay buffer (50 mM HEPES-Na with 5 mM MgCl2, 1 mM CaCl2, and 0.5% fatty acid-free bovine serum albumin, pH=7.5). Compounds were dissolved in DMSO and diluted to different concentrations with assay buffer, followed by adding commercial cell membranes expressing recombinant human S1P receptors (1, 2, 3, 4, and 5) in the assay buffer at room temperature in 96-well plate. [32P]S1P solution was then added to give a final volume of 150 μL containing 0.1 nM of [32P]S1P and 1 μg of membrane protein per well. Competitive binding was performed for 60 min at room temperature and terminated by collecting the membranes onto 96-well glass fiber (GF/B) filtration plates (Millipore, Billerica, Mass.). Each filter was washed with 200 μL of assay buffer for five times. The filter bound radionuclide was measured by a Beckman LS3801 scintillation counter using Cherenkov counting. The reported IC50 values were calculated using the 4 parameter equation, least-square non-linear regression curve-fit, with GraphPad Prism software (GraphPad Software, Inc). Each assay was repeated at least three times with duplicate wells for each compound; the reported values (mean±SD, nM) are calculated from the average of all assays. Assays for compounds which showed no activity (IC50>1000 nM) were only repeated twice. | B | 9.4 | pIC50 | 0.4 | nM | IC50 | US-10676467-B2. Compositions for binding sphingosine-1-phosphate receptor 1 (S1P1), imaging of S1P1, and methods of use thereof (2020) |
| 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 | Agonist activity at S1P3 (unknown origin) expressed in PathHunter CHO-K1 EDG1 beta-arrestin cells assessed as beta-arrestin recruitment | F | 7.66 | pEC50 | 22 | nM | EC50 | J Med Chem (2023) 66: 10381-10412 [PMID:37489798] |
| 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 | Agonist activity at S1P3 (unknown origin) expressed in CHO cells assessed as Ca2+ activation | F | 8.52 | pEC50 | 3 | nM | EC50 | J Med Chem (2023) 66: 10381-10412 [PMID:37489798] |
| 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 | 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 | 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] |
| S1P4 receptor/Sphingosine 1-phosphate receptor 4 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] |
| ChEMBL | In Vitro Binding Assay: Newly synthesized compounds were first evaluated for binding potency toward S1P1 by a [32P]S1P competitive binding assay following published procedure (J. Rosenberg, H. Liu, Z. Tu, A practical process for the preparation of [32P]S1P and binding assay for S1P receptor ligands, Appl. Radiat. Isot. 102 (2015) 5-9), and using S1P as a reference compound. [32P]S1P was first prepared by incubating sphingosine and [γ-32P]ATP with sphingosine kinase 1 as previously reported (J. Rosenberg, H. Liu, Z. Tu, A practical process for the preparation of [32P]S1P and binding assay for S1P receptor ligands, Appl. Radiat. Isot. 102 (2015) 5-9). [32P]S1P was dissolved in DMSO, and then diluted in the assay buffer (50 mM HEPES-Na with 5 mM MgCl2, 1 mM CaCl2, and 0.5% fatty acid-free bovine serum albumin, pH=7.5). Compounds were dissolved in DMSO and diluted to different concentrations with assay buffer, followed by adding commercial cell membranes expressing recombinant human S1P receptors (1, 2, 3, 4, and 5) in the assay buffer at room temperature in 96-well plate. [32P]S1P solution was then added to give a final volume of 150 μL containing 0.1 nM of [32P]S1P and 1 μg of membrane protein per well. Competitive binding was performed for 60 min at room temperature and terminated by collecting the membranes onto 96-well glass fiber (GF/B) filtration plates (Millipore, Billerica, Mass.). Each filter was washed with 200 μL of assay buffer for five times. The filter bound radionuclide was measured by a Beckman LS3801 scintillation counter using Cherenkov counting. The reported IC50 values were calculated using the 4 parameter equation, least-square non-linear regression curve-fit, with GraphPad Prism software (GraphPad Software, Inc). Each assay was repeated at least three times with duplicate wells for each compound; the reported values (mean±SD, nM) are calculated from the average of all assays. Assays for compounds which showed no activity (IC50>1000 nM) were only repeated twice. | B | 6.82 | pIC50 | 151 | nM | IC50 | US-10676467-B2. Compositions for binding sphingosine-1-phosphate receptor 1 (S1P1), imaging of S1P1, and methods of use thereof (2020) |
| 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] |
| 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 | 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 | 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 | 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 | Agonist activity at S1P4 (unknown origin) expressed in PathHunter CHO-K1 EDG1 beta-arrestin cells assessed as beta-arrestin recruitment | F | 7.04 | pEC50 | 92 | nM | EC50 | J Med Chem (2023) 66: 10381-10412 [PMID:37489798] |
| 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] |
| ChEMBL | Agonist activity at S1P4 (unknown origin) expressed in CHO cells assessed as Ca2+ activation | F | 8.05 | pEC50 | 9 | nM | EC50 | J Med Chem (2023) 66: 10381-10412 [PMID:37489798] |
| 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 5 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 | In Vitro Binding Assay: Newly synthesized compounds were first evaluated for binding potency toward S1P1 by a [32P]S1P competitive binding assay following published procedure (J. Rosenberg, H. Liu, Z. Tu, A practical process for the preparation of [32P]S1P and binding assay for S1P receptor ligands, Appl. Radiat. Isot. 102 (2015) 5-9), and using S1P as a reference compound. [32P]S1P was first prepared by incubating sphingosine and [γ-32P]ATP with sphingosine kinase 1 as previously reported (J. Rosenberg, H. Liu, Z. Tu, A practical process for the preparation of [32P]S1P and binding assay for S1P receptor ligands, Appl. Radiat. Isot. 102 (2015) 5-9). [32P]S1P was dissolved in DMSO, and then diluted in the assay buffer (50 mM HEPES-Na with 5 mM MgCl2, 1 mM CaCl2, and 0.5% fatty acid-free bovine serum albumin, pH=7.5). Compounds were dissolved in DMSO and diluted to different concentrations with assay buffer, followed by adding commercial cell membranes expressing recombinant human S1P receptors (1, 2, 3, 4, and 5) in the assay buffer at room temperature in 96-well plate. [32P]S1P solution was then added to give a final volume of 150 μL containing 0.1 nM of [32P]S1P and 1 μg of membrane protein per well. Competitive binding was performed for 60 min at room temperature and terminated by collecting the membranes onto 96-well glass fiber (GF/B) filtration plates (Millipore, Billerica, Mass.). Each filter was washed with 200 μL of assay buffer for five times. The filter bound radionuclide was measured by a Beckman LS3801 scintillation counter using Cherenkov counting. The reported IC50 values were calculated using the 4 parameter equation, least-square non-linear regression curve-fit, with GraphPad Prism software (GraphPad Software, Inc). Each assay was repeated at least three times with duplicate wells for each compound; the reported values (mean±SD, nM) are calculated from the average of all assays. Assays for compounds which showed no activity (IC50>1000 nM) were only repeated twice. | B | 8.51 | pIC50 | 3.1 | nM | IC50 | US-10676467-B2. Compositions for binding sphingosine-1-phosphate receptor 1 (S1P1), imaging of S1P1, and methods of use thereof (2020) |
| 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 | Fluorescence Detection (FLIPR) Assay: The sample to be tested was dissolved in DMSO and diluted with detection buffer solution in 3-fold dilution. A reagent and a positive control were diluted in the same way. The reactions of the agonist, the reagent and the positive control were detected by a device of FLIPRTETRA with a total detection time of 180 s to estimate the ability to activate GPCR (S1P5) of each compound. | B | 7.64 | pEC50 | 23 | nM | EC50 | US-11584726-B2. Amino alcohol derivative, pharmaceutical composition and application thereof (2023) |
| 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 | 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 | Agonist activity at S1P5 (unknown origin) expressed in CHO cells assessed as Ca2+ activation | F | 8.22 | pEC50 | 6 | nM | EC50 | J Med Chem (2023) 66: 10381-10412 [PMID:37489798] |
| 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] |
| Translocator protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5742] [GtoPdb: 2879] [UniProtKB: P30536] | ||||||||
| ChEMBL | PDSP Secondary Binding target: TSPO - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 5.51 | pKi | 3115.3 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| 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 36:
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]
