SEW2871 [Ligand Id: 2926] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL224720 (SEW-2871) |
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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 | - | - | 7.7 | pKi | 18 | nM | Ki | J Biol Chem (2004) 279: 13839-48 [PMID:14732717] |
| ChEMBL | Displacement of [33P]sphingosine 1 phosphate from human S1P1 receptor expressed in CHO cells | B | 7.43 | pIC50 | 37 | nM | IC50 | J Med Chem (2004) 47: 6662-6665 [PMID:15615513] |
| ChEMBL | Displacement of [33P]S1P from human S1P1R expressed in CHO cell membranes | B | 7.43 | pIC50 | 37 | nM | IC50 | ACS Med Chem Lett (2011) 2: 97-101 [PMID:24900286] |
| 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 | 6.57 | pEC50 | 270 | nM | EC50 | Bioorg Med Chem Lett (2012) 22: 527-531 [PMID:22104144] |
| ChEMBL | Inhibition of S1P1 receptor (unknown origin) | B | 7.89 | pEC50 | 13 | nM | EC50 | Bioorg Med Chem Lett (2018) 28: 3585-3591 [PMID:30409535] |
| GtoPdb | - | - | 7.9 | pEC50 | 12.6 | nM | EC50 |
Mol Pharmacol (2008) 74: 1308-18 [PMID:18708635]; J Biol Chem (2004) 279: 13839-48 [PMID:14732717] |
| S1P1 receptor in Mouse [GtoPdb: 275] [UniProtKB: O08530] | ||||||||
| GtoPdb | - | - | 7.68 | pEC50 | 20.7 | nM | EC50 | 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] | ||||||||
| ChEMBL | Displacement of [33P]sphingosine 1 phosphate from human S1P3 receptor expressed in CHO cells | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2004) 47: 6662-6665 [PMID:15615513] |
| ChEMBL | Displacement of [33P]S1P from human S1P3R expressed in CHO cell membranes | B | 8 | pIC50 | >10 | nM | IC50 | ACS Med Chem Lett (2011) 2: 97-101 [PMID:24900286] |
| ChEMBL | Agonist activity at human S1P3 receptor expressed in CHO-K1 cells co-expressing Gq/i5 G-protein assessed as calcium mobilization by FLIPR assay | F | 4.6 | pEC50 | >25000 | nM | EC50 | Bioorg Med Chem Lett (2012) 22: 527-531 [PMID:22104144] |
| S1P2 receptor/Sphingosine 1-phosphate receptor Edg-5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2955] [GtoPdb: 276] [UniProtKB: O95136] | ||||||||
| ChEMBL | Displacement of [33P]sphingosine 1 phosphate from human S1P2 receptor expressed in CHO cells | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2004) 47: 6662-6665 [PMID:15615513] |
| S1P4 receptor/Sphingosine 1-phosphate receptor Edg-6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3230] [GtoPdb: 278] [UniProtKB: O95977] | ||||||||
| ChEMBL | Displacement of [33P]sphingosine 1 phosphate from human S1P4 receptor expressed in CHO cells | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2004) 47: 6662-6665 [PMID:15615513] |
| S1P5 receptor/Sphingosine 1-phosphate receptor Edg-8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2274] [GtoPdb: 279] [UniProtKB: Q9H228] | ||||||||
| ChEMBL | Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells | B | 5.34 | pIC50 | 4600 | nM | IC50 | J Med Chem (2004) 47: 6662-6665 [PMID:15615513] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
