siponimod [Ligand Id: 9289] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2336071 (Baf312, BAF-312, BAF312, NVP-BAF312-NX, Siponimod) |
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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] | ||||||||
| ChEMBL | Agonist activity at human S1P1 receptor transfected in CHO cells incubated for 10 to 15 mins prior to GTPgamma35S addition measured after 120 mins by GTPgamma35S binding assay | F | 9.4 | pEC50 | 0.4 | nM | EC50 | ACS Med Chem Lett (2013) 4: 333-337 [PMID:24900670] |
| GtoPdb | In a GTPγS binding assay | - | 9.4 | pEC50 | 0.4 | nM | EC50 |
ACS Med Chem Lett (2013) 4: 333-7 [PMID:24900670]; Drug Metab Dispos (2018) 46: 1001-1013 [PMID:29735753] |
| GtoPdb | - | - | 10.11 | pEC50 | 0.08 | nM | EC50 | PLoS One (2019) 14: e0226154 [PMID:31805144] |
| S1P3 receptor/Sphingosine 1-phosphate receptor Edg-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3892] [GtoPdb: 277] [UniProtKB: Q99500] | ||||||||
| GtoPdb | In a GTPγS binding assay | - | 5.3 | pEC50 | 5000 | nM | EC50 | ACS Med Chem Lett (2013) 4: 333-7 [PMID:24900670] |
| ChEMBL | Agonist activity at human S1P3 receptor transfected in CHO cells incubated for 10 to 15 mins prior to GTPgamma35S addition measured after 120 mins by GTPgamma35S binding assay | F | 5.3 | pEC50 | 5000 | nM | EC50 | ACS Med Chem Lett (2013) 4: 333-337 [PMID:24900670] |
| S1P4 receptor/Sphingosine 1-phosphate receptor Edg-6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3230] [GtoPdb: 278] [UniProtKB: O95977] | ||||||||
| GtoPdb | In a GTPγS binding assay | - | 6.12 | pEC50 | 750 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 6377-89 [PMID:24125884] |
| ChEMBL | Agonist activity at human S1P4 receptor expressed in CHO cells by [35S]GTPgammaS binding assay | F | 6.12 | pEC50 | 750 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 6377-6389 [PMID:24125884] |
| S1P5 receptor/Sphingosine 1-phosphate receptor Edg-8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2274] [GtoPdb: 279] [UniProtKB: Q9H228] | ||||||||
| ChEMBL | Agonist activity at human S1P5 receptor expressed in CHO cells by [35S]GTPgammaS binding assay | F | 9.01 | pEC50 | 0.98 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 6377-6389 [PMID:24125884] |
| GtoPdb | In a GTPγS binding assay | - | 9.01 | pEC50 | 0.98 | nM | EC50 |
Bioorg Med Chem Lett (2013) 23: 6377-89 [PMID:24125884]; Br J Pharmacol (2012) 167: 1035-47 [PMID:22646698]; Nurs Times (1998) 94: 55-7 [PMID:9735753] |
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]
