siponimod [Ligand Id: 9289] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2336071 (Baf312, BAF-312, BAF312, Mayzent, NVP-BAF312-NX, Siponimod)
  • S1P1 receptor/Sphingosine 1-phosphate receptor Edg-1 in Human [ChEMBL: CHEMBL4333] [GtoPdb: 275] [UniProtKB: P21453]
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  • S1P3 receptor/Sphingosine 1-phosphate receptor Edg-3 in Human [ChEMBL: CHEMBL3892] [GtoPdb: 277] [UniProtKB: Q99500]
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  • S1P4 receptor/Sphingosine 1-phosphate receptor Edg-6 in Human [ChEMBL: CHEMBL3230] [GtoPdb: 278] [UniProtKB: O95977]
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  • S1P5 receptor/Sphingosine 1-phosphate receptor Edg-8 in Human [ChEMBL: CHEMBL2274] [GtoPdb: 279] [UniProtKB: Q9H228]
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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 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]