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ChEMBL ligand: CHEMBL2336071 (Baf312, BAF-312, BAF312, Mayzent, NVP-BAF312-NX, Siponimod) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]