ponesimod [Ligand Id: 9320] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1096146 (ACT-128800, Ponesimod, Ponvory)
  • 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 in Human [GtoPdb: 278] [UniProtKB: O95977]
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  • S1P5 receptor in Human [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 Inhibition of S1PR1 (unknown origin) expressed in CHOK1 cells after 90 mins by beta-arresting recuitment assay F 7.9 pIC50 12.59 nM IC50 Bioorg Med Chem Lett (2018) 28: 3255-3259 [PMID:30143424]
ChEMBL Agonist activity at human recombinant S1P1 receptor expressed in CHO cells by GTPgammaS binding assay F 8.01 pEC50 9.7 nM EC50 J Med Chem (2010) 53: 4198-4211 [PMID:20446681]
GtoPdb In a radioligand binding assay using membranes from CHO cells expressing human S1P1 - 8.04 pEC50 9.1 nM EC50 J Med Chem (2010) 53: 4198-211 [PMID:20446681]
S1P3 receptor/Sphingosine 1-phosphate receptor Edg-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3892] [GtoPdb: 277] [UniProtKB: Q99500]
GtoPdb In a radioligand binding assay using membranes from CHO cells expressing human S1P2 - 5.68 pIC50 2068 nM IC50 J Med Chem (2010) 53: 4198-211 [PMID:20446681]
ChEMBL Agonist activity at human recombinant S1P3 receptor expressed in CHO cells by GTPgammaS binding assay F 6.96 pEC50 109 nM EC50 J Med Chem (2010) 53: 4198-4211 [PMID:20446681]
S1P4 receptor in Human [GtoPdb: 278] [UniProtKB: O95977]
GtoPdb In a radioligand binding assay using membranes from CHO cells expressing human S1P4 - 5.71 pIC50 1956 nM IC50 J Med Chem (2010) 53: 4198-211 [PMID:20446681]
S1P5 receptor in Human [GtoPdb: 279] [UniProtKB: Q9H228]
GtoPdb In a radioligand binding assay using membranes from CHO cells expressing human S1P5 - 6.85 pIC50 142 nM IC50 J Med Chem (2010) 53: 4198-211 [PMID:20446681]

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]