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ChEMBL ligand: CHEMBL1096146 (ACT-128800, Ponesimod, Ponvory) |
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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 | 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 32:
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]