CYM5181 [Ligand Id: 2927] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1452805 |
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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 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4333] [GtoPdb: 275] [UniProtKB: P21453] | ||||||||
| ChEMBL | S1P1 assay: The method involves contacting the receptor with a suitable concentration of an inventive compound to bring about activation of the receptor. The contacting can take place in vitro, for example in carrying out an assay to determine the S1P receptor activation activity of an inventive compound undergoing experimentation related to a submission for regulatory approval. | B | 8.43 | pEC50 | 3.7 | nM | EC50 | US-10544136-B2. Modulators of sphingosine phosphate receptors (2020) |
| GtoPdb | - | - | 8.47 | pEC50 | - | - | - | Mol Pharmacol (2008) 74: 1308-18 [PMID:18708635] |
| ChEMBL | Agonist activity at human S1PR1 expressed in CHO cells coexpressing CRE-beta-lactamase reporter assessed as inhibition of forskolin-stimulated beta-lactamase expression | F | 8.5 | pEC50 | 3.16 | nM | EC50 | Eur J Med Chem (2023) 250: 115182-115182 [PMID:36758307] |
| S1P3 receptor/Sphingosine 1-phosphate receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3892] [GtoPdb: 277] [UniProtKB: Q99500] | ||||||||
| ChEMBL | S1P1 assay: The method involves contacting the receptor with a suitable concentration of an inventive compound to bring about activation of the receptor. The contacting can take place in vitro, for example in carrying out an assay to determine the S1P receptor activation activity of an inventive compound undergoing experimentation related to a submission for regulatory approval. | B | 6.18 | pEC50 | 661 | nM | EC50 | US-10544136-B2. Modulators of sphingosine phosphate receptors (2020) |
ChEMBL data shown on this page come from version 36:
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]
