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ChEMBL ligand: CHEMBL1368758 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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S1P2 receptor in Human [GtoPdb: 276] [UniProtKB: O95136] | ||||||||
GtoPdb | - | - | 7.77 | pIC50 | 17 | nM | IC50 | Biochem Biophys Res Commun (2002) 299: 483-7 [PMID:12445827] |
S1P2 receptor/Sphingosine 1-phosphate receptor 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3616360] [GtoPdb: 276] [UniProtKB: P47752] | ||||||||
ChEMBL | Antagonist activity at rat S1P2 receptor | F | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (2018) 61: 9811-9840 [PMID:29969256] |
GtoPdb | - | - | 7.77 | pIC50 | 17 | nM | IC50 |
Gastroenterology (2003) 124: 459-69 [PMID:12557151]; Biochem Biophys Res Commun (2002) 299: 483-7 [PMID:12445827] |
S1P1 receptor/Sphingosine 1-phosphate receptor Edg-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4333] [GtoPdb: 275] [UniProtKB: P21453] | ||||||||
ChEMBL | Displacement of [32P]S1P from recombinant human S1PR1 expressed in CHOK1 cell membranes pretreated for 30 mins followed by [32P]S1P addition measured after 60 mins by scintillation counting method | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 488-496 [PMID:29249563] |
ChEMBL | Displacement of [32P]S1P from recombinant human S1PR1 expressed in commercial cell membranes incubated for 60 mins by scintillation counting method | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem (2019) 27: 3619-3631 [PMID:31279524] |
S1P3 receptor/Sphingosine 1-phosphate receptor Edg-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3892] [GtoPdb: 277] [UniProtKB: Q99500] | ||||||||
ChEMBL | Displacement of [32P]S1P from recombinant human S1PR3 expressed in Chem1 cell membranes co-expressing Galpha15 pretreated for 30 mins followed by [32P]S1P addition measured after 60 mins by scintillation counting method | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 488-496 [PMID:29249563] |
ChEMBL | Displacement of [32P]S1P from recombinant human S1PR3 expressed in commercial cell membranes incubated for 60 mins by scintillation counting method | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem (2019) 27: 3619-3631 [PMID:31279524] |
S1P2 receptor/Sphingosine 1-phosphate receptor Edg-5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2955] [GtoPdb: 276] [UniProtKB: O95136] | ||||||||
ChEMBL | Binding affinity to S1PR2 (unknown origin) by SPR assay | B | 5.71 | pKd | 1960 | nM | Kd | Eur J Med Chem (2022) 227: 113923-113923 [PMID:34688013] |
ChEMBL | Inhibition of S1PR2 (unknown origin) | B | 7.16 | pIC50 | 68.5 | nM | IC50 | J Med Chem (2021) 64: 17656-17689 [PMID:34905377] |
ChEMBL | Displacement of [32P]S1P from recombinant human S1PR2 expressed in commercial cell membranes incubated for 60 mins by scintillation counting method | B | 7.18 | pIC50 | 66.8 | nM | IC50 | Bioorg Med Chem (2019) 27: 3619-3631 [PMID:31279524] |
ChEMBL | Displacement of [32P]S1P from recombinant human S1PR2 expressed in Chem1 cell membranes co-expressing Galpha15 pretreated for 30 mins followed by [32P]S1P addition measured after 60 mins by scintillation counting method | B | 7.23 | pIC50 | 58.4 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 488-496 [PMID:29249563] |
ChEMBL | Antagonist activity at human S1P2 receptor | F | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (2018) 61: 9811-9840 [PMID:29969256] |
ChEMBL | Antagonist activity at S1P2 (unknown origin) | F | 7.77 | pIC50 | 17 | nM | IC50 | J Med Chem (2021) 64: 14557-14586 [PMID:34581584] |
GtoPdb | - | - | 7.77 | pIC50 | 17 | nM | IC50 | Biochem Biophys Res Commun (2002) 299: 483-7 [PMID:12445827] |
ChEMBL | Antagonist activity at S1P2 receptor (unknown origin) | B | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 1479-1482 [PMID:25746814] |
S1P2 receptor in Rat [GtoPdb: 276] [UniProtKB: P47752] | ||||||||
GtoPdb | - | - | 7.77 | pIC50 | 17 | nM | IC50 |
Gastroenterology (2003) 124: 459-69 [PMID:12557151]; Biochem Biophys Res Commun (2002) 299: 483-7 [PMID:12445827] |
S1P4 receptor/Sphingosine 1-phosphate receptor Edg-6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3230] [GtoPdb: 278] [UniProtKB: O95977] | ||||||||
ChEMBL | Displacement of [32P]S1P from recombinant human S1PR4 expressed in commercial cell membranes incubated for 60 mins by scintillation counting method | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem (2019) 27: 3619-3631 [PMID:31279524] |
S1P5 receptor/Sphingosine 1-phosphate receptor Edg-8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2274] [GtoPdb: 279] [UniProtKB: Q9H228] | ||||||||
ChEMBL | Displacement of [32P]S1P from recombinant human S1PR5 expressed in commercial cell membranes incubated for 60 mins by scintillation counting method | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem (2019) 27: 3619-3631 [PMID:31279524] |
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]