JTE-013 [Ligand Id: 2917] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL1368758 |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 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 | 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 33:
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]
