VPC12249 [Ligand Id: 2909] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL327240 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| LPA1 receptor/Lysophosphatidic acid receptor Edg-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3819] [GtoPdb: 272] [UniProtKB: Q92633] | ||||||||
| ChEMBL | In vitro ability to antagonize LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 1 in HEK293T cell lines | F | 5.6 | pIC50 | 2490 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 2735-2740 [PMID:15125924] |
| LPA1 receptor in Mouse [GtoPdb: 272] [UniProtKB: P61793] | ||||||||
| GtoPdb | - | - | 6.86 | pKi | 137 | nM | Ki | Mol Pharmacol (2001) 60: 1173-80 [PMID:11723223] |
| LPA3 receptor/Lysophosphatidic acid receptor Edg-7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3250] [GtoPdb: 274] [UniProtKB: Q9UBY5] | ||||||||
| GtoPdb | - | - | 6.37 | pKi | - | - | - | Mol Pharmacol (2001) 60: 1173-80 [PMID:11723223] |
| ChEMBL | In vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell lines | F | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 2735-2740 [PMID:15125924] |
| GtoPdb | - | - | 6.37 | pIC50 | 428 | nM | IC50 |
Curr Med Chem (2008) 15: 2122-31 [PMID:18781939]; Mol Pharmacol (2001) 60: 1173-80 [PMID:11723223] |
| S1P3 receptor in Human [GtoPdb: 277] [UniProtKB: Q99500] | ||||||||
| GtoPdb | - | - | 6.5 | pEC50 | - | - | - | Bioorg Med Chem (2007) 15: 663-77 [PMID:17113298] |
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]
