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 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]
