AM095 [Ligand Id: 6988] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2182052 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| LPA4 receptor/Lysophosphatidic acid receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5968] [GtoPdb: 94] [UniProtKB: Q99677] | ||||||||
| ChEMBL | Antagonist activity at human LPA4 receptor expressed in rat B103 cells assessed as inhibition of LPA-induced calcium mobilization preincubated for 30 mins followed by LPA induction by FLIPR Calcium 4 dye-based fluorometric analysis | F | 5.1 | pIC50 | >8000 | nM | IC50 | Medchemcomm (2015) 6: 13-23 |
| LPA5 receptor/Lysophosphatidic acid receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5700] [GtoPdb: 124] [UniProtKB: Q9H1C0] | ||||||||
| ChEMBL | Antagonist activity at human LPA5 receptor expressed in rat B103 cells assessed as inhibition of LPA-induced calcium mobilization preincubated for 30 mins followed by LPA induction by FLIPR Calcium 4 dye-based fluorometric analysis | F | 5.1 | pIC50 | >8000 | nM | IC50 | Medchemcomm (2015) 6: 13-23 |
| LPA1 receptor/Lysophosphatidic acid receptor Edg-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3819] [GtoPdb: 272] [UniProtKB: Q92633] | ||||||||
| GtoPdb | - | - | 6.1 | pIC50 | - | - | - | J Pharmacol Exp Ther (2011) 336: 693-700 [PMID:21159750] |
| ChEMBL | Antagonist activity at LPA1 in human lung fibroblasts assessed as inhibition of LPA-induced contraction after 18 hrs by 3D collagen gel contraction assay | F | 6.82 | pIC50 | 150 | nM | IC50 | J Med Chem (2012) 55: 7920-7939 [PMID:22894757] |
| ChEMBL | Antagonist activity at human LPA1 receptor expressed in CHO cells assessed as inhibition of LPA-induced calcium mobilization preincubated for 30 mins followed by LPA induction by FLIPR Calcium 4 dye-based fluorometric analysis | F | 7.6 | pIC50 | 25 | nM | IC50 | Medchemcomm (2015) 6: 13-23 |
| LPA1 receptor in Mouse [GtoPdb: 272] [UniProtKB: P61793] | ||||||||
| GtoPdb | - | - | 6.11 | pIC50 | 778 | nM | IC50 | J Pharmacol Exp Ther (2011) 336: 693-700 [PMID:21159750] |
| LPA2 receptor/Lysophosphatidic acid receptor Edg-4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3724] [GtoPdb: 273] [UniProtKB: Q9HBW0] | ||||||||
| ChEMBL | Antagonist activity at human LPA2 receptor expressed in rat B103 cells assessed as inhibition of LPA-induced calcium mobilization preincubated for 30 mins followed by LPA induction by FLIPR Calcium 4 dye-based fluorometric analysis | F | 5.1 | pIC50 | >8000 | nM | IC50 | Medchemcomm (2015) 6: 13-23 |
| LPA3 receptor/Lysophosphatidic acid receptor Edg-7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3250] [GtoPdb: 274] [UniProtKB: Q9UBY5] | ||||||||
| ChEMBL | Antagonist activity at human LPA3 receptor expressed in CHO cells assessed as inhibition of LPA-induced calcium mobilization preincubated for 30 mins followed by LPA induction by FLIPR Calcium 4 dye-based fluorometric analysis | F | 5.1 | pIC50 | >8000 | nM | IC50 | Medchemcomm (2015) 6: 13-23 |
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]
