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 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]
