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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 |
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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 | B | 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 | B | 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 | B | 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 | B | 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 | B | 5.1 | pIC50 | >8000 | nM | IC50 | MedChemComm (2015) 6: 13-23 |
ChEMBL data shown on this page come from version 28:
Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]