AM095 [Ligand Id: 6988] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2182052
  • LPA4 receptor/Lysophosphatidic acid receptor 4 in Human [ChEMBL: CHEMBL5968] [GtoPdb: 94] [UniProtKB: Q99677]
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  • LPA5 receptor/Lysophosphatidic acid receptor 5 in Human [ChEMBL: CHEMBL5700] [GtoPdb: 124] [UniProtKB: Q9H1C0]
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  • LPA1 receptor/Lysophosphatidic acid receptor Edg-2 in Human [ChEMBL: CHEMBL3819] [GtoPdb: 272] [UniProtKB: Q92633]
  • LPA1 receptor in Mouse [GtoPdb: 272] [UniProtKB: P61793]
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  • LPA2 receptor/Lysophosphatidic acid receptor Edg-4 in Human [ChEMBL: CHEMBL3724] [GtoPdb: 273] [UniProtKB: Q9HBW0]
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  • LPA3 receptor/Lysophosphatidic acid receptor Edg-7 in Human [ChEMBL: CHEMBL3250] [GtoPdb: 274] [UniProtKB: Q9UBY5]
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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 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, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]