MRS2578 [Ligand Id: 1753] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1321988
  • P2Y6 receptor/Pyrimidinergic receptor P2Y6 in Human [ChEMBL: CHEMBL4714] [GtoPdb: 326] [UniProtKB: Q15077]
  • P2Y6 receptor/Pyrimidinergic receptor P2Y6 in Rat [ChEMBL: CHEMBL3543] [GtoPdb: 326] [UniProtKB: Q63371]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
P2Y6 receptor/Pyrimidinergic receptor P2Y6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4714] [GtoPdb: 326] [UniProtKB: Q15077]
GtoPdb - - 7.4 pIC50 - - - Biochem Pharmacol (2004) 67: 1763-70 [PMID:15081875]
ChEMBL Antagonist activity at P2Y6 receptor (unknown origin) F 7.43 pIC50 37 nM IC50 Bioorg Med Chem (2018) 26: 366-375 [PMID:29254895]
ChEMBL Antagonist activity at human P2Y6 receptor expressed in human 1321N1 cells assessed as inhibition of UDP-induced inositol-1-phosphate accumulation preincubated for 30 mins followed by UDP addition and measured after 30 mins by liquid scintillation counting method F 7.43 pIC50 37 nM IC50 Bioorg Med Chem Lett (2021) 41: 128008-128008 [PMID:33831560]
P2Y6 receptor/Pyrimidinergic receptor P2Y6 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3543] [GtoPdb: 326] [UniProtKB: Q63371]
GtoPdb - - 7 pIC50 - - - Biochem Pharmacol (2004) 67: 1763-70 [PMID:15081875]
ChEMBL Antagonist activity at rat P2Y6 receptor expressed in human 1321N1 cells assessed as inhibition of UDP-induced inositol-1-phosphate accumulation preincubated for 30 mins followed by UDP addition and measured after 30 mins by liquid scintillation counting method F 7.01 pIC50 98 nM IC50 Bioorg Med Chem Lett (2021) 41: 128008-128008 [PMID:33831560]

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]