MRS2698 [Ligand Id: 1733] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL373780 (2'-amino-2-thio-UTP, MRS-2698)
  • P2Y2 receptor/Purinergic receptor P2Y2 in Human [ChEMBL: CHEMBL4398] [GtoPdb: 324] [UniProtKB: P41231]
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  • P2Y4 receptor/Pyrimidinergic receptor P2Y4 in Human [ChEMBL: CHEMBL2123] [GtoPdb: 325] [UniProtKB: P51582]
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  • P2Y6 receptor/Pyrimidinergic receptor P2Y6 in Human [ChEMBL: CHEMBL4714] [GtoPdb: 326] [UniProtKB: Q15077]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
P2Y2 receptor/Purinergic receptor P2Y2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4398] [GtoPdb: 324] [UniProtKB: P41231]
ChEMBL Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C F 8.1 pEC50 8 nM EC50 J Med Chem (2007) 50: 1166-1176 [PMID:17302398]
ChEMBL Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay F 8.1 pEC50 8 nM EC50 Bioorg Med Chem (2008) 16: 6319-6332 [PMID:18514530]
ChEMBL Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assay F 8.1 pEC50 8 nM EC50 J Med Chem (2010) 53: 1673-1685 [PMID:20095577]
ChEMBL Agonist activity at human P2Y2 F 8.1 pEC50 8 nM EC50 J Med Chem (2011) 54: 4018-4033 [PMID:21528910]
GtoPdb - - 8.1 pEC50 - - - J Med Chem (2007) 50: 1166-76 [PMID:17302398]
P2Y4 receptor/Pyrimidinergic receptor P2Y4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2123] [GtoPdb: 325] [UniProtKB: P51582]
ChEMBL Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C F 5.62 pEC50 2400 nM EC50 J Med Chem (2007) 50: 1166-1176 [PMID:17302398]
ChEMBL Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay F 5.62 pEC50 2400 nM EC50 Bioorg Med Chem (2008) 16: 6319-6332 [PMID:18514530]
P2Y6 receptor/Pyrimidinergic receptor P2Y6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4714] [GtoPdb: 326] [UniProtKB: Q15077]
ChEMBL Agonist activity at human recombinant P2Y6 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C F 5 pEC50 >10000 nM EC50 J Med Chem (2007) 50: 1166-1176 [PMID:17302398]

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]