MRS2500 [Ligand Id: 1724] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL444278 (MRS-2500)
  • P2Y1 receptor/Purinergic receptor P2Y1 in Human [ChEMBL: CHEMBL4315] [GtoPdb: 323] [UniProtKB: P47900]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
P2Y1 receptor/Purinergic receptor P2Y1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4315] [GtoPdb: 323] [UniProtKB: P47900]
GtoPdb - - 9.1 pKi - - - Biochem Pharmacol (2004) 68: 1995-2002 [PMID:15476670];
J Med Chem (2003) 46: 4974-87 [PMID:14584948]
ChEMBL Inhibition of [3H]5 binding to P2Y purinoceptor 1 expressed in Sf9 cells B 9.11 pKi 0.78 nM Ki J. Med. Chem. (2003) 46: 4974-4987 [PMID:14584948]
ChEMBL Binding affinity to human P2Y1 receptor B 9.11 pKi 0.78 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 3338-3343 [PMID:18445527]
ChEMBL Displacement of [3H]2-chloro-N 6- methyl-( N )-methanocarba-2'-deoxyadenosine 3 ' ,5 '-bis-phosphate from human P2Y1 expressed in baculovirus infected insect Sf9 cells after 30 mins by scintillation spectrometric method B 9.11 pKi 0.78 nM Ki Eur J Med Chem (2018) 158: 302-310 [PMID:30223118]
ChEMBL Antagonistic activity against P2Y purinoceptor 1 F 8.08 pIC50 8.4 nM IC50 J. Med. Chem. (2003) 46: 4974-4987 [PMID:14584948]

ChEMBL data shown on this page come from version 31:

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]