BMS compound 16 [PMID:23368907] [Ligand Id: 5808] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2333770
  • P2Y1 receptor/Purinergic receptor P2Y1 in Human [ChEMBL: CHEMBL4315] [GtoPdb: 323] [UniProtKB: P47900]
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  • P2Y11 receptor/Purinergic receptor P2Y11 in Human [ChEMBL: CHEMBL4867] [GtoPdb: 327] [UniProtKB: Q96G91]
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  • P2Y12 receptor/Purinergic receptor P2Y12 in Human [ChEMBL: CHEMBL2001] [GtoPdb: 328] [UniProtKB: Q9H244]
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  • P2Y14 receptor/Purinergic receptor P2Y14 in Human [ChEMBL: CHEMBL4518] [GtoPdb: 330] [UniProtKB: Q15391]
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  • P2Y2 receptor/Purinergic receptor P2Y2 in Human [ChEMBL: CHEMBL4398] [GtoPdb: 324] [UniProtKB: P41231]
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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
P2Y1 receptor/Purinergic receptor P2Y1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4315] [GtoPdb: 323] [UniProtKB: P47900]
GtoPdb Inhibition of [3H]2MeSADP binding to P2Y1 receptors expressed in COS-7 cells. - 6.92 pKi 120 nM Ki Nature (2015) 520: 317-21 [PMID:25822790]
ChEMBL Displacement of [beta-33P]-2MeS-ADP from human P2Y1 receptor transfected in HEK293 cells assessed as residual [beta-33P] bound to plate after 1 hr by scintillation counting analysis B 8.22 pKi 6 nM Ki J Med Chem (2013) 56: 1704-1714 [PMID:23368907]
ChEMBL Binding affinity to human P2Y1 receptor B 8.22 pKi 6 nM Ki Bioorg Med Chem Lett (2013) 23: 3239-3243 [PMID:23602442]
ChEMBL Displacement of [33P]-2MeS-ADP from human P2Y1 receptor expressed in HEK293 cells after 1 hr by scintillation counting analysis B 8.22 pKi 6 nM Ki J Med Chem (2013) 56: 9275-9295 [PMID:24164581]
ChEMBL Antagonist activity at human P2Y1 receptor assessed as inhibition constant B 8.22 pKi 6 nM Ki RSC Med Chem (2021) 12: 1046-1064 [PMID:34355177]
ChEMBL Inhibition of human P2Y1 assessed as inhibition constant B 8.22 pKi 6 nM Ki J Med Chem (2016) 59: 9981-10005 [PMID:27413802]
ChEMBL Antagonist activity at P2Y1 receptor in platelet-enriched human plasma assessed as 2.5 uM ADP-induced platelet aggregation preincubated for 1 min followed by ADP induction measured at 5 mins by aggregometric analysis B 5.68 pIC50 2100 nM IC50 J Med Chem (2013) 56: 9275-9295 [PMID:24164581]
ChEMBL Inhibition of human P2Y1 B 5.68 pIC50 2100 nM IC50 J Med Chem (2016) 59: 9981-10005 [PMID:27413802]
ChEMBL Antagonist activity at human P2Y1R expressed in HEK293 cells assessed as inhibition of ADP-induced IP3 production preincubated for 0.5 hrs followed by ADP stimulation by ELISA F 6.46 pIC50 350 nM IC50 J Med Chem (2022) 65: 15967-15990 [PMID:36394994]
ChEMBL Antagonist activity at P2Y1 (unknown origin) expressed in human 1321N1 cells assessed as induction of calcium stimulation by fluo-4 dye based assay F 6.55 pIC50 280 nM IC50 Eur J Med Chem (2018) 158: 302-310 [PMID:30223118]
ChEMBL Antagonist activity at P2Y1 receptor in washed human platelets assessed as 1 uM 2-methylthio-ADP-induced calcium flux by FLIPR assay F 7.54 pIC50 29 nM IC50 J Med Chem (2013) 56: 9275-9295 [PMID:24164581]
P2Y11 receptor/Purinergic receptor P2Y11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4867] [GtoPdb: 327] [UniProtKB: Q96G91]
ChEMBL Inhibition of human P2Y11 receptor B 4.82 pKi >15000 nM Ki J Med Chem (2013) 56: 1704-1714 [PMID:23368907]
P2Y12 receptor/Purinergic receptor P2Y12 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2001] [GtoPdb: 328] [UniProtKB: Q9H244]
ChEMBL Displacement of [beta-33P]-2MeS-ADP from human P2Y12 receptor transfected in HEK293 cells assessed as [beta-33P] bound to cells after 1 hr by scintillation counting analysis B 4.15 pKi >70000 nM Ki J Med Chem (2013) 56: 1704-1714 [PMID:23368907]
P2Y14 receptor/Purinergic receptor P2Y14 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4518] [GtoPdb: 330] [UniProtKB: Q15391]
ChEMBL Inhibition of human P2Y14 receptor B 5.46 pKi 3500 nM Ki J Med Chem (2013) 56: 1704-1714 [PMID:23368907]
P2Y2 receptor/Purinergic receptor P2Y2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4398] [GtoPdb: 324] [UniProtKB: P41231]
ChEMBL Inhibition of human P2Y2 receptor B 4.82 pKi >15000 nM Ki J Med Chem (2013) 56: 1704-1714 [PMID:23368907]
P2Y6 receptor/Pyrimidinergic receptor P2Y6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4714] [GtoPdb: 326] [UniProtKB: Q15077]
ChEMBL Inhibition of human P2Y6 receptor B 4.82 pKi >15000 nM Ki J Med Chem (2013) 56: 1704-1714 [PMID:23368907]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]