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]
1 CHEMBL2333770_lig_chart_1 Purinergic receptor P2Y1 Human
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  • P2Y11 receptor/Purinergic receptor P2Y11 in Human [ChEMBL: CHEMBL4867] [GtoPdb: 327] [UniProtKB: Q96G91]
  • This target only has 1 pki data point
2 CHEMBL2333770_lig_chart_2 Purinergic receptor P2Y11 Human
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  • P2Y12 receptor/Purinergic receptor P2Y12 in Human [ChEMBL: CHEMBL2001] [GtoPdb: 328] [UniProtKB: Q9H244]
  • This target only has 1 pki data point
3 CHEMBL2333770_lig_chart_3 Purinergic receptor P2Y12 Human
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  • P2Y14 receptor/Purinergic receptor P2Y14 in Human [ChEMBL: CHEMBL4518] [GtoPdb: 330] [UniProtKB: Q15391]
  • This target only has 1 pki data point
4 CHEMBL2333770_lig_chart_4 Purinergic receptor P2Y14 Human
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  • P2Y2 receptor/Purinergic receptor P2Y2 in Human [ChEMBL: CHEMBL4398] [GtoPdb: 324] [UniProtKB: P41231]
  • This target only has 1 pki data point
5 CHEMBL2333770_lig_chart_5 Purinergic receptor P2Y2 Human
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  • P2Y6 receptor/Pyrimidinergic receptor P2Y6 in Human [ChEMBL: CHEMBL4714] [GtoPdb: 326] [UniProtKB: Q15077]
  • This target only has 1 pki data point
6 CHEMBL2333770_lig_chart_6 Pyrimidinergic receptor P2Y6 Human
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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 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 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 B 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 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]