ticagrelor [Ligand Id: 1765] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL398435 (AR-C126532XX, Brilique, Ticagrelor, Brilinta, AZD6140, AZD-6140)
  • P2Y12 receptor/Purinergic receptor P2Y12 in Human [ChEMBL: CHEMBL2001] [GtoPdb: 328] [UniProtKB: Q9H244]
  • P2Y12 receptor/Purinergic receptor P2Y12 in Rat [ChEMBL: CHEMBL2188] [GtoPdb: 328] [UniProtKB: Q9EPX4]
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  • Equilibrative nucleoside transporter 1 in Human [GtoPdb: 1117] [UniProtKB: Q99808]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
P2Y12 receptor/Purinergic receptor P2Y12 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2001] [GtoPdb: 328] [UniProtKB: Q9H244]
GtoPdb - - 7.85 pKi 14 nM Ki J Med Chem (2012) 55: 8615-29 [PMID:22984835]
ChEMBL Displacement of [33P]2-MeS-ADP from human recombinant P2Y12 receptor expressed in CHO cell membranes by scintillation counting method B 7.85 pKi 14 nM Ki J. Med. Chem. (2012) 55: 8615-8629 [PMID:22984835]
GtoPdb Binding data obtained using washed platelets in 96-well plates, with [125I]-P2Y12 antagonist as radioligand. - 8.7 pKi 1.99 nM Ki Bioorg Med Chem Lett (2007) 17: 6013-8 [PMID:17827008]
ChEMBL Displacement of [125I] labeled ligand from human P2Y12 receptor in human platelets B 8.7 pKi 2 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 6013-6018 [PMID:17827008]
ChEMBL Antagonist activity at P2Y12 receptor in human platelet-rich plasma assessed as inhibition of ADP-induced platelet aggregation incubated for 5 mins prior to ADP-challenge by light transmission-based assay B 6.3 pIC50 500 nM IC50 Bioorg. Med. Chem. Lett. (2014) 24: 141-146 [PMID:24332627]
ChEMBL Inhibition of P2Y12 in human platelet rich plasma assessed as reduction in ADP-induced platelet aggregation pre-incubated before ADP addition and measured after 10 mins by Bruker spectrophotometry B 6.49 pIC50 320 nM IC50 Bioorg Med Chem (2017) 25: 5260-5267 [PMID:28789912]
ChEMBL Antagonist activity at P2Y12 receptor (unknown origin) B 8.3 pIC50 5.01 nM IC50 Bioorg. Med. Chem. Lett. (2016) 26: 2739-2754 [PMID:27133596]
P2Y12 receptor/Purinergic receptor P2Y12 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2188] [GtoPdb: 328] [UniProtKB: Q9EPX4]
ChEMBL Antagonist activity at P2Y12 receptor in Sprague-Dawley rat platelet rich plasma assessed as inhibition of ADP-induced aggregation B 5.38 pIC50 4160 nM IC50 J. Med. Chem. (2014) 57: 7293-7316 [PMID:25075638]
ChEMBL Antagonist activity at P2Y12 receptor in rat platelet-rich plasma assessed as inhibition of ADP-induced platelet aggregation incubated for 5 mins prior to ADP-challenge by light transmission-based assay B 6 pIC50 <1000 nM IC50 Bioorg. Med. Chem. Lett. (2014) 24: 141-146 [PMID:24332627]
Equilibrative nucleoside transporter 1 in Human [GtoPdb: 1117] [UniProtKB: Q99808]
GtoPdb - - 7.3 pKi - - - J Cardiovasc Pharmacol Ther (2014) 19: 209-19 [PMID:24414167]

ChEMBL data shown on this page come from version 28:

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]