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

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ChEMBL ligand: CHEMBL398435 (AR-C126532XX, AZD-6140, AZD6140, Brilinta, Brilique, Possia, Ticagrelor)
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  • 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
P2Y13 receptor/P2Y purinoceptor 13 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3321651] [GtoPdb: 329] [UniProtKB: Q9BPV8]
ChEMBL Antagonist activity at human P2Y13R expressed in HEK293 cells assessed as inhibition of 2MeSADP-induced cAMP production preincubated for 0.5 hrs followed by 2MeSADP stimulation by cAMP-glo assay F 5.85 pIC50 1398 nM IC50 J Med Chem (2022) 65: 15967-15990 [PMID:36394994]
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 in human whole blood assessed as suppression of ADP-induced decrease in PGE1-induced VASP phosphorylation measured after 10 mins by immunostaining based flow cytometric analysis B 5.29 pIC50 5140 nM IC50 J Med Chem (2020) 63: 15752-15772 [PMID:33307675]
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 Inhibition of P2Y12 receptor in human platelet assessed as reduction in ADP-induced VASP phosphorylation by flow cytometry F 7.41 pIC50 39 nM IC50 RSC Med Chem (2021) 12: 1414-1427 [PMID:34458743]
ChEMBL Inhibition of P2Y12 (unknown origin) B 8 pIC50 10 nM IC50 Bioorg Med Chem Lett (2022) 71: 128837-128837 [PMID:35640763]
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 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]