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Synonyms: AR-C126532XX | AZD6140 | Brilinta® | Brilique® | compound 17 [PMID: 17827008]
ticagrelor is an approved drug (EMA (2010), FDA (2011))
Compound class: Synthetic organic
Comment: Ticagrelor is a selective P2Y12 receptor antagonist .
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
View more information in the IUPHAR Pharmacology Education Project: ticagrelor
1. Armstrong D, Summers C, Ewart L, Nylander S, Sidaway JE, van Giezen JJ. (2014)
Characterization of the adenosine pharmacology of ticagrelor reveals therapeutically relevant inhibition of equilibrative nucleoside transporter 1.
J Cardiovasc Pharmacol Ther, 19 (2): 209-19. [PMID:24414167]
2. Hoffmann K, Lutz DA, Straßburger J, Baqi Y, Müller CE, von Kügelgen I. (2014)
Competitive mode and site of interaction of ticagrelor at the human platelet P2Y12 -receptor.
J Thromb Haemost, 12 (11): 1898-905. [PMID:25186974]
3. Springthorpe B, Bailey A, Barton P, Birkinshaw TN, Bonnert RV, Brown RC, Chapman D, Dixon J, Guile SD, Humphries RG et al.. (2007)
From ATP to AZD6140: the discovery of an orally active reversible P2Y12 receptor antagonist for the prevention of thrombosis.
Bioorg Med Chem Lett, 17 (21): 6013-8. [PMID:17827008]
4. Zech G, Hessler G, Evers A, Weiss T, Florian P, Just M, Czech J, Czechtizky W, Görlitzer J, Ruf S et al.. (2012)
Identification of high-affinity P2Y₁₂ antagonists based on a phenylpyrazole glutamic acid piperazine backbone.
J Med Chem, 55 (20): 8615-29. [PMID:22984835]