- Guide to PHARMACOLOGY
Synonyms: AZD 1283 | AZD-1283
Compound class: Synthetic organic
Comment: Antagonist of P2Y12 developed as non-nucleoside analogue alternative to marketed inhibitors such as ticagrelor [1,4]. An antiplatelet agent that is orally bioavailable and has improved drug-like properties was discovered through optimization of AZD1283 .
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.✖
1. Bach P, Antonsson T, Bylund R, Björkman JA, Österlund K, Giordanetto F, van Giezen JJ, Andersen SM, Zachrisson H, Zetterberg F. (2013)
Lead optimization of ethyl 6-aminonicotinate acyl sulfonamides as antagonists of the P2Y12 receptor. separation of the antithrombotic effect and bleeding for candidate drug AZD1283.
J Med Chem, 56 (17): 7015-24. [PMID:23899349]
2. Bach P, Boström J, Brickmann K, Burgess LE, Clarke D, Groneberg RD, Harvey DM, Laird ER, O'Sullivan M, Zetterberg F. (2013)
5-alkyl-1,3-oxazole derivatives of 6-amino-nicotinic acids as alkyl ester bioisosteres are antagonists of the P2Y12 receptor.
Future Med Chem, 5 (17): 2037-56. [PMID:24215345]
3. Kong D, Xue T, Guo B, Cheng J, Liu S, Wei J, Lu Z, Liu H, Gong G, Lan T et al.. (2019)
Optimization of P2Y12 Antagonist Ethyl 6-(4-((Benzylsulfonyl)carbamoyl)piperidin-1-yl)-5-cyano-2-methylnicotinate (AZD1283) Led to the Discovery of an Oral Antiplatelet Agent with Improved Druglike Properties.
J Med Chem, 62 (6): 3088-3106. [PMID:30843696]
4. Zhang K, Zhang J, Gao ZG, Zhang D, Zhu L, Han GW, Moss SM, Paoletta S, Kiselev E, Lu W et al.. (2014)
Structure of the human P2Y12 receptor in complex with an antithrombotic drug.
Nature, 509 (7498): 115-8. [PMID:24670650]