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Article ; Online: Discovery of Potent and Selective Quinoxaline-Based Protease-Activated Receptor 4 (PAR4) Antagonists for the Prevention of Arterial Thrombosis.

Zhang, Xiaojun / Jiang, Wen / Richter, Jeremy M / Bates, J Alex / Reznik, Samuel K / Stachura, Sylwia / Rampulla, Richard / Doddalingappa, Dyamanna / Ulaganathan, Sankar / Hua, Ji / Bostwick, Jeffrey S / Sum, Chi / Posy, Shana / Malmstrom, Sarah / Dickey, Joyce / Harden, David / Lawrence, R Michael / Guarino, Victor R / Schumacher, William A /
Wong, Pancras / Yang, Jing / Gordon, David A / Wexler, Ruth R / Priestley, E Scott

Journal of medicinal chemistry

2024  Volume 67, Issue 5, Page(s) 3571–3589

Abstract: PAR4 is a promising antithrombotic target with potential for separation of efficacy from bleeding risk relative to current antiplatelet therapies. In an effort to discover a novel PAR4 antagonist chemotype, a quinoxaline-based HTS ... ...

Abstract PAR4 is a promising antithrombotic target with potential for separation of efficacy from bleeding risk relative to current antiplatelet therapies. In an effort to discover a novel PAR4 antagonist chemotype, a quinoxaline-based HTS hit
MeSH term(s) Animals ; Fibrinolytic Agents/pharmacology ; Fibrinolytic Agents/therapeutic use ; Macaca fascicularis ; Quinoxalines/pharmacology ; Quinoxalines/therapeutic use ; Receptors, Thrombin ; Thrombin ; Hemorrhage ; Thrombosis/drug therapy ; Thrombosis/prevention & control ; Receptor, PAR-1 ; Blood Platelets ; Platelet Aggregation
Chemical Substances protease-activated receptor 4 (JWE1M73YZN) ; Fibrinolytic Agents ; Quinoxalines ; Receptors, Thrombin ; Thrombin (EC 3.4.21.5) ; Receptor, PAR-1
Language English
Publishing date 2024-02-22
Publishing country United States
Document type Journal Article
ZDB-ID 218133-2
ISSN 1520-4804 ; 0022-2623
ISSN (online) 1520-4804
ISSN 0022-2623
DOI 10.1021/acs.jmedchem.3c01986
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