226915-90-8Relevant academic research and scientific papers
Discovery of Potent Orally Active Protease-Activated Receptor 1 (PAR1) Antagonists Based on Andrographolide
Liu, Jun,Sun, Bin,Zhao, Xiaoyu,Xing, Jie,Gao, Yanhui,Chang, Wenqiang,Ji, Jianbo,Zheng, Hongbo,Cui, Changyi,Ji, Aiguo,Lou, Hongxiang
, p. 7166 - 7185 (2017/09/07)
Protease-activated receptor-1 (PAR1), a G-protein-coupled receptor, plays a critical role in thrombin-mediated platelet aggregation. It is regarded as a promising antithrombosis target that is unlikely to result in bleeding. Here, we describe the synthesi
Theramutein modulators
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Page/Page column 192, (2010/02/17)
This invention relates to agents that are inhibitors or activators of variant forms of endogenous proteins and novel methods of identifying such variants. Of particular interest are inhibitors and activators of endogenous protein variants, encoded by genes which have mutated, which variants often arise or are at least first identified as having arisen following exposure to a chemical agent which is known to be an inhibitor or activator of the corresponding unmutated endogenous protein.
THERAMUTEIN MODULATORS
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Page/Page column 227, (2008/12/07)
This invention relates to agents that are inhibitors or activators of variant forms of endogenous proteins and novel methods of identifying such variants. Of particular interest are inhibitors and activators of endogenous protein variants, encoded by genes which have mutated, which variants often arise or are at least first identified as having arisen following exposure to a chemical agent which is known to be an inhibitor or activator of the corresponding unmutated endogenous protein.
Metabolism-based identification of a potent thrombin receptor antagonist
Clasby, Martin C.,Chackalamannil, Samuel,Czarniecki, Michael,Doller, Dario,Eagen, Keith,Greenlee, William,Kao, Grace,Lin, Yan,Tsai, Hsingan,Xia, Yan,Ahn, Ho-Sam,Agans-Fantuzzi, Jacqueline,Boykow, George,Chintala, Madhu,Foster, Carolyn,Smith-Torhan, April,Alton, Kevin,Bryant, Matthew,Hsieh, Yunsheng,Lau, Janice,Palamanda, Jairam
, p. 129 - 138 (2008/02/03)
The metabolism of our prototypical thrombin receptor antagonist 1, K i = 2.7 nM, was studied and three major metabolites (2, 4, and 5) were found. The structures of the metabolites were verified independently by synthesis. Compound 4 was shown
THROMBIN RECEPTOR ANTAGONISTS
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Page 80, (2010/11/30)
Heterocyclic-substituted tricyclics of formula (I) or a pharmaceutically acceptable salt thereof, wherein: the single dotted line represents an optional double bond; the double dotted line represents an optional single bond; n is 0-2; Q is optionally subs
