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• W2007164485 abstract "Prostaglandin D2 (PGD2) plays a key role in mediating allergic reactions seen in asthma, allergic rhinitis, and atopic dermatitis. PGD2 exerts its activity through two G protein-coupled receptors (GPCRs), prostanoid D receptor (DP or DP1), and chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTH2 or DP2). We report the optimization of a series of phenylacetic acid derivatives in an effort to improve the dual activity of AMG 009 against DP and CRTH2. These efforts led to the discovery of AMG 853 (2-(4-(4-(tert-butylcarbamoyl)-2-(2-chloro-4-cyclopropylphenyl sulfonamido)phenoxy)-5-chloro-2-fluorophenyl)acetic acid), which is being evaluated in human clinical trials for asthma." @default.
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• W2007164485 date "2011-03-02" @default.
• W2007164485 modified "2023-10-10" @default.
• W2007164485 title "Discovery of AMG 853, a CRTH2 and DP Dual Antagonist" @default.
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• W2007164485 doi "https://doi.org/10.1021/ml1002234" @default.
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