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- W2076349669 abstract "Structure–activity relationships have been established by exploring the eastern and western side of 5-thiazolyleacetic acids as CRTH2 (chemoattractant receptor-homologous molecule expressed on Th2 cells) antagonists. Benzhydryl motifs in the 2-position of the thiazole was found to be most advantageous. The 4-thiazole position should either carry 3- or 4-fluorophenyl rings or a 4-pyridyl suitably substituted in the flanking 2-position. Several compounds with single digit nanomolar binding affinity and full antagonistic efficacy for human CRTH2 receptor were obtained. The compound series display a good PK profile and selectivity over a large number of other targets." @default.
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- W2076349669 date "2010-02-01" @default.
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- W2076349669 title "Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 2" @default.
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- W2076349669 doi "https://doi.org/10.1016/j.bmcl.2009.12.015" @default.
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