10.1021/jm060657g.s001 Trond Ulven Trond Ulven Jean-Marie Receveur Jean-Marie Receveur Marie Grimstrup Marie Grimstrup Øystein Rist Øystein Rist Thomas M. Frimurer Thomas M. Frimurer Lars-Ole Gerlach Lars-Ole Gerlach Jesper Mosolff Mathiesen Jesper Mosolff Mathiesen Evi Kostenis Evi Kostenis Lena Uller Lena Uller Thomas Högberg Thomas Högberg Novel Selective Orally Active CRTH2 Antagonists for Allergic Inflammation Developed from in Silico Derived Hits American Chemical Society 2006 CRTH 2 CRTH 2 Antagonists ADME Silico Derived HitsHits mucus cell hyperplasia novel compound class 2006-11-16 00:00:00 Journal contribution https://acs.figshare.com/articles/journal_contribution/Novel_Selective_Orally_Active_CRTH2_Antagonists_for_Allergic_Inflammation_Developed_from_in_Silico_Derived_Hits/3047260 Hits from an in silico derived focused library for CRTH2 were transformed into highly selective antagonists with favorable ADME properties. Oral administration of 4-bromo-2-(1-phenyl-1<i>H</i>-pyrazole-4-carbonyl)phenoxyacetic acid (<b>19</b>) inhibited peribronchial eosinophilia and mucus cell hyperplasia in a mouse model of allergic asthma, supporting the therapeutic potential of this novel compound class. In addition, this selective pharmacological tool compound provides further evidence for CRTH2 as a relevant therapeutic target for treatment of Th2- and eosinophil-related inflammation.