title: 2-(1H-Pyrazol-4-yl)acetic acids as CRTh2 antagonists.
abstract: High throughput screening identified the pyrazole-4-acetic acid substructure as CRTh2 receptor antagonists. Optimisation of the compounds uncovered a tight SAR but also identified some low nanomolar inhibitors.
authors.affiliation: Almirall R&D Centre, Laureano Miró, 408-410, 08980 Sant Feliu de Llobregat, Barcelona, Spain.
authors.forename: Miriam
authors.initials: M
authors.lastname: Andrés
authors.forename: Mónica
authors.initials: M
authors.lastname: Bravo
authors.forename: Maria Antonia
authors.initials: MA
authors.lastname: Buil
authors.forename: Marta
authors.initials: M
authors.lastname: Calbet
authors.forename: Jordi
authors.initials: J
authors.lastname: Castro
authors.forename: Teresa
authors.initials: T
authors.lastname: Domènech
authors.forename: Peter
authors.initials: P
authors.lastname: Eichhorn
authors.forename: Manel
authors.initials: M
authors.lastname: Ferrer
authors.forename: Elena
authors.initials: E
authors.lastname: Gómez
authors.forename: Martin D
authors.initials: MD
authors.lastname: Lehner
authors.forename: Imma
authors.initials: I
authors.lastname: Moreno
authors.forename: Richard S
authors.initials: RS
authors.lastname: Roberts
authors.forename: Sara
authors.initials: S
authors.lastname: Sevilla
mesh_terms: D000085:Acetates / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D000818:Animals; D006207:Half-Life; D057166:High-Throughput Screening Assays; D011485:Protein Binding; D011720:Pyrazoles / Q000737:chemistry*; D051381:Rats; D011971:Receptors, Immunologic / Q000037:antagonists & inhibitors* / Q000378:metabolism; D011982:Receptors, Prostaglandin / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D000085:Acetates; D011720:Pyrazoles; D011971:Receptors, Immunologic; D011982:Receptors, Prostaglandin; C031280:pyrazole; C036293:prostaglandin D2 receptor