The pharmacophore model (Hypo1) with a well prediction capacity for CysLT(1) 
antagonists was developed using Catalyst/HypoGen program. Virtual screening 
against an in-house database consisted of carboxylated chalcones using Hypo1 was 
performed. Retrieved hits 26a, 26b, 27a, and 27b were synthesized and biological 
evaluated, the results of which demonstrated that these compounds showed 
moderate to good CysLT(1) antagonistic activities. This study indicated that the 
generated model (Hypo1) is a reliable and useful tool in lead optimization for 
novel CysLT(1) antagonists.