Structure-activity relationship of cinnamic acylsulfonamide analogues on the human EP3 prostanoid receptor

Abstract Potent and selective antagonists of the human EP 3 receptor have been identified. The structure–activity relationship of the chemical series was conducted and we found several analogues displaying sub-nanomolar K i values at the EP 3 receptor and micromolar activities at the EP 1 , EP 2 and EP 4 receptors. The effect of added human serum albumin (HSA) on the binding affinity at the EP 3 receptor was also investigated.