To provide a highly active LPA and a method of screening therewith.There is provided a method of screening a preventive and/or therapeutic substance for diseases in which LPA takes part, characterized in that a compound represented by any of formula (I), (II) and (III): [wherein the meaning of characters are described in the description] is used. The compounds obtained by the screening method or the screening kit of the present invention, their salts, their solvates and prodrugs thereof would modulate the binding of highly active LPA with LPA receptor in human and other mammals, so that they can be used as a preventive and/or therapeutic agent for diseases in which LPA takes part, for example, urinary diseases, central nervous diseases, inflammatory diseases, circulatory diseases, cancer, diabetes, immune system disorders and alimentary diseases.