In one aspect, the present invention provides a method of modulating an Edg-3 receptor mediated biological activity in a cell. A cell expressing the Edg-3 receptor is contacted with a modulator of the Edg-3 receptor sufficient to modulate the Edg-3 receptor mediated biological activity. In another aspect, the present invention provides a method for modulating an Edg-3 receptor mediated biological activity in a subject. A therapeutically effective amount of a modulator of the Edg-3 receptor is administered to the subject. In yet another aspect, compounds and composition useful for modulation of the Edg-3 receptor are presented.