| Abstract
| - Two compounds, obtained by random screening, and displaying micromolar activities on the μopiate receptor were used as starting points for optimization. In that work, the traditionalconcept of the activity of a compound (related to one or a few targets) was extended to thecomprehensive pharmacological profile of that compound on more than 70 receptors, transporters, and channels relevant to a CNS-oriented project. Using the two complementary designstrategies based on two similarity concepts described in the previous paper, we have obtainedanalogues with IC50 values ranging between 0.9 nM and a few micromolar on the μ receptorand displaying qualitatively different profiles. We discuss here, both on a case-by-case basisand from a statistical standpoint, the pharmacological profiles in light of the two similarityconcepts.
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