Numerous targets are quite difficult to affect with classical small molecule agents. These targets include protein-protein interactions and plain surfaces without specific features which do not allow a small molecule to “dig in” or be attached to them.
Typical cut-offs on the primary stages are Rule of 5 and Rule of 4. However, newly approved drugs go beyond those rules more and more often, especially in antibacterial, antifungal, cardiac drugs. Compounds aimed at these diseases tend to be larger and more polar than Ro5 could possibly offer.
Macrocyclic compounds possess features that push them out of the traditional Druglikeness space. At the same time, these features allow them to act in the cases small molecules seem to not being able to.
In Chemspace Macrocyclic Compounds set, we have included the custom-designed scaffolds of non-peptidic nature that could be further modified as well as totally assembled macrocyclic molecules. For more information, please contact us at firstname.lastname@example.org.