Figure 5. Structural features and activity α-helix mimetic compound mixtures.

A. Scaffold structure of α-helix mimetics and classification of α-helix mimetic compound mixture inhibitors of importin α/β mediated nuclear import. Each α-helix mimetic compound mixture contains a specific R_i and R_i+4 group and a mixture of 20 different structures at the R_i+7 position. Confirmed and validated α-helix mimetic compound mixture inhibitor hits are represented by a black square on the heat map. Please, refer to Supplemental Figure S2 for side chain nomenclature. B. Average % inhibition over the 20-compound mixtures of the complete α-helix mimetic library which contain the specified side chain at the R_i position (the average of all 20 variations of R_i+4 containing the specified R_i fixed). C. Average % inhibition over the 20 mixtures of the α-helix mimetic library, which contain the specified side chain at the R_i+4 position (the average of all 20 variations of R_i containing the specified R_i+4 fixed).