Fig. 8: Points of connection serve as an effective strategy for linker optimization in early-phase drug discovery efforts. | Communications Chemistry

Fig. 8: Points of connection serve as an effective strategy for linker optimization in early-phase drug discovery efforts.

From: Linking ATP and allosteric sites to achieve superadditive binding with bivalent EGFR kinase inhibitors

Fig. 8

To best optimize for compound binding, flexibility and fragment binding mode can be altered through alternative points of connection between the linker and fragment. Subsequent optimization of linker-enabled interactions as well as structure-guided optimization for potency and medicinal chemistry properties would follow using more conventional lead optimization strategies.

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