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Modulation of multiple targets within relevant biological pathways and networks is increasingly being recognized as a superior approach towards the next generation of treatments for diseases with complex, polygenic aetiology such as psychiatric disorders. Consequently, there is an ever-increasing interest in deliberate and rational design of ligands that act selectively on specific multiple targets (designed polypharmacology). These compounds have been described as Designed Multiple Ligands (DMLs), and the process in which they are discovered and optimized is referred to as Multi Target Drug Discovery (MTDD). This chapter describes the current state of the art, challenges and future directions in this field.

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