Think Biologically, Act Chemically.

A drug is a sophisticated molecule, purposely evolved, resulting from the accumulation of knowledge learned and exploited from simpler molecules over time. Advanced molecules with increased sophistication and capability are derived from simpler, less sophisticated structures with less capabilities. Medicinal chemists do not find, stumble upon, accidentally discover, screen for, or construct drugs. We molecules through the use of feedback cycles; we emphasize efficiency and simplicity in pursuit of multiproperty homeostasis; and we design and learn from molecular outliers. This Miniperspective illustrates inspirational themes from nature including evolution, feedback cycles, homeostasis, efficiency, and mutation. These biological themes are then exemplified in modern medicinal chemistry practices, such as design-make-test-analyze cycles (feedback), balancing molecular properties (homeostasis), defining the minimum pharmacophore (simplicity, efficiency), understanding molecular outliers (mutants), and the unifying concept of molecular evolution.