In drug discovery, the 3D structure of proteins is crucial for the success of drugs. The increased use of sp -hybridized carbon atoms (Fsp ) is key, as it correlates with a drug's effectiveness and safety. This trend, known as 'Escape from Flatland', involves increasing Fsp 3 in drugs for better alignment with protein structures, enhancing selectivity and efficacy. This strategy improves target interaction and reduces side effects, balancing effective treatment with minimal negative effects.