Nature excels at specificity. For example, our biological system is made of building blocks that are one enantiomer but not the other such as D-sugars, and L-amino acids. This specificity extends to medicines, where often only one enantiomer is effective while the other may have no effect or could be toxic. Nature also relies on a limited set of efficient and selective reactions such as phosphorylation, acetylation, glycosylation, etc., to drive essential biological processes unlike the hundreds of different types of chemical reactions we perform in the lab. Furthermore, in a typical drug discovery campaign, only 1 out of 200,000 to 1 million compounds screened ultimately becomes an approved medicine, a process that usually spans 10-15 years—underscoring once again nature’s remarkable specificity. In this presentation, I will share my journey over the past 9 years where we have tried to address these specificities by exploring different synthetic strategies with the goal of leveraging these advancements for medicinal applications. I will discuss how we can synthesize specific enantiomers more efficiently through asymmetric cooperative catalysis[1] and organometallic catalysis[2]. Additionally, I will demonstrate how we can modulate phosphorylation—a crucial reaction in biological systems—using synthetic molecules[3]. Finally, I will cover how high-throughput experimentation (HTE) and direct-to-biology (D2B) techniques can accelerate the drug discovery process.[4]