Chirality is an inherent aspect of biology, and interactions between biomolecules are often
influenced by stereochemistry and topographic complexity. This has implications for how …

Stereochemical and skeletal complexity are particularly important vis‐à‐vis the cross‐talks
between a small molecule and a complementary active site of a biological target. This …

Proteins are often enantioselective towards their binding partners. When designing small
molecules to interact with these targets, one should consider stereoselectivity. As …

When designing small molecules to interact with the targets, one should consider stereo
selectivity. As considerations for exploring structure space evolve, chirality is increasingly …

Natural products that act as highly specific, small-molecule protein-binding agents and as
modulators of protein-protein interactions are highly complex and exhibit functional groups …

High-throughput screening is the dominant method used to identify lead compounds in drug
discovery. As such, the makeup of screening libraries largely dictates the biological targets …

Background:'Diversity'is often cited as a crucial consideration when generating compound
collections for biological screening. However, what exactly does one mean by 'diversity'and …

The medicinal chemistry community has become increasingly aware of the value of tracking
calculated physical properties such as molecular weight, topological polar surface area …

Systematic and quantitative measurements of the roles of stereochemistry and skeleton-
dependent conformational restriction were made using multidimensional screening. We first …

Identification of new biological targets combined with combinatorial medicinal chemistry has
enormous potential to facilitate the discovery of new therapeutics. However, these new …