Small-molecule drug discovery can be viewed as a challenging multidimensional problem in
which various characteristics of compounds—including efficacy, pharmacokinetics and …

The allure of phenotypic screening, combined with the industry preference for target-based
approaches, has prompted the development of innovative chemical biology technologies …

Identifying ligand binding sites on proteins is a critical step in target-based drug discovery.
Current approaches to this require resource-intensive screening of large libraries of lead …

Over the past decade, a more comprehensive, large-scale approach to studying cancer
genetics and biology has revealed the challenges of tumor heterogeneity, adaption …

Medicinal polypharmacology is one answer to the complex reality of multifactorial human
diseases that are often unresponsive to single-targeted treatment. It is an admittance that …

Most neurological diseases have a multifactorial nature and the number of molecular
mechanisms discovered as underpinning these diseases is continuously evolving. The old …

Transient receptor potential canonical (TRPC) channels are highly homologous,
nonselective cation channels that form many homo-and heterotetrameric channels. These …

High-quality small molecule chemical probes are extremely valuable for biological research
and target validation. However, frequent use of flawed small-molecule inhibitors produces …

Fragment‐like natural products were identified as ligand‐efficient chemical matter for hit‐to‐
lead development and chemical‐probe discovery. Relying on a computational method using …

Most existing antibiotics were discovered through screens of environmental microbes,
particularly the streptomycetes, for the capacity to prevent the growth of pathogenic bacteria …