Covalent drugs have been used to treat diseases for more than a century, but tools that
facilitate the rational design of covalent drugs have emerged more recently. The purposeful …

Many drugs, or their antecedents, were discovered through observation of their effects on
normal or disease physiology. For the past generation, this phenotypic drug discovery …

Covalent drugs have made a major impact on human health but until recently were shunned
by the pharmaceutical industry over concerns about the potential for toxicity. A resurgence …

Most human proteins lack chemical probes, and several large-scale and generalizable small-
molecule binding assays have been introduced to address this problem. How compounds …

Fragment‐based drug discovery (FBDD) is now established as a complementary approach
to high‐throughput screening (HTS). Contrary to HTS, where large libraries of drug‐like …

High‐throughput (HT) screening drug discovery, during which thousands or millions of
compounds are screened, remains the key methodology for identifying active chemical …

Creatine kinases (CKs) provide local ATP production in periods of elevated energetic
demand, such as during rapid anabolism and growth. Thus, creatine energetics has …

Cysteine is one of the least abundant amino acids in proteins of many organisms, which
plays a crucial role in catalysis, signal transduction, and redox regulation of gene …

Targeted protein degradation refers to the use of small molecules to induce the selective
degradation of proteins. In its most common form, this degradation is achieved through …

Activity-based protein profiling (ABPP) is a versatile strategy for identifying and
characterizing functional protein sites and compounds for therapeutic development …