RESOURCES

Both a thyroid hormone receptor (THR)-beta agonist, resmetirom and a glucagon-like peptide-1 (GLP-1) receptor agonist, semaglutide were recently approved for treating noncirrhotic metabolic dysfunction-associated steatohepatitis (MASH) with moderate to advanced liver fibrosis.

Human epidermal growth factor receptor 2 (HER2) is a member of the human epidermal growth factor receptor tyrosine kinase family that regulates cell proliferation, survival, and differentiation.

Acute myeloid leukemia (AML) is the most common acute leukemia diagnosed in adults. DNA-hypomethylating agents (HMAs), such as decitabine and azacitidine, are widely used to treat AML and myelodysplastic syndromes (MDS).

Clinical attrition of drug candidates is frequently driven by unforeseen safety liabilities, which are often associated with off-target pharmacological interactions.

Secondary pharmacology is increasingly used to identify off-target activities with potential clinical safety relevance.

Suzetrigine, the first FDA-approved non-opioid analgesic targeting hNav1.8, marks a pivotal moment in the evolution of pain therapeutics.

Secondary pharmacology identifies off-target interactions that may drive undesirable clinical effects, supporting lead optimization, candidate selection for early risk assessment

In early drug discovery, Caco-2 cells are widely used to estimate intestinal permeability.

Neurotoxicity is a major cause of drug attrition with central nervous system (CNS) affected the most.

WEE1 is a key regulator of the G2/M cell cycle checkpoint, inhibiting CDK1 to allow DNA repair before mitosis.

Clinical attrition of drug candidates is frequently driven by unforeseen safety liabilities, which are often associated with off-target pharmacological interactions.

The Adenosine A_2A Receptor (A_2AR) was selected as a representative GPCR to establish an integrated fragment‑based discovery workflow capable of screening fragments on the active receptor state.