The functioning of bioluminescent systems in most of the known marine organisms is based
on the oxidation reaction of the same substrate—coelenterazine (CTZ), catalyzed by …

Luminescence is characterized by the spontaneous emission of light resulting from either
chemical or biological reactions. Because of their high sensitivity, reduced background …

Most bromodomain inhibitors mimic the interactions of the natural acetylated lysine (KAc)
histone substrate through key interactions with conserved asparagine and tyrosine residues …

NanoBRET assays, which utilize bioluminescence energy resonance transfer (BRET), have
been widely adopted in drug discovery for measuring both protein-protein interactions and …

Protein–protein interactions (PPIs) are increasingly recognized for their roles in functional
cellular networks and their importance in disease-targeting contexts. Assessing PPI in the …

116 SLAS Discovery 25 (2) assays can be used in a drug discovery cascade to drive
potency and selectivity. Thus, assays for both compound–target and target–histone …

Contemporary drug discovery typically quantifies the effect of a molecule on a biological
target using the equilibrium-derived measurements of IC 50, EC 50, or K D. Kinetic …

The significance of measuring association and dissociation rates (kon and koff) in addition
the dissociation constant (KD) when designing and developing new chemical entities is now …

Summary The Kinetic Intra-Cellular Assay (KICA) is a recombinant cell-based technique that
utilizes NanoBRET technology. KICA enables the measurement of intracellular binding …