Application Note
Rapid Assay Development And Optimization For Small Molecule Drug Discovery
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•Technical Note: Rapid Assay Development And Optimization For Small Molecule Drug Discovery
By Bio-Rad Laboratories, Inc.
The drug discovery and development process requires assays amenable to high throughput, where large libraries of small molecules are screened to identify those that interact with high affinity to their protein target. Being able to perform this type of analysis with an assay that has a short development time is key. At later stages in the drug development process, the affinity of the small molecule lead compound is evaluated against human serum albumin and other relevant serum proteins to fully understand its absorption, distribution, metabolism, and excretion (ADME). The affinity and specificity of the lead compound must also be tested in several animal models in order to choose the most appropriate one for initial toxicity studies. High sensitivity and reproducibility for these binding assays, while maintaining throughput, is an absolute requirement in this process.
Surface plasmon resonance (SPR) can give detailed information on the binding affinity and kinetics of an interaction, without the need for a molecular tag or label. Labeling adds extra time and cost to assay development and can in some cases interfere with the molecular interaction by occluding a binding site (Cooper 2002). SPR technology can be used to design information-rich assays that provide a quantitative ranking of interaction affinities and the active concentration of protein ligand, which can be extremely valuable in the early stages of drug discovery (Huber and Mueller 2006). However, to be useful to the drug discovery process, interaction studies using SPR must be fast and cost effective to develop and be amenable to medium to high throughput.
Click Here To Download:•Technical Note: Rapid Assay Development And Optimization For Small Molecule Drug Discovery
