Category: Assay Development and Screening
Fragment screening provides insights in the selection of various chemotypes that are developed into hit classes of interest. The key challenge in screening fragments is the weak binding affinity (mM range) of these very small molecules (< 300 daltons). Traditional high-throughput fragment screening methods includes bioNMR, surface plasmon resonance and differential scanning fluorimeter. In this presentation, we demonstrate the utility of a radioligand binding assay in fragment screening. It is noteworthy to mention that the membrane protein target presented here is usually intractable with traditional biophysics-based fragment approaches.
Artjohn Villafania– Senior Scientist, Merck, Fort Lee, NJ
Fort Lee, NJ
My current position is in the biophysics group within the screening and compound profiling department. My current role is responsible in developing and implementing fragment screening. This role also includes profiling and characterization of compounds using various biophysical methods. My recent experience is predominantly involved the characterizations of compounds using biophysical methods including differential scanning calorimetry, surface plasmon resonance, circular dichroism and stopped-flow. I have also have a strong background in enzymology, particularly in enzyme kinetics and global progress curve analysis.