Category: Assay Development and Screening
Fragment-based lead discovery is a critical component in the early stages of many drug discovery efforts. Validated hits from fragment libraries screened by various techniques can often have advantages over larger drug-like molecules, such as higher flexibility in follow-up medicinal chemistry, higher potential ligand efficiency, and the ability to combine fragments hits into a larger high-affinity lead molecule. Screening these small molecular weight (averaging ~200 Da) molecules by label-free methods is an attractive approach, but requires high sensitivity for mass-dependent technologies such as surface plasmon resonance (SPR). By employing an intrinsically more sensitive sensing technology based on waveguide-enabled grating-coupled interferometry (GCI), the Creoptix WAVEdelta platform expands the screening space at the critical early stages of fragment-based lead discovery. Herein, we demonstrate such a screen by characterizing binding of a small fragment library to the kinase p38alpha.
Richard Isaacs– Applications Specialist, Creoptix, Inc., Westborough, MA