Fragment Screening of Massively-Parallel Ligand Arrays Using the Carterra^® Ultra^® SPR Platform

Key Highlights

• Carterra Ultra® offers the enhanced speed and sensitivity necessary to support Fragment Based Lead Discovery (FBLD).
• Ultra’s large ligand array allows for many targets, off targets, mutants, and multiple species to be measured in parallel; a 100-fold enhancement over other SPR systems.
• Utilize ready-made panels of biotinylated-proteins to standardize the assay parameters so you can move directly to finding hits and drive your medicinal chemistry programs.

Introduction

Fragment-Based Lead Discovery (FBLD) has emerged as a core approach to early-stage hit finding in drug discovery programs1. This form of drug discovery is distinguished by the screening of libraries of very small chemical compounds (heavy atom count < 17), that bind with low-affinity (double digit micromolar to millimolar K_D) to therapeutic targets. Screening small compounds allows for an efficient sampling of the chemical space relevant to medicinal chemistry. The identified binders, in concert with X-ray co-crystal or cryo-electron microscopy structures, serve to provide a map of how chemical matter can interact efficiently with the targets.

Posted by Anthony M. Giannetti, PhD