Fragment-based drug design (FBDD) has become a popular platform for the identification of lead candidates in drug discovery programs alongside structure-based drug design, and high throughput screening. In 2021 over 70% of the drugs approved by the FDA were non-protein based and therefore the ability to measure the kinetics & affinity across a range of molecular sizes is critical during initial selection.

The detection and characterization of these binding events is facilitated by sensitive biophysical technologies capable of detecting low affinity interactions of low molecular weight compounds. Surface plasmon resonance (SPR) is a core technology in many pharma and biotechnology settings for this purpose as SPR has the required sensitivity and throughput to provide complete fragment screens on libraries of several thousand compounds in just a few weeks per target.

Initial analysis of the kinetics and affinity determined by fixed concentration injections ranging from 0.01--100 µM are shown in Table 1 and the associated sensorgram shown in Figure 1A