Target Identification and Validation
Identifying Promising Targets in Early Drug Discovery
- Easily develop and perform high throughput target ID screens
- Characterize a wide variety of analytes from small molecule fragments to biologics
Identifying and characterizing promising therapeutic targets is the first step in the drug discovery process. Validating these targets then becomes critical before investing additional time and resources to development. Label-free binding technologies such as Bio-Layer Interferometry (BLI) and Surface Plasmon Resonance (SPR) systems are indispensable tools in both the target identification and validation processes, with high throughput binding screens quickly established.
The Octet systems are used to identify binding targets and accurately characterize rates of complex formation (ka), complex stability (kd, dissociation) and affinities (KD)
Large Molecules Kinetics Characterization
The Octet family of instruments accurately measures kinetic constants by bringing the detection surface directly to the sample. This fluidics-free approach to label-free, real-time analysis streamlines laboratory workflow, expedites assay development, and allows for direct measurement of crude samples.
Protein - Small Molecules and Peptide Kinetics & Affinity Characterization
In small molecule drug discovery, the path to lead molecules can stem from many sources or starting points including fragment screening, high throughput screening, de novo structural design, etc. The determination and evaluation of the affinity of small molecule binding to a therapeutic target is a significant component of the drug discovery process. The hit-to-lead and lead optimization process are essential to accurately determine biological potency in vitro so that structure-activity relationships (SAR) can be used for efficient structural design. Octet BLI and Pioneer SPR platforms are used to characterize small molecule and peptide systems.
Fragment-based drug design has become an increasingly popular platform for the identification of lead candidates in drug discovery programs. The detection and characterization of fragment binding events is facilitated by sensitive biophysical technologies capable of detecting low affinity interactions of low molecular weight compounds. The Pioneer FE has the necessary sensitivity and throughput to provide complete fragment screens on libraries of several thousand compounds in just a few weeks per target.