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 becomes critical before investing additional time and resources for further development. Label-free binding technologies such as Bio-Layer Interferometry (BLI) and Surface Plasmon Resonance (SPR) systems are indispensable tools in target identification and validation processes where high throughput binding screens can be quickly established.
Octet® systems are used to identify binding targets and accurately characterize rates of complex formation (ka, association), complex stability (kd, dissociation) and affinities (KD)
Featured Applications
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 workflows, expedites assay development and allows for direct measurement of crude samples.
Protein - Small Molecules and Peptide Kinetics and Affinity Characterization
In small molecule drug discovery, the path to lead molecules can stem from many starting points including fragment screening or de novo structural design. Determining and evaluating 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 processes are essential to accurately determine biological potency in vitro so structure-activity relationships (SAR) can be used for efficient structural design. The Octet® BLI platform and the Octet® SF3 SPR can be readily used to characterize small molecule and peptide lead candidates where both platforms provide a unique set of advantages from sensitivity, throughput and ready-to-use biosensors to match your workflow needs.
Fragment Screening
Fragment-based drug design (FBDD) 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 Octet® SF3 system has the necessary sensitivity and throughput to provide complete fragment screens on libraries of several thousand compounds in just a few weeks per target.
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