Label-Free Affinity & Kinetic Characterization
Establishing an in-depth understanding of binding interactions between biological or small molecules is vital to elucidating ligand-receptor binding mechanisms and stability during the development of drug molecules. Drugs that exhibit similar affinities could exhibit diverse binding mechanisms and kinetics. Hence, the evaluation of affinity constants in conjunction with the association and dissociation rates provides crucial information for lead selection. Octet® assays have become increasingly valuable for affinity and kinetic characterization of biomolecules providing detailed binding profiles of biomolecules.
Large Molecules Kinetics Characterization
The Octet® family of instruments accurately measure kinetic constants by bringing the detection surface directly to the sample, eliminating the need for microfluidics. This unique approach utilizing label-free, real-time analysis streamlines laboratory workflows and expedites assay development. It allows direct measurement from crude samples while minimizing instrument maintenance. It is extremely versatile in large molecules kinetics characterization and enables rapid assay optimization to allow for the analysis of molecules ranging from recombinant proteins and antibodies to viruses and nanoparticles.
Fc Receptor Binding Assays on the Octet® System
The selection of desired antibody-based therapeutics is often based on their binding properties, including binding to FcγRs. Antibodies are sometimes engineered to achieve desired FcγRs binding properties, as their binding can greatly impact their safety and efficacy to both the target and to FcγRs.
- Octet® systems offer a high- throughput and sensitive solution for Fc receptor binding analysis
- A variety of assay-ready biosensor surfaces are available and allow for flexibility and rapid optimization of assays
Small Molecule and Peptide Binding Kinetics
The discovery of small molecule and peptide lead molecules can stem from many sources including, fragment screening, high throughput screening and de novo structural design amongst others. Determining and evaluating the affinity of small molecule binding to a therapeutic target is a significant component of the drug discovery process and lead optimization. The hit-to-lead and lead optimization process are essential to accurately determine biological potency in vitro so that structure-activity relationships (SARs) can be used for efficient structural design. Learn how Octet® R Series of Systems, Octet® RH16, Octet® RH96 and Pioneer SPR platforms can be used to characterize small molecule and peptide binding.
Target binding characterization is an essential analytical step for selecting high affinity and highly specific biologics regardless of the types of molecules The characterization of biological molecules with relatively high-affinity target binding (KD <1 nM) is often quite challenging due to the need for high-sensitivity analytical platforms capable of detecting slight changes in responses. The Pioneer SPR is a high sensitivity instrument that utilizes next generation SPR injections to improve the efficiency of the characterization process by determining the kinetics and affinity in a single step. The next-generation OneStep gradient injection featured on the Pioneer platform dramatically increases the speed of affinity characterization while maintaining accuracy and high confidence in results.