Octet® BLI Workflows in Small-Molecule Interaction Discovery and Characterization Application Guide
Small-molecule drugs comprised the majority of all new drug approvals in recent years. Small-molecule drug development, however, remains a challenging and time-consuming process. Low molecular weight leads, low solubility, and non-specific binding propensities highlight a few challenges researchers must circumvent in small-molecule drug discovery workflows.
Label-free binding technologies such as Bio-Layer Interferometry (BLI) on the Octet® platform serve as an invaluable tool in drug development workflows by providing a direct confirmation of small-molecule binding to drug targets that is useful in hit-identification. Octet® BLI assays further help characterize interactions by measuring binding affinity and kinetics that serve as critical attributes in lead selection.
Overview
This application guide describes how Octet® BLI binding kinetic and affinity data can be utilized in small-molecule drug discovery programs from hit identification, characterization, and structure-based drug design and optimization workflows.
Document type: Application Guide
Page count: 8
Read time: 20 minutes
Last updated: January 1, 2023
Author: Nilshad Salim, PhD, Sartorius, Fremont, CA
Applications covered: Small-molecule binding, Drug discovery, High‑throughput screening, Kinetics, Lead identification and optimization
Download this application guide to learn:
- Typical Small-Molecule Characterization Assay Workflow Set-up
- Examples of Small-Molecule Binding Screens
- Structure-Kinetic Relationships
- Characterizing In Vitro Mechanism of Action of Small-Molecule Modulators of Capsid Assembly
- Structure-Based Design of Slimmer BIRB-796 Analogs to Inhibit MAPK13
- Small Molecules Immobilized as Ligands for Target Validation Studies
- Determining dCK Binding to Substrates and Kinase Inhibitors
