Hit-to-lead optimization represents a crucial phase in the drug discovery process, where initial hits are refined into lead compounds with improved potency, selectivity, and pharmacokinetic properties. This phase requires a multidisciplinary approach, integrating various strategies to identify and optimize promising drug candidates.
As a small-molecule drug discovery CRO, Alfa Chemistry provides full-process early-stage drug development services. Our DNA-encoded libraries (DELs) technology platform can not only identify promising hit compounds, but also use them as a starting point to develop millions to billions of molecules to improve the activity and other drug-like properties of the starting molecules. Furthermore, after discovering hits through DELs technology, we are also capable of optimizing them into leads. Our services include:
Hit Expansion by DNA-Encoded Libraries (DELs)
DNA-encoded libraries (DELs) revolutionize hit expansion by screening vast chemical space with unprecedented speed and efficiency.
Structure-based drug design employs computational modeling and structural biology techniques to guide hit-to-lead optimization.
Through combinatorial chemistry and automated synthesis platforms, parallel synthesis expedites the exploration of chemical space, enabling the identification of lead compounds with desirable drug-like properties.
Enzymatic assays, receptor binding assays, and other biochemical techniques assess compound-target interactions, guiding lead optimization efforts with mechanistic insights.
Surface plasmon resonance (SPR), isothermal titration calorimetry (ITC), and nuclear magnetic resonance (NMR) spectroscopy offer insights into binding kinetics, thermodynamics, and structural changes.
Cellular assays evaluate compound activity in disease-relevant cellular environments, guiding lead selection based on efficacy, toxicity, and mechanism of action.
Hit-to-lead optimization is a critical phase in drug discovery, requiring a multifaceted approach to identify and optimize lead compounds. At Alfa Chemistry, our comprehensive services encompass hit expansion, structure-based design, parallel synthesis, and a range of biochemical, biophysical, and cellular assays. Contact us today to learn more about our services and discover how we can empower your journey towards innovation and success.