Lead Discovery

High-content screening (HCS) is a technology used in biological research and drug discovery that combines automated microscopy, image analysis, and data visualization to study large numbers of cells or other biological samples simultaneously.

Target validation is the first and crucial step in new drug discovery. Target validation can be chemical or genetic, respectively, through chemical substances to regulate target proteins or through genetic technology, to achieve the ultimate therapeutic effect. Target validation in the early stages of new drug discovery provides support for identifying and validating the relevance of known or novel targets to specific diseases, thereby increasing the success rate of clinical trials. Candidate targets that pass validation experiments then enter the hit identification phase of the project.

The entry point of chemical procedures in drug development research is usually to identify high activity specific molecules in appropriate target assay. This initial hit can be produced in many ways. Therefore, it is important to employ alternative hit-identification strategies that are able to tackle a variety of biological macromolecular targets and to identify pharmacologically relevant compounds.

Hit to lead, also called lead generation, is the prerequisite of the construction of new drug’s molecular structure, and is the key step of new drug development. The purpose of this stage is to obtain each hit series and to produce more effective and selective compounds with pharmacokinetic properties. This stage evaluates and undergoes limited optimization to identify promising lead compounds, and then synthesizing the analogs.

Lead optimization is a diversified operation in drug discovery. It improves the target’s study of specificity, selectivity, pharmacodynamics, pharmacokinetics, and toxicology by altering the chemical structure of compounds or biological products to produce the preclinical drug candidates. In order to understand the necessity of lead optimization, it is important to determine the basic characteristics of lead, including potency, bioavailability, duration, safety and drug acceptability.

Chemical resynthesis is critical in drug discovery. With the development of a series of effective synthetic drug agents, knowledge about molecular modifications evolves, which is likely to lead to biologically active molecules. One of the most important sources of new drugs in modern science comes from the efforts of chemical resynthesis.

Structure-based drug discovery refers to drug development based on protein structure. Starting from the known structure of the target protein, based on molecular recognition, with the help of relevant calculation methods, the structure-activity relationship of the compound can be quickly established, and new hit compounds can be discovered. Through structure-based drug discovery and fragment-based drug discovery as supplements, we provide customers with an efficient and rapid technology platform for drug development.