Hit-to-lead (H2L) is a crucial phase in drug discovery where initial compounds identified as 'hits' are optimized and refined to become 'lead' compounds with improved efficacy, selectivity, and pharmacokinetic properties. This process involves a series of chemical modifications and biological evaluations to enhance the drug's potential for further development.

Hit-to-lead

Drug discovery is a complex and multi-disciplinary process aimed at identifying new candidate medications, which involves target identification, lead compound discovery, and preclinical testing. The process is often lengthy and costly, requiring collaboration across various scientific fields to ensure the safety and efficacy of new drugs before they reach clinical trials.

Drug Discovery

Initial compounds

Hit compounds

Lead compounds

Improved efficacy

Selectivity refers to the ability of a system, process, or organism to preferentially choose or react with certain elements, compounds, or signals over others. This concept is crucial in fields like chemistry, biology, and engineering, where it impacts the efficiency, specificity, and outcome of reactions and processes.

Selectivity

Pharmacokinetic properties

Chemical modifications involve the alteration of a molecule's structure through the addition, removal, or transformation of functional groups, thereby impacting its physical and chemical properties. This process is crucial in fields such as drug development, where it is used to enhance efficacy, stability, and reduce toxicity of therapeutic agents.

Chemical Modifications

Biological evaluations

Drug development is a complex, multi-stage process that involves the discovery, design, testing, and regulatory approval of new pharmaceuticals to ensure they are safe and effective for human use. It requires collaboration among scientists, clinicians, and regulatory bodies, and can take over a decade with high financial investment and risk of failure at various stages.

Concepts

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