Abstract
Phenotypic assays are tools essential for drug discovery. Phenotypic assays have different types of endpoints depending on the goals; (1) empirical endpoints for basic research to understand the underlying biology that will lead to identification of translation biomarkers, (2) empirical endpoints to identify undesired effects related to toxicity of drug candidates, and (3) knowledge-based endpoints (biomarkers) for drug discovery which ideally are translational biomarkers that will be used to identify new drug candidates and their corresponding molecular mechanisms of action. The value of phenotypic assays is increased through effective alignment of phenotypic assay endpoints with the objectives of the relevant stage in the drug discovery and development cycle.
Highlights
The goal of the paper is to provide awareness that a key feature of phenotypic assays for drug discovery is the relationship of the measured endpoint to a biomarker that translates to the desired clinical response
In the early research phase phenotypic assays can be used to increase understanding of the disease and to identify potential translational biomarkers, while in the application phase in which the underlying knowledge of the disease is translated to treatments phenotypic assays should be aligned with translational biomarkers
The phenotype most relevant to the practice of drug discovery is a phenotype that directly translated to the clinical disease
Summary
Reviewed by: Hong Wang, Eli Lilly & Co., USA Thomas Novak, Cellular Dynamics International, USA. Phenotypic assays are tools essential for drug discovery. Phenotypic assays have different types of endpoints depending on the goals; (1) empirical endpoints for basic research to understand the underlying biology that will lead to identification of translation biomarkers, (2) empirical endpoints to identify undesired effects related to toxicity of drug candidates, and (3) knowledge-based endpoints (biomarkers) for drug discovery which ideally are translational biomarkers that will be used to identify new drug candidates and their corresponding molecular mechanisms of action. The value of phenotypic assays is increased through effective alignment of phenotypic assay endpoints with the objectives of the relevant stage in the drug discovery and development cycle
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