Targeted Small Molecule

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The application of genomic and proteomic approaches to target identification combined with high content in vitro screening and in vivo phenotypic validation have accelerated efforts to identify novel targets. However, there remains a critical need to reduce failures during the early stages of the drug discovery process that lead to high attrition rates.

Several methodologies employed at various stages in small molecule discovery can aid scientists in reaching more informed decisions regarding the viability of a target candidate much earlier in the process:

  • Lead optimization strategies now focus not only on improving compound selectivity and potency, but also improving the ADME-Tox properties of lead candidates in order to reduce attrition rates at earlier stages in the discovery process.
  • In vitro pharmacokinetic screens are permitting the early elimination of poor drug candidates prior to costly and time-consuming in vivo experiments.
  • Quantitative in vivo imaging is enabling a more holistic, cost-effective approach to improving drug efficacy, and provides a clearer view of clinical predictivity.

PerkinElmer’s innovative in vivo and in vitro approaches to target discovery, screening, lead optimization and pre-clinical testing solutions enable scientists to make better decisions at every step, resulting in more cost-effective, efficient and predictive drug development: