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The technological advances in molecular biology and human genome sequencing have made it possible to rapidly produce a large number of biological targets, thus initiating a new era of molecular target-based screening for modern drug discovery.

The target is usually a single gene, gene product or molecular mechanism identified based on genetic analysis or biological observation. It is divided into two classes: genetic targets or mechanistic targets. Genetic targets refer to genes or gene products that have been found to carry mutations or that confer a higher disease risk. While mechanistic targets represent receptors, genes, enzymes, and so on that are usually genetically indistinguishable from the normal population.

The target-based method is a reasonable method for screening drug candidates targeting a biomolecule that causes diseases. In recent years, with the advancement of high-throughput experimental techniques, target-based approach has been widely used in drug discovery. The approach is not limited to small molecule drug discovery. Antibody drugs and other protein biologics are usually discovered through target-based approaches, and the discovery of gene therapy and nucleic acid-based therapeutics is inherently target based as well.

An advantage of target-based screening is that it is easier to execute than phenotypic approaches, operating with knowledge of a drug's molecular mechanisms from an earlier stage, and are generally faster, simpler, and less costly to develop and run. When a molecular target is known, drug discovery efforts can utilize computational modeling, crystallography, binding kinetics, and molecular pharmacology to understand how a drug interacts with a target, allowing efficient structure-activity relationship (SAR) development, biomarker development, and the discovery of future generations of drugs acting at the target.

Target-based Screening

Creative Bioarray's target-based screening platform serve as a primary screening to guide SAR programs. The team's experience in assay development and validation helps to advance the programs to the next stage. Our comprehensive methods allow pharmaceutical and biotechnological companies to fully understand the target profile of the compounds under development or already in the market. Some of the target-based screening methods are mentioned as follows:

  • Mass spectrometry-based method
  • Gas chromatography-mass spectrometry (GC-MS)
  • Liquid chromatography-mass spectrometry (LC-MS)
  • Ultra-performance liquid chromatography-mass spectrometry (UPLC-MS)
  • Nuclear magnetic resonance spectroscopy (NMR)
  • Thermal shift or calorimetry-based method
  • Affinity-based method

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