Assay Development & Screening

Assay development and screening are critical processes in drug discovery, aimed at identifying compounds that have the desired biological activity. Assay development involves designing and optimizing experimental procedures to measure the effect potential drug candidates have on their biological targets. Screening then allows us to test large libraries of compounds rapidly and efficiently against these assays. Hits from this primary screen are further validated and optimized through secondary assays to ensure their target interaction, efficacy, and specificity. At CLS we have extensive experience of in vitro Screening and deliver customised, instructive, and efficient screening programs to progress fully characterised hits through drug discovery programs. We offer high and medium-throughput screening approaches using biophysical, biochemical, phenotypic, and cell-based assays. Our technologies allow cost-effective identification of hit compounds from any type of compound library, including our proprietary fragment library.

‍Biochemical Screening:

Biochemical screening uses purified enzymes, receptors, or other biomolecules to assess how a compound influences specific biochemical reactions. We offer ultra-high-throughput (UHT) screening methods through our trusted partner to analyse large compound libraries rapidly. This approach will allow you to identify molecules that exhibit the correct activity profile against the target biomolecule. The successful hits from your biochemical screen can then progress to further stages of drug development, serving as a foundation for understanding the molecular mechanisms underlying drug-target interactions.

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Biophysical Screening:

Biophysical screening complements biochemical methods by providing insights into the physical properties of drug-target interactions. We offer techniques such as surface plasmon resonance (SPR), grating-coupled interferometry (GCI), isothermal titration calorimetry (ITC), differential scanning fluorimetry (DSF), nuclear magnetic resonance (NMR), and X-ray crystallography to study the structural aspects of molecular binding. These biophysical methods offer a more detailed understanding of how a drug candidate interacts with its target on a molecular level, providing information on binding affinities, kinetics, and thermodynamics. This structural information is crucial for optimizing your hit compounds and guiding medicinal chemistry efforts to enhance the potency and selectivity of your potential drug.

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‍Cellular Screening:

Cellular screening involves evaluating the effects of potential drug candidates within a cellular context, providing a more physiologically relevant assessment of drug activity. We use cell-based assays to study how compounds influence cell viability, proliferation, or specific cellular functions. This step is essential for understanding how a drug may behave in a complex biological environment, considering factors such as cell permeability, metabolism, and potential off-target effects. Cellular screening helps bridge the gap between biochemical and biophysical screening with isolated targets and the later stages involving tissues and animal models and clinical trials.

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