How important are high-quality cell lines & kinase assays in drug discovery?
In the dynamic field of small molecule drug discovery, both cell lines and kinase assays play essential roles in evaluating drug efficacy, selectivity, and mechanism of action. Cell lines provide a physiologically relevant environment to assess compound activity in a cellular context, while kinase assays offer precise measurements of enzyme function and inhibitor potency. The latest in kinase assay technologies further enhance these studies by enabling real-time kinetic measurements, leading to better-informed decisions in hit identification, lead optimisation. Together, these tools provide critical insights that drive the identification and development of effective drug candidates.
Here we go into detail about why both parts can heavily contribute towards the success of your project.
The role of cell lines in drug discovery
Cell-based assays serve as a bridge between in vitro biochemical studies and in vivo efficacy models, providing critical insights into the behavior of small molecules within a biological system. BPS Bioscience specialises in the development of engineered cell lines expressing key drug targets, such as:
- Kinases: Central to signal transduction pathways, kinases are among the most targeted protein families in drug development.
- Immune checkpoints: Critical for immuno-oncology research, these targets help assess small molecule modulation of immune cell activity.
- Epigenetic modifiers: Enzymes regulating gene expression, playing pivotal roles in cancer and other diseases.
- Proteases and other enzymes: Essential for a wide range of therapeutic areas, including metabolic and infectious diseases.
Using these cell lines, researchers can perform high-throughput screening (HTS), functional validation, and mechanism-of-action (MoA) studies to assess the efficacy, specificity, and toxicity of small molecule inhibitors.
Kinase assays: Precision in drug screening
Protein kinases are major targets in small molecule drug discovery, given their roles in regulating cell growth, differentiation, and apoptosis. AssayQuant Technologies has revolutionised kinase assay development with its PhosphoSens® technology, which offers unparalleled advantages:
- Real-time kinetic measurements: Unlike traditional endpoint assays, PhosphoSens® enables continuous monitoring of phosphorylation events, allowing researchers to analyse inhibitor binding and efficacy in real time.
- High sensitivity and precision: The fluorescence-based system minimises background noise and enhances signal detection, making it ideal for detecting weak inhibitors and ensuring reproducibility.
- Broad kinase coverage: AssayQuant provides assays for a comprehensive range of kinases, supporting diverse drug discovery programs.
By utilising AssayQuant’s kinase assays, researchers can rapidly evaluate kinase inhibitors, determine IC50 values, and analyse inhibitor selectivity - all crucial steps in the lead optimisation process.
Integrating BPS Bioscience cell lines with AssayQuant kinase assays
The true power of small molecule drug discovery lies in integrating multiple advanced technologies to streamline target validation and compound screening. By combining BPS Bioscience’s engineered cell lines with AssayQuant’s kinase assays, researchers can:
- Screen for potent inhibitors: Use kinase-expressing cell lines to test the effects of small molecules in a biologically relevant context.
- Validate target engagement: Employ biochemical assays to confirm direct binding and activity modulation.
- Optimise lead compounds: Analyse dose-response relationships, off-target effects, and cellular efficacy to refine promising candidates.
- Accelerate drug development: Reduce attrition rates by using highly predictive preclinical models early in the pipeline.
For researchers engaged in small molecule drug discovery, leveraging the complementary strengths of BPS Bioscience’s engineered cell lines and AssayQuant’s kinase assays provides a powerful approach to identifying and characterising new therapeutic candidates. By integrating these state-of-the-art tools, scientists can enhance the efficiency, accuracy, and success rate of their drug discovery efforts, ultimately bringing novel treatments to market faster and more effectively.
Explore More
Interested in enhancing your small molecule drug discovery workflow? Learn more about BPS Bioscience’s cell lines and explore AssayQuant’s kinase assays, or contact our drug discovery specialists.