Lead Discovery: Screening and Optimization




After a drug target is identified and validated, research now focuses on lead discovery, also known as lead identification and screening, in which multiple drug candidates are developed. Leads must be shown to reach the target and modulate its activity in vivo while acting within acceptable safety margins. At this stage, high-throughput screening is typically used to identify promising candidates for a lead (hit-to-lead). Show more

Potential leads are evaluated for a range of properties that can include selectivity, binding mechanism(s) and kinetic analysis, dose-response curves, tractability to modifications, potency, in vitro toxicity, and orthogonal testing. Based on the results of this initial testing regimen, new lead-related candidates are evaluated, for example, antibodies optimized by protein engineering for increased efficacy and specificity or reduced immunogenicity. This stage is known as lead optimization. Show less


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Solutions for Lead Discovery: Screening and Optimization

Gene Expression

Gene Expression

Measure gene expression and copy number variation (CNV) in response to lead molecule screening with high sensitivity and absolute quantitation using Droplet Digital™ PCR. Utilize our automated real-time PCR systems and liquid handling systems for higher-throughput analysis needs.

Droplet Digital PCR Systems
Real-Time PCR Automation

PCR Instrument Validation Tools and Services


Protein Purification and Quantification

Protein Purification and Quantification

Choose from a broad selection of chromatography columns and resins and modular FPLC systems for rapid purification of your lead molecules, antibodies or other proteins of interest. Evaluate and quantitate proteins using a range of complementary technologies.

Multiplex Immunoassays
Western Blotting Reagents and Equipment
GS-900™ Calibrated Densitometer and Regulatory Tools
NGC™ Medium-Pressure Chromatography Systems
Chromatography Columns and Resins

Cell Analysis

Cell Screening

For evaluation of the effects of lead molecules on cells, as in high-content screening (HCS) methods, Bio-Rad offers equipment for cell imaging, counting, and sorting, and flow cytometry.

Cell Imaging
Cell Counting
Cell Sorting and Flow Cytometry
Antibodies for Flow Cytometry


Antibodies and Isotyping

Choose from an extensive range of antibodies for use in your screening assays or utilize our custom antibody services.

Antibodies by Application
Antibodies by Target Species
HuCAL® Custom Antibody Services
Human Immunoglobulin Isotyping Assays
Immunology Antibodies
Isotype Controls

Additional Methodologies and Research Within Drug Discovery and Development

Biomarker Discovery

Biomarker Discovery
The use of biomarkers across drug discovery and development and into the clinic is key to enabling close monitoring of a drug candidate’s effects. Biomarkers can range from specific molecules such as a protein, a gene sequence, or expressed RNA to physiological parameters such as blood pressure. Biomarkers may be detected in a specific location or tissue or in plasma and other bodily fluids.

Biochemical and Cellular Assays

Biochemical and Cellular Assays
Biochemical and cellular pharmacology teams develop and validate assays to support research across drug discovery and development. These assays range from discovery approaches with high sample throughput to high-content analysis to gain an understanding of biological response both in vitro and in vivo.

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