Lead Discovery Services

BellBrook scientists will use their extensive biochemistry and enzymology expertise to identify actives from your virtual screen, prioritize your HTS hits, or generate quantitative data to drive your SAR/medicinal chemistry efforts.

We will work closely with you to define the specific parameters that are important for your lead discovery program and implement the most efficient and cost-effective assays and/or kinetic analyses.

Lead Discovery Services Include:

Inhibitor Screening – To identify or confirm activity with the target.
Inhibitor Potency Profiling – Dose-response with target and/or related proteins. Fast IC₅₀ results. Application Note: Inhibitor Dose Response Measurement with the EPIGEN Methyltransferase Assay Kit
Inhibitor Selectivity Profiling
Residence Time Measurements – Determination of k_off using ‘jump dilution’ enzymatic assay method. Application Note: Measuring Kinase Inhibitor Residence Times with the Transcreener® ADP² FP Assay
Mechanism of Action Studies – Kinetic analysis to define the mode of inhibition.

Example Target Families

Protein Kinases
Lipid Kinases
Carbohydrate Kinases
ATPases
Acetyltransferases
HDACs
GTPases, GAPs, GEFs
Phosphodiesterases
Helicases
Ligases/Synthetases
Glycosyltransferases

Featured Autoimmune Targets

Accelerating the Drug Discovery Process

Contact Us to Learn More

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