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 target
Inhibitor Potency Profiling – dose response with target and/or related proteins
Application Note: Inhibitor Dose Response Measurement with the EPIGEN Methyltransferase Assay Kit
Residence Time Measurements – determination of koff 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 mode of inhibition
Inhibitor Selectivity Profiling

Example Targets:

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

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.

Lead Discovery Services Include:

Example Targets:

Accelerating the Drug Discovery Process