BellBrook labs

Whether you want to screen 2M compounds or perform SAR on 20, you need a robust, reliable biochemical assay that has been optimized for your target.

Leveraging BellBrook’s assay development expertise will save you time and money. Your project will be handled by the same BellBrook scientists who developed the Transcreener assays and have optimized them for more than 100 different enzyme targets, including kinases, ATPase, GTPases, glycosyltransferases, ligases/synthetases, and phosphodiesterases. We will define the exact conditions needed for initial velocity detection of your enzyme with outstanding signal:noise; Z’ values of 0.7 to 0.9 are typical. We will tailor our efforts to meet your specific needs, for example minimizing consumption of limited reagents or enabling simultaneous screening for inhibitors and activators. And we will work fast. If your target enzyme is in good shape, we can generally complete the assay development within two to four weeks.

Assay Development Services Include:

• Target Protein Sourcing/Production – If the target protein is available from the customer or a vendor, we will test it for purity and functional activity; if not, we will produce it using the most efficient and cost effective expression and purification strategy.

• Assay Optimization with Target Protein – We will determine the optimal buffer composition, enzyme concentration, and reaction time and optimize detection reagents to produce the maximal signal under initial velocity conditions

• Assay Validation – Depending on customer needs, validation could include dose responses with control inhibitors, determination of kinetic parameters, pilot screens with targeted libraries, or interference screens.

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
• Residence Time Measurements – determination of koff using ‘jump dilution’ enzymatic assay method
• Mechanism of Action Studies – kinetic analysis to define mode of inhibition
• Inhibitor Selectivity Profiling

BellBrook Labs provides a variety of biochemical assay development and lead discovery services to advance your target into a screen faster and with confidence.

Assay Development Services Include:

• Assay Development – Custom Assay Development
• Target Protein Sourcing/Production
• Assay Optimization with Target Protein
• Assay Validation – Pilot Screens, Interference Screens

Lead Discovery Services Include:

• Inhibitor Screening
• Inhibitor Potency Profiling
• Inhibitor Selectivity Profiling
• Residence Time Measurements
• Mechanism of Action Studies

The Transcreener ADP Kinase Assay is a universal assay platform that relies on the direct detection of ADP to monitor kinase activity. As a homogenous assay, it can be used for high throughput screening. The platform has been validated in millions of wells for drug discovery.

Chose between a variety of services including:

• HTS Compatible Assay Development
• Target Protein Sourcing/Production
• Assay Optimization with Target Protein
• Assay Validation - Pilot Screens, Interference Screens
• Inhibitor Screening, potency and selectivity profiling
• Residence Time Measurements
• Mechanism of Action Studies

Transcreener® ADP2 Assay
Transcreener® UDP2 Assay
Transcreener® GDP Assay
Transcreener® AMP/GMP Detection Assay