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.
Triaging Non-Stoichiometric Inhibitors – Run assays under different conditions such as varying detergent and enzyme concentrations.

How It Works

Choose Your Target

If you don't see your target listed below, please inquire. We may have experience with that target or a similar one within an enzyme family. Click on a target below to learn more.

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

Featured Targets
cGAS
CD73
CD39
ENPP1
IKK-beta
TBK1
AMPK
EZH2
JAK1
JAK3
OAS1

Talk To A Scientist

Let's talk science. We'd like to learn more about your target, your goals, and how we can accelerate your lead discovery. We are flexible with differing substrate concentrations e.g., ATP for kinases.

We'll Do The Work

Send us your compounds. We'll use proven Transcreener Assays to measure enzyme activity. These measurements can be used to determine IC₅₀ values, measure residence time, mechanism of action studies, triage non-stoichiometric inhibitors, and more. Assays will be performed at our lab in Madison, WI.

Quickly Provide a Report & Support

We'll provide a full report including the raw data and results of the experiments. We can keep things as simple or complex as you like.

Contact Us to Learn More

Please fill out the form below. We will respond quickly to get the conversation moving and learn how we can help. We keep things discrete, confidential, and professional.

See Examples of Assay Validation, Triaging NSIs, Compound Profiling, MOA, and Measuring Residence Time With Transcreener Assays in This Poster from BellBrook Labs

Download the Poster

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.