Drug Discovery Services Offered By BellBrook Labs

BellBrook’s drug discovery services specialize in small molecule modulators for enzyme drug targets. We have conducted assay development & lead discovery for over 15 years. Our experts work diligently with varieties of customers in early-stage drug discovery programs. From assay development to lead discovery, we provide quality data to accelerate programs.

Lead Discovery Services Graphic

Assay Development Services Include

  • Target Protein Sourcing/Production

    If the target protein is available from the customer or 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 & optimize detection reagents to produce 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 target libraries, or interference screens.

Accelerate drug discovery without adding headcount. In today’s lean biotech environment, timelines are tight and budgets tighter—yet the pressure to move faster never stops. BellBrook Labs plugs into your workflow with assay development, screening, and hit-to-lead services built for speed, scientific rigor, and clear go/no-go decisions.

Example Assay Optimization with Human cGAS

BellBrook scientists performed a detection of purified, full-length human cGAS with the Transcreener cGAMP FP Assay. Linear response is shown from polarization data converted to cGAMP using a standard curve.

Human cGAS Enzyme Titration

Assay Development Services cGAS Titration

Linear Response Curve

cGAS Assay Linear Reponse Curve

Lead Discovery Services

  • Inhibitor Screening

    To identify or confirm activity with the target.

  • Inhibitor Potency Profiling

    Dose-response with target and/or related proteins. Fast IC50 results.

  • Inhibitor Selectivity Profiling
  • Residence Time Measurements

    Determination of koff using ‘jump dilution’ enzymatic assay method.

  • 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.

  • Evaluate Compound-Target Binding

    Run thermal shift assays to confirm compound-target engagement via shifts in melting temperature.

Scientists Performing Lead Drug Discovery Services

Example Inhibitor Screening & Profiling With Human cGAS

BellBrook scientists performed an inhibitor screening & inhibitor potency profiling of cGAS using the Transcreener cGAMP cGAS Assay.

Inhibitor Screening

Pilot cGAMP Assay Pilot Screen

Shown above is a screen of 1600 compounds. cGAS was used at 10 nM, compounds were at 10 μM. Z = 0.62, Z’ = 0.7 illustrate a robust screening assay. Hits were determined to be anything outside three standard deviations from the mean.

Inhibitor Potency Profiling

IC50 of cGAS Inhibitor

Confirmation of a screening hit using the Transcreener cGAMP cGAS Assay in the FP format. Follow-up assays to triage screening hits can be used to select bona fide inhibitors for advancement into medicinal chemistry/SAR.

How Do Our Drug Discovery Services Work?

  • 1

    Choose Your Target

    If you don’t see your target listed below, please inquire. We are developing assays for new targets all the time. We may have experience with that target or a similar one within an enzyme family. Click on a target below to learn more.

  • 2

    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 program.

  • 3

    We’ll Do The Work

    We’ll develop an HTS-ready assay using a proven Transcreener technique to measure enzymatic activity. Assays will be performed in a timely manner at our lab in Madison, WI.

  • 4

    Quickly Provide a Report & Support

    We’ll provide a report including the raw data and results of the experiments. We can keep things as simple or complex as you like, and provide protocol ready for HTS and hit-to-lead.

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

Transcreener® HTS Assay Overview For Drug Discovery Services

BellBrook’s Transcreener® HTS assay platform is ideally suited for the detailed biochemical and kinetic analyses required for hit-to-lead programs. Transcreener® is an extensively validated HTS platform that produces robust FP, TR-FRET, and FI signals for nucleotides produced by enzymes; e.g. ADP for kinases. It has been used to screen tens of millions of wells over the last 10 years in pharma and biotech labs.

Transcreener Overview for Drug Discovery Services

Because they use direct immunodetection of nucleotides, Transcreener® assays can provide more reliable results than alternative methods that rely on complicated assay schemes. In addition, the ability to run Transcreener® assays in continuous mode enables analysis of inhibitor binding kinetics, such as residence time, which is increasingly recognized as an important factor for drug efficacy. For our services, additional assay methods will be employed as needed to meet customer requirements.

Why Choose BellBrook Labs to Accelerate Your Program?

Leveraging BellBrook’s services expertise will save you time and money. Your project will be handled by the same BellBrook scientists who developed the Transcreener assay and have optimized them for more than 100 different enzymes, including kinases, ATPases, GTPases, glycosyltransferases, ligases/synthetases, and phosphodiesterases. 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 services within two to four weeks.

“The assay itself has good reproducibility and provides a clear readout on our enzyme activity. The most important piece, however, is the level of attention to our project and rapid turnaround time. The staff at BellBrook Know what they are doing.”

“The ADP assay is a great choice for measuring activity for any ADP-generating enzyme in both real time and endpoint formats. The universal detection system has been very useful for more challenging targets.”

“Excellent blend of simplicity & good science. Excellent technical support”

Resources

Find the right resources to help you get to your solution faster.

Contact Us to Learn More About Drug Discovery Services

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Frequently Asked Questions

BellBrook delivers a comprehensive suite of drug discovery services driven by decades of enzymology experience:

  • Biochemical Assay Development Services

  • Lead Discovery Services

  • Specialized profiling offerings: ATPase, GTPase, Helicase, cGAS/STING, and Thermal Shift Assays

  • We specialize in small-molecule modulators for enzyme drug targets, with nearly two decades of experience in assay development and lead discovery.

  • Our core detection platform is Transcreener® HTS technology, recognized for robust detection of nucleotides (e.g., ADP, GDP) via FP, FI, or TR-FRET, with high reproducibility and minimal compound interference.

  • Choose Your Target – Even if your target isn’t listed, we likely have experience or can develop a tailored solution.

  • Consult with a Scientist – Discuss your goals, timelines, and dataset needs in detail.

  • We Execute the Work – In our Madison, WI lab, we develop HTS-ready assays using proven Transcreener techniques.

  • Report & Support – You’ll receive raw data, analysis, and ready-to-use HTS/hit-to-lead protocols.

  • Assay Development – Includes target protein handling, optimization of buffers and conditions, and validation through dose-response, kinetic, or interference screens.

  • Lead Discovery – Services such as inhibitor screening, potency and selectivity profiling, residence time measurement, mechanism-of-action studies, triage of non-stoichiometric inhibitors, and compound-binding verification via thermal shift assays.

  • Target-Specific Profiling – Including ATPase, GTPase, helicase, and cGAS/STING profiling—each using tailored assay formats and real-time collaboration.

  • Expertise in Enzymology – Our team includes the very scientists who developed Transcreener technology, optimizing assays for over 100 enzyme targets.

  • Speed – Rapid project turnaround—many assays are completed within 2 to 4 weeks if enzymes are well-prepared.

  • Proven Platform – Transcreener is a mature, widely-adopted HTS platform, trusted across pharma and biotech.

  • Customized Service – Tailored workflows, minimized reagent usage, and direct scientific collaboration ensure efficiency and precision.

  • Real-World Testimonials – Clients highlight reproducibility, technical support, and quick turnaround as standout strengths

BellBrook supports a broad range of enzyme classes, including:

  • Protein kinases, lipid/metabolic kinases

  • Acetyltransferases, HDACs

  • GTPases/GAPs/GEFs

  • ATPases, phosphodiesterases, helicases

  • Nucleotidases, ligases/synthetases, glycosyltransferases

  • Examples: cGAS, TREX1, ENPP1, CD73, OAS1, PLK1, VPS4A, PARG, POLQ, PARP, SIRT
  • Mix-and-Read Format – Simple, homogeneous assays without complex coupling steps.

  • Direct Nucleotide Detection – Reduces interference and improves data clarity.

  • Broad Applicability – Robust detection across thousands of enzyme targets with FP, FI, and TR-FRET formats.

  • Continuous/Kinetic Capability – Supports analysis like residence time that’s critical for pharmacological relevance.