Learn More About BellBrook's Assay Development & Lead Discovery Services

Assay Development Services Offered By BellBrook Labs

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

Drug Discovery Process

Assay Development Services

Scientists Performing Assay Development Services
  • Target Protein Sourcing/Production - If the target protein is available from the customer or vendor, we will test it for 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 parameteres, pilot screens with target libraries or interference screens.

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

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

Screen of 1600 compounds. cGAS was used at 10 nM, compounds at 10 μM. Z = 0.62, Z' = 0.7 illustrate a robust screening assay. Hits were determined to be anything outside of 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 selective bonafide inhibitors for advancement into medicinal chemistry/SAR. 

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. 

Example Target Families
Protein Kinases
Lipid Kinases
Carbohydrate Kinases
GTPases, GAPs, GEFs

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. 

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. 

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.

Download Our App Note

Case Study Demonstrating BellBrook's Assay Services

Case Study Assay Development Services

"A Biotech company working on a new pipeline is interested in an assay to screen their novel drug target. They have just completed a virtual screen with their AI technology and had a few hundred hits that seem promising. Now they needed help to determine if these hits were real. They understand screening but don’t have the internal capabilities to run assays and perform follow-up triaging such as dose-response curves. The Biotech needed a partner whose biochemical assay and enzymology experience could help push their program forward from virtual hits through hit-to-lead. They found out about BellBrook Labs through a web search for the target and left a message through the website."...

Download the case study to learn how BellBrook Labs developed a solution for this company.

Transcreener® HTS Assay Overview For Assay Development 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. 

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 Transcreeer 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.  

Contact Us to Learn More About Assay Development Services

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