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

Assay Development Services

Lead Discovery Services

Transcreener Overview

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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.

Assay Development Services

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 & 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 targeted 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

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Lead Discovery Services

Scientists Performing Lead Drug 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 k_off 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.

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

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

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.

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How Do Our Drug Discovery Services Work?

Choose Your Target

Please inquire if you do not see your target. We may have experience with that target or a similar one within an enzyme family. If you want to learn more about a target, click on the target listed below.

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

Example Targets
cGAS	AMPK	WRN Exonuclease
CD73	JAK1	RIPK1
CD39	JAK3	RIPK2
DDX3	EZH2	p97
ENPP1	PKR	KHK
IKK-beta	MAPK8
CD38	ADK
OAS1	TREX1
TBK1	GALNT2
NSP13	GALNT3
NUDT5	PRMT4

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

Send us your compounds. We'll use proven Transcreener Assays 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 full report including the raw data and results of the experiments. We can keep things as simple or complex as you like.

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 more complicated schemes involving coupling enzymes. 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.

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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 assays and have optimized them for more than 100 different enzyme targets, including kinases, ATPase, 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.

Advantage of BellBrook's Drug Discovery Services

Contact Us to Learn More About Drug Discovery Services

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