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cGAS/STING Profiling Services

Profiling for several cGAS/STING pathway targets using our trusted Transcreener Assay technology. Work with expert scientists who have developed and optimized Transcreener assays for more than 100 different enzymes.

  • Customizable Assay Conditions
  • Quick Turnaround Times!
  • Accurate Results with Proven Technology
  • Direct Collaboration with Real Scientists

BellBrook Labs is a small, custom shop. We are able to customize assay conditions as needed to suit a project's requirements and run compounds as soon as we receive them here in our lab in Madison, WI, providing faster results for your program. The best part - you will collaborate directly with a BellBrook scientist, who are experts in biochemistry and enzymology. 

Our Transcreener Assay is an extensively validated technology that has been used in millions of wells by large pharma. It is based on a novel direct detection method that reduces compound interference and the risk of false positives in a screen.

  • Compounds can be tested at a single concentration or in dose-response mode for the determination of IC50 values
  • Assay conditions can be customized to meet customer needs, e.g., saturating or non-saturating substrate or effector concentrations
  • Better understand off-target effects of your small molecule
  • Data results from the extensively validated Transcreener assay technology that is highly specific and robust
  • Assay conditions can be customized to meet customer needs, e.g., saturating or non-saturating substrate or effector concentrations

Interested in our cGAS/STING profiling services? Contact a BellBrook Scientist:

cGAS/STING Targets

cGAS/STING profiling is available for the enzyme targets listed in the table below. Click on a target to learn more. We continue to develop assays for new helicase targets all the time. If you don't see your target listed, please inquire. We may still have experience with that target and can develop an assay that will advance your program needs.

Example Targets
Click Me ArrowcGAS
Click Me ArrowENPP1
Click Me ArrowTREX1
Click Me ArrowIKKβ
Click Me ArrowTBK1
Click Me ArrowOAS1

Inhibitor Screening for cGAS/STING Pathway Targets

Identify or confirm activity with the target. We can perform single-dose screens as well as multi-dose screening. Screening size can be with our library or yours and range from 100 to 100,000 compounds.

TREX1 Pilot Screen

TREX1 Pilot Screen Data

Example screen with 3056 compounds from the Enamine Discovery Diversity set. A total of 15 potential inhibitors were identified with polarization values ≥ 3 standard deviations above the mean. Z = 0.88 illustrate a robust screening assay.

Hits can then be assayed in dose-response mode for hit confirmation and follow-up SAR.

Follow-up Inhibitor Potency Profiling

Dose-response with target and/or related proteins. We run dose-response assays quickly with the validated Transcreener suite of assays.

Confirmation of a screening hit using the Transcreener dAMP Exonuclease FP Assay. The control compound, Suramin, had an IC50 = 3.0 µM

Follow-up assays to triage screening hits can be used to selective bonafide inhibitors for advancement into medicinal chemistry/SAR.

TREX1 Dose Response Curve

Trex1 dose-response curves v3

Inhibitor Selectivity Profiling

Better understand off-target effects of your compound.

Selectivity Profiling Against TREX2

Inhibitior Selectivity Profiling for TREX1

Transcreener Assays allows selectivity profiling against other enzymes. Here, our scientists used the Transcreener dAMP Exonuclease Assay to selectivity profile versus TREX2.

Both compounds are more than 50-fold less potent for TREX2, while Suramin, a positive control, inhibits TREX1 and TREX2 at similar IC50 (3.0 µM for TREX1 and 3.5 µM for TREX2).

How Do Our cGAS/STING Profiling Services Work?

Choose a cGAS/STING Target

Services are available for customers interested in a single or multiple target(s). If you don't see your target listed, please inquire. We are developing assays for new targets all the time. 

Example Targets
Click Me ArrowcGAS
Click Me ArrowENPP1
Click Me ArrowTREX1
Click Me ArrowIKKβ
Click Me ArrowTBK1
Click Me ArrowOAS1

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.

Application Note Preview Image

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 helicases, 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 listed here, we can generally complete the services within one to two weeks. 

Advantage of BellBrook's Drug Discovery Services

Contact a BellBrook Scientist

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.

Related Resources

Interconnections Between the DNA Damage Response and Innate Immunity

There is extensive crosstalk between the DNA damage response (DDR) pathways and innate immune pathways. Both the individual pathways and the interconnections between them are a focus for exciting new small molecule drug therapeutics that target cancers and debilitating autoimmune disorders. The Transcreener HTS Assay platform accelerates these efforts by providing a robust and easy-to-use biochemical assay to measure activity of key enzymes in the innate immune and DDR pathway.

In this guide, we provide an overview of the DDR and innate immune pathway, and describe Transcreener Assays and Assay Systems for key therapeutic targets. The enzyme targets discussed include:

DDR

  • POLQ
  • WRN
  • PARP1
  • PARG
  • DNA PK

Innate Immunity

  • cGAS
  • TREX1
  • TBK1
  • IKKβ
  • IRAK4
  • ENPP1
  • CD38
  • OAS-1
  • RIG-I/MDA5
  • DDX3
  • CD39
  • CD73
DNA Damage Response and Innate Immunity Preview
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