Custom, Quick, and Accurate Profiling Services for Helicase Targets

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 ADP2 Assay is an extensively validated technology that has been used in millions of wells by large pharma. It is based on a novel direct ADP detection method that reduces compound interference and the risk of false positives in a screen.

Heliscreener RNA Unwinding Assay is designed to measure the unwinding activity of RNA Helicases. Either or both assays can be performed for screening or Hit-to-Lead campaigns.

  • 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 ATP or effector concentrations
  • Fast results - we process your data individually as soon as we receive your compounds (no waiting until the end of the month)
  • Data results from the extensively validated Transcreener assay technology that is highly specific and robust

Interested in our helicase profiling services? Contact a BellBrook Scientist:

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Helicase Targets

Helicase 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.

Inhibitor Screening for Helicase Enzyme Targets – ATP Hydrolysis

Examples of Dose Response Curves using Transcreener’s ADP Assay.

DDX1

DDX1 Dose Response Curve

IC50 = 0.34 µM

DDX3

DDX3 Dose Response Curve for Helicase Profiling

IC50 = 6.36 µM

DDX5

DDX5 Dose Response Curve Helicase Profiling

IC50 = 0.12 µM

DDX17

DDX17 Dose Response Curve with L-798106

IC50 = 171.5 µM

WRN

Dose Response Data With WRN Helicase Assay

IC50 = 0.03 µM

POLQ

POLQ Dose Response Curve for Helicase Profiling

IC50 = 0.92 µM

RIG-I

RIG-I Dose Response with BVT 948 Only

IC50 = 3.56 µM

MDA5

MDA5 Dose Response Curve with Suramin Only

IC50 = 0.34 µM

Inhibitor Screening for Helicase Enzyme Targets – RNA Unwinding

Examples of Dose Response Curves using the Heliscreener RNA Unwinding Assay.

DDX3

DDX3 DRC with SPP-86 using Heliscreener

IC50 = 0.178 µM

DDX5

DDX5 DRC with SPP-86 using Heliscreener

IC50 = 1.43 µM

DHX9

DHX9 DRC with SPP-86 using Heliscreener

IC50 = 49.13 µM

DDX17

DDX17 DRC with SPP-86 using Heliscreener

IC50 = 1.62 µM

How Do Our Helicase Profiling Services Work?

  • 1

    Choose a Helicase Target

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

  • 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

    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.

  • 4

    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.

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.

“Some CROs reserve their best teams for high profile customers. If you’re not right there with them you get less experienced teams… BellBrook understands enzyme kinetics, so it made that part of the project so much easier. The larger CRO didn’t seem to have the expertise we needed in this area.”

“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”

“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 Transcreener AMP/GMP Assay is extremely straightforward to use and is very sensitive. In a UV-based enzyme assay I needed 1 µM enzyme to see a decent signal; however using the Transcreener AMP assay I only need 10 nM. Also, BellBrook Labs have been very helpful with the assay development. Their representative has been very willing to quickly help me get my assay up and running.”

“Through the process of developing and validating an assay for HTS applications, I generated a very nice data package of robust high quality data.”

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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