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.
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.
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.
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.
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.
Better understand off-target effects of your compound.
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).
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.
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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:
POLQ
WRN
PARP1
PARG
DNA PK
cGAS
TREX1
TBK1
IKKβ
IRAK4
ENPP1
CD38
OAS-1
RIG-I/MDA5
DDX3
CD39
CD73
Enter your contact info and learn more about The DNA Damage Response and Innate Immunity.
Find the right resources to help you get to your solution faster.
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.
BellBrook Labs
1232 Fourier Drive, Suite 115
Madison, Wisconsin 53717 USA
(608) 443-2400
info@bellbrooklabs.com
