Nuclear Receptor Assays
Target-specific Assays

Nuclear Receptor Assay Services

Nuclear receptors are transcription factors that are regulated by small hydrophobic ligands such as hormones or vitamins. Upon ligand binding, nuclear receptors translocate into the nucleus to bind DNA and modulate the expression of their target genes to regulate a variety of cellular mechanisms such as growth, proliferation, metabolism, or homeostasis on a transcriptional level. Nuclear receptors are successfully targeted in the clinic to treat, for example, cancer, cardiovascular or autoimmune diseases.

Reaction Biology offers a suite of assays to support the discovery of new drugs to modulate nuclear receptors with the following advantages:

  • Cell-based assays allow for drug testing in the physiological and complex environment of intact cells
  • Our luciferase reporter assay format measures the activity of the nuclear receptors on the target gene expression, therefore, a large variety of drugs can be tested such as modulators of translocation, activity, structural changes, dimerization, etc.
  • We offer low and large scale drug screening

List of Targets

Further nuclear receptor assays can be setup immediately upon request. Please inquire.

Nuclear Receptor Assay Details

  • Assay Setup
Assay Setup

Setups: Single-dose screening in duplicates or IC50 value determination with 10 concentrations. Other screening formats are available upon request.

Controls: No inhibitor (DMSO vehicle) control and for every assay, one target-specific control compound is tested in 10-dose IC50 format.

Turnaround time: 10-15 business days for standard projects. Expedited scheduling and data delivery can be arranged prior to the commencement of the studies.

Report: The raw data, % enzyme activity and control compound IC50 values will be reported in Excel format for single-dose assays. For IC50 orders, raw data, IC50 values, and curve fitting will be delivered in Excel format. Assay conditions, target, and substrate information are available upon request. Requirements for this information should be noted prior to the commencement of the study.

Screening facility: This assay is performed at our screening facility in Malvern, PA, US.

Compound requirements: In brief, for a standard project, 100 µl of a 10 mM DMSO stock or 2-3 mg of solid material is needed. Less material is needed for large-scale screening. Please refer to our FAQs for information regarding compound preparation and shipping.