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

Target HGNC symbol Synonyms Data
AR AR Androgen receptor, AIS, NR3C4, SMAX1, HUMARA Data sheet
FXR NR1H4 Farnesoid X receptor, RIP14, HRR1, HRR-1
PXR NR1I2 Pregnane X receptor, steroid and xenobiotic sensing nuclear receptor (SXR) Data sheet

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

Assay Details

Assay setup

Setups: IC50 value determination in an 8-dose duplicate assay format. Free choice for screening of the kinase targets of your choice. New target development/validation is available upon request.

Controls: We use DMSO as a negative control. In every project, testing of a standard reference compound is included in IC50 assay format as well.

Turnaround time: We strive to complete your project within 2-3 weeks. Expedited scheduling and data delivery can be arranged prior to study commencement.

Report: A detailed report including assay conditions and comprehensive evaluation of data as well as raw data for each analysis will be provided.

Screening location: Malvern, PA, USA

Compound requirements: In brief, 50 to 100 µl of a 10 to 50 mM DMSO stock or 2-3 mg solid material is needed. Please refer to our FAQs for information regarding compound preparation and shipping.