GeneBLAzer® Validated Assays for Nuclear Receptors (NRs) provide you with a reliable, rapid, and sensitive method for analyzing the intracellular status of NRs upon exposure to drug candidates or other stimuli. These functional assays allow for measurement of receptor activation or inhibition by compounds and can be used to determine compound potency and selectivity.

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All GeneBLAzer® Validated Assays provide superior response profiles as a result of response element optimization and use of optimal clones. GeneBLAzer® Validated Assays for NRs:
  • Provide ready-to-screen, ratiometric assays for disease relevant NR targets
  • Are functionally validated to ensure high-quality results each and every time
  • Can be designed with your desired target and cell line through our Custom Assay Services program.

GeneBLAzer® Validated Assays for NRs are tested and documented to show a high level of performance. These assays are shown to meet the following specifications:
  • Z’-factor of >0.6
  • Appropriate EC50 responses to known agonists and antagonists
  • Mycoplasma negative
  • DMSO tolerance up to 1%
  • Optimized stimulation time, cell density, and substrate loading times

GeneBLAzer® Validated Assays for Nuclear Receptors Mechanism of Action

 GeneBLAzer Validated Assays

GeneBLAzer® Nuclear Receptor Assays use a β-lactamase cDNA under transcriptional control of an Upstream Activator Sequence (UAS). The UAS is activated by the GAL4 transcription factor (DNA binding domain), which is expressed as a fusion protein with the target receptor ligand binding domain. Upon ligand binding, the GAL4(DBD)-NR(LBD) fusion protein translocates to the nucleus, where it binds to the UAS which controls transcription of β-lactamase.

GeneBLAzer® Validated Assays for Nuclear Receptors Select Validation Data

Dose response curves for a panel of known agonists are shown in the GeneBLAzer® ERB Assay. The rank order of potency of these agonists is consistent with known literature values.
 GeneBLAzer Known Agonists
Dose response curves of a panel of partial agonist/antagonist compounds are shown in the ERB Assay, and the results are consistent with known literature values. These compounds are partial agonists as well as antagonists for Era, but only antagonists for ERB. For antagonist mode, cells were tested in the presence of EC80 amounts of estradiol.
GeneBLAzer Partial Agonist Antagonist