Every PolarScreen™ Competitive Binding Assay for Nuclear Receptors includes protein, a proprietary fluorescent Fluormone™ ligand, and an optimized buffer system. When the NR binds to the Fluormone™ ligand, the resulting complex yields a high polarization value. If the test compound displaces the Fluormone™ ligand from the complex, the polarization value is lowered. Since this occurs only in the presence of a test compound, the shift in polarization value enables you to accurately and conveniently determine relative affinity of a test compound for the NR.

   
Figure 1. Fluormone™ ligands are biologically relevant steroid derivatives, designed to achieve nanomolar binding affinities and robust Z’-factors. Development of these Fluormone™ ligands required expert chemistry and manipulation of buffer composition. Assay are optimized for maximum stability of instrumentation platforms, and to tolerate solvents typically found in compound libraries.

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PolarScreen™ Nuclear Receptor Competitive Binding Assays Screening Data

  
Figure 2. Competition data using the AR Competitor Assay, Green, generated on a 384-well plate. The concentration of the test compound that results in a half-maximal shift in polarization value equals the IC50 of the test compound, which is a measure of the relative affinity of the test compound for the androgen receptor ligand binding domain.
   
 
Figure 3. A subset of the Prestwick Bioactive Compound Library (bar code: 28151401), rich in nuclear receptor ligands was screened at 10 µM in the AR Competitor Assay, Green. Approximately 10% of the compounds were identified as hits because they displaced the Fluormone™ AL Green tracer from ARLBD (His-GST), and 1% of the library exhibited interfering compound fluorescence.

 

 

 

 

Ordering Information

Sku Name Size Price Qty
P2893 PolarScreen™ Glucocorticoid Receptor Competitor Assay Kit, Red 100 x 100 µL assays USD 814.00
P2816 PolarScreen™ Glucocorticoid Receptor Competitor Assay Kit, Green 100 x 100 µL assays USD 760.00
P2895 PolarScreen™ Progesterone Receptor Competitor Assay Kit, Green 100 x 100 µL assays USD 760.00
P2614 PolarScreen™ ER Alpha Competitor Assay, Green 10,000 assays USD 5,760.00
P2615 PolarScreen™ ERbeta; Competitor Assay, Green 2,000 x 100 µL assays USD 5,760.00
P2698 PolarScreen™ ER Alpha Competitor Assay, Green 2,500 assays USD 1,776.00
P2962 PolarScreen™ Progesterone Receptor Competitor Assay Kit, Red 100 x 100 µL assays USD 814.00
P3018 PolarScreen™ Androgen Receptor Competitor Assay Kit, Green 400 x 40 µL assays USD 1,254.00
PV4569 PolarScreen™ VDR Competitor Assay, Red 400 x 40 µL USD 1,306.00
PV4293 PolarScreen™ Androgen Receptor Competitor Assay Kit, Red 400 x 40 µL assays USD 1,306.00
PV6136 PolarScreen™ PPARγ-Competitor Assay Kit, Green 400 x 40 µL assays USD 1,254.00

For research use only. Not intended for any animal or human therapeutic or diagnostic use.