Our LanthaScreen Nuclear Receptor Competitive Binding Assay contains all the needed reagents you need to conduct compound affinity testing:
The nuclear receptor (NR) protein is indirectly labeled with terbium via the anti-GST antibody bound to the GST tag on the receptor. When this labeled protein binds to the Fluormone™ ligand, a high TR-FRET ratio will result. If a test compound that binds to the NR protein is added to the reaction, the test compound will compete with the Fluormone™ ligand, resulting in a lower TR-FRET ratio. Since the change in TR-FRET ratio only occurs in the presence of a competitor, it can be used as a convenient and accurate indicator of the relative affinity of the test compound for the NR (Figure 1 below).
Figure 1. Assay schematic of a Nuclear Receptor LanthaScreen®
|Target||Alias(es)||Accession number||LanthaScreen® Competitive Binding Assay (TR-FRET)|
|Estrogen receptor alpha||ER Alpha, ERA, ESR1, NR3A1||NP_000116.2||A15887|
|Estrogen receptor beta||ER Beta, ERB, ESR2, NR3A2||NP_001428.1||A15895|
|Glucocorticoid receptor||GR, GCCR, GCR, NR3C1||NP_000167||A15901|
|Peroxisome proliferator-activated receptor alpha||PPAR Alpha, PPARA, NR1C1||NP_005027||PV4892|
|Peroxisome proliferator-activated receptor delta||PPAR Delta, PPARD, NR1C2||NP_006229||PV4893|
|Peroxisome proliferator-activated receptor gamma||PPAR Gamma, PPARG, NR1C3||NP_005028||PV4894|
|Pregnane X receptor||PXR(SXR), NR1I2||NP_003880.3||PV4839|
For Research Use Only. Not for use in diagnostic procedures.