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nhrELECT - Personalized Screening & Profiling

Customized screening and profiling against select nuclear hormone receptors. Choose from our collection of over 20 whole cell, functional assays that measure receptor activity by monitoring NHR translocation or NHR-coactivator interactions. This simple, fast and cost-effective alternative to in house screening and profiling is a direct, non imaging approach that results in fewer off target liabilities compared to traditional reporter assays that has multiple applications including compound specificity and  toxicity studies.

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Panel Features & Benefits

  • Customized screening and profiling - choose from >20 functional NHR assays
  • Multiple assay readouts - nuclear translocation and NHR co-activator interaction
  • Agonist, antagonist, inverse agonist, allosteric modulator modes available
  • High quality reproducible data – superior assay windows & robust performance (Z' > 0.6)
  • Broad applications – specificity and compound toxicity/liability
How it Works

Assay Performance

Ideal for Screening and Profiling

The simplicity and versatility of the PathHunter® NHRTRANS and NHRPRO assays make these assays ideal for screening and profiling to look for agonists, antagonists, inverse agonists.

Profiling of Functional, Cell-Based Nuclear Hormone Receptors

               ERRα                                   ERRα                                   GR    
        Agonist Mode             Inverse Agonist Mode          Antagonist Mode

Agonist (Left) and Inverse agonist (Middle) profiling of Estrogen related receptor alpha, ERRα and antagonist profile of glucocorticoid receptor, GR (Right).


A panel of 76 nuclear receptor ligands were screened against the PathHunter® PPARα, PPARδ, and PPARγ cell lines .
 

nhrELECT Assay Panel

Listed below are the assays currently available for screening and profiling.

 
Target Gene ▲Common NameProtein Interaction
ARAndrogen receptor (AR)X
ERαEstrogen receptor 1 (ESR1)X
FXRNuclear receptor subfamily 1, group H, member 4 (NR1H4)X
GRNuclear receptor subfamily 3, group C, member 1 (glucocorticoid receptor) (NR3C1)X
LXRαNuclear receptor subfamily 1, group H, member 3 (Liver X receptor α) (NR1H3)X
LXRβNuclear receptor subfamily 1, group H, member 2 (Liver X receptor β) (NR1H2)X
LXRβ-NCoR1Nuclear receptor subfamily 1, group H, member 2 (Liver X receptor β) (NR1H2)X
MRNuclear receptor subfamily 3, group C, member 2 (Mineralcorticoid receptor) (NR3C2)X
PPARαPeroxisome Proliferator Activated Receptor alpha (PPARA)X
PPARγPeroxisome Proliferator Activated Receptor gamma (PPARG)X
PPARδPeroxisome Proliferator Activated Receptor delta (PPARD)X
PRαProgesterone receptor α (PGR)X
PRβProgesterone receptor β (PGR)X
RARαRetinoic acid receptor, alpha (RARA)X
RARβRetinoic acid receptor, beta (RARB)X
RXRαRetinoid X receptor, alpha (RXRA)X
RXRγRetinoid X receptor, gamma (RXRG)X
THRαThyroid hormone receptor, alpha (THRA)X
THRβThyroid hormone receptor, beta (THRB)X

Data Analysis & Interpretation 

Definitions

Percent Activity/Inhibition

The results for single concentration (primary screen) for tested compound(s) are reported in your study report and spreadsheets as '% Activity' or '% Inhibition' and are calculated in the following manner:
 

% Activity
(Agonist Mode) =
100% x
[
Mean RLU (test sample)- Mean RLU(vehicle control)

Mean MAX RLU (control ligand)- Mean RLU (vehicle control)
]
 

test sample = client supplied compound
vehicle control = DMSO (0% activity)
control ligand = control compound (100% activity)

 

% Inhibition
(Antagonist mode) =
100% x
[ 1- 
Mean RLU (test sample)- Mean RLU(vehicle control)

Mean MAX RLU (control ligand)- Mean RLU (vehicle control)
]
 

test sample = client supplied compound
vehicle control = DMSO (0% activity)
EC80 control = control compound (80% activity) 

 

Dose Response Curve (EC50/IC50)

The results for 10-point dose response curve compound/target interactions are reported in the study report and spreadsheets as EC50/IC50, which are values derived using the Hill equation:

hill equation