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nhrE/IC50ELECT

Quantitate compound potency against any NHRscan functional cell-based assay.  Agonist half maximal effective concentrations (EC50s) and antagonist half maximal inhibitory concentrations (IC50s) are calculated from duplicate 10-point dose-response curves. Measurements are made under optimized conditions to generate consistent and reproducible data that reliably reflects the drug’s potency.

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Platform Highlights and Benefits

  • 10-point dose response curve in duplicate
  • Agonist and antagonist modes available
  • Superior assay windows & robust performance (Z' > 0.6)
  • Broad applications – specificity and compound toxicity/liability
  • Rapid turn around times
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).

 

nhrE/IC50ELECT 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 

What does the term EC50 mean?

The term half maximal effective concentration (EC50) refers to the concentration of a drug or biologic which induces a response halfway between the baseline and the maximum. Therefore, the EC50 of a compound or biologic represents the concentration where 50% of it’s maximal effect can be observed. It is commonly used as a measure of the drug’s potency.

What does an IC50 measure?

The term half maximal inhibitory concentration (EC50) is a measure of the effectiveness of a compound to inhibit a given biological response. Therefore, the IC50 of a compound or biologic represents the half maximal (50%) inhibitory concentration and is commonly used as a measure of antagonist drug’s potency.

How are the EC50/IC50s calculated?

For each compound/GPCR target interaction, dose response curves  are generated using 10 concentrations of agonist or antagonist (10-point curve). The results are reported as EC50/IC50 which derived using the Hill equation:

hill equation