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® NHR_TRANS and NHR_PRO 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 Name	Protein Interaction
AR	Androgen receptor (AR)	X
ERα	Estrogen receptor 1 (ESR1)	X
FXR	Nuclear receptor subfamily 1, group H, member 4 (NR1H4)	X
GR	Nuclear receptor subfamily 3, group C, member 1 (glucocorticoid receptor) (NR3C1)	X
LXRα	Nuclear receptor subfamily 1, group H, member 3 (Liver X receptor α) (NR1H3)	X
LXRβ	Nuclear receptor subfamily 1, group H, member 2 (Liver X receptor β) (NR1H2)	X
LXRβ-NCoR1	Nuclear receptor subfamily 1, group H, member 2 (Liver X receptor β) (NR1H2)	X
MR	Nuclear receptor subfamily 3, group C, member 2 (Mineralcorticoid receptor) (NR3C2)	X
PPARα	Peroxisome Proliferator Activated Receptor alpha (PPARA)	X
PPARγ	Peroxisome Proliferator Activated Receptor gamma (PPARG)	X
PPARδ	Peroxisome Proliferator Activated Receptor delta (PPARD)	X
PRα	Progesterone receptor α (PGR)	X
PRβ	Progesterone receptor β (PGR)	X
RARα	Retinoic acid receptor, alpha (RARA)	X
RXRα	Retinoid X receptor, alpha (RXRA)	X
RXRγ	Retinoid X receptor, gamma (RXRG)	X
THRα	Thyroid hormone receptor, alpha (THRA)	X
THRβ	Thyroid 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

[

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:

nhrELECT℠ - Personalized Screening & Profiling