Nuclear Receptor Profiling -

Services

NHRscan^℠ - Nuclear Hormone Receptor Panel

LeadHunter^® Discovery Services, offers a large menu of cell-based nuclear hormone receptor (NHR) assays to examine the effects of chemicals, drugs and nutrients on nuclear receptor activity. We offer over 20 different cellular assays that monitor receptor activation by either nuclear translocation or NHR co-activator interaction - but without the lengthy compound incubation times inherent with traditional reporter gene assays. Screen compounds against our complete panel of assays or select your own customized group of receptors based on therapeutic relevance (Toxicology, Metabolic Diseases, Endocrinology). Our experienced and highly-qualified service team will provide you the data you need, quickly and without using your own internal resources to allow you to meet your project needs.

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Powered by the PathHunter^® technology, our NHR assays are whole cell, functional assays that measure NHR translocation and NHR-coactivator interaction. Unlike standard reporter gene assays, these assays are chemiluminescent and do not require lengthy 16-24 hour compound incubations making them ideal assays for screening and profiling.

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Panel Highlights and Benefit

Functionally validated cell lines – high quality results every time
High quality, functional data - Accurate, precise and reproducible
Flexible options – either pre-defined panels of personalized assay selection
Agonist and antagonist modes available
Broad applications – specificity and compound toxicity/liability
Rapid data turnaround time

Choose from the following:

Co-Activator Interaction (NHR_PRO) Measure interactions between the NHR and Steroid Receptor Co-activator Peptides (SRCP).		Nuclear Translocation (NHR_TRANS) Measure receptor activity based on translocation of the NHR following ligand stimulation.
How it Works		How it Works

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.

A panel of 76 nuclear receptor ligands were screened against the PPARα, PPARδ, and PPARγ cell lines (Right Panel).

Profiling of known Agonists (Left) and Antagonists (Right) against the PathHunter® NHRTRANS assay showing the expected pharmacology.

Determine Mechanism of Action

LeadHunter Discovery Services can provide you complete characterization of your lead compounds by offering multiple readouts for the same nuclear receptor. Using a combination of translocation and protein-protein interaction assays for the same NHR target, the LeadHunter team will help you study the mechanism of action of your lead compound in order to better predict compound activity in vivo.


The PathHunter GR Nuclear translocation assay shows no inhibition after addition of Mifepristone (B) while the NHR_PRO GR assay shows almost complete inhibition of the Dexamethasone response, indicating that Mifepristone acts on the target of interest by blocking co-activator recruitment.

Flexible Screening & Profiling Options

LeadHunter Discovery Services reduces the time and costs associated with drug discovery. Whether you are interested in full panel screening and profiling, or selecting a subset of assays, we offer the selection and flexibility to support your drug discovery needs.

Overview of NHRscan℠ Panels & Services

Services	Assays	Pre-configured Panel	Customizable?	Turnaround Times*
nhrMAX	19	Yes	No	6 weeks
nhrELECT	26	No	Yes	4 weeks
nhrE/IC50ELECT	26	No	Yes	4 weeks
nhrDUO	5	No	Yes	4 weeks

*For nhrMAX, turnaround time is calculated based on fixed start date of the panel run. Although standard turnaround times for all other services are 4 weeks, express turnaround times of 10 days can also be requested.

nhrMAX

19 Assays - the most comprehensive panel of functional NHR assays

A comprehensive panel of 19 NHR protein-interaction assays to measure steroid cofactor recruitment to the NHR being tested. Broad applications including specificity & compound liability.

nhrELECT

A flexible approach to personalized screening

A flexible approach to personalized nuclear receptor profiling. Select from our collection of 26 NHR assays to create a customized assay panel of any size using only of NHRs relevant to your programs.

nhrE/IC50ELECT

Quantitative binding affinity of compound-NHR interactions

Quantitative affinity measurement (10-point dose-response curve, performed in duplicate) against any NHR assay. Measurements are made under optimized conditions and can be determined for any NHR/compound combination.

nhrDUO

Multiple functional readouts for the same receptor

Ideal tool for studying compound action by comparing pharmacology of the same NHR target using both protein interaction (NHR_PRO) and translocation (NHR_TRANS) readouts.

NHRscan℠ Assay List

Listed below are the cell-based NHR targets available for screening and profiling. Assays in the table may be sorted by column name.

Target Gene ▲	Common Name	Nuclear Translocation	Protein Interaction
AR	Androgen receptor (AR)	X	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	X
LXRα	Nuclear receptor subfamily 1, group H, member 3 (Liver X receptor α) (NR1H3)	X	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	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	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

NHRscan℠ - Nuclear Hormone Receptor Panel