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nhrMAX - Nuclear Hormone Receptor Assay Panel

nhrMAX is a comprehensive panel of validated cell-based nuclear hormone receptor (NHR) assays that allows for rapid, reliable and sensitive measurements of NHR activation or inhibition following compound treatment. nhrMAX utilizes our proprietary protein-interaction technology to measure steroid cofactor recruitment to the NHR being tested. This approach provides a direct readout of nuclear receptor activation and can be used to determine compound potency and selectivity with minimal off-target effects common with traditional reporter gene assays.

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Panel Features & Benefits

  • Comprehensive menu of 19 validated cell based assays
  • Single assay readout for easy comparison across all targets
  • All cell lines functionally validated to ensure high-quality results every time
  • Broad applications – specificity and compound toxicity/liability
  • Agonist and antagonist modes available
  • Regularly scheduled panel dates
  • Multiple targets available in alternate format for confirmation studies
How it Works

Assay Performance

The nhrMAX panel can be used to identify a specific ligand interaction with a receptor based on the interaction between the NHR and Steroid Receptor Coactivator Peptides (SRCP). The assay is ideal for novel inhibitor screening and pre-toxicity analysis.

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.

ERα NHRPRO Assay

NHR_pro_assay_format_PathHunter-(1).png NHR_PathHunterScreenProfile.png
Profiling of known ligands of the ERα Receptor showing the expected pharmacology in the PathHunter® NHRPRO assay format (Left Panel). A panel of 76 nuclear receptor ligands were screened against the PPARα, PPARδ, and PPARγ cell lines (Right Panel).

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.


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


 

nhrMAX 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

To ensure your compounds are included in the Test Date of your choosing, submit your compounds and PO by the date indicated in the "Compounds & PO Due" column below.

2017 gpcrMAX and orphanMAX Panel Run Schedule

Panel Test Dates Compounds & PO Due Report & Invoicing
gpcrMAX,
orphanMAX
January 31 January 27 February 28
March 14 March 10 April 11
April 25 April 21 May 23
June 6 June 2 July 4
July 18 July 14 August 15
August 29 August 25 September 26
October 10 October 6 November 7
November 28 November 22 December 26
 

2017 nhrMAX, tkMAX, and pathMAX Panel Run Schedule

Panel Test Dates Compounds & PO Due Report & Invoicing

nhrMAX,
tkMAX, pathMAX

February 14 February 10 March 14
March 28 March 24 April 25
May 9 May 5 June 6
June 20 June 16 July 18
August 1 July 28 August 29
September 12 September 8 October 10
October 24 October 20 November 21