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.
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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.
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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.
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 |
| RARβ | Retinoic acid receptor, beta (RARB) | | 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 |