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
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Agonist (Left) and Inverse agonist (Middle) profiling of Estrogen related receptor alpha, ERRα and antagonist profile of glucocorticoid receptor, GR (Right).
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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 |
| 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 |
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:
