Table 1. A summary of the KD data calculated for GR01 and GR02.
| Ligand | huGR | huAR | huPR | huER | huMR | msGR | rtGR |
|---|---|---|---|---|---|---|---|
| Ref. | 2.03 × 10–9 | 4.96 × 10–10 | 6.27 × 10–10 | 6.94 × 10–9 | 1.41 × 10–8 | ND | ND |
| GR01 | 3.86 × 10–9 | 1.46 × 10–6 | 1.06 × 10–6 | 9.78 × 10–7 | 2.12 × 10–7 | ND | ND |
| GR02 | 1.59 × 10–8 | 1.26 × 10–6 | 2.42 × 10–7 | 2.07 × 10–5 | 4.03 × 10–6 | 6.71 × 10–9 | 6.18 × 10–9 |
Data were calculated with competition binding assays displacing 3H-steroid agonists for the respective human (hu), mouse (ms), and rat (rt) nuclear hormone receptor on cells. Data are reported as [M]. Reference compounds (Ref.) are positive control agonists or antagonists: dexamethasone (GR), dihydrotestosterone (AR), progesterone (PR), 4-OH-tamoxifen (ER), and eplerenone (MR). ND = not determined.