Table 2.
Inhibition of AR dimerization by AR antagonists
| Compound | AR wild type | AR W742C | AR W742L |
|---|---|---|---|
| Darolutamide | 100 ± 10 | 420 ± 140 | 180 ± 30 |
| (S,R)‐darolutamide | 70 ± 30 | 380 ± 90 | 160 ± 10 |
| (S,S)‐darolutamide | 120 ± 20 | 520 ± 130 | 190 ± 90 |
| Keto‐darolutamide | 120 ± 30 | 580 ± 140 | 190 ± 70 |
| Enzalutamide | 180 ± 80 | 2,090 ± 1301 | 2,180 ± 2201 |
| Apalutamide | 130 ± 40 | 1,450 ± 501 | 1,040 ± 1801 |
| Bicalutamide | 340 ± 701 | Ago: 130 ± 10% | Ago: 120 ± 30% |
Notes: Mean IC50 ± SD values from three biological replicates are given in nM. Cells were treated with 10 nM R1881. In case agonistic activity was observed, the value is shown in bold and gives the % activity measured with 10 μM compound only, in comparison to treatment with 10 nM R1881 which was set to 100%. Statistical analysis was performed with t‐test on average pIC50 values. Superscript indicates inhibitory activity that is significantly lower than that of darolutamide. Ago, agonism.