Table 2. Transcriptional Reporter Assay Activity of 9–16 and 19–29 in LNCaP F877L (Mutant) and LNCaP AR cs (WT) Cells.

compound	LNCaP F877La IC50 (nM)b	LNCaP WTa IC50 (nM)b
1	not fit	117 ± 66
4	98 ± 63	191 ± 120
9	>15000c	>15000d
10	5012 ± 207	11220 ± 3826e
11	676 ± 170	1380 ± 141
12	525 ± 322	646 ± 113
13	759 ± 81	1096 ± 7
14	339 ± 119	398 ± 52
15	1660 ± 1081	>30000
16	178 ± 86	219 ± 116
18	145 ± 32	112 ± 28
19	93 ± 32	93 ± 30
20	102 ± 10	100 ± 20
21	123 ± 39	126 ± 8
22	257 ± 13	191 ± 11
23	170 ± 37	229 ± 25
24	132 ± 33	148 ± 39
25	174 ± 4	209 ± 6
(S)-26	112 ± 116	178 ± 41
(S)-27	151 ± 26	170 ± 19
(R)-28	65 ± 47	52 ± 37
(R)-29	78 ± 10	72 ± 23

^aLNCaP F877L and LNCaP WT reporter assays were repeated two times or more. All compounds except 1 were antagonists in AR F877L, and all were antagonists in the AR WT.

^bMax inhibition >90% for all compounds unless specifically mentioned.

^cMax inhibition 52%.

^dMax inhibition 35%.

^eMax inhibition 80%.