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. Author manuscript; available in PMC: 2021 Aug 12.
Published in final edited form as: J Med Chem. 2020 Oct 23;63(21):12642–12665. doi: 10.1021/acs.jmedchem.0c00943

Table 3.

In Vitro AR Activity of 21a–21j (Series II)

graphic file with name nihms-1646976-t0052.jpg
ID (R1) Structure of the A-ring
(A)		 Binding (Ki) / Transactivation (IC50) (μM) SARD Activity (% degradation) F.L. DC50 (μM)
Ki (DHT = 1 nM)a IC50a Full Lengtha (LNCaP) at 1 μM Splice Varianta (22RV1) at 10 μM
21a (4-F) graphic file with name nihms-1646976-t0053.jpg >10 0.062 54 81 0.88
21b (4-CF3) graphic file with name nihms-1646976-t0054.jpg 2.286 0.208 10 N.A.b -
21c (4-CN) graphic file with name nihms-1646976-t0055.jpg 0.089 0.059 10 N.A.b -
21d (4-NHCOOtBu) graphic file with name nihms-1646976-t0056.jpg >10 6.108 - N.A.b -
21e (4-F) graphic file with name nihms-1646976-t0057.jpg >10 0.427 42 0 -
21f (4-F) graphic file with name nihms-1646976-t0058.jpg N.A.b Partial Agonist N.A.b N.A.b -
21g (4-F) graphic file with name nihms-1646976-t0059.jpg >10 No effect 0 N.A.b
21h (4-F) graphic file with name nihms-1646976-t0060.jpg >10 No effect N.A. N.A. -
21i (4-F) graphic file with name nihms-1646976-t0061.jpg N.A. 2.470 75 N.A. N.A.
21j (4-F) graphic file with name nihms-1646976-t0062.jpg N.A. 5.450 N.A.b N.A. -
a

AR binding, transactivation, and degradation assays were performed and values are reported as described in Table 2.

b

N.A. indicates data not available.