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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 5.

In Vitro AR Activity of 29a–29f (Series IV)

graphic file with name nihms-1646976-t0064.jpg
ID (R1) Linker Binding (Ki) / Transactivation (IC50) (μM) SARD Activity (% degradation) F.L. DC50 (μM)
Ki (DHT = 1 nM)a IC50a Full Lengtha (LNCaP) at 1 μM, 10 μM Splice Varianta (22RV1) at 10 μM
29a (4-F) (R-isomer) graphic file with name nihms-1646976-t0065.jpg >10 0.192 84 N.A.b -
29b (4-F) graphic file with name nihms-1646976-t0066.jpg >10 0.462 60 70 0.74
29c (4-F) graphic file with name nihms-1646976-t0067.jpg >10 2.124 35 40 -
29d (4-F) graphic file with name nihms-1646976-t0068.jpg N.A.b 1.131 18, 50c N.A.b -
29e (4-NH2) graphic file with name nihms-1646976-t0069.jpg >10 0.901 N.A. 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.

c

The two values indicate SARD assays run with 1 and 10 μM of antagonist.