TABLE 3.

AR binding affinity of nonsteroidal AR ligands with a para-CN in the A-ring and multiple substituents in the B-ring

Compound	R1	R2	R3	R4	R5	Ki(nm)
S-1	H	H	F	H	H	6.1 ± 0.2
C-25	F	H	F	H	H	4.5 ± 0.4
C-26	H	F	F	H	H	4.1 ± 0.6
C-27	Cl	H	Cl	H	H	20 ± 0.2
C-28	H	Cl	Cl	H	H	5.0 ± 0.2
C-29	F	F	F	F	F	6.8 ± 0.4

The K_i value of S-1 was previously reported in Ref. 11. The AR binding affinity (K_i) of each compound of interested was determined using a competitive binding assay as described in Materials and Methods. Data represent the mean ± sd of three experiments.