Template:Bicalutamide and other antiandrogens at the androgen and progesterone receptors

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Bicalutamide and other antiandrogens at the androgen and progesterone receptors

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Template:No selflink AR PR-B
Ki (nM) IC50 (nM) Imax (%) IC50 (nM) Imax (%)
Template:No selflink 117 157 78 1,819 88
Template:No selflink 14 26 48 >10,000 12
Template:No selflink 27 15 83 2,013 90
Template:No selflink 22 5 75 0.18 96
Notes: IC50 values are for functional antagonism. Imax is maximal inhibition. Sources: [1]

References

  1. Hamann LG, Higuchi RI, Zhi L, Edwards JP, Wang XN, Marschke KB, Kong JW, Farmer LJ, Jones TK (1998). "Synthesis and biological activity of a novel series of nonsteroidal, peripherally selective androgen receptor antagonists derived from 1,2-dihydropyridono[5,6-g]quinolines". J. Med. Chem. 41 (4): 623–39. doi:10.1021/jm970699s. PMID 9484511.