Template:Affinities of bicalutamide at steroid hormone receptors

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Affinities of bicalutamide at steroid hormone receptors

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Compound AR PR ER GR MR
Template:No selflink 14–54 3,500–7,200 >1,000,000 44,000–320,000 ≥360,000
Template:No selflink 0.5–3.1 280–440 38,000–340,000 2,700–20,000 2,100–2,300
Notes: Values are Ki or IC50 (nM) for binding inhibition (affinity). Sources: [1][2][3][4]

References

  1. Hanada K, Furuya K, Yamamoto N, Nejishima H, Ichikawa K, Nakamura T, Miyakawa M, Amano S, Sumita Y, Oguro N (November 2003). "Bone anabolic effects of S-40503, a novel nonsteroidal selective androgen receptor modulator (SARM), in rat models of osteoporosis". Biol. Pharm. Bull. 26 (11): 1563–9. doi:10.1248/bpb.26.1563. PMID 14600402.
  2. Nagata N, Miyakawa M, Amano S, Furuya K, Yamamoto N, Nejishima H, Inoguchi K (2011). "Tetrahydroquinolines as a novel series of nonsteroidal selective androgen receptor modulators: structural requirements for better physicochemical and biological properties". Bioorg. Med. Chem. Lett. 21 (21): 6310–3. doi:10.1016/j.bmcl.2011.08.118. PMID 21944856.
  3. Nagata N, Miyakawa M, Amano S, Furuya K, Yamamoto N, Inoguchi K (2011). "Design and synthesis of tricyclic tetrahydroquinolines as a new series of nonsteroidal selective androgen receptor modulators (SARMs)". Bioorg. Med. Chem. Lett. 21 (6): 1744–7. doi:10.1016/j.bmcl.2011.01.073. PMID 21349712.
  4. Kinoyama I, Taniguchi N, Toyoshima A, Nozawa E, Kamikubo T, Imamura M, Matsuhisa A, Samizu K, Kawanimani E, Niimi T, Hamada N, Koutoku H, Furutani T, Kudoh M, Okada M, Ohta M, Tsukamoto S (2006). "(+)-(2R,5S)-4-[4-cyano-3-(trifluoromethyl)phenyl]-2,5-dimethyl-N-[6-(trifluoromethyl)pyridin-3- yl]piperazine-1-carboxamide (YM580) as an orally potent and peripherally selective nonsteroidal androgen receptor antagonist". J. Med. Chem. 49 (2): 716–26. doi:10.1021/jm050293c. PMID 16420057.