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Template:Relative affinities of first-generation nonsteroidal antiandrogens for the androgen receptor

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Relative affinities of first-generation nonsteroidal antiandrogens for the androgen receptor
Species IC50Tooltip Half maximal inhibitory concentration (nM) RBATooltip Relative binding affinity (ratio)
Bicalutamide 2-Hydroxyflutamide Nilutamide Bica / 2-OH-flu Bica / nilu Ref
Rat 190 700 ND 4.0 ND [1]
Rat ~400 ~900 ~900 2.3 2.3 [2]
Rat ND ND ND 3.3 ND [3]
Rata 3595 4565 18620 1.3 5.2 [4]
Human ~300 ~700 ~500 2.5 1.6 [5]
Human ~100 ~300 ND ~3.0 ND [6]
Humana 2490 2345 5300 1.0 2.1 [4]
Footnotes: a = Controversial data. Sources: [7][8]

References

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  1. ^ Furr BJ, Valcaccia B, Curry B, Woodburn JR, Chesterson G, Tucker H (June 1987). "ICI 176,334: a novel non-steroidal, peripherally selective antiandrogen". The Journal of Endocrinology. 113 (3): R7–R9. doi:10.1677/joe.0.113R007. PMID 3625091.
  2. ^ Teutsch G, Goubet F, Battmann T, Bonfils A, Bouchoux F, Cerede E, Gofflo D, Gaillard-Kelly M, Philibert D (January 1994). "Non-steroidal antiandrogens: synthesis and biological profile of high-affinity ligands for the androgen receptor". The Journal of Steroid Biochemistry and Molecular Biology. 48 (1): 111–119. doi:10.1016/0960-0760(94)90257-7. PMID 8136296. S2CID 31404295.
  3. ^ Winneker RC, Wagner MM, Batzold FH (December 1989). "Studies on the mechanism of action of Win 49596: a steroidal androgen receptor antagonist". Journal of Steroid Biochemistry. 33 (6): 1133–1138. doi:10.1016/0022-4731(89)90420-2. PMID 2615358.
  4. ^ a b Luo S, Martel C, Leblanc G, Candas B, Singh SM, Labrie C, Simard J, Bélanger A, Labrie F (1996). "Relative potencies of Flutamide and Casodex: preclinical studies". Endocrine Related Cancer. 3 (3): 229–241. doi:10.1677/erc.0.0030229. ISSN 1351-0088.
  5. ^ Ayub M, Levell MJ (August 1989). "The effect of ketoconazole related imidazole drugs and antiandrogens on [3H] R 1881 binding to the prostatic androgen receptor and [3H]5 alpha-dihydrotestosterone and [3H]cortisol binding to plasma proteins". Journal of Steroid Biochemistry. 33 (2): 251–255. doi:10.1016/0022-4731(89)90301-4. PMID 2788775.
  6. ^ Kemppainen JA, Wilson EM (July 1996). "Agonist and antagonist activities of hydroxyflutamide and Casodex relate to androgen receptor stabilization". Urology. 48 (1): 157–163. doi:10.1016/S0090-4295(96)00117-3. PMID 8693644.
  7. ^ Kolvenbag GJ, Furr BJ, Blackledge GR (December 1998). "Receptor affinity and potency of non-steroidal antiandrogens: translation of preclinical findings into clinical activity". Prostate Cancer and Prostatic Diseases. 1 (6): 307–314. doi:10.1038/sj.pcan.4500262. PMID 12496872. S2CID 33497597.
  8. ^ Furr BJ (1998). "Antiandrogen binding to androgen receptors and the consequences". In Wirth M, Altwein JE, Schmitz-Dräger B, Kuptz S (eds.). Molecular Biology of Prostate Cancer. Walter de Gruyter. pp. 92–. ISBN 978-3-11-080727-1.
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