Target Validation Information
Target ID T46521
Target Name mRNA of androgen receptor
Target Type
Clinical Trial
Drug Potency against Target 6-N-propyl -4-trifluoromethylquinolin-2(1H)-one Drug Info Ki = 54 nM [528470]
6-amino-4-trifluoromethylquinolin-2(1H)-one Drug Info IC50 = 26 nM [528470]
AL-43 Drug Info Ki = 1230 nM [526567]
4-(isopropylthio)-2-methoxybenzonitrile Drug Info IC50 = 29 nM [529954]
2-methoxy-4-(2-methoxyphenylthio)benzonitrile Drug Info IC50 = 35 nM [529954]
EUGENOL Drug Info IC50 = 19000 nM [530785]
1,2-dibromo-4-(1,2-dibromoethyl)cyclohexane Drug Info IC50 = 42.7 nM [528558]
LGD-2226 Drug Info Ki = 1.5 nM [528648]
3,2'-bis-trifluoromethyl-biphenyl-4-carbonitrile Drug Info IC50 = 10.9 nM [529009]
LG-120838 Drug Info IC50 = 1062 nM [534728]
6-Hydroxyflavanone Drug Info IC50 = 3300 nM [530256]
CP-409069 Drug Info Ki = 650 nM [526345]
EPIERENONE Drug Info Ki = 8892 nM [529171]
CP-394531 Drug Info Ki = 130 nM [526345]
4-(p-tolyloxy)-2-(trifluoromethyl)benzonitrile Drug Info IC50 = 4000 nM [530022]
NSC-19028 Drug Info IC50 = 5900 nM [530256]
5-Methoxyflavone Drug Info IC50 = 8700 nM [530256]
KAEMPFEROL Drug Info IC50 = 9700 nM [530256]
APIGENIN Drug Info IC50 = 5200 nM [530256]
2-methoxy-4-(m-tolyloxy)benzonitrile Drug Info IC50 = 197 nM [529954]
4-(m-tolyloxy)-2-(trifluoromethyl)benzonitrile Drug Info IC50 = 770 nM [530022]
2-methoxy-4-(p-tolyloxy)benzonitrile Drug Info IC50 = 209 nM [529954]
4-(isopentylthio)-2-(trifluoromethyl)benzonitrile Drug Info IC50 = 519 nM [529954]
4-(cyclobutylmethylthio)-2-methoxybenzonitrile Drug Info IC50 = 441 nM [529954]
4-(o-tolylthio)-2-(trifluoromethyl)benzonitrile Drug Info IC50 = 225 nM [529954]
3-methoxy-4-(m-tolyloxy)benzonitrile Drug Info IC50 = 353 nM [529954]
4-(butylthio)-2-methoxybenzonitrile Drug Info IC50 = 84 nM [529954]
4-(2,6-dimethylphenylthio)-2-methoxybenzonitrile Drug Info IC50 = 43 nM [529954]
3-methoxy-4-(p-tolyloxy)benzonitrile Drug Info IC50 = 5210 nM [529954]
2-methoxy-4-(propylthio)benzonitrile Drug Info IC50 = 40 nM [529954]
4-(propylthio)-2-(trifluoromethyl)benzonitrile Drug Info IC50 = 23 nM [529954]
4-(mesitylthio)-2-(trifluoromethyl)benzonitrile Drug Info IC50 = 1340 nM [529954]
4-(mesitylthio)-2-methoxybenzonitrile Drug Info IC50 = 69 nM [529954]
4-(isopentylthio)-2-methoxybenzonitrile Drug Info IC50 = 1730 nM [529954]
4-(cyclopropylmethylthio)-2-methoxybenzonitrile Drug Info IC50 = 169 nM [529954]
4-(o-tolyloxy)-2-(trifluoromethyl)benzonitrile Drug Info IC50 = 743 nM [530022]
3-chloro-4-(o-tolyloxy)benzonitrile Drug Info IC50 = 64 nM [530022]
4-(isopropylthio)-2-(trifluoromethyl)benzonitrile Drug Info IC50 = 89 nM [529954]
2-methoxy-4-(o-tolyloxy)benzonitrile Drug Info IC50 = 81 nM [529954]
4-(butylthio)-2-(trifluoromethyl)benzonitrile Drug Info IC50 = 838 nM [529954]
3-chloro-4-(o-tolylthio)benzonitrile Drug Info IC50 = 78 nM [529954]
BMS-564929 Drug Info Ki = 14 nM [530061]
2-chloro-4-(o-tolyloxy)benzonitrile Drug Info IC50 = 57 nM [530022]
PF-0998425 Drug Info IC50 = 43 nM [529750]
RU-58841 Drug Info IC50 = 40 nM [529750]
2'-Hydroxy-3-methoxy-biphenyl-4-carbonitrile Drug Info IC50 = 20.1 nM [529750]
YM-175735 Drug Info IC50 = 200 nM [527978]
WAY-252623 Drug Info IC50 = 2300 nM [529781]
3-methoxy-4-(o-tolyloxy)benzonitrile Drug Info IC50 = 115 nM [529954]
ZK-230211 Drug Info IC50 = 54 nM [525950]
ONAPRISTONE Drug Info IC50 = 269 nM [526633]
WAY-255348 Drug Info IC50 = 196 nM [529352]
RU-56187 Drug Info IC50 = 15 nM [530839]
RU-43044 Drug Info Ki = 90 nM [526345]
4-(mesityloxy)-2-(trifluoromethyl)benzonitrile Drug Info IC50 = 812 nM [530022]
LGD-5552 Drug Info Ki = 910 nM [529166]
LG-121071 Drug Info Ki = 11 nM [528792]
NSC-26745 Drug Info IC50 = 300 nM [530256]
References
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Ref 528470J Med Chem. 2006 Oct 19;49(21):6143-6.Discovery of 6-N,N-bis(2,2,2-trifluoroethyl)amino- 4-trifluoromethylquinolin-2(1H)-one as a novel selective androgen receptor modulator.
Ref 526567J Med Chem. 2003 Mar 13;46(6):1016-30.Nonsteroidal selective glucocorticoid modulators: the effect of C-10 substitution on receptor selectivity and functional potency of 5-allyl-2,5-dihydro-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines.
Ref 529954Bioorg Med Chem Lett. 2009 Mar 1;19(5):1310-3. Epub 2009 Jan 27.4-(Alkylthio)- and 4-(arylthio)-benzonitrile derivatives as androgen receptor antagonists for the topical suppression of sebum production.
Ref 529954Bioorg Med Chem Lett. 2009 Mar 1;19(5):1310-3. Epub 2009 Jan 27.4-(Alkylthio)- and 4-(arylthio)-benzonitrile derivatives as androgen receptor antagonists for the topical suppression of sebum production.
Ref 530785Bioorg Med Chem Lett. 2010 Apr 1;20(7):2111-4. Epub 2010 Feb 21.Effect of essential oils, such as raspberry ketone and its derivatives, on antiandrogenic activity based on in vitro reporter gene assay.
Ref 528558J Med Chem. 2006 Dec 14;49(25):7366-72.Identification of the brominated flame retardant 1,2-dibromo-4-(1,2-dibromoethyl)cyclohexane as an androgen agonist.
Ref 528648Bioorg Med Chem Lett. 2007 Mar 15;17(6):1527-31. Epub 2007 Jan 8.Novel selective androgen receptor modulators: SAR studies on 6-bisalkylamino-2-quinolinones.
Ref 529009Bioorg Med Chem Lett. 2007 Oct 15;17(20):5529-32. Epub 2007 Aug 19.Preparation of 4-aryl-2-trifluoromethylbenzonitrile derivatives as androgen receptor antagonists for topical suppression of sebum production.
Ref 534728J Med Chem. 1998 Oct 22;41(22):4354-9.5-Benzylidene 1,2-dihydrochromeno[3,4-f]quinolines, a novel class of nonsteroidal human progesterone receptor agonists.
Ref 530256Bioorg Med Chem Lett. 2009 Aug 15;19(16):4706-10. Epub 2009 Jun 23.Effect of flavonoids on androgen and glucocorticoid receptors based on in vitro reporter gene assay.
Ref 526345J Med Chem. 2002 Jun 6;45(12):2417-24.Discovery of potent, nonsteroidal, and highly selective glucocorticoid receptor antagonists.
Ref 529171J Med Chem. 2007 Dec 27;50(26):6443-5. Epub 2007 Nov 27.(S)-N-{3-[1-cyclopropyl-1-(2,4-difluoro-phenyl)-ethyl]-1H-indol-7-yl}-methanesulfonamide: a potent, nonsteroidal, functional antagonist of themineralocorticoid receptor.
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Ref 530022Bioorg Med Chem Lett. 2009 Apr 15;19(8):2176-8. Epub 2009 Mar 3.Diphenyl ethers as androgen receptor antagonists for the topical suppression of sebum production.
Ref 530256Bioorg Med Chem Lett. 2009 Aug 15;19(16):4706-10. Epub 2009 Jun 23.Effect of flavonoids on androgen and glucocorticoid receptors based on in vitro reporter gene assay.
Ref 530256Bioorg Med Chem Lett. 2009 Aug 15;19(16):4706-10. Epub 2009 Jun 23.Effect of flavonoids on androgen and glucocorticoid receptors based on in vitro reporter gene assay.
Ref 530256Bioorg Med Chem Lett. 2009 Aug 15;19(16):4706-10. Epub 2009 Jun 23.Effect of flavonoids on androgen and glucocorticoid receptors based on in vitro reporter gene assay.
Ref 530256Bioorg Med Chem Lett. 2009 Aug 15;19(16):4706-10. Epub 2009 Jun 23.Effect of flavonoids on androgen and glucocorticoid receptors based on in vitro reporter gene assay.
Ref 529954Bioorg Med Chem Lett. 2009 Mar 1;19(5):1310-3. Epub 2009 Jan 27.4-(Alkylthio)- and 4-(arylthio)-benzonitrile derivatives as androgen receptor antagonists for the topical suppression of sebum production.
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Ref 529954Bioorg Med Chem Lett. 2009 Mar 1;19(5):1310-3. Epub 2009 Jan 27.4-(Alkylthio)- and 4-(arylthio)-benzonitrile derivatives as androgen receptor antagonists for the topical suppression of sebum production.
Ref 529954Bioorg Med Chem Lett. 2009 Mar 1;19(5):1310-3. Epub 2009 Jan 27.4-(Alkylthio)- and 4-(arylthio)-benzonitrile derivatives as androgen receptor antagonists for the topical suppression of sebum production.
Ref 529954Bioorg Med Chem Lett. 2009 Mar 1;19(5):1310-3. Epub 2009 Jan 27.4-(Alkylthio)- and 4-(arylthio)-benzonitrile derivatives as androgen receptor antagonists for the topical suppression of sebum production.
Ref 529954Bioorg Med Chem Lett. 2009 Mar 1;19(5):1310-3. Epub 2009 Jan 27.4-(Alkylthio)- and 4-(arylthio)-benzonitrile derivatives as androgen receptor antagonists for the topical suppression of sebum production.
Ref 529954Bioorg Med Chem Lett. 2009 Mar 1;19(5):1310-3. Epub 2009 Jan 27.4-(Alkylthio)- and 4-(arylthio)-benzonitrile derivatives as androgen receptor antagonists for the topical suppression of sebum production.
Ref 529954Bioorg Med Chem Lett. 2009 Mar 1;19(5):1310-3. Epub 2009 Jan 27.4-(Alkylthio)- and 4-(arylthio)-benzonitrile derivatives as androgen receptor antagonists for the topical suppression of sebum production.
Ref 529954Bioorg Med Chem Lett. 2009 Mar 1;19(5):1310-3. Epub 2009 Jan 27.4-(Alkylthio)- and 4-(arylthio)-benzonitrile derivatives as androgen receptor antagonists for the topical suppression of sebum production.
Ref 529954Bioorg Med Chem Lett. 2009 Mar 1;19(5):1310-3. Epub 2009 Jan 27.4-(Alkylthio)- and 4-(arylthio)-benzonitrile derivatives as androgen receptor antagonists for the topical suppression of sebum production.
Ref 529954Bioorg Med Chem Lett. 2009 Mar 1;19(5):1310-3. Epub 2009 Jan 27.4-(Alkylthio)- and 4-(arylthio)-benzonitrile derivatives as androgen receptor antagonists for the topical suppression of sebum production.
Ref 529954Bioorg Med Chem Lett. 2009 Mar 1;19(5):1310-3. Epub 2009 Jan 27.4-(Alkylthio)- and 4-(arylthio)-benzonitrile derivatives as androgen receptor antagonists for the topical suppression of sebum production.
Ref 529954Bioorg Med Chem Lett. 2009 Mar 1;19(5):1310-3. Epub 2009 Jan 27.4-(Alkylthio)- and 4-(arylthio)-benzonitrile derivatives as androgen receptor antagonists for the topical suppression of sebum production.
Ref 529954Bioorg Med Chem Lett. 2009 Mar 1;19(5):1310-3. Epub 2009 Jan 27.4-(Alkylthio)- and 4-(arylthio)-benzonitrile derivatives as androgen receptor antagonists for the topical suppression of sebum production.
Ref 529954Bioorg Med Chem Lett. 2009 Mar 1;19(5):1310-3. Epub 2009 Jan 27.4-(Alkylthio)- and 4-(arylthio)-benzonitrile derivatives as androgen receptor antagonists for the topical suppression of sebum production.
Ref 529954Bioorg Med Chem Lett. 2009 Mar 1;19(5):1310-3. Epub 2009 Jan 27.4-(Alkylthio)- and 4-(arylthio)-benzonitrile derivatives as androgen receptor antagonists for the topical suppression of sebum production.
Ref 530022Bioorg Med Chem Lett. 2009 Apr 15;19(8):2176-8. Epub 2009 Mar 3.Diphenyl ethers as androgen receptor antagonists for the topical suppression of sebum production.
Ref 530022Bioorg Med Chem Lett. 2009 Apr 15;19(8):2176-8. Epub 2009 Mar 3.Diphenyl ethers as androgen receptor antagonists for the topical suppression of sebum production.
Ref 529954Bioorg Med Chem Lett. 2009 Mar 1;19(5):1310-3. Epub 2009 Jan 27.4-(Alkylthio)- and 4-(arylthio)-benzonitrile derivatives as androgen receptor antagonists for the topical suppression of sebum production.
Ref 529954Bioorg Med Chem Lett. 2009 Mar 1;19(5):1310-3. Epub 2009 Jan 27.4-(Alkylthio)- and 4-(arylthio)-benzonitrile derivatives as androgen receptor antagonists for the topical suppression of sebum production.
Ref 529954Bioorg Med Chem Lett. 2009 Mar 1;19(5):1310-3. Epub 2009 Jan 27.4-(Alkylthio)- and 4-(arylthio)-benzonitrile derivatives as androgen receptor antagonists for the topical suppression of sebum production.
Ref 529954Bioorg Med Chem Lett. 2009 Mar 1;19(5):1310-3. Epub 2009 Jan 27.4-(Alkylthio)- and 4-(arylthio)-benzonitrile derivatives as androgen receptor antagonists for the topical suppression of sebum production.
Ref 530061J Med Chem. 2009 May 14;52(9):2794-8.N-aryl-oxazolidin-2-imine muscle selective androgen receptor modulators enhance potency through pharmacophore reorientation.
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Ref 529750J Med Chem. 2008 Nov 13;51(21):7010-4. Epub 2008 Oct 16.Rational design and synthesis of 4-((1R,2R)-2-hydroxycyclohexyl)-2(trifluoromethyl)benzonitrile (PF-998425), a novel, nonsteroidal androgen receptor antagonist devoid of phototoxicity for dermatological indications.
Ref 529750J Med Chem. 2008 Nov 13;51(21):7010-4. Epub 2008 Oct 16.Rational design and synthesis of 4-((1R,2R)-2-hydroxycyclohexyl)-2(trifluoromethyl)benzonitrile (PF-998425), a novel, nonsteroidal androgen receptor antagonist devoid of phototoxicity for dermatological indications.
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Ref 525950J Med Chem. 2000 Dec 28;43(26):5010-6.Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist.
Ref 526633Bioorg Med Chem Lett. 2003 Jun 16;13(12):2075-8.Development of progesterone receptor antagonists from 1,2-dihydrochromeno[3,4-f]quinoline agonist pharmacophore.
Ref 529352J Med Chem. 2008 Mar 27;51(6):1861-73. Epub 2008 Mar 5.Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348).
Ref 530839Bioorg Med Chem. 2010 May 1;18(9):3159-68. Epub 2010 Mar 19.Structure-activity relationships of bioisosteric replacement of the carboxylic acid in novel androgen receptor pure antagonists.
Ref 526345J Med Chem. 2002 Jun 6;45(12):2417-24.Discovery of potent, nonsteroidal, and highly selective glucocorticoid receptor antagonists.
Ref 530022Bioorg Med Chem Lett. 2009 Apr 15;19(8):2176-8. Epub 2009 Mar 3.Diphenyl ethers as androgen receptor antagonists for the topical suppression of sebum production.
Ref 529166Proc Natl Acad Sci U S A. 2007 Dec 4;104(49):19244-9. Epub 2007 Nov 21.Antiinflammatory glucocorticoid receptor ligand with reduced side effects exhibits an altered protein-protein interaction profile.
Ref 528792J Med Chem. 2007 May 17;50(10):2486-96. Epub 2007 Apr 17.Novel series of potent, nonsteroidal, selective androgen receptor modulators based on 7H-[1,4]oxazino[3,2-g]quinolin-7-ones.
Ref 530256Bioorg Med Chem Lett. 2009 Aug 15;19(16):4706-10. Epub 2009 Jun 23.Effect of flavonoids on androgen and glucocorticoid receptors based on in vitro reporter gene assay.

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