Target Validation Information
TTD ID T46521
Target Name Androgen receptor messenger RNA (AR mRNA)
Type of Target
Clinical trial
Drug Potency against Target Drug Info IC50 = 2300 nM [15]
1,2-dibromo-4-(1,2-dibromoethyl)cyclohexane Drug Info IC50 = 42.7 nM [7]
2'-Hydroxy-3-methoxy-biphenyl-4-carbonitrile Drug Info IC50 = 20.1 nM [14]
2-chloro-4-(o-tolyloxy)benzonitrile Drug Info IC50 = 57 nM [17]
2-methoxy-4-(2-methoxyphenylthio)benzonitrile Drug Info IC50 = 35 nM [16]
2-methoxy-4-(m-tolyloxy)benzonitrile Drug Info IC50 = 197 nM [16]
2-methoxy-4-(o-tolyloxy)benzonitrile Drug Info IC50 = 81 nM [16]
2-methoxy-4-(p-tolyloxy)benzonitrile Drug Info IC50 = 209 nM [16]
2-methoxy-4-(propylthio)benzonitrile Drug Info IC50 = 40 nM [16]
3,2'-bis-trifluoromethyl-biphenyl-4-carbonitrile Drug Info IC50 = 10.9 nM [10]
3-chloro-4-(o-tolyloxy)benzonitrile Drug Info IC50 = 64 nM [17]
3-chloro-4-(o-tolylthio)benzonitrile Drug Info IC50 = 78 nM [16]
3-methoxy-4-(m-tolyloxy)benzonitrile Drug Info IC50 = 353 nM [16]
3-methoxy-4-(o-tolyloxy)benzonitrile Drug Info IC50 = 115 nM [16]
3-methoxy-4-(p-tolyloxy)benzonitrile Drug Info IC50 = 5210 nM [16]
4-(2,6-dimethylphenylthio)-2-methoxybenzonitrile Drug Info IC50 = 43 nM [16]
4-(butylthio)-2-(trifluoromethyl)benzonitrile Drug Info IC50 = 838 nM [16]
4-(butylthio)-2-methoxybenzonitrile Drug Info IC50 = 84 nM [16]
4-(cyclobutylmethylthio)-2-methoxybenzonitrile Drug Info IC50 = 441 nM [16]
4-(cyclopropylmethylthio)-2-methoxybenzonitrile Drug Info IC50 = 169 nM [16]
4-(isopentylthio)-2-(trifluoromethyl)benzonitrile Drug Info IC50 = 519 nM [16]
4-(isopentylthio)-2-methoxybenzonitrile Drug Info IC50 = 1730 nM [16]
4-(isopropylthio)-2-(trifluoromethyl)benzonitrile Drug Info IC50 = 89 nM [16]
4-(isopropylthio)-2-methoxybenzonitrile Drug Info IC50 = 29 nM [16]
4-(m-tolyloxy)-2-(trifluoromethyl)benzonitrile Drug Info IC50 = 770 nM [17]
4-(mesityloxy)-2-(trifluoromethyl)benzonitrile Drug Info IC50 = 812 nM [17]
4-(mesitylthio)-2-(trifluoromethyl)benzonitrile Drug Info IC50 = 1340 nM [16]
4-(mesitylthio)-2-methoxybenzonitrile Drug Info IC50 = 69 nM [16]
4-(o-tolyloxy)-2-(trifluoromethyl)benzonitrile Drug Info IC50 = 743 nM [17]
4-(o-tolylthio)-2-(trifluoromethyl)benzonitrile Drug Info IC50 = 225 nM [16]
4-(p-tolyloxy)-2-(trifluoromethyl)benzonitrile Drug Info IC50 = 4000 nM [17]
4-(propylthio)-2-(trifluoromethyl)benzonitrile Drug Info IC50 = 23 nM [16]
5-Methoxyflavone Drug Info IC50 = 8700 nM [19]
6-amino-4-trifluoromethylquinolin-2(1H)-one Drug Info IC50 = 26 nM [6]
6-Hydroxyflavanone Drug Info IC50 = 3300 nM [19]
6-N-propyl -4-trifluoromethylquinolin-2(1H)-one Drug Info Ki = 54 nM [6]
AL-43 Drug Info Ki = 1230 nM [3]
APIGENIN Drug Info IC50 = 5200 nM [19]
BAY 86-5044 Drug Info IC50 = 54 nM [1]
BMS-564929 Drug Info Ki = 14 nM [18]
CP-394531 Drug Info Ki = 130 nM [2]
CP-409069 Drug Info Ki = 650 nM [2]
Epierenone Drug Info Ki = 8892 nM [12]
EUGENOL Drug Info IC50 = 19000 nM [20]
flavone Drug Info IC50 = 5900 nM [19]
KAEMPFEROL Drug Info IC50 = 9700 nM [19]
LG-120838 Drug Info IC50 = 1062 nM [22]
LG-121071 Drug Info Ki = 11 nM [9]
LGD-2226 Drug Info Ki = 1.5 nM [8]
LGD-5552 Drug Info Ki = 910 nM [11]
NSC-26745 Drug Info IC50 = 300 nM [19]
ONAPRISTONE Drug Info IC50 = 269 nM [4]
PF-0998425 Drug Info IC50 = 43 nM [14]
RU-43044 Drug Info Ki = 90 nM [2]
RU-56187 Drug Info IC50 = 15 nM [21]
RU-58841 Drug Info IC50 = 40 nM [14]
WAY-255348 Drug Info IC50 = 196 nM [13]
YM-175735 Drug Info IC50 = 200 nM [5]
References
REF 1 Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist. J Med Chem. 2000 Dec 28;43(26):5010-6.
REF 2 Discovery of potent, nonsteroidal, and highly selective glucocorticoid receptor antagonists. J Med Chem. 2002 Jun 6;45(12):2417-24.
REF 3 Nonsteroidal selective glucocorticoid modulators: the effect of C-10 substitution on receptor selectivity and functional potency of 5-allyl-2,5-dih... J Med Chem. 2003 Mar 13;46(6):1016-30.
REF 4 Development of progesterone receptor antagonists from 1,2-dihydrochromeno[3,4-f]quinoline agonist pharmacophore. Bioorg Med Chem Lett. 2003 Jun 16;13(12):2075-8.
REF 5 (+)-(2R,5S)-4-[4-cyano-3-(trifluoromethyl)phenyl]-2,5-dimethyl-N-[6-(trifluoromethyl)pyridin-3- yl]piperazine-1-carboxamide (YM580) as an orally po... J Med Chem. 2006 Jan 26;49(2):716-26.
REF 6 Discovery of 6-N,N-bis(2,2,2-trifluoroethyl)amino- 4-trifluoromethylquinolin-2(1H)-one as a novel selective androgen receptor modulator. J Med Chem. 2006 Oct 19;49(21):6143-6.
REF 7 Identification of the brominated flame retardant 1,2-dibromo-4-(1,2-dibromoethyl)cyclohexane as an androgen agonist. J Med Chem. 2006 Dec 14;49(25):7366-72.
REF 8 Novel selective androgen receptor modulators: SAR studies on 6-bisalkylamino-2-quinolinones. Bioorg Med Chem Lett. 2007 Mar 15;17(6):1527-31.
REF 9 Novel series of potent, nonsteroidal, selective androgen receptor modulators based on 7H-[1,4]oxazino[3,2-g]quinolin-7-ones. J Med Chem. 2007 May 17;50(10):2486-96.
REF 10 Preparation of 4-aryl-2-trifluoromethylbenzonitrile derivatives as androgen receptor antagonists for topical suppression of sebum production. Bioorg Med Chem Lett. 2007 Oct 15;17(20):5529-32.
REF 11 Antiinflammatory glucocorticoid receptor ligand with reduced side effects exhibits an altered protein-protein interaction profile. Proc Natl Acad Sci U S A. 2007 Dec 4;104(49):19244-9.
REF 12 (S)-N-{3-[1-cyclopropyl-1-(2,4-difluoro-phenyl)-ethyl]-1H-indol-7-yl}-methanesulfonamide: a potent, nonsteroidal, functional antagonist of the mine... J Med Chem. 2007 Dec 27;50(26):6443-5.
REF 13 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-... J Med Chem. 2008 Mar 27;51(6):1861-73.
REF 14 Rational design and synthesis of 4-((1R,2R)-2-hydroxycyclohexyl)-2(trifluoromethyl)benzonitrile (PF-998425), a novel, nonsteroidal androgen recepto... J Med Chem. 2008 Nov 13;51(21):7010-4.
REF 15 Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic tr... J Med Chem. 2008 Nov 27;51(22):7161-8.
REF 16 4-(Alkylthio)- and 4-(arylthio)-benzonitrile derivatives as androgen receptor antagonists for the topical suppression of sebum production. Bioorg Med Chem Lett. 2009 Mar 1;19(5):1310-3.
REF 17 Diphenyl ethers as androgen receptor antagonists for the topical suppression of sebum production. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2176-8.
REF 18 N-aryl-oxazolidin-2-imine muscle selective androgen receptor modulators enhance potency through pharmacophore reorientation. J Med Chem. 2009 May 14;52(9):2794-8.
REF 19 Effect of flavonoids on androgen and glucocorticoid receptors based on in vitro reporter gene assay. Bioorg Med Chem Lett. 2009 Aug 15;19(16):4706-10.
REF 20 Effect of essential oils, such as raspberry ketone and its derivatives, on antiandrogenic activity based on in vitro reporter gene assay. Bioorg Med Chem Lett. 2010 Apr 1;20(7):2111-4.
REF 21 Structure-activity relationships of bioisosteric replacement of the carboxylic acid in novel androgen receptor pure antagonists. Bioorg Med Chem. 2010 May 1;18(9):3159-68.
REF 22 5-Benzylidene 1,2-dihydrochromeno[3,4-f]quinolines, a novel class of nonsteroidal human progesterone receptor agonists. J Med Chem. 1998 Oct 22;41(22):4354-9.

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