| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T11211 | ||||
| Target Name | Androgen receptor | ||||
| Target Type | Successful |
||||
| Drug Potency against Target | RU-59063 | Drug Info | Ki = 2.23 nM | [525861] | |
| 6,11-dihydrothiochromeno[4,3-b]indol-8-ol | Drug Info | IC50 = 4500 nM | [528123] | ||
| 1,2-dibromo-4-(1,2-dibromoethyl)cyclohexane | Drug Info | IC50 = 163 nM | [528558] | ||
| ZANOTERONE | Drug Info | Ki = 2200 nM | [525925] | ||
| Mibolerone | Drug Info | Ki = 0.75 nM | [525861] | ||
| 11-methyl-6,11-dihydro-5H-benzo[a]carbazol-9-ol | Drug Info | IC50 = 30 nM | [528123] | ||
| ZANOTERONE | Drug Info | Ki = 2000 nM | [527548] | ||
| References | |||||
| Ref 525861 | J Med Chem. 2000 Aug 24;43(17):3344-7.Design, synthesis, and pharmacological characterization of 4-[4, 4-dimethyl-3-(4-hydroxybutyl)-5-oxo-2-thioxo-1-imidazolidinyl]- 2-iodobenzonitrile as a high-affinity nonsteroidal androgen receptor ligand. | ||||
| Ref 528123 | Bioorg Med Chem Lett. 2006 Jun 15;16(12):3233-7. Epub 2006 Apr 5.Discovery of indole-containing tetracycles as a new scaffold for androgen receptor ligands. | ||||
| Ref 528558 | J 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 525925 | J Med Chem. 2000 Nov 30;43(24):4629-35.Chiral derivatives of 2-cyclohexylideneperhydro-4,7-methanoindenes, a novel class of nonsteroidal androgen receptor ligand: synthesis, X-ray analysis, and biological activity. | ||||
| Ref 525861 | J Med Chem. 2000 Aug 24;43(17):3344-7.Design, synthesis, and pharmacological characterization of 4-[4, 4-dimethyl-3-(4-hydroxybutyl)-5-oxo-2-thioxo-1-imidazolidinyl]- 2-iodobenzonitrile as a high-affinity nonsteroidal androgen receptor ligand. | ||||
| Ref 528123 | Bioorg Med Chem Lett. 2006 Jun 15;16(12):3233-7. Epub 2006 Apr 5.Discovery of indole-containing tetracycles as a new scaffold for androgen receptor ligands. | ||||
| Ref 527548 | J Med Chem. 1992 May 15;35(10):1663-70.Antiandrogenic steroidal sulfonyl heterocycles. Utility of electrostatic complementarity in defining bioisosteric sulfonyl heterocycles. | ||||
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