Reaction Details | |||
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Target | Androgen receptor | ||
Ligand | BDBM18169 | ||
Substrate/Competitor | BDBM18161 | ||
Meas. Tech. | Receptor Binding and Transactivation Assay | ||
pH | 7.4±n/a | ||
Temperature | 295.15±n/a K | ||
Ki | 1.5±n/a nM | ||
EC50 | 281±n/a nM | ||
Comments | Intrinsic relative activity to DHT is 63%. | ||
Citation | Sun, C; Robl, JA; Wang, TC; Huang, Y; Kuhns, JE; Lupisella, JA; Beehler, BC; Golla, R; Sleph, PG; Seethala, R; Fura, A; Krystek, Sr; An, Y; Malley, MF; Sack, JS; Salvati, ME; Grover, GJ; Ostrowski, J; Hamann, LG Discovery of potent, orally-active, and muscle-selective androgen receptor modulators based on an N-aryl-hydroxybicyclohydantoin scaffold. J Med Chem49:7596-9 (2006) [PubMed] Article | ||
More Info.: | Get all data from this article, Solution Info, Assay Method | ||
Androgen receptor | |||
Name: | Androgen receptor | ||
Synonyms: | ANDR_HUMAN | AR | Androgen Receptor | Androgen receptor (AR) | Androgen receptor/Baculoviral IAP repeat-containing protein 2 | DHTR | Dihydrotestosterone receptor | NR3C4 | Nuclear receptor subfamily 3 group C member 4 | ||
Type: | Receptor | ||
Mol. Mass.: | 99185.27 | ||
Organism: | Homo sapiens (Human) | ||
Description: | CHO cells were stably transfected with human AR gene. | ||
Residue: | 920 | ||
Sequence: |
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BDBM18169 | |||
BDBM18161 | |||
Name | BDBM18169 | ||
Synonyms: | (7S,7aR)-7-hydroxy-2-(4-nitronaphthalen-1-yl)-hexahydro-1H-pyrrolo[1,2-a]imidazolidine-1,3-dione | N-aryl-bicyclic hydantoin, (+)10a | ||
Type | Small organic molecule | ||
Emp. Form. | C16H13N3O5 | ||
Mol. Mass. | 327.2915 | ||
SMILES | O[C@H]1CCn2c1c(O)n(-c1ccc([N+]([O-])=O)c3ccccc13)c2=O |r,wD:1.0,(-7.31,4.33,;-6.4,3.09,;-6.88,1.62,;-5.63,.72,;-4.39,1.62,;-4.86,3.09,;-3.62,3.99,;-3.62,5.53,;-2.37,3.09,;-.83,3.09,;.03,4.36,;1.57,4.25,;2.24,2.87,;3.78,2.76,;4.45,1.37,;4.64,4.03,;1.38,1.59,;2.05,.21,;1.19,-1.07,;-.35,-.96,;-1.02,.43,;-.16,1.7,;-2.85,1.62,;-1.94,.38,)| | ||
Structure |