Reaction Details | |||
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Target | Androgen receptor | ||
Ligand | BDBM18173 | ||
Substrate/Competitor | BDBM18161 | ||
Meas. Tech. | Receptor Binding Assay (Ki) and Transactivation Assay (EC50) | ||
pH | 7.6±n/a | ||
Temperature | 295.15±n/a K | ||
Ki | 14±3 nM | ||
EC50 | 7.8±2 nM | ||
Citation | Nirschl, AA; Zou, Y; Krystek, SR; Sutton, JC; Simpkins, LM; Lupisella, JA; Kuhns, JE; Seethala, R; Golla, R; Sleph, PG; Beehler, BC; Grover, GJ; Egan, D; Fura, A; Vyas, VP; Li, YX; Sack, JS; Kish, KF; An, Y; Bryson, JA; Gougoutas, JZ; DiMarco, J; Zahler, R; Ostrowski, J; Hamann, LG N-aryl-oxazolidin-2-imine muscle selective androgen receptor modulators enhance potency through pharmacophore reorientation. J Med Chem52:2794-8 (2009) [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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BDBM18173 | |||
BDBM18161 | |||
Name | BDBM18173 | ||
Synonyms: | 4-[(7R,7aS)-7-hydroxy-1,3-dioxo-hexahydro-1H-pyrrolo[1,2-a]imidazolidin-2-yl]-2-chloro-3-methylbenzonitrile | BMS-564929 | CHEMBL229264 | ||
Type | Small organic molecule | ||
Emp. Form. | C14H12ClN3O3 | ||
Mol. Mass. | 305.716 | ||
SMILES | Cc1c(Cl)c(ccc1-n1c(O)c2[C@H](O)CCn2c1=O)C#N |r,wU:12.13,(.01,.36,;.81,1.67,;2.35,1.63,;3.09,.28,;3.16,2.94,;2.42,4.3,;.88,4.34,;.08,3.02,;-1.46,3.02,;-1.94,4.49,;-1.03,5.73,;-3.48,4.49,;-4.72,5.39,;-4.72,6.93,;-5.97,4.49,;-5.5,3.02,;-3.95,3.02,;-2.71,2.12,;-2.71,.58,;4.7,2.9,;6.24,2.9,)| | ||
Structure |