Target
Androgen receptor
Ligand
BDBM18161
Substrate
BDBM18161
Meas. Tech.
Receptor Binding and Transactivation Assay
pH
7.4±n/a
Temperature
295.15±n/a K
Ki
0.3±n/a nM
EC50
2.8±n/a nM
Comments
Intrinsic relative activity to DHT is 100%.
Citation
 Sun, CRobl, JAWang, TCHuang, YKuhns, JELupisella, JABeehler, BCGolla, RSleph, PGSeethala, RFura, AKrystek, SrAn, YMalley, MFSack, JSSalvati, MEGrover, GJOstrowski, JHamann, LG Discovery of potent, orally-active, and muscle-selective androgen receptor modulators based on an N-aryl-hydroxybicyclohydantoin scaffold. J Med Chem 49:7596-9 (2006) [PubMed]  Article 
Target
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:
MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGLEGESLGCSGSAAAGSSGTLELPSTLSLYKSGALDEAAAYQSRDYYNFPLALAGPPPPPPPPHPHARIKLENPLDYGSAWAAAAAQCRYGDLASLHGAGAAGPGSGSPSAAASSSWHTLFTAEEGQLYGPCGGGGGGGGGGGGGGGGGGGGGGGEAGAVAPYGYTRPPQGLAGQESDFTAPDVWYPGGMVSRVPYPSPTCVKSEMGPWMDSYSGPYGDMRLETARDHVLPIDYYFPPQKTCLICGDEASGCHYGALTCGSCKVFFKRAAEGKQKYLCASRNDCTIDKFRRKNCPSCRLRKCYEAGMTLGARKLKKLGNLKLQEEGEASSTTSPTEETTQKLTVSHIEGYECQPIFLNVLEAIEPGVVCAGHDNNQPDSFAALLSSLNELGERQLVHVVKWAKALPGFRNLHVDDQMAVIQYSWMGLMVFAMGWRSFTNVNSRMLYFAPDLVFNEYRMHKSRMYSQCVRMRHLSQEFGWLQITPQEFLCMKALLLFSIIPVDGLKNQKFFDELRMNYIKELDRIIACKRKNPTSCSRRFYQLTKLLDSVQPIARELHQFTFDLLIKSHMVSVDFPEMMAEIISVQVPKILSGKVKPIYFHTQ
  
Inhibitor
Name:
BDBM18161
Synonyms:
(1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadecan-5-one | (5alpha,17beta)-17-hydroxyandrostan-3-one | CHEMBL27769 | DHT | Dihydrotestosterone | [3H]DHT
Type:
Steroid
Emp. Form.:
C19H30O2
Mol. Mass.:
290.4403
SMILES:
[H][C@@]12CC[C@H](O)[C@@]1(C)CC[C@@]1([H])[C@@]2([H])CC[C@@]2([H])CC(=O)CC[C@]12C |r|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
BDBM18161
Synonyms:
(1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadecan-5-one | (5alpha,17beta)-17-hydroxyandrostan-3-one | CHEMBL27769 | DHT | Dihydrotestosterone | [3H]DHT
Type:
Steroid
Emp. Form.:
C19H30O2
Mol. Mass.:
290.4403
SMILES:
[H][C@@]12CC[C@H](O)[C@@]1(C)CC[C@@]1([H])[C@@]2([H])CC[C@@]2([H])CC(=O)CC[C@]12C |r|
Structure:
Search PDB for entries with ligand similarity: