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TargetAndrogen Receptor
LigandBDBM18172
Substrate/CompetitorBDBM18161
Meas. Tech.Receptor Binding and Transactivation Assay
pH7.4±n/a
Temperature295.15±n/a K
Ki 5.3±n/a nM
IC50 60±n/a nM
EC50 1298±n/a nM
CommentsIntrinsic relative activity to DHT is 49%.
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 Chem49:7596-9 (2006) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
Androgen Receptor
Name:Androgen Receptor
Synonyms:AR | Androgen receptor (AR) | 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:
MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQ
QQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQ
SALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSAD
LKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELC
KAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAG
KSTEDTAEYSPFKGGYTKGLEGESLGCSGSAAAGSSGTLELPSTLSLYKSGALDEAAAYQ
SRDYYNFPLALAGPPPPPPPPHPHARIKLENPLDYGSAWAAAAAQCRYGDLASLHGAGAA
GPGSGSPSAAASSSWHTLFTAEEGQLYGPCGGGGGGGGGGGGGGGGGGGGGGGEAGAVAP
YGYTRPPQGLAGQESDFTAPDVWYPGGMVSRVPYPSPTCVKSEMGPWMDSYSGPYGDMRL
ETARDHVLPIDYYFPPQKTCLICGDEASGCHYGALTCGSCKVFFKRAAEGKQKYLCASRN
DCTIDKFRRKNCPSCRLRKCYEAGMTLGARKLKKLGNLKLQEEGEASSTTSPTEETTQKL
TVSHIEGYECQPIFLNVLEAIEPGVVCAGHDNNQPDSFAALLSSLNELGERQLVHVVKWA
KALPGFRNLHVDDQMAVIQYSWMGLMVFAMGWRSFTNVNSRMLYFAPDLVFNEYRMHKSR
MYSQCVRMRHLSQEFGWLQITPQEFLCMKALLLFSIIPVDGLKNQKFFDELRMNYIKELD
RIIACKRKNPTSCSRRFYQLTKLLDSVQPIARELHQFTFDLLIKSHMVSVDFPEMMAEII
SVQVPKILSGKVKPIYFHTQ
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BDBM18172
NameBDBM18172
Synonyms:4-[(7S,7aR)-7-hydroxy-1,3-dioxo-hexahydro-1H-pyrrolo[1,2-a]imidazolidin-2-yl]naphthalene-1-carbonitrile | N-aryl-bicyclic hydantoin, (+)10b
TypeSmall organic molecule
Emp. Form.C17H13N3O3
Mol. Mass.307.3034
SMILESO[C@H]1CCn2c1c(O)n(-c1ccc(C#N)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,;5.32,2.76,;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
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BDBM18161
NameBDBM18161
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
TypeSteroid
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
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