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TargetAndrogen receptor
LigandBDBM18593
Substrate/CompetitorBDBM18161
Meas. Tech.AR Transcriptional Activation Assay and MDA Whole-Cell Binding Assay
pH7.4±n/a
Temperature310.15±n/a K
Ki 6.6±2.8 nM
EC50 7.9±5.3 nM
CommentshAR agonist efficacy = 125 +/- 27 %
Citation van Oeveren, AMotamedi, MMartinborough, EZhao, SShen, YWest, SChang, WKallel, AMarschke, KBLópez, FJNegro-Vilar, AZhi, L Novel selective androgen receptor modulators: SAR studies on 6-bisalkylamino-2-quinolinones. Bioorg Med Chem Lett17:1527-31 (2007) [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:
MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQ
QQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQ
SALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSAD
LKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELC
KAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAG
KSTEDTAEYSPFKGGYTKGLEGESLGCSGSAAAGSSGTLELPSTLSLYKSGALDEAAAYQ
SRDYYNFPLALAGPPPPPPPPHPHARIKLENPLDYGSAWAAAAAQCRYGDLASLHGAGAA
GPGSGSPSAAASSSWHTLFTAEEGQLYGPCGGGGGGGGGGGGGGGGGGGGGGGEAGAVAP
YGYTRPPQGLAGQESDFTAPDVWYPGGMVSRVPYPSPTCVKSEMGPWMDSYSGPYGDMRL
ETARDHVLPIDYYFPPQKTCLICGDEASGCHYGALTCGSCKVFFKRAAEGKQKYLCASRN
DCTIDKFRRKNCPSCRLRKCYEAGMTLGARKLKKLGNLKLQEEGEASSTTSPTEETTQKL
TVSHIEGYECQPIFLNVLEAIEPGVVCAGHDNNQPDSFAALLSSLNELGERQLVHVVKWA
KALPGFRNLHVDDQMAVIQYSWMGLMVFAMGWRSFTNVNSRMLYFAPDLVFNEYRMHKSR
MYSQCVRMRHLSQEFGWLQITPQEFLCMKALLLFSIIPVDGLKNQKFFDELRMNYIKELD
RIIACKRKNPTSCSRRFYQLTKLLDSVQPIARELHQFTFDLLIKSHMVSVDFPEMMAEII
SVQVPKILSGKVKPIYFHTQ
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM18593
BDBM18161
NameBDBM18593
Synonyms:6-[(2-hydroxyethyl)(2,2,2-trifluoroethyl)amino]-4-(trifluoromethyl)-1,2-dihydroquinolin-2-one | 6-bisalkylamino-2-quinolinone, 6r
TypeSmall organic molecule
Emp. Form.C14H12F6N2O2
Mol. Mass.354.2477
SMILESOCCN(CC(F)(F)F)c1ccc2[nH]c(=O)cc(c2c1)C(F)(F)F
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: