Ki Summary new BindingDB logo
myBDB logout
Reaction Details
Report a problem with these data
TargetAndrogen Receptor
LigandBDBM18197
Substrate/CompetitorBDBM18161
Meas. Tech.AR Transcriptional Activation Assay and MDA Whole-Cell Binding Assay
pH7.4±n/a
Temperature310.15±n/a K
Ki 4.0±1.0 nM
EC50 3.5±1.3 nM
Commentsefficacy=88 +/- 5 %.
Citation Higuchi RIArienti KLLópez FJMani NSMais DECaferro TRLong YOJones TKEdwards JPZhi LSchrader WTNegro-Vilar AMarschke KB Novel series of potent, nonsteroidal, selective androgen receptor modulators based on 7H-[1,4]oxazino[3,2-g]quinolin-7-ones. J Med Chem 50:2486-96 (2007) [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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM18197
BDBM18161
NameBDBM18197
Synonyms:1-(2,2,2-trifluoroethyl)-9-(trifluoromethyl)-1H,2H,3H,6H,7H-quinolino[7,6-b][1,4]oxazin-7-one | 7H-[1,4]Oxazino[3,2-g]quinolin-7-one based compound, 10f
TypeSmall organic molecule
Emp. Form.C14H10F6N2O2
Mol. Mass.352.2318
SMILESFC(F)(F)CN1CCOc2cc3[nH]c(=O)cc(c3cc12)C(F)(F)F
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: