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TargetAndrogen Receptor
LigandBDBM18579
Substrate/CompetitorBDBM18161
Meas. Tech.AR Transcriptional Activation Assay and MDA Whole-Cell Binding Assay
pH7.4±n/a
Temperature310.15±n/a K
Ki 2.3±n/a nM
EC50 0.4±0 nM
CommentshAR agonist efficacy = 110 +/- 7 %
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 Lett 17:1527-31 (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
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  Blast E-value cutoff:
BDBM18579
BDBM18161
NameBDBM18579
Synonyms:6-[(2-chloro-2,2-difluoroethyl)(2,2-difluoroethyl)amino]-4-(trifluoromethyl)-1,2-dihydroquinolin-2-one | 6-bisalkylamino-2-quinolinone, 6d
TypeSmall organic molecule
Emp. Form.C14H10ClF7N2O
Mol. Mass.390.684
SMILESFC(F)CN(CC(F)(F)Cl)c1ccc2[nH]c(=O)cc(c2c1)C(F)(F)F
Structure
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