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TargetAndrogen Receptor
LigandBDBM18524
Substrate/CompetitorBDBM18161
Meas. Tech.AR Transcriptional Activation Assay and MDA Whole-Cell Binding Assay
pH7.4±n/a
Temperature310.15±n/a K
Ki 4.6±n/a nM
EC50 0.2±0.02 nM
CommentsAgonist efficacy is 95 +/- 2 %.With I.V. dosing, the half-life was 1.7 h. Oral dosing at 10 mg/kg resulted in an AUC of 3.15 ug.h/mL with oral bioavailability of 43%.
Citation Martinborough EShen YOeveren ALong YOLau TLMarschke KBChang WYLópez FJVajda EGRix PJViveros OHNegro-Vilar AZhi L Substituted 6-(1-Pyrrolidine)quinolin-2(1H)-ones as Novel Selective Androgen Receptor Modulators. J Med Chem 50:5049-52 (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:
BDBM18524
BDBM18161
NameBDBM18524
Synonyms:6-[bis(2,2,2-trifluoroethyl)amino]-4-(trifluoromethyl)-1,2-dihydroquinolin-2-one | CHEMBL436784 | LGD2226
TypeSmall organic molecule
Emp. Form.C14H9F9N2O
Mol. Mass.392.2197
SMILESFC(F)(F)CN(CC(F)(F)F)c1ccc2[nH]c(=O)cc(c2c1)C(F)(F)F
Structure
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