| Reaction Details |
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 | Report a problem with these data |
| Target | Androgen receptor |
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| Ligand | BDBM18521 |
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| Substrate/Competitor | BDBM18161 |
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| Meas. Tech. | AR Transcriptional Activation Assay and MDA Whole-Cell Binding Assay |
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| pH | 7.4±n/a |
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| Temperature | 310.15±n/a K |
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| Ki | 10±n/a nM |
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| EC50 | 12±0.2 nM |
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| Comments | Agonist efficacy is 101 +/- 5 %. |
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| Citation |  Martinborough, E; Shen, Y; Oeveren, A; Long, YO; Lau, TL; Marschke, KB; Chang, WY; López, FJ; Vajda, EG; Rix, PJ; Viveros, OH; Negro-Vilar, A; Zhi, L Substituted 6-(1-Pyrrolidine)quinolin-2(1H)-ones as Novel Selective Androgen Receptor Modulators. J Med Chem50:5049-52 (2007) [PubMed] Article |
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| More Info.: | Get all data from this article, Solution Info, Assay Method |
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| Androgen receptor |
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| Name: | Androgen receptor |
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| 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 |
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| Type: | Receptor |
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| Mol. Mass.: | 99185.27 |
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| Organism: | Homo sapiens (Human) |
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| Description: | CHO cells were stably transfected with human AR gene.
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| Residue: | 920 |
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| Sequence: | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQ
QQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQ
SALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSAD
LKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELC
KAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAG
KSTEDTAEYSPFKGGYTKGLEGESLGCSGSAAAGSSGTLELPSTLSLYKSGALDEAAAYQ
SRDYYNFPLALAGPPPPPPPPHPHARIKLENPLDYGSAWAAAAAQCRYGDLASLHGAGAA
GPGSGSPSAAASSSWHTLFTAEEGQLYGPCGGGGGGGGGGGGGGGGGGGGGGGEAGAVAP
YGYTRPPQGLAGQESDFTAPDVWYPGGMVSRVPYPSPTCVKSEMGPWMDSYSGPYGDMRL
ETARDHVLPIDYYFPPQKTCLICGDEASGCHYGALTCGSCKVFFKRAAEGKQKYLCASRN
DCTIDKFRRKNCPSCRLRKCYEAGMTLGARKLKKLGNLKLQEEGEASSTTSPTEETTQKL
TVSHIEGYECQPIFLNVLEAIEPGVVCAGHDNNQPDSFAALLSSLNELGERQLVHVVKWA
KALPGFRNLHVDDQMAVIQYSWMGLMVFAMGWRSFTNVNSRMLYFAPDLVFNEYRMHKSR
MYSQCVRMRHLSQEFGWLQITPQEFLCMKALLLFSIIPVDGLKNQKFFDELRMNYIKELD
RIIACKRKNPTSCSRRFYQLTKLLDSVQPIARELHQFTFDLLIKSHMVSVDFPEMMAEII
SVQVPKILSGKVKPIYFHTQ
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| BDBM18521 |
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| BDBM18161 |
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| Name | BDBM18521 |
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| Synonyms: | 6-(1-Pyrrolidine)quinolin-2(1H)-one, 4f | 6-[(2R,5R)-2-(chloromethyl)-5-methylpyrrolidin-1-yl]-4-(trifluoromethyl)-1,2-dihydroquinolin-2-one |
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| Type | Small organic molecule |
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| Emp. Form. | C16H16ClF3N2O |
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| Mol. Mass. | 344.759 |
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| SMILES | C[C@@H]1CC[C@H](CCl)N1c1ccc2[nH]c(=O)cc(c2c1)C(F)(F)F |r| |
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| Structure | 
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