Reaction Details |
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Target | Androgen receptor |
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Ligand | BDBM18543 |
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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 | 50±7 nM |
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IC50 | 67±11 nM |
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Comments | hAR antagonist efficacy = 86 +/- 2 %. |
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Citation | van Oeveren, A; Pio, BA; Tegley, CM; Higuchi, RI; Wu, M; Jones, TK; Marschke, KB; Negro-Vilar, A; Zhi, L Discovery of an androgen receptor modulator pharmacophore based on 2-quinolinones. Bioorg Med Chem Lett17:1523-6 (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 |
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.
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Residue: | 920 |
Sequence: | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQ
QQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQ
SALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSAD
LKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELC
KAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAG
KSTEDTAEYSPFKGGYTKGLEGESLGCSGSAAAGSSGTLELPSTLSLYKSGALDEAAAYQ
SRDYYNFPLALAGPPPPPPPPHPHARIKLENPLDYGSAWAAAAAQCRYGDLASLHGAGAA
GPGSGSPSAAASSSWHTLFTAEEGQLYGPCGGGGGGGGGGGGGGGGGGGGGGGEAGAVAP
YGYTRPPQGLAGQESDFTAPDVWYPGGMVSRVPYPSPTCVKSEMGPWMDSYSGPYGDMRL
ETARDHVLPIDYYFPPQKTCLICGDEASGCHYGALTCGSCKVFFKRAAEGKQKYLCASRN
DCTIDKFRRKNCPSCRLRKCYEAGMTLGARKLKKLGNLKLQEEGEASSTTSPTEETTQKL
TVSHIEGYECQPIFLNVLEAIEPGVVCAGHDNNQPDSFAALLSSLNELGERQLVHVVKWA
KALPGFRNLHVDDQMAVIQYSWMGLMVFAMGWRSFTNVNSRMLYFAPDLVFNEYRMHKSR
MYSQCVRMRHLSQEFGWLQITPQEFLCMKALLLFSIIPVDGLKNQKFFDELRMNYIKELD
RIIACKRKNPTSCSRRFYQLTKLLDSVQPIARELHQFTFDLLIKSHMVSVDFPEMMAEII
SVQVPKILSGKVKPIYFHTQ
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BDBM18543 |
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BDBM18161 |
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Name | BDBM18543 |
Synonyms: | 7-(butylamino)-4-(trifluoromethyl)-1,2-dihydroquinolin-2-one | alkylamino-2-quinolinone, 9c |
Type | Small organic molecule |
Emp. Form. | C14H15F3N2O |
Mol. Mass. | 284.2769 |
SMILES | CCCCNc1ccc2c(cc(=O)[nH]c2c1)C(F)(F)F |
Structure |
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