Reaction Details |
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Target | Androgen receptor |
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Ligand | BDBM18590 |
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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 | 6.0±1.1 nM |
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EC50 | 1.6±0.8 nM |
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Comments | hAR agonist efficacy = 67 +/- 7 % |
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Citation | van Oeveren, A; Motamedi, M; Martinborough, E; Zhao, S; Shen, Y; West, S; Chang, W; Kallel, A; Marschke, KB; López, FJ; Negro-Vilar, A; Zhi, L Novel selective androgen receptor modulators: SAR studies on 6-bisalkylamino-2-quinolinones. Bioorg Med Chem Lett17:1527-31 (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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BDBM18590 |
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BDBM18161 |
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Name | BDBM18590 |
Synonyms: | 6-[(2,2-dichloroethyl)(2,2,2-trifluoroethyl)amino]-4-(trifluoromethyl)-1,2-dihydroquinolin-2-one | 6-bisalkylamino-2-quinolinone, 6o |
Type | Small organic molecule |
Emp. Form. | C14H10Cl2F6N2O |
Mol. Mass. | 407.138 |
SMILES | FC(F)(F)CN(CC(Cl)Cl)c1ccc2[nH]c(=O)cc(c2c1)C(F)(F)F |
Structure |
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