Reaction Details |
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Target | Androgen receptor |
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Ligand | BDBM18522 |
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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 | 1.5±0.2 nM |
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EC50 | 7.1±0.4 nM |
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Comments | Agonist efficacy is 109 +/- 13 %.With I.V. dosing, the half-life was 2.7 h. Oral dosing at 14.6 mg/kg resulted in an AUC of 11.8 ug.h/mL with oral bioavailability of 100%. |
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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 |
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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BDBM18522 |
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BDBM18161 |
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Name | BDBM18522 |
Synonyms: | 6-(1-Pyrrolidine)quinolin-2(1H)-one, 6a | 6-[(2R,5R)-2-methyl-5-[(1R)-2,2,2-trifluoro-1-hydroxyethyl]pyrrolidin-1-yl]-4-(trifluoromethyl)-1,2-dihydroquinolin-2-one | CHEMBL467888 | LGD2941 |
Type | Small organic molecule |
Emp. Form. | C17H16F6N2O2 |
Mol. Mass. | 394.3116 |
SMILES | C[C@@H]1CC[C@H]([C@@H](O)C(F)(F)F)N1c1ccc2[nH]c(=O)cc(c2c1)C(F)(F)F |r| |
Structure |
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