Reaction Details |
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Target | Androgen receptor |
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Ligand | BDBM18525 |
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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 | 70±n/a nM |
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IC50 | 128±25 nM |
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Comments | Antagonist efficacy is 76 +/- 3 %. |
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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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BDBM18525 |
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BDBM18161 |
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Name | BDBM18525 |
Synonyms: | Bicalutamide | CHEMBL409 | N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorobenzene)sulfonyl]-2-hydroxy-2-methylpropanamide | US11046713, Example Bicalutamide | US20230382870, Bicalutumide | US9126941, Bicalutamide | US9682960, CAS |
Type | Small organic molecule |
Emp. Form. | C18H14F4N2O4S |
Mol. Mass. | 430.373 |
SMILES | CC(O)(CS(=O)(=O)c1ccc(F)cc1)C(=O)Nc1ccc(C#N)c(c1)C(F)(F)F |
Structure |
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