Reaction Details |
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Target | Androgen receptor |
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Ligand | BDBM50363359 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_801332 (CHEMBL1947977) |
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IC50 | 371±n/a nM |
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Citation | Guo, C; Kephart, S; Ornelas, M; Gonzalez, J; Linton, A; Pairish, M; Nagata, A; Greasley, S; Elleraas, J; Hosea, N; Engebretsen, J; Fanjul, AN Discovery of 3-aryloxy-lactam analogs as potent androgen receptor full antagonists for treating castration resistant prostate cancer. Bioorg Med Chem Lett22:1230-6 (2012) [PubMed] Article |
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More Info.: | Get all data from this article, 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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BDBM50363359 |
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n/a |
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Name | BDBM50363359 |
Synonyms: | CHEMBL1947183 |
Type | Small organic molecule |
Emp. Form. | C18H21F3N2O3 |
Mol. Mass. | 370.3661 |
SMILES | CC(CO)CN1CC(C)(C)[C@@H](Oc2ccc(C#N)c(c2)C(F)(F)F)C1=O |r| |
Structure |
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