Reaction Details |
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Target | Androgen receptor |
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Ligand | BDBM18675 |
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Substrate/Competitor | BDBM26258 |
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Meas. Tech. | Competitive Radioligand Displacement Assay |
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pH | 7.4±n/a |
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Temperature | 277.15±n/a K |
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Ki | 4.6±0.3 nM |
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Comments | IC50=17400 +/- 4900 for inhibiting growth of prostate cancer cell line, LNCaP. |
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Citation | Hwang, DJ; Yang, J; Xu, H; Rakov, IM; Mohler, ML; Dalton, JT; Miller, DD Arylisothiocyanato selective androgen receptor modulators (SARMs) for prostate cancer. Bioorg Med Chem14:6525-38 (2006) [PubMed] Article |
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More Info.: | Get all data from this article, Inhibition_Run data, Solution Info, Assay Method |
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Androgen receptor |
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Name: | Androgen receptor |
Synonyms: | ANDR_RAT | Androgen receptor (AR) | Ar | Estrogen receptor | Nr3c4 | androgen |
Type: | Enzyme |
Mol. Mass.: | 98219.08 |
Organism: | Rattus norvegicus (Rat) |
Description: | P15207 |
Residue: | 902 |
Sequence: | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREAIQNPGPRHPEAASIAPPGACLQQRQET
SPRRRRRQQHPEDGSPQAHIRGTTGYLALEEEQQPSQQQSASEGHPESGCLPEPGAATAP
GKGLPQQPPAPPDQDDSAAPSTLSLLGPTFPGLSSCSADIKDILSEAGTMQLLQQQQQQQ
QQQQQQQQQQQQQQQEVISEGSSSVRAREATGAPSSSKDSYLGGNSTISDSAKELCKAVS
VSMGLGVEALEHLSPGEQLRGDCMYASLLGGPPAVRPTPCAPLAECKGLSLDEGPGKGTE
ETAEYSSFKGGYAKGLEGESLGCSGSSEAGSSGTLEIPSSLSLYKSGAVDEAAAYQNRDY
YNFPLALSGPPHPPPPTHPHARIKLENPSDYGSAWAAAAAQCRYGDLASLHGGSVAGPST
GSPPATASSSWHTLFTAEEGQLYGPGGGGGSSSPSDAGPVAPYGYTRPPQGLASQEGDFS
ASEVWYPGGVVNRVPYPSPSCVKSEMGPWMENYSGPYGDMRLDSTRDHVLPIDYYFPPQK
TCLICGDEASGCHYGALTCGSCKVFFKRAAEGKQKYLCASRNDCTIDKFRRKNCPSCRLR
KCYEAGMTLGARKLKKLGNLKLQEEGENSSAGSPTEDPSQKMTVSHIEGYECQPIFLNVL
EAIEPGVVCAGHDNNQPDSFAALLSSLNELGERQLVHVVKWAKALPGFRNLHVDDQMAVI
QYSWMGLMVFAMGWRSFTNVNSRMLYFAPDLVFNEYRMHKSRMYSQCVRMRHLSQEFGWL
QITPQEFLCMKALLLFSIIPVDGLKNQKFFDELRMNYIKELDRIIACKRKNPTSCSRRFY
QLTKLLDSVQPIARELHQFTFDLLIKSHMVSVDFPEMMAEIISVQVPKILSGKVKPIYFH
TQ
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BDBM18675 |
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BDBM26258 |
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Name | BDBM18675 |
Synonyms: | (2S)-2-hydroxy-3-(4-isothiocyanatophenoxy)-2-methyl-N-[4-nitro-3-(trifluoromethyl)phenyl]propanamide | BMC146525 arylisothiocyanato derivative, S-23 | Nonsteroidal AR Ligand, S-16 |
Type | Small organic molecule |
Emp. Form. | C18H14F3N3O5S |
Mol. Mass. | 441.381 |
SMILES | CC(O)(COc1ccc([N-]C#[S+])cc1)C(=O)Nc1ccc(c(c1)C(F)(F)F)[N+]([O-])=O |
Structure |
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