Reaction Details |
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Target | Progesterone receptor |
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Ligand | BDBM18656 |
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Substrate/Competitor | BDBM18660 |
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Meas. Tech. | Luciferase Reporter Assay |
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Ki | 3300±n/a nM |
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Citation | Kinoyama, I; Taniguchi, N; Toyoshima, A; Nozawa, E; Kamikubo, T; Imamura, M; Matsuhisa, A; Samizu, K; Kawanimani, E; Niimi, T; Hamada, N; Koutoku, H; Furutani, T; Kudoh, M; Okada, M; Ohta, M; Tsukamoto, S (+)-(2R,5S)-4-[4-cyano-3-(trifluoromethyl)phenyl]-2,5-dimethyl-N-[6-(trifluoromethyl)pyridin-3- yl]piperazine-1-carboxamide (YM580) as an orally potent and peripherally selective nonsteroidal androgen receptor antagonist. J Med Chem49:716-26 (2006) [PubMed] Article |
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More Info.: | Get all data from this article, Solution Info, Assay Method |
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Progesterone receptor |
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Name: | Progesterone receptor |
Synonyms: | Nr3c3 | Nuclear receptor subfamily 3 group C member 3 | PR | PRGR_RAT | Pgr | Progesterone Receptor (PR) | Progesterone receptor |
Type: | PROTEIN |
Mol. Mass.: | 99414.34 |
Organism: | Rattus norvegicus |
Description: | ChEMBL_159714 |
Residue: | 923 |
Sequence: | MTELQAKDPRTLHTSGAAPSPTHVGSPLLARLDPDPFQGSQHSDASSVVSPIPISLDRLL
FSRSCQAQELPDEKTQNQQSLSDVEGAFSGVEASRRRSRNPRAPEKDSRLLDSVLDTLLA
PSGPEQSQTSPPACEAITSWCLFGPELPEDPRSVPATKGLLSPLMSRPESKAGDSSGTGA
GQKVLPKAVSPPRQLLLPTSGSAHWPGAGVKPSQQPATVEVEEDGGLETEGSAGPLLKSK
PRALEGMCSGGGVTANAPGAAPGGVTLVPKEDSRFSAPRVSLEQDAPVAPGRSPLATTVV
DFIHVPILPLNHALLAARTRQLLEGDSYDGGAAAQVPFAPPRGSPSAPSPPVPCGDFPDC
TYPPEGDPKEDGFPVYGEFQPPGLKIKEEEEGTEAASRSPRPYLLAGASAATFPDFPLPP
RPPRAPPSRPGEAAVAAPSAAVSPVSSSGSALECILYKAEGAPPTQGSFAPLPCKPPAAS
SCLLPRDSLPAAPTSSAAPAIYPPLGLNGLPQLGYQAAVLKDSLPQVYPPYLNYLRPDSE
ASQSPQYGFDSLPQKICLICGDEASGCHYGVLTCGSCKVFFKRAMEGQHNYLCAGRNDCI
VDKIRRKNCPACRLRKCCQAGMVLGGRKFKKFNKVRVMRALDGVALPQSVAFPNESQTLG
QRITFSPNQEIQLVPPLINLLMSIEPDVVYAGHDNTKPDTSSSLLTSLNQLGERQLLSVV
KWSKSLPGFRNLHIDDQITLIQYSWMSLMVFGLGWRSYKHVSGQMLYFAPDLILNEQRMK
ELSFYSLCLTMWQIPQEFVKLQVTHEEFLCMKVLLLLNTIPLEGLRSQSQFEEMRSSYIR
ELIKAIGLRQKGVVPSSQRFYQLTKLLDSLHDLVKQLHLYCLNTFIQSRALAVEFPEMMS
EVIAAQLPKILAGMVKPLLFHKK
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BDBM18656 |
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BDBM18660 |
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Name | BDBM18656 |
Synonyms: | (2R,5S)-4-[4-cyano-3-(trifluoromethyl)phenyl]-2,5-dimethyl-N-[6-(trifluoromethyl)pyridin-3-yl]piperazine-1-carboxamide | N-Arylpiperazine-1-carboxamide Derivative, 33a | YM580 |
Type | Small organic molecule |
Emp. Form. | C21H19F6N5O |
Mol. Mass. | 471.3989 |
SMILES | C[C@@H]1CN([C@@H](C)CN1C(=O)Nc1ccc(nc1)C(F)(F)F)c1ccc(C#N)c(c1)C(F)(F)F |r| |
Structure |
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