Reaction Details |
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Target | Progesterone receptor |
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Ligand | BDBM18616 |
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Substrate/Competitor | BDBM8903 |
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Meas. Tech. | Competitive Ligand Binding Assay, GR-Mediated Agonist Activity Assay, and IL-6 Repression Assay |
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Ki | 1400±n/a nM |
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Citation | Hudson, AR; Roach, SL; Higuchi, RI; Phillips, DP; Bissonnette, RP; Lamph, WW; Yen, J; Li, Y; Adams, ME; Valdez, LJ; Vassar, A; Cuervo, C; Kallel, EA; Gharbaoui, CJ; Mais, DE; Miner, JN; Marschke, KB; Rungta, D; Negro-Vilar, A; Zhi, L Synthesis and characterization of nonsteroidal glucocorticoid receptor modulators for multiple myeloma. J Med Chem50:4699-709 (2007) [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 | PGR | PR | PRGR_HUMAN | progesterone |
Type: | Protein |
Mol. Mass.: | 98979.52 |
Organism: | Homo sapiens (Human) |
Description: | P06401 |
Residue: | 933 |
Sequence: | MTELKAKGPRAPHVAGGPPSPEVGSPLLCRPAAGPFPGSQTSDTLPEVSAIPISLDGLLF
PRPCQGQDPSDEKTQDQQSLSDVEGAYSRAEATRGAGGSSSSPPEKDSGLLDSVLDTLLA
PSGPGQSQPSPPACEVTSSWCLFGPELPEDPPAAPATQRVLSPLMSRSGCKVGDSSGTAA
AHKVLPRGLSPARQLLLPASESPHWSGAPVKPSPQAAAVEVEEEDGSESEESAGPLLKGK
PRALGGAAAGGGAAAVPPGAAAGGVALVPKEDSRFSAPRVALVEQDAPMAPGRSPLATTV
MDFIHVPILPLNHALLAARTRQLLEDESYDGGAGAASAFAPPRSSPCASSTPVAVGDFPD
CAYPPDAEPKDDAYPLYSDFQPPALKIKEEEEGAEASARSPRSYLVAGANPAAFPDFPLG
PPPPLPPRATPSRPGEAAVTAAPASASVSSASSSGSTLECILYKAEGAPPQQGPFAPPPC
KAPGASGCLLPRDGLPSTSASAAAAGAAPALYPALGLNGLPQLGYQAAVLKEGLPQVYPP
YLNYLRPDSEASQSPQYSFESLPQKICLICGDEASGCHYGVLTCGSCKVFFKRAMEGQHN
YLCAGRNDCIVDKIRRKNCPACRLRKCCQAGMVLGGRKFKKFNKVRVVRALDAVALPQPV
GVPNESQALSQRFTFSPGQDIQLIPPLINLLMSIEPDVIYAGHDNTKPDTSSSLLTSLNQ
LGERQLLSVVKWSKSLPGFRNLHIDDQITLIQYSWMSLMVFGLGWRSYKHVSGQMLYFAP
DLILNEQRMKESSFYSLCLTMWQIPQEFVKLQVSQEEFLCMKVLLLLNTIPLEGLRSQTQ
FEEMRSSYIRELIKAIGLRQKGVVSSSQRFYQLTKLLDNLHDLVKQLHLYCLNTFIQSRA
LSVEFPEMMSEVIAAQLPKILAGMVKPLLFHKK
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BDBM18616 |
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BDBM8903 |
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Name | BDBM18616 |
Synonyms: | (18Z)-18-{[3-(hydroxymethyl)thiophen-2-yl]methylidene}-12-methoxy-3,5,5-trimethyl-17-oxa-6-azatetracyclo[8.8.0.0^{2,7}.0^{11,16}]octadeca-1(10),2(7),3,8,11,13,15-heptaen-13-ol | Alcohol, 8 |
Type | Small organic molecule |
Emp. Form. | C26H25NO4S |
Mol. Mass. | 447.546 |
SMILES | COc1c(O)ccc2O\C(=C/c3sccc3CO)c3c(ccc4NC(C)(C)C=C(C)c34)-c12 |t:28| |
Structure |
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