| Reaction Details |
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 | Report a problem with these data |
| Target | Glucocorticoid receptor |
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| Ligand | BDBM18627 |
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| Substrate/Competitor | BDBM18207 |
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| Meas. Tech. | GR Binding Assay and GRAF Assay |
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| pH | 8±n/a |
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| Temperature | 277.15±n/a K |
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| IC50 | 1.1±n/a nM |
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| EC50 | 4.8±n/a nM |
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| Comments | VP16 agonism = 59 %. |
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| Citation |  Link, JT; Sorensen, B; Patel, J; Grynfarb, M; Goos-Nilsson, A; Wang, J; Fung, S; Wilcox, D; Zinker, B; Nguyen, P; Hickman, B; Schmidt, JM; Swanson, S; Tian, Z; Reisch, TJ; Rotert, G; Du, J; Lane, B; von Geldern, TW; Jacobson, PB Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators. J Med Chem48:5295-304 (2005) [PubMed] Article |
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| More Info.: | Get all data from this article, Solution Info, Assay Method |
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| Glucocorticoid receptor |
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| Name: | Glucocorticoid receptor |
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| Synonyms: | GCR_HUMAN | GR | GRL | Glucocorticoid | Glucocorticoid receptor (GRFP) | NR3C1 | Nuclear receptor subfamily 3 group C member 1 |
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| Type: | Enzyme |
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| Mol. Mass.: | 85656.87 |
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| Organism: | Homo sapiens (Human) |
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| Description: | P04150 |
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| Residue: | 777 |
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| Sequence: | MDSKESLTPGREENPSSVLAQERGDVMDFYKTLRGGATVKVSASSPSLAVASQSDSKQRR
LLVDFPKGSVSNAQQPDLSKAVSLSMGLYMGETETKVMGNDLGFPQQGQISLSSGETDLK
LLEESIANLNRSTSVPENPKSSASTAVSAAPTEKEFPKTHSDVSSEQQHLKGQTGTNGGN
VKLYTTDQSTFDILQDLEFSSGSPGKETNESPWRSDLLIDENCLLSPLAGEDDSFLLEGN
SNEDCKPLILPDTKPKIKDNGDLVLSSPSNVTLPQVKTEKEDFIELCTPGVIKQEKLGTV
YCQASFPGANIIGNKMSAISVHGVSTSGGQMYHYDMNTASLSQQQDQKPIFNVIPPIPVG
SENWNRCQGSGDDNLTSLGTLNFPGRTVFSNGYSSPSMRPDVSSPPSSSSTATTGPPPKL
CLVCSDEASGCHYGVLTCGSCKVFFKRAVEGQHNYLCAGRNDCIIDKIRRKNCPACRYRK
CLQAGMNLEARKTKKKIKGIQQATTGVSQETSENPGNKTIVPATLPQLTPTLVSLLEVIE
PEVLYAGYDSSVPDSTWRIMTTLNMLGGRQVIAAVKWAKAIPGFRNLHLDDQMTLLQYSW
MFLMAFALGWRSYRQSSANLLCFAPDLIINEQRMTLPCMYDQCKHMLYVSSELHRLQVSY
EEYLCMKTLLLLSSVPKDGLKSQELFDEIRMTYIKELGKAIVKREGNSSQNWQRFYQLTK
LLDSMHEVVENLLNYCFQTFLDKTMSIEFPEMLAEIITNQIPKYSNGNIKKLLFHQK
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| BDBM18627 |
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| BDBM18207 |
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| Name | BDBM18627 |
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| Synonyms: | (10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]-14-hydroxy-15-methyl-14-(prop-1-yn-1-yl)tetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-1,6-dien-5-one | Mifeprex | Mifepristone | RU-486 | RU486 (tetramethyl-rhodamine conjugated) |
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| Type | Small organic molecule |
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| Emp. Form. | C29H35NO2 |
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| Mol. Mass. | 429.5937 |
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| SMILES | [H][C@@]12CC[C@@](O)(C#CC)[C@@]1(C)C[C@@H](C1=C3CCC(=O)C=C3CC[C@@]21[H])c1ccc(cc1)N(C)C |r,c:14,20| |
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| Structure | 
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