| Reaction Details |
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 | Report a problem with these data |
| Target | Glucocorticoid receptor |
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| Ligand | BDBM18628 |
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| Substrate/Competitor | BDBM18207 |
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| Meas. Tech. | Competitive Ligand Binding Assay, GR-Mediated Antagonist Activity Assay, and IL-6 Repression Assay |
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| pH | 7.5±n/a |
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| Temperature | 277.15±n/a K |
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| Ki | 1.4±0.2 nM |
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| IC50 | 0.4±0.1 nM |
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| EC50 | 0.3±0.1 nM |
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| Comments | GRE activation antagonist mode efficacy is 97 +/- 0.5 %. It is a full GRE activation antagonist, which demonstrated reduced agonist activity in the TAT GRE activation assay in comparison to dexamethasone. |
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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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| 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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| BDBM18628 |
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| BDBM18207 |
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| Name | BDBM18628 |
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| Synonyms: | (18Z)-12-methoxy-3,5,5-trimethyl-18-{[3-(2,2,2-trifluoro-1-hydroxyethyl)thiophen-2-yl]methylidene}-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 | secondary alcohol, 15 |
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| Type | Small organic molecule |
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| Emp. Form. | C27H24F3NO4S |
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| Mol. Mass. | 515.544 |
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| SMILES | COc1c(O)ccc2O\C(=C/c3sccc3C(O)C(F)(F)F)c3c(ccc4NC(C)(C)C=C(C)c34)-c12 |t:32| |
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| Structure | 
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