| Reaction Details |
|---|
 | Report a problem with these data |
| Target | Glucocorticoid receptor |
|---|
| Ligand | BDBM18632 |
|---|
| Substrate/Competitor | BDBM18207 |
|---|
| Meas. Tech. | Competitive Ligand Binding Assay, GR-Mediated Antagonist Activity Assay, and IL-6 Repression Assay |
|---|
| pH | 7.5±n/a |
|---|
| Temperature | 277.15±n/a K |
|---|
| Ki | 1.2±n/a nM |
|---|
| IC50 | 1.6±0.1 nM |
|---|
| EC50 | 1.3±0.9 nM |
|---|
| Comments | GRE activation antagonist mode efficacy is 96 +/- 2.3 %. |
|---|
| 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 |
|---|
| More Info.: | Get all data from this article, Solution Info, Assay Method |
|---|
| |
| Glucocorticoid receptor |
|---|
| Name: | Glucocorticoid receptor |
|---|
| Synonyms: | GCR_HUMAN | GR | GRL | Glucocorticoid | Glucocorticoid receptor (GRFP) | NR3C1 | Nuclear receptor subfamily 3 group C member 1 |
|---|
| Type: | Enzyme |
|---|
| Mol. Mass.: | 85656.87 |
|---|
| Organism: | Homo sapiens (Human) |
|---|
| Description: | P04150 |
|---|
| Residue: | 777 |
|---|
| Sequence: | MDSKESLTPGREENPSSVLAQERGDVMDFYKTLRGGATVKVSASSPSLAVASQSDSKQRR
LLVDFPKGSVSNAQQPDLSKAVSLSMGLYMGETETKVMGNDLGFPQQGQISLSSGETDLK
LLEESIANLNRSTSVPENPKSSASTAVSAAPTEKEFPKTHSDVSSEQQHLKGQTGTNGGN
VKLYTTDQSTFDILQDLEFSSGSPGKETNESPWRSDLLIDENCLLSPLAGEDDSFLLEGN
SNEDCKPLILPDTKPKIKDNGDLVLSSPSNVTLPQVKTEKEDFIELCTPGVIKQEKLGTV
YCQASFPGANIIGNKMSAISVHGVSTSGGQMYHYDMNTASLSQQQDQKPIFNVIPPIPVG
SENWNRCQGSGDDNLTSLGTLNFPGRTVFSNGYSSPSMRPDVSSPPSSSSTATTGPPPKL
CLVCSDEASGCHYGVLTCGSCKVFFKRAVEGQHNYLCAGRNDCIIDKIRRKNCPACRYRK
CLQAGMNLEARKTKKKIKGIQQATTGVSQETSENPGNKTIVPATLPQLTPTLVSLLEVIE
PEVLYAGYDSSVPDSTWRIMTTLNMLGGRQVIAAVKWAKAIPGFRNLHLDDQMTLLQYSW
MFLMAFALGWRSYRQSSANLLCFAPDLIINEQRMTLPCMYDQCKHMLYVSSELHRLQVSY
EEYLCMKTLLLLSSVPKDGLKSQELFDEIRMTYIKELGKAIVKREGNSSQNWQRFYQLTK
LLDSMHEVVENLLNYCFQTFLDKTMSIEFPEMLAEIITNQIPKYSNGNIKKLLFHQK
|
|
|
|---|
| BDBM18632 |
|---|
| BDBM18207 |
|---|
| Name | BDBM18632 |
|---|
| Synonyms: | (18Z)-18-{[3-(1-hydroxyethyl)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, 20 |
|---|
| Type | Small organic molecule |
|---|
| Emp. Form. | C27H27NO4S |
|---|
| Mol. Mass. | 461.573 |
|---|
| SMILES | COc1c(O)ccc2O\C(=C/c3sccc3C(C)O)c3c(ccc4NC(C)(C)C=C(C)c34)-c12 |t:29| |
|---|
| Structure | 
|
|---|
Search and Browse
