Reaction Details |
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Target | Glucocorticoid receptor |
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Ligand | BDBM50214944 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_447642 (CHEMBL896649) |
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Ki | 2.5±n/a nM |
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Citation | Ardecky, RJ; Hudson, AR; Phillips, DP; Tyhonas, JS; Deckhut, C; Lau, TL; Li, Y; Martinborough, EA; Roach, SL; Higuchi, RI; Lopez, FJ; Marschke, KB; Miner, JN; Karanewsky, DS; Negro-Vilar, A; Zhi, L 5(Z)-benzylidene-1,2-dihydro-9-hydroxy-10-methoxy-2,2,4-trimethyl-5H-1-aza-6-oxa-chrysenes as non-steroidal glucocorticoid receptor modulators. Bioorg Med Chem Lett17:4158-62 (2007) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Glucocorticoid receptor |
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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
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BDBM50214944 |
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n/a |
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Name | BDBM50214944 |
Synonyms: | 10-methoxy-2,2,4-trimethyl-5-[1-m-tolyl-meth-(Z)-ylidene]-2,4a,5,12a-tetrahydro-1H-6-oxa-1-aza-chrysen-9-ol | CHEMBL232760 |
Type | Small organic molecule |
Emp. Form. | C28H29NO3 |
Mol. Mass. | 427.5348 |
SMILES | COc1c(O)ccc2O\C(=C/c3cccc(C)c3)C3=C(C=CC4NC(C)(C)C=C(C)C34)c12 |w:22.22,30.31,c:21,t:19,28| |
Structure |
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