Reaction Details |
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Target | Glucocorticoid receptor |
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Ligand | BDBM50338322 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_728111 (CHEMBL1687053) |
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IC50 | 5.9±n/a nM |
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Citation | Hudson, AR; Higuchi, RI; Roach, SL; Adams, ME; Vassar, A; Syka, PM; Mais, DE; Miner, JN; Marschke, KB; Zhi, L Discovery of orally available tetrahydroquinoline-based glucocorticoid receptor agonists. Bioorg Med Chem Lett21:1697-700 (2011) [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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BDBM50338322 |
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n/a |
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Name | BDBM50338322 |
Synonyms: | (+/-)-(3R,4S)-5-fluoro-6-(1H-indol-7-yl)-2,2,4,8-tetramethyl-1,2,3,4-tetrahydroquinolin-3-ol | CHEMBL1682419 |
Type | Small organic molecule |
Emp. Form. | C21H23FN2O |
Mol. Mass. | 338.4185 |
SMILES | C[C@@H]1[C@@H](O)C(C)(C)Nc2c(C)cc(c(F)c12)-c1cccc2cc[nH]c12 |r| |
Structure |
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