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TargetGlucocorticoid receptor
LigandBDBM50417882
Substrate/Competitorn/a
Meas. Tech.ChEMBL_716756 (CHEMBL1670638)
IC50 2±n/a nM
Citation Diallo, HAngell, DCBarnett, HABiggadike, KCoe, DMCooper, TWCraven, AGray, JRHouse, DJack, TIKeeling, SPMacdonald, SJMcLay, IMOliver, STaylor, SJUings, IJWellaway, N Discovery of a potent series of non-steroidal nona-trifluoromethyl carbinol glucocorticoid receptor agonists with reduced lipophilicity. Bioorg Med Chem Lett21:1126-33 (2011) [PubMed]  Article
More Info.:Get all data from this article,  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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50417882
n/a
NameBDBM50417882
Synonyms:CHEMBL1668072
TypeSmall organic molecule
Emp. Form.C29H37N5O2S
Mol. Mass.519.701
SMILESCC(C)Nc1ccc(cc1)-n1ncc2c(NC[C@H](C)NS(=O)(=O)c3c(C)cc(C)cc3C)cc(C)cc12 |r|
Structure
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