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TargetGlucocorticoid receptor
LigandBDBM50014433
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1350754 (CHEMBL3266139)
IC50 4.5±n/a nM
Citation Edman, KAhlgren, RBengtsson, MBladh, HBäckström, SDahmén, JHenriksson, KHillertz, PHulikal, VJerre, AKinchin, LKåse, CLepistö, MMile, INilsson, SSmailagic, ATaylor, JTjörnebo, AWissler, LHansson, T The discovery of potent and selective non-steroidal glucocorticoid receptor modulators, suitable for inhalation. Bioorg Med Chem Lett24:2571-7 (2014) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Glucocorticoid receptor
Name:Glucocorticoid receptor
Synonyms:GCR_RAT | Glucocorticoid | Glucocorticoid Receptor (GR) | Glucocorticoid receptor | Grl | Nr3c1
Type:Enzyme Catalytic Domain
Mol. Mass.:87556.83
Organism:RAT
Description:Glucocorticoid 0 RAT::P06536
Residue:795
Sequence:
MDSKESLAPPGRDEVPGSLLGQGRGSVMDFYKSLRGGATVKVSASSPSVAAASQADSKQQ
RILLDFSKGSTSNVQQRQQQQQQQQQQQQQQQQQQQPDLSKAVSLSMGLYMGETETKVMG
NDLGYPQQGQLGLSSGETDFRLLEESIANLNRSTSVPENPKSSTSATGCATPTEKEFPKT
HSDASSEQQNRKSQTGTNGGSVKLYPTDQSTFDLLKDLEFSAGSPSKDTNESPWRSDLLI
DENLLSPLAGEDDPFLLEGNTNEDCKPLILPDTKPKIKDTGDTILSSPSSVALPQVKTEK
DDFIELCTPGVIKQEKLGPVYCQASFSGTNIIGNKMSAISVHGVSTSGGQMYHYDMNTAS
LSQQQDQKPVFNVIPPIPVGSENWNRCQGSGEDSLTSLGALNFPGRSVFSNGYSSPGMRP
DVSSPPSSSSAATGPPPKLCLVCSDEASGCHYGVLTCGSCKVFFKRAVEGQHNYLCAGRN
DCIIDKIRRKNCPACRYRKCLQAGMNLEARKTKKKIKGIQQATAGVSQDTSENPNKTIVP
AALPQLTPTLVSLLEVIEPEVLYAGYDSSVPDSAWRIMTTLNMLGGRQVIAAVKWAKAIL
GLRNLHLDDQMTLLQYSWMFLMAFALGWRSYRQSSGNLLCFAPDLIINEQRMSLPCMYDQ
CKHMLFVSSELQRLQVSYEEYLCMKTLLLLSSVPKEGLKSQELFDEIRMTYIKELGKAIV
KREGNSSQNWQRFYQLTKLLDSMHEVVENLLTYCFQTFLDKTMSIEFPEMLAEIITNQIP
KYSNGNIKKLLFHQK
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50014433
n/a
NameBDBM50014433
Synonyms:CHEMBL3261425
TypeSmall organic molecule
Emp. Form.C25H30FN7O2S
Mol. Mass.511.615
SMILESC[C@@H](CNc1cccc2n(ncc12)-c1ccc(F)nc1)NS(=O)(=O)c1c(C)nn(C2CCCC2)c1C |r|
Structure
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