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TargetGlucocorticoid receptor
LigandBDBM50402494
Substrate/Competitorn/a
Meas. Tech.ChEMBL_886649 (CHEMBL2216234)
Ki 5±n/a nM
Citation Hunt, HJRay, NCHynd, GSutton, JSajad, MO'Connor, EAhmed, SLockey, PDaly, SBuckley, GClark, RDRoe, RBlasey, CBelanoff, J Discovery of a novel non-steroidal GR antagonist with in vivo efficacy in the olanzapine-induced weight gain model in the rat. Bioorg Med Chem Lett22:7376-80 (2012) [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:
BDBM50402494
n/a
NameBDBM50402494
Synonyms:CHEMBL2204047
TypeSmall organic molecule
Emp. Form.C23H22Cl2N2O2
Mol. Mass.429.339
SMILESClc1cccc(Cc2c([nH]c(=O)[nH]c2=O)[C@@H]2CC[C@@H](CC2)c2ccccc2)c1Cl |r,wU:15.15,18.22,(47.9,-44.62,;46.57,-45.39,;45.23,-44.61,;43.88,-45.36,;43.88,-46.9,;45.21,-47.69,;45.21,-49.25,;43.88,-50.03,;43.88,-51.59,;42.53,-52.35,;41.2,-51.59,;39.85,-52.38,;41.2,-50.04,;42.55,-49.27,;42.55,-47.73,;45.19,-52.36,;45.19,-53.9,;46.5,-54.67,;47.84,-53.91,;47.84,-52.37,;46.52,-51.59,;49.17,-54.69,;50.5,-53.93,;51.82,-54.7,;51.82,-56.25,;50.48,-57.01,;49.17,-56.23,;46.57,-46.93,;47.9,-47.71,)|
Structure
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