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TargetGlucocorticoid receptor
LigandBDBM50372926
Substrate/Competitorn/a
Meas. Tech.ChEMBL_466159 (CHEMBL950163)
Ki 5.1±n/a nM
Citation Clark, RDRay, NCWilliams, KBlaney, PWard, SCrackett, PHHurley, CDyke, HJClark, DELockey, PDevos, RWong, MPorres, SSBright, CPJenkins, REBelanoff, J 1H-Pyrazolo[3,4-g]hexahydro-isoquinolines as selective glucocorticoid receptor antagonists with high functional activity. Bioorg Med Chem Lett18:1312-7 (2008) [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
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  Blast E-value cutoff:
BDBM50372926
n/a
NameBDBM50372926
Synonyms:CHEMBL411852
TypeSmall organic molecule
Emp. Form.C30H33FN4O3S
Mol. Mass.548.671
SMILESCC(C)(C)c1ccc(cc1)S(=O)(=O)N1CCC2=Cc3c(C[C@]2(COCCC#N)C1)cnn3-c1ccc(F)cc1 |t:17|
Structure
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