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TargetGlucocorticoid receptor
LigandBDBM50110731
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1510382
Ki 2.7±n/a nM
Citation Luz JGCarson MWCondon BClawson DPustilnik AKohlman DTBarr RJBean JSDill MJSindelar DKMaletic MCoghlan MJ Indole Glucocorticoid Receptor Antagonists Active in a Model of Dyslipidemia Act via a Unique Association with an Agonist Binding Site. J Med Chem 58:6607-18 (2015) [PubMed]
More Info.:Get all data from this article,  Assay Method
 
Glucocorticoid receptor
Name:Glucocorticoid receptor
Synonyms:GR | Glucocorticoid | Glucocorticoid receptor (GRFP) | 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:
BDBM50110731
n/a
NameBDBM50110731
Synonyms:CHEMBL3605926
TypeSmall organic molecule
Emp. Form.C29H34FN3O3S
Mol. Mass.523.662
SMILESCOc1cc(F)ccc1-c1c(CN(C)Cc2ccccc2)[nH]c2c(NS(C)(=O)=O)cc(cc12)C(C)(C)C |(-1,4.66,;-.24,3.69,;1.29,3.91,;1.86,5.34,;3.38,5.55,;3.84,6.7,;4.33,4.34,;3.76,2.91,;2.23,2.7,;1.76,1.24,;2.66,.02,;4.2,.03,;4.98,-1.29,;4.37,-2.37,;6.52,-1.28,;7.3,-2.61,;8.84,-2.59,;9.62,-3.92,;8.87,-5.26,;7.33,-5.27,;6.54,-3.95,;1.76,-1.24,;.3,-.77,;-1.03,-1.55,;-1.02,-3.09,;-2.35,-3.87,;-3.42,-3.26,;-2.35,-5.1,;-3.42,-4.49,;-2.38,-.77,;-2.38,.77,;-1.03,1.55,;.3,.77,;-3.72,1.53,;-4.78,.91,;-3.72,2.76,;-4.79,2.14,)|
Structure
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