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TargetGlucocorticoid receptor
LigandBDBM50041911
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1446327 (CHEMBL3374293)
IC50 17±n/a nM
Citation Harcken, CRiether, DLiu, PRazavi, HPatel, ULee, TBosanac, TWard, YRalph, MChen, ZSouza, DNelson, RMKukulka, AFadra-Khan, TNZuvela-Jelaska, LPatel, MThomson, DSNabozny, GH Optimization of drug-like properties of nonsteroidal glucocorticoid mimetics and identification of a clinical candidate. ACS Med Chem Lett5:1318-23 (2014) [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:
BDBM50041911
n/a
NameBDBM50041911
Synonyms:CHEMBL3358932
TypeSmall organic molecule
Emp. Form.C24H28F3N3O2
Mol. Mass.447.4932
SMILESCC(C)(CC(O)(Cc1cc2cc(ncc2[nH]1)N1CCOCC1)C(F)(F)F)c1ccccc1
Structure
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