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TargetGlucocorticoid receptor
LigandBDBM50340667
Substrate/Competitorn/a
Meas. Tech.ChEMBL_739804 (CHEMBL1762864)
IC50 3.5±n/a nM
Citation Hudson, ARHiguchi, RIRoach, SLValdez, LJAdams, MEVassar, ARungta, DSyka, PMMais, DEMarschke, KBZhi, L Nonsteroidal 2,3-dihydroquinoline glucocorticoid receptor agonists with reduced PEPCK activation. Bioorg Med Chem Lett21:1654-7 (2011) [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:
BDBM50340667
n/a
NameBDBM50340667
Synonyms:5,7-difluoro-6-(1H-indol-7-yl)-2,2-dimethyl-2,3-dihydroquinolin-4(1H)-one O-tert-butyl oxime | CHEMBL1762201
TypeSmall organic molecule
Emp. Form.C23H25F2N3O
Mol. Mass.397.4609
SMILESCC(C)(C)O\N=C1/CC(C)(C)Nc2cc(F)c(c(F)c12)-c1cccc2cc[nH]c12 |(1.19,-17.96,;-.14,-18.72,;-1.46,-17.95,;-.15,-17.18,;-.15,-20.26,;-1.48,-21.02,;-1.49,-22.55,;-.16,-23.34,;-.18,-24.88,;1.14,-24.1,;1.14,-25.65,;-1.52,-25.64,;-2.84,-24.86,;-4.17,-25.62,;-5.49,-24.85,;-6.82,-25.61,;-5.49,-23.31,;-4.16,-22.54,;-4.16,-21,;-2.83,-23.32,;-6.81,-22.53,;-6.81,-20.99,;-8.15,-20.21,;-9.48,-20.99,;-9.49,-22.53,;-10.63,-23.56,;-10.01,-24.97,;-8.47,-24.81,;-8.15,-23.3,)|
Structure
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