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TargetGlucocorticoid receptor
LigandBDBM50340671
Substrate/Competitorn/a
Meas. Tech.ChEMBL_739803 (CHEMBL1762863)
Ki 0.4±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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50340671
n/a
NameBDBM50340671
Synonyms:5,7-difluoro-6-(1H-indol-7-yl)-2,2-dimethyl-2,3-dihydroquinolin-4(1H)-one O-ethyl oxime | CHEMBL1762200
TypeSmall organic molecule
Emp. Form.C21H21F2N3O
Mol. Mass.369.4077
SMILESCCO\N=C1/CC(C)(C)Nc2cc(F)c(c(F)c12)-c1cccc2cc[nH]c12 |(32.44,-6.26,;31.1,-7.02,;31.09,-8.55,;29.76,-9.31,;29.75,-10.85,;31.08,-11.63,;31.07,-13.18,;32.39,-12.4,;32.39,-13.94,;29.72,-13.93,;28.4,-13.16,;27.07,-13.91,;25.75,-13.14,;24.42,-13.9,;25.76,-11.6,;27.08,-10.83,;27.09,-9.3,;28.41,-11.61,;24.43,-10.83,;24.43,-9.28,;23.09,-8.51,;21.76,-9.28,;21.76,-10.82,;20.61,-11.86,;21.24,-13.27,;22.77,-13.1,;23.09,-11.59,)|
Structure
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