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TargetGlucocorticoid receptor
LigandBDBM18721
Substrate/CompetitorBDBM18207
Meas. Tech.Fluorescence Polarization Competitive Binding Assay.
pH7.4±n/a
Temperature295.15±n/a K
IC50 84±n/a nM
Citation Takahashi, HBekkali, YCapolino, AJGilmore, TGoldrick, SEKaplita, PVLiu, LNelson, RMTerenzio, DWang, JZuvela-Jelaska, LProudfoot, JNabozny, GThomson, D Discovery and SAR study of novel dihydroquinoline-containing glucocorticoid receptor agonists. Bioorg Med Chem Lett17:5091-5 (2007) [PubMed]  Article
More Info.:Get all data from this article,  Inhibition_Run data,   Solution Info,  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:
BDBM18721
BDBM18207
NameBDBM18721
Synonyms:6-(5-fluoro-2-methoxyphenyl)-2,2-dimethyl-4-{[(2-phenylethyl)sulfanyl]methyl}-1,2-dihydroquinoline | dihydroquinoline compound, 44 | dihydroquinoline-based ligand, 37
TypeSmall organic molecule
Emp. Form.C27H28FNOS
Mol. Mass.433.581
SMILESCOc1ccc(F)cc1-c1ccc2NC(C)(C)C=C(CSCCc3ccccc3)c2c1 |t:18|
Structure
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