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Target
Glucocorticoid receptor
Ligand
BDBM50577709
Substrate
n/a
Meas. Tech.
ChEMBL_2130771 (CHEMBL4840200)
IC50
251±n/a nM
Citation
 Kennedy, BJ; Lato, AM; Fisch, AR; Burke, SJ; Kirkland, JK; Prevatte, CW; Dunlap, LE; Smith, RT; Vogiatzis, KD; Collier, JJ; Campagna, SR Potent Anti-Inflammatory, Arylpyrazole-Based Glucocorticoid Receptor Agonists That Do Not Impair Insulin Secretion. ACS Med Chem Lett 12:1568-1577 (2021) [PubMed]  Article
Target
Name:
Glucocorticoid receptor
Synonyms:
GCR_RAT | Glucocorticoid | Glucocorticoid Receptor (GR) | Glucocorticoid receptor | Grl | Nr3c1
Type:
Enzyme Catalytic Domain
Mol. Mass.:
87556.83
Organism:
RAT
Description:
Glucocorticoid 0 RAT::P06536
Residue:
795
Sequence:
MDSKESLAPPGRDEVPGSLLGQGRGSVMDFYKSLRGGATVKVSASSPSVAAASQADSKQQRILLDFSKGSTSNVQQRQQQQQQQQQQQQQQQQQQQPDLSKAVSLSMGLYMGETETKVMGNDLGYPQQGQLGLSSGETDFRLLEESIANLNRSTSVPENPKSSTSATGCATPTEKEFPKTHSDASSEQQNRKSQTGTNGGSVKLYPTDQSTFDLLKDLEFSAGSPSKDTNESPWRSDLLIDENLLSPLAGEDDPFLLEGNTNEDCKPLILPDTKPKIKDTGDTILSSPSSVALPQVKTEKDDFIELCTPGVIKQEKLGPVYCQASFSGTNIIGNKMSAISVHGVSTSGGQMYHYDMNTASLSQQQDQKPVFNVIPPIPVGSENWNRCQGSGEDSLTSLGALNFPGRSVFSNGYSSPGMRPDVSSPPSSSSAATGPPPKLCLVCSDEASGCHYGVLTCGSCKVFFKRAVEGQHNYLCAGRNDCIIDKIRRKNCPACRYRKCLQAGMNLEARKTKKKIKGIQQATAGVSQDTSENPNKTIVPAALPQLTPTLVSLLEVIEPEVLYAGYDSSVPDSAWRIMTTLNMLGGRQVIAAVKWAKAILGLRNLHLDDQMTLLQYSWMFLMAFALGWRSYRQSSGNLLCFAPDLIINEQRMSLPCMYDQCKHMLFVSSELQRLQVSYEEYLCMKTLLLLSSVPKEGLKSQELFDEIRMTYIKELGKAIVKREGNSSQNWQRFYQLTKLLDSMHEVVENLLTYCFQTFLDKTMSIEFPEMLAEIITNQIPKYSNGNIKKLLFHQK
  
Inhibitor
Name:
BDBM50577709
Synonyms:
CHEMBL4867686
Type:
Small organic molecule
Emp. Form.:
C27H29FN2O2
Mol. Mass.:
432.5298
SMILES:
[H][C@@]1(CCCC2=Cc3c(C[C@]12C)cnn3-c1ccc(OC)cc1)[C@@](C)(O)c1ccc(F)cc1 |r,t:5|
Structure:
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