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TargetGlucocorticoid receptor
LigandBDBM19199
Substrate/Competitorn/a
Meas. Tech.ChEMBL_2130771 (CHEMBL4840200)
IC50 16±n/a nM
Citation Kennedy, BJLato, AMFisch, ARBurke, SJKirkland, JKPrevatte, CWDunlap, LESmith, RTVogiatzis, KDCollier, JJCampagna, SR Potent Anti-Inflammatory, Arylpyrazole-Based Glucocorticoid Receptor Agonists That Do Not Impair Insulin Secretion. ACS Med Chem Lett12:1568-1577 (2021) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Glucocorticoid receptor
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:
MDSKESLAPPGRDEVPGSLLGQGRGSVMDFYKSLRGGATVKVSASSPSVAAASQADSKQQ
RILLDFSKGSTSNVQQRQQQQQQQQQQQQQQQQQQQPDLSKAVSLSMGLYMGETETKVMG
NDLGYPQQGQLGLSSGETDFRLLEESIANLNRSTSVPENPKSSTSATGCATPTEKEFPKT
HSDASSEQQNRKSQTGTNGGSVKLYPTDQSTFDLLKDLEFSAGSPSKDTNESPWRSDLLI
DENLLSPLAGEDDPFLLEGNTNEDCKPLILPDTKPKIKDTGDTILSSPSSVALPQVKTEK
DDFIELCTPGVIKQEKLGPVYCQASFSGTNIIGNKMSAISVHGVSTSGGQMYHYDMNTAS
LSQQQDQKPVFNVIPPIPVGSENWNRCQGSGEDSLTSLGALNFPGRSVFSNGYSSPGMRP
DVSSPPSSSSAATGPPPKLCLVCSDEASGCHYGVLTCGSCKVFFKRAVEGQHNYLCAGRN
DCIIDKIRRKNCPACRYRKCLQAGMNLEARKTKKKIKGIQQATAGVSQDTSENPNKTIVP
AALPQLTPTLVSLLEVIEPEVLYAGYDSSVPDSAWRIMTTLNMLGGRQVIAAVKWAKAIL
GLRNLHLDDQMTLLQYSWMFLMAFALGWRSYRQSSGNLLCFAPDLIINEQRMSLPCMYDQ
CKHMLFVSSELQRLQVSYEEYLCMKTLLLLSSVPKEGLKSQELFDEIRMTYIKELGKAIV
KREGNSSQNWQRFYQLTKLLDSMHEVVENLLTYCFQTFLDKTMSIEFPEMLAEIITNQIP
KYSNGNIKKLLFHQK
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM19199
n/a
NameBDBM19199
Synonyms:(R)-[(4aR,5S)-1-(4-fluorophenyl)-4a-methyl-1H,4H,4aH,5H,6H,7H,8H-cyclohexa[f]indazol-5-yl](3,4-difluoro-5-methoxyphenyl)methanol | CHEMBL313062 | N-Arylpyrazolo[3,2-c]-Based Ligand, 18
TypeSmall organic molecule
Emp. Form.C26H25F3N2O2
Mol. Mass.454.4841
SMILES[H][C@@]1(CCCC2=Cc3c(C[C@]12C)cnn3-c1ccc(F)cc1)[C@@H](O)c1cc(F)c(F)c(OC)c1 |r,t:5|
Structure
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