Reaction Details Report a problem with these data
Target
Glucocorticoid receptor
Ligand
BDBM19191
Substrate
n/a
Meas. Tech.
ChEMBL_2130771 (CHEMBL4840200)
IC50
40±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
More Info.:
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:
BDBM19191
Synonyms:
(R)-[(4aR,5S)-1-(4-fluorophenyl)-4a-methyl-1H,4H,4aH,5H,6H,7H,8H-cyclohexa[f]indazol-5-yl](phenyl)methanol | N-Arylpyrazolo[3,2-c]-Based Ligand, 10
Type:
Small organic molecule
Emp. Form.:
C25H25FN2O
Mol. Mass.:
388.4772
SMILES:
[H][C@@]1(CCCC2=Cc3c(C[C@]12C)cnn3-c1ccc(F)cc1)[C@@H](O)c1ccccc1 |r,t:5|