Target
Glucocorticoid receptor
Ligand
BDBM332697
Substrate
n/a
Meas. Tech.
GRE Agonist Assay
EC50
25.1±n/a nM
Citation
 Ripa, LELawitz, KLepistö, MJHemmerling, MEdman, KLLinas, A 1-alkyl-6-oxo-1,6-dihydropyridin-3-yl compounds and use as SGRM modulators US Patent  US10196374 Publication Date 2/5/2019 
Target
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:
MDSKESLTPGREENPSSVLAQERGDVMDFYKTLRGGATVKVSASSPSLAVASQSDSKQRRLLVDFPKGSVSNAQQPDLSKAVSLSMGLYMGETETKVMGNDLGFPQQGQISLSSGETDLKLLEESIANLNRSTSVPENPKSSASTAVSAAPTEKEFPKTHSDVSSEQQHLKGQTGTNGGNVKLYTTDQSTFDILQDLEFSSGSPGKETNESPWRSDLLIDENCLLSPLAGEDDSFLLEGNSNEDCKPLILPDTKPKIKDNGDLVLSSPSNVTLPQVKTEKEDFIELCTPGVIKQEKLGTVYCQASFPGANIIGNKMSAISVHGVSTSGGQMYHYDMNTASLSQQQDQKPIFNVIPPIPVGSENWNRCQGSGDDNLTSLGTLNFPGRTVFSNGYSSPSMRPDVSSPPSSSSTATTGPPPKLCLVCSDEASGCHYGVLTCGSCKVFFKRAVEGQHNYLCAGRNDCIIDKIRRKNCPACRYRKCLQAGMNLEARKTKKKIKGIQQATTGVSQETSENPGNKTIVPATLPQLTPTLVSLLEVIEPEVLYAGYDSSVPDSTWRIMTTLNMLGGRQVIAAVKWAKAIPGFRNLHLDDQMTLLQYSWMFLMAFALGWRSYRQSSANLLCFAPDLIINEQRMTLPCMYDQCKHMLYVSSELHRLQVSYEEYLCMKTLLLLSSVPKDGLKSQELFDEIRMTYIKELGKAIVKREGNSSQNWQRFYQLTKLLDSMHEVVENLLNYCFQTFLDKTMSIEFPEMLAEIITNQIPKYSNGNIKKLLFHQK
  
Inhibitor
Name:
BDBM332697
Synonyms:
US10196374, Example 23
Type:
Small organic molecule
Emp. Form.:
C28H30F2N4O3
Mol. Mass.:
508.5596
SMILES:
CCn1cc(ccc1=O)-n1ncc2cc(O[C@@H]([C@@H](NC(=O)C(C)(F)F)C(C)C)c3ccccc3)ccc12 |r|
Structure:
Search PDB for entries with ligand similarity: