Target
Glucocorticoid receptor
Ligand
BDBM50338321
Substrate
n/a
Meas. Tech.
ChEMBL_728109 (CHEMBL1687051)
EC50
0.9±n/a nM
Citation
 Hudson, ARHiguchi, RIRoach, SLAdams, MEVassar, ASyka, PMMais, DEMiner, JNMarschke, KBZhi, L Discovery of orally available tetrahydroquinoline-based glucocorticoid receptor agonists. Bioorg Med Chem Lett 21:1697-700 (2011) [PubMed]  Article 
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:
BDBM50338321
Synonyms:
(+/-)-(3R,4S)-6-(1H-indol-7-yl)-2,2,4,5,8-pentamethyl-1,2,3,4-tetrahydroquinolin-3-ol | CHEMBL1682420
Type:
Small organic molecule
Emp. Form.:
C22H26N2O
Mol. Mass.:
334.4546
SMILES:
C[C@@H]1[C@@H](O)C(C)(C)Nc2c(C)cc(c(C)c12)-c1cccc2cc[nH]c12 |r|
Structure:
Search PDB for entries with ligand similarity: