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Target
Glucocorticoid receptor
Ligand
BDBM50298028
Substrate
n/a
Meas. Tech.
ChEMBL_585102 (CHEMBL1059179)
EC50
7900±n/a nM
Citation
 Thompson, SK; Washburn, DG; Frazee, JS; Madauss, KP; Hoang, TH; Lapinski, L; Grygielko, ET; Glace, LE; Trizna, W; Williams, SP; Duraiswami, C; Bray, JD; Laping, NJ Rational design of orally-active, pyrrolidine-based progesterone receptor partial agonists. Bioorg Med Chem Lett 19:4777-80 (2009) [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:
BDBM50298028
Synonyms:
(S)-2-chloro-4-((1-methylpyrrolidin-3-yl)(2-(trifluoromethyl)benzyl)amino)benzonitrile | 2-chloro-4-{[(3S)-1-methylpyrrolidin-3-yl][2-(trifluoromethyl)benzyl]amino}benzonitrile | CHEMBL558664
Type:
Small organic molecule
Emp. Form.:
C20H19ClF3N3
Mol. Mass.:
393.833
SMILES:
CN1CC[C@@H](C1)N(Cc1ccccc1C(F)(F)F)c1ccc(C#N)c(Cl)c1 |r|
Structure:
Search PDB for entries with ligand similarity: