Ki Summary BindingDB logo
myBDB logout
Reaction Details
Report a problem with these data
TargetGlucocorticoid receptor
LigandBDBM50449067
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1295699 (CHEMBL3129511)
IC50 5.0±n/a nM
Citation Harcken, CRiether, DKuzmich, DLiu, PBetageri, RRalph, MEmmanuel, MReeves, JTBerry, ASouza, DNelson, RMKukulka, AFadra, TNZuvela-Jelaska, LDinallo, RBentzien, JNabozny, GHThomson, DS Identification of highly efficacious glucocorticoid receptor agonists with a potential for reduced clinical bone side effects. J Med Chem57:1583-98 (2014) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Glucocorticoid receptor
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:
MDSKESLTPGREENPSSVLAQERGDVMDFYKTLRGGATVKVSASSPSLAVASQSDSKQRR
LLVDFPKGSVSNAQQPDLSKAVSLSMGLYMGETETKVMGNDLGFPQQGQISLSSGETDLK
LLEESIANLNRSTSVPENPKSSASTAVSAAPTEKEFPKTHSDVSSEQQHLKGQTGTNGGN
VKLYTTDQSTFDILQDLEFSSGSPGKETNESPWRSDLLIDENCLLSPLAGEDDSFLLEGN
SNEDCKPLILPDTKPKIKDNGDLVLSSPSNVTLPQVKTEKEDFIELCTPGVIKQEKLGTV
YCQASFPGANIIGNKMSAISVHGVSTSGGQMYHYDMNTASLSQQQDQKPIFNVIPPIPVG
SENWNRCQGSGDDNLTSLGTLNFPGRTVFSNGYSSPSMRPDVSSPPSSSSTATTGPPPKL
CLVCSDEASGCHYGVLTCGSCKVFFKRAVEGQHNYLCAGRNDCIIDKIRRKNCPACRYRK
CLQAGMNLEARKTKKKIKGIQQATTGVSQETSENPGNKTIVPATLPQLTPTLVSLLEVIE
PEVLYAGYDSSVPDSTWRIMTTLNMLGGRQVIAAVKWAKAIPGFRNLHLDDQMTLLQYSW
MFLMAFALGWRSYRQSSANLLCFAPDLIINEQRMTLPCMYDQCKHMLYVSSELHRLQVSY
EEYLCMKTLLLLSSVPKDGLKSQELFDEIRMTYIKELGKAIVKREGNSSQNWQRFYQLTK
LLDSMHEVVENLLNYCFQTFLDKTMSIEFPEMLAEIITNQIPKYSNGNIKKLLFHQK
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50449067
n/a
NameBDBM50449067
Synonyms:CHEMBL3126938
TypeSmall organic molecule
Emp. Form.C24H28F4N4O2
Mol. Mass.480.4983
SMILESCc1ccc(F)cc1C(C)(C)CC(O)(Cc1cc2nc(ncc2[nH]1)N1CCOCC1)C(F)(F)F
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: