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Target
Glucocorticoid receptor
Ligand
BDBM50423192
Substrate
n/a
Meas. Tech.
ChEMBL_448639 (CHEMBL897791)
IC50
3.0±n/a nM
Citation
 Clackers, M; Coe, DM; Demaine, DA; Hardy, GW; Humphreys, D; Inglis, GG; Johnston, MJ; Jones, HT; House, D; Loiseau, R; Minick, DJ; Skone, PA; Uings, I; McLay, IM; Macdonald, SJ Non-steroidal glucocorticoid agonists: the discovery of aryl pyrazoles as A-ring mimetics. Bioorg Med Chem Lett 17:4737-45 (2007) [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:
BDBM50423192
Synonyms:
CHEMBL237973
Type:
Small organic molecule
Emp. Form.:
C26H28F4N4O2
Mol. Mass.:
504.5197
SMILES:
CCC1(CC(O)(CNC(=O)c2cnn(c2N)-c2ccc(F)cc2)C(F)(F)F)CCCc2ccccc12
Structure:
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