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Target
Glucocorticoid receptor
Ligand
BDBM50340663
Substrate
n/a
Meas. Tech.
ChEMBL_739896 (CHEMBL1762956)
EC50
250±n/a nM
Citation
 Hudson, AR; Higuchi, RI; Roach, SL; Valdez, LJ; Adams, ME; Vassar, A; Rungta, D; Syka, PM; Mais, DE; Marschke, KB; Zhi, L Nonsteroidal 2,3-dihydroquinoline glucocorticoid receptor agonists with reduced PEPCK activation. Bioorg Med Chem Lett 21:1654-7 (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:
BDBM50340663
Synonyms:
5,7-difluoro-2,2-dimethyl-6-(3-methyl-1H-indol-7-yl)-2,3-dihydroquinolin-4(1H)-one O-isopropyl oxime | CHEMBL1762204
Type:
Small organic molecule
Emp. Form.:
C23H25F2N3O
Mol. Mass.:
397.4609
SMILES:
CC(C)O\N=C1/CC(C)(C)Nc2cc(F)c(c(F)c12)-c1cccc2c(C)c[nH]c12 |(2.4,-30.12,;1.06,-30.88,;-.26,-30.1,;1.05,-32.41,;-.28,-33.17,;-.29,-34.71,;1.04,-35.49,;1.03,-37.04,;2.35,-36.26,;2.35,-37.8,;-.32,-37.79,;-1.64,-37.01,;-2.97,-37.77,;-4.29,-37,;-5.62,-37.76,;-4.28,-35.46,;-2.96,-34.69,;-2.95,-33.16,;-1.63,-35.47,;-5.61,-34.69,;-5.61,-33.14,;-6.94,-32.37,;-8.27,-33.14,;-8.28,-34.68,;-9.43,-35.71,;-10.77,-34.94,;-8.8,-37.13,;-7.27,-36.96,;-6.94,-35.45,)|
Structure:
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