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Target
Glucocorticoid receptor
Ligand
BDBM50216491
Substrate
n/a
Meas. Tech.
ChEMBL_886649 (CHEMBL2216234)
Ki
8±n/a nM
Citation
 Hunt, HJ; Ray, NC; Hynd, G; Sutton, J; Sajad, M; O'Connor, E; Ahmed, S; Lockey, P; Daly, S; Buckley, G; Clark, RD; Roe, R; Blasey, C; Belanoff, J Discovery of a novel non-steroidal GR antagonist with in vivo efficacy in the olanzapine-induced weight gain model in the rat. Bioorg Med Chem Lett 22:7376-80 (2012) [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:
BDBM50216491
Synonyms:
5-benzyl-6-(4-phenylpiperidin-1-yl)pyrimidine-2,4(1H,3H)-dione | CHEMBL230675
Type:
Small organic molecule
Emp. Form.:
C22H23N3O2
Mol. Mass.:
361.4369
SMILES:
O=c1[nH]c(N2CCC(CC2)c2ccccc2)c(Cc2ccccc2)c(=O)[nH]1
Structure:
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