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Target
Glucocorticoid receptor
Ligand
BDBM332678
Substrate
n/a
Meas. Tech.
ChEMBL_1759553 (CHEMBL4194561)
IC50
<3.0±n/a nM
Citation
 Ripa, L; Edman, K; Dearman, M; Edenro, G; Hendrickx, R; Ullah, V; Chang, HF; Lepistö, M; Chapman, D; Geschwindner, S; Wissler, L; Svanberg, P; Lawitz, K; Malmberg, J; Nikitidis, A; Olsson, RI; Bird, J; Llinas, A; Hegelund-Myrbäck, T; Berger, M; Thorne, P; Harrison, R; Köhler, C; Drmota, T Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile. J Med Chem 61:1785-1799 (2018) [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:
BDBM332678
Synonyms:
US10196374, Example 6
Type:
Small organic molecule
Emp. Form.:
C26H24ClF3N4O3
Mol. Mass.:
532.942
SMILES:
CC(C)[C@H](NC(=O)C(F)(F)F)[C@H](Oc1ccc2n(ncc2c1)-c1ccc(=O)n(C)c1)c1cccc(Cl)c1 |r|
Structure:
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