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Target
Glucocorticoid receptor
Ligand
BDBM50457404
Substrate
n/a
Meas. Tech.
ChEMBL_1759560 (CHEMBL4194568)
IC50
1.6±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:
BDBM50457404
Synonyms:
CHEMBL4217597
Type:
Small organic molecule
Emp. Form.:
C27H22F3N5O4
Mol. Mass.:
537.4899
SMILES:
C[C@H](O)[C@H](NC(=O)c1nnc(C)o1)[C@H](Oc1ccc2n(ncc2c1)-c1ccc(F)cc1)c1cc(F)cc(F)c1 |r|
Structure:
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