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Target
Glucocorticoid receptor
Ligand
BDBM381369
Substrate
n/a
Meas. Tech.
Biological Evaluation
IC50
<50±n/a nM
Citation
 Pinkerton, AB; Hassig, CA; Jackson, MR; Ardecky, RJ; Pass, I Inhibitors of glucocorticoid receptor translocation US Patent  US10272074 Publication Date 4/30/2019 
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:
BDBM381369
Synonyms:
4-chloro-1-(1,1-dioxidotetrahydro- 2H-thiopyran-4-yl)-3-methyl-N-(4- (trifluoromethyl)phenyl)-1H- pyrazolo[3,4-b]pyridine-5- carboxamide | US10272074, Example 202
Type:
Small organic molecule
Emp. Form.:
C20H18ClF3N4O3S
Mol. Mass.:
486.895
SMILES:
Cc1nn(C2CCS(=O)(=O)CC2)c2ncc(C(=O)Nc3ccc(cc3)C(F)(F)F)c(Cl)c12
Structure:
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