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Target
Glucocorticoid receptor
Ligand
BDBM381436
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
More Info.:
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:
BDBM381436
Synonyms:
4-Chloro-3-methyl-1-(5-methyl- thiazol-2-ylmethyl)-1H- pyrazolo[3,4-b]pyridine-5- carboxylic acid (4-trifluoromethyl- phenyl)-amide | US10272074, Example 269
Type:
Small organic molecule
Emp. Form.:
C20H15ClF3N5OS
Mol. Mass.:
465.879
SMILES:
Cc1cnc(Cn2nc(C)c3c(Cl)c(cnc23)C(=O)Nc2ccc(cc2)C(F)(F)F)s1