| Reaction Details |
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 | Report a problem with these data |
| Target | Glucocorticoid receptor |
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| Ligand | BDBM50499243 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1537770 (CHEMBL3737649) |
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| Ki | 8.5±n/a nM |
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| Citation |  Hunt, HJ; Belanoff, JK; Golding, E; Gourdet, B; Phillips, T; Swift, D; Thomas, J; Unitt, JF; Walters, I 1H-Pyrazolo[3,4-g]hexahydro-isoquinolines as potent GR antagonists with reduced hERG inhibition and an improved pharmacokinetic profile. Bioorg Med Chem Lett25:5720-5 (2015) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| Glucocorticoid receptor |
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| Name: | Glucocorticoid receptor |
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| Synonyms: | GCR_RAT | Glucocorticoid | Glucocorticoid Receptor (GR) | Glucocorticoid receptor | Grl | Nr3c1 |
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| Type: | Enzyme Catalytic Domain |
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| Mol. Mass.: | 87556.83 |
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| Organism: | RAT |
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| Description: | Glucocorticoid 0 RAT::P06536 |
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| Residue: | 795 |
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| Sequence: | MDSKESLAPPGRDEVPGSLLGQGRGSVMDFYKSLRGGATVKVSASSPSVAAASQADSKQQ
RILLDFSKGSTSNVQQRQQQQQQQQQQQQQQQQQQQPDLSKAVSLSMGLYMGETETKVMG
NDLGYPQQGQLGLSSGETDFRLLEESIANLNRSTSVPENPKSSTSATGCATPTEKEFPKT
HSDASSEQQNRKSQTGTNGGSVKLYPTDQSTFDLLKDLEFSAGSPSKDTNESPWRSDLLI
DENLLSPLAGEDDPFLLEGNTNEDCKPLILPDTKPKIKDTGDTILSSPSSVALPQVKTEK
DDFIELCTPGVIKQEKLGPVYCQASFSGTNIIGNKMSAISVHGVSTSGGQMYHYDMNTAS
LSQQQDQKPVFNVIPPIPVGSENWNRCQGSGEDSLTSLGALNFPGRSVFSNGYSSPGMRP
DVSSPPSSSSAATGPPPKLCLVCSDEASGCHYGVLTCGSCKVFFKRAVEGQHNYLCAGRN
DCIIDKIRRKNCPACRYRKCLQAGMNLEARKTKKKIKGIQQATAGVSQDTSENPNKTIVP
AALPQLTPTLVSLLEVIEPEVLYAGYDSSVPDSAWRIMTTLNMLGGRQVIAAVKWAKAIL
GLRNLHLDDQMTLLQYSWMFLMAFALGWRSYRQSSGNLLCFAPDLIINEQRMSLPCMYDQ
CKHMLFVSSELQRLQVSYEEYLCMKTLLLLSSVPKEGLKSQELFDEIRMTYIKELGKAIV
KREGNSSQNWQRFYQLTKLLDSMHEVVENLLTYCFQTFLDKTMSIEFPEMLAEIITNQIP
KYSNGNIKKLLFHQK
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| BDBM50499243 |
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| n/a |
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| Name | BDBM50499243 |
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| Synonyms: | CHEMBL3735203 |
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| Type | Small organic molecule |
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| Emp. Form. | C28H21Cl2FN4O3S |
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| Mol. Mass. | 583.461 |
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| SMILES | Fc1ccc(cc1)-n1ncc2C[C@@]3(CN(CCC3=Cc12)S(=O)(=O)c1ccc(Cl)c(Cl)c1)C(=O)c1ccccn1 |r,c:19| |
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| Structure | 
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