Reaction Details |
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Target | Glucocorticoid receptor |
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Ligand | BDBM50415811 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_625087 (CHEMBL1112536) |
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IC50 | 501.19±n/a nM |
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Citation | Rimland, J; Dunne, A; Hunjan, SS; Sasse, R; Uings, I; Montanari, D; Caivano, M; Shah, P; Standing, D; Gray, D; Brown, D; Cairns, W; Trump, R; Smith, PW; Bertheleme, N; D'Alessandro, P; Gul, S; Vimal, M; Smith, DN; Watson, SP The identification a novel, selective, non-steroidal, functional glucocorticoid receptor antagonist. Bioorg Med Chem Lett20:2340-3 (2010) [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 |
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: | MDSKESLTPGREENPSSVLAQERGDVMDFYKTLRGGATVKVSASSPSLAVASQSDSKQRR
LLVDFPKGSVSNAQQPDLSKAVSLSMGLYMGETETKVMGNDLGFPQQGQISLSSGETDLK
LLEESIANLNRSTSVPENPKSSASTAVSAAPTEKEFPKTHSDVSSEQQHLKGQTGTNGGN
VKLYTTDQSTFDILQDLEFSSGSPGKETNESPWRSDLLIDENCLLSPLAGEDDSFLLEGN
SNEDCKPLILPDTKPKIKDNGDLVLSSPSNVTLPQVKTEKEDFIELCTPGVIKQEKLGTV
YCQASFPGANIIGNKMSAISVHGVSTSGGQMYHYDMNTASLSQQQDQKPIFNVIPPIPVG
SENWNRCQGSGDDNLTSLGTLNFPGRTVFSNGYSSPSMRPDVSSPPSSSSTATTGPPPKL
CLVCSDEASGCHYGVLTCGSCKVFFKRAVEGQHNYLCAGRNDCIIDKIRRKNCPACRYRK
CLQAGMNLEARKTKKKIKGIQQATTGVSQETSENPGNKTIVPATLPQLTPTLVSLLEVIE
PEVLYAGYDSSVPDSTWRIMTTLNMLGGRQVIAAVKWAKAIPGFRNLHLDDQMTLLQYSW
MFLMAFALGWRSYRQSSANLLCFAPDLIINEQRMTLPCMYDQCKHMLYVSSELHRLQVSY
EEYLCMKTLLLLSSVPKDGLKSQELFDEIRMTYIKELGKAIVKREGNSSQNWQRFYQLTK
LLDSMHEVVENLLNYCFQTFLDKTMSIEFPEMLAEIITNQIPKYSNGNIKKLLFHQK
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BDBM50415811 |
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n/a |
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Name | BDBM50415811 |
Synonyms: | CHEMBL1093055 |
Type | Small organic molecule |
Emp. Form. | C24H24ClN5O2 |
Mol. Mass. | 449.933 |
SMILES | Cc1noc(C)c1-c1ccc(CNC(=O)c2cnc3n(ncc3c2Cl)C2CCCC2)cc1 |
Structure |
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