Reaction Details |
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Target | Glucocorticoid receptor |
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Ligand | BDBM50411030 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_372316 (CHEMBL869706) |
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EC50 | 9.1±n/a nM |
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Citation | Barker, M; Clackers, M; Copley, R; Demaine, DA; Humphreys, D; Inglis, GG; Johnston, MJ; Jones, HT; Haase, MV; House, D; Loiseau, R; Nisbet, L; Pacquet, F; Skone, PA; Shanahan, SE; Tape, D; Vinader, VM; Washington, M; Uings, I; Upton, R; McLay, IM; Macdonald, SJ Dissociated nonsteroidal glucocorticoid receptor modulators; discovery of the agonist trigger in a tetrahydronaphthalene-benzoxazine series. J Med Chem49:4216-31 (2006) [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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BDBM50411030 |
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n/a |
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Name | BDBM50411030 |
Synonyms: | CHEMBL210077 |
Type | Small organic molecule |
Emp. Form. | C25H25F3N2O4 |
Mol. Mass. | 474.4722 |
SMILES | CCC1(CC(O)(C(=O)Nc2ccc3c(c2)c(C)noc3=O)C(F)(F)F)CCCc2ccccc12 |
Structure |
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