Reaction Details |
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Target | Glucocorticoid receptor |
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Ligand | BDBM19236 |
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Substrate/Competitor | BDBM18207 |
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Meas. Tech. | GR Binding Assay and GRAF Assay |
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pH | 8±n/a |
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Temperature | 277.15±n/a K |
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IC50 | 1.8±n/a nM |
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EC50 | 330±n/a nM |
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Citation | Link, JT; Sorensen, B; Patel, J; Grynfarb, M; Goos-Nilsson, A; Wang, J; Fung, S; Wilcox, D; Zinker, B; Nguyen, P; Hickman, B; Schmidt, JM; Swanson, S; Tian, Z; Reisch, TJ; Rotert, G; Du, J; Lane, B; von Geldern, TW; Jacobson, PB Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators. J Med Chem48:5295-304 (2005) [PubMed] Article |
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More Info.: | Get all data from this article, Solution Info, 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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BDBM19236 |
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BDBM18207 |
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Name | BDBM19236 |
Synonyms: | 2-{2-bromo-5-[4-({[(2,4-difluorophenyl)methyl](3-methanesulfonamido-2-methylphenyl)amino}methyl)phenoxy]phenoxy}acetic acid | GR sulfonamide modulator, 13 |
Type | Small organic molecule |
Emp. Form. | C30H27BrF2N2O6S |
Mol. Mass. | 661.511 |
SMILES | Cc1c(NS(C)(=O)=O)cccc1N(Cc1ccc(Oc2ccc(Br)c(OCC(O)=O)c2)cc1)Cc1ccc(F)cc1F |
Structure |
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