Reaction Details |
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Target | Glucocorticoid receptor |
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Ligand | BDBM50356049 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_775646 (CHEMBL1913330) |
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IC50 | 8±n/a nM |
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Citation | Betageri, R; Gilmore, T; Kuzmich, D; Kirrane, TM; Bentzien, J; Wiedenmayer, D; Bekkali, Y; Regan, J; Berry, A; Latli, B; Kukulka, AJ; Fadra, TN; Nelson, RM; Goldrick, S; Zuvela-Jelaska, L; Souza, D; Pelletier, J; Dinallo, R; Panzenbeck, M; Torcellini, C; Lee, H; Pack, E; Harcken, C; Nabozny, G; Thomson, DS Non-steroidal dissociated glucocorticoid agonists: indoles as A-ring mimetics and function-regulating pharmacophores. Bioorg Med Chem Lett21:6842-51 (2011) [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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BDBM50356049 |
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n/a |
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Name | BDBM50356049 |
Synonyms: | CHEMBL1911649 |
Type | Small organic molecule |
Emp. Form. | C23H22F4N2O2 |
Mol. Mass. | 434.4266 |
SMILES | COc1ccc(F)cc1C(C)(C)CC(O)(Cc1cc2cc(ccc2[nH]1)C#N)C(F)(F)F |
Structure |
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