Reaction Details |
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Target | Glucocorticoid receptor |
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Ligand | BDBM50001768 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1338546 (CHEMBL3241423) |
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IC50 | 2.0±n/a nM |
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Citation | Razavi, H; Riether, D; Harcken, C; Bentzien, J; Dinallo, RM; Souza, D; Nelson, RM; Kukulka, A; Fadra-Khan, TN; Pack, EJ; Zuvela-Jelaska, L; Pelletier, J; Panzenbeck, M; Torcellini, CA; Proudfoot, JR; Nabozny, GH; Thomson, DS Discovery of a potent and dissociated non-steroidal glucocorticoid receptor agonist containing an alkyl carbinol pharmacophore. Bioorg Med Chem Lett24:1934-40 (2014) [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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BDBM50001768 |
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n/a |
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Name | BDBM50001768 |
Synonyms: | CHEMBL3233281 |
Type | Small organic molecule |
Emp. Form. | C24H31FN2O |
Mol. Mass. | 382.5141 |
SMILES | Cc1ccc(F)cc1C(C)(C)C[C@@](O)(Cc1cc2cnccc2[nH]1)C(C)(C)C |r| |
Structure |
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