Reaction Details |
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Target | Glucocorticoid receptor |
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Ligand | BDBM50449076 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1295699 (CHEMBL3129511) |
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IC50 | 13±n/a nM |
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Citation | Harcken, C; Riether, D; Kuzmich, D; Liu, P; Betageri, R; Ralph, M; Emmanuel, M; Reeves, JT; Berry, A; Souza, D; Nelson, RM; Kukulka, A; Fadra, TN; Zuvela-Jelaska, L; Dinallo, R; Bentzien, J; Nabozny, GH; Thomson, DS Identification of highly efficacious glucocorticoid receptor agonists with a potential for reduced clinical bone side effects. J Med Chem57:1583-98 (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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BDBM50449076 |
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n/a |
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Name | BDBM50449076 |
Synonyms: | CHEMBL3126952 |
Type | Small organic molecule |
Emp. Form. | C26H25F4N3O |
Mol. Mass. | 471.4898 |
SMILES | Cc1ccc(F)cc1C(C)(C)CC(O)(Cc1cc2cc(nnc2[nH]1)-c1ccccc1)C(F)(F)F |
Structure |
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