Reaction Details |
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Target | Glucocorticoid receptor |
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Ligand | BDBM50414605 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_580474 (CHEMBL1052501) |
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IC50 | 0.316±n/a nM |
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Citation | Biggadike, K; Caivano, M; Clackers, M; Coe, DM; Hardy, GW; Humphreys, D; Jones, HT; House, D; Miles-Williams, A; Skone, PA; Uings, I; Weller, V; McLay, IM; Macdonald, SJ Highly tractable, sub-nanomolar non-steroidal glucocorticoid receptor agonists. Bioorg Med Chem Lett19:4846-50 (2009) [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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BDBM50414605 |
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n/a |
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Name | BDBM50414605 |
Synonyms: | CHEMBL556231 |
Type | Small organic molecule |
Emp. Form. | C26H22F6N4O2 |
Mol. Mass. | 536.4689 |
SMILES | CCN(CC(O)(CNc1cccc2n(ncc12)-c1ccc(F)cc1)C(F)(F)F)C(=O)c1c(F)cccc1F |
Structure |
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