| Reaction Details |
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 | Report a problem with these data |
| Target | Glucocorticoid receptor |
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| Ligand | BDBM50417616 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_698234 (CHEMBL1646704) |
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| EC50 | 100±n/a nM |
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| Citation |  Brown, AR; Bosies, M; Cameron, H; Clark, J; Cowley, A; Craighead, M; Elmore, MA; Firth, A; Goodwin, R; Goutcher, S; Grant, E; Grassie, M; Grove, SJ; Hamilton, NM; Hampson, H; Hillier, A; Ho, KK; Kiczun, M; Kingsbury, C; Kultgen, SG; Littlewood, PT; Lusher, SJ; Macdonald, S; McIntosh, L; McIntyre, T; Mistry, A; Morphy, JR; Nimz, O; Ohlmeyer, M; Pick, J; Rankovic, Z; Sherborne, B; Smith, A; Speake, M; Spinks, G; Thomson, F; Watson, L; Weston, M Discovery and optimisation of a selective non-steroidal glucocorticoid receptor antagonist. Bioorg Med Chem Lett21:137-40 (2010) [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 |
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| Synonyms: | GCR_HUMAN | GR | GRL | Glucocorticoid | Glucocorticoid receptor (GRFP) | NR3C1 | Nuclear receptor subfamily 3 group C member 1 |
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| Type: | Enzyme |
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| Mol. Mass.: | 85656.87 |
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| Organism: | Homo sapiens (Human) |
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| Description: | P04150 |
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| Residue: | 777 |
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| Sequence: | MDSKESLTPGREENPSSVLAQERGDVMDFYKTLRGGATVKVSASSPSLAVASQSDSKQRR
LLVDFPKGSVSNAQQPDLSKAVSLSMGLYMGETETKVMGNDLGFPQQGQISLSSGETDLK
LLEESIANLNRSTSVPENPKSSASTAVSAAPTEKEFPKTHSDVSSEQQHLKGQTGTNGGN
VKLYTTDQSTFDILQDLEFSSGSPGKETNESPWRSDLLIDENCLLSPLAGEDDSFLLEGN
SNEDCKPLILPDTKPKIKDNGDLVLSSPSNVTLPQVKTEKEDFIELCTPGVIKQEKLGTV
YCQASFPGANIIGNKMSAISVHGVSTSGGQMYHYDMNTASLSQQQDQKPIFNVIPPIPVG
SENWNRCQGSGDDNLTSLGTLNFPGRTVFSNGYSSPSMRPDVSSPPSSSSTATTGPPPKL
CLVCSDEASGCHYGVLTCGSCKVFFKRAVEGQHNYLCAGRNDCIIDKIRRKNCPACRYRK
CLQAGMNLEARKTKKKIKGIQQATTGVSQETSENPGNKTIVPATLPQLTPTLVSLLEVIE
PEVLYAGYDSSVPDSTWRIMTTLNMLGGRQVIAAVKWAKAIPGFRNLHLDDQMTLLQYSW
MFLMAFALGWRSYRQSSANLLCFAPDLIINEQRMTLPCMYDQCKHMLYVSSELHRLQVSY
EEYLCMKTLLLLSSVPKDGLKSQELFDEIRMTYIKELGKAIVKREGNSSQNWQRFYQLTK
LLDSMHEVVENLLNYCFQTFLDKTMSIEFPEMLAEIITNQIPKYSNGNIKKLLFHQK
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| BDBM50417616 |
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| n/a |
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| Name | BDBM50417616 |
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| Synonyms: | CHEMBL1645403 |
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| Type | Small organic molecule |
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| Emp. Form. | C20H18F3N5O3S |
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| Mol. Mass. | 465.449 |
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| SMILES | COc1ncc(cc1-c1ccc(cc1)[C@@H](C)NS(=O)(=O)c1cn(C)nc1C(F)(F)F)C#N |r| |
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| Structure | 
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