Reaction Details |
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Target | Glucocorticoid receptor |
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Ligand | BDBM50014439 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1350746 (CHEMBL3266131) |
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IC50 | 4.6±n/a nM |
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Citation | Edman, K; Ahlgren, R; Bengtsson, M; Bladh, H; Bäckström, S; Dahmén, J; Henriksson, K; Hillertz, P; Hulikal, V; Jerre, A; Kinchin, L; Kåse, C; Lepistö, M; Mile, I; Nilsson, S; Smailagic, A; Taylor, J; Tjörnebo, A; Wissler, L; Hansson, T The discovery of potent and selective non-steroidal glucocorticoid receptor modulators, suitable for inhalation. Bioorg Med Chem Lett24:2571-7 (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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BDBM50014439 |
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n/a |
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Name | BDBM50014439 |
Synonyms: | CHEMBL3261420 |
Type | Small organic molecule |
Emp. Form. | C26H28FN3O2S |
Mol. Mass. | 465.583 |
SMILES | C[C@@H](CCc1cccc2n(ncc12)-c1ccc(F)cc1)NS(=O)(=O)c1c(C)cc(C)cc1C |r| |
Structure |
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