Reaction Details |
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Target | Glucocorticoid receptor |
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Ligand | BDBM50439617 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_977683 (CHEMBL2423841) |
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IC50 | 3800±n/a nM |
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Citation | Hasui, T; Ohra, T; Ohyabu, N; Asano, K; Matsui, H; Mizukami, A; Habuka, N; Sogabe, S; Endo, S; Siedem, CS; Tang, TP; Gauthier, C; De Meese, LA; Boyd, SA; Fukumoto, S Design, synthesis, and structure-activity relationships of dihydrofuran-2-one and dihydropyrrol-2-one derivatives as novel benzoxazin-3-one-based mineralocorticoid receptor antagonists. Bioorg Med Chem21:5983-94 (2013) [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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BDBM50439617 |
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n/a |
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Name | BDBM50439617 |
Synonyms: | CHEMBL2419306 |
Type | Small organic molecule |
Emp. Form. | C19H14FNO4 |
Mol. Mass. | 339.3172 |
SMILES | CC1OC(=O)C(=C1c1ccc2OCC(=O)Nc2c1)c1ccc(F)cc1 |c:5| |
Structure |
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