Reaction Details |
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Target | Glucocorticoid receptor |
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Ligand | BDBM50440243 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_982008 (CHEMBL2428212) |
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Ki | 5.1±n/a nM |
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Citation | Sheppeck, JE; Gilmore, JL; Xiao, HY; Dhar, TG; Nirschl, D; Doweyko, AM; Sack, JS; Corbett, MJ; Malley, MF; Gougoutas, JZ; Mckay, L; Cunningham, MD; Habte, SF; Dodd, JH; Nadler, SG; Somerville, JE; Barrish, JC Discovery of potent and selective nonsteroidal indazolyl amide glucocorticoid receptor agonists. Bioorg Med Chem Lett23:5442-7 (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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BDBM50440243 |
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n/a |
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Name | BDBM50440243 |
Synonyms: | CHEMBL2426662 |
Type | Small organic molecule |
Emp. Form. | C26H22FN5OS |
Mol. Mass. | 471.549 |
SMILES | CC(C)([C@@H](c1ccccc1)c1ccc2n(ncc2c1)-c1ccc(F)cc1)C(=O)Nc1nncs1 |r| |
Structure |
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