Reaction Details |
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Target | Glucocorticoid receptor |
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Ligand | BDBM50048341 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1459138 (CHEMBL3370899) |
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EC50 | 11±n/a nM |
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Citation | Gong, H; Yang, M; Xiao, Z; Doweyko, AM; Cunningham, M; Wang, J; Habte, S; Holloway, D; Burke, C; Shuster, D; Gao, L; Carman, J; Somerville, JE; Nadler, SG; Salter-Cid, L; Barrish, JC; Weinstein, DS Discovery of acylurea isosteres of 2-acylaminothiadiazole in the azaxanthene series of glucocorticoid receptor agonists. Bioorg Med Chem Lett24:3268-73 (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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BDBM50048341 |
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n/a |
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Name | BDBM50048341 |
Synonyms: | CHEMBL3315063 | US9593113, Example 28 |
Type | Small organic molecule |
Emp. Form. | C28H28N4O5 |
Mol. Mass. | 500.5457 |
SMILES | CC(C)([C@H]1c2ccccc2Oc2nc(ccc12)-c1ccc(cc1)C(=O)N1CCOCC1)C(=O)NC(N)=O |r| |
Structure |
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