Reaction Details |
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Target | Glucocorticoid receptor |
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Ligand | BDBM50355748 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_776318 (CHEMBL1914169) |
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EC50 | 187±n/a nM |
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Citation | Weinstein, DS; Gong, H; Doweyko, AM; Cunningham, M; Habte, S; Wang, JH; Holloway, DA; Burke, C; Gao, L; Guarino, V; Carman, J; Somerville, JE; Shuster, D; Salter-Cid, L; Dodd, JH; Nadler, SG; Barrish, JC Azaxanthene based selective glucocorticoid receptor modulators: design, synthesis, and pharmacological evaluation of (S)-4-(5-(1-((1,3,4-thiadiazol-2-yl)amino)-2-methyl-1-oxopropan-2-yl)-5H-chromeno[2,3-b]pyridin-2-yl)-2-fluoro-N,N-dimethylbenzamide (BMS-776532) and its methylene homologue (BMS-791 J Med Chem54:7318-33 (2011) [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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BDBM50355748 |
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n/a |
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Name | BDBM50355748 |
Synonyms: | CHEMBL1911144 |
Type | Small organic molecule |
Emp. Form. | C24H20N4O2S |
Mol. Mass. | 428.506 |
SMILES | CC(C)([C@H]1c2ccccc2Oc2nc(ccc12)-c1ccccc1)C(=O)Nc1nncs1 |r| |
Structure |
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