| Reaction Details |
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 | Report a problem with these data |
| Target | Glucocorticoid receptor |
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| Ligand | BDBM19192 |
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| Substrate/Competitor | BDBM18207 |
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| Meas. Tech. | GR Binding Assay and Human IL-6 Assay |
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| pH | 7.5±n/a |
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| Temperature | 277.15±n/a K |
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| IC50 | 5.3±n/a nM |
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| EC50 | 9.7±n/a nM |
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| Citation |  Thompson, CF; Quraishi, N; Ali, A; Mosley, RT; Tata, JR; Hammond, ML; Balkovec, JM; Einstein, M; Ge, L; Harris, G; Kelly, TM; Mazur, P; Pandit, S; Santoro, J; Sitlani, A; Wang, C; Williamson, J; Miller, DK; Yamin, TT; Thompson, CM; O'Neill, EA; Zaller, D; Forrest, MJ; Carballo-Jane, E; Luell, S Novel glucocorticoids containing a 6,5-bicyclic core fused to a pyrazole ring: synthesis, in vitro profile, molecular modeling studies, and in vivo experiments. Bioorg Med Chem Lett17:3354-61 (2007) [PubMed] Article |
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| More Info.: | Get all data from this article, Inhibition_Run data, Solution Info, Assay Method |
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| Glucocorticoid receptor |
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| Name: | Glucocorticoid receptor |
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| Synonyms: | GCR_HUMAN | GR | GRL | Glucocorticoid | Glucocorticoid receptor (GRFP) | NR3C1 | Nuclear receptor subfamily 3 group C member 1 |
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| Type: | Enzyme |
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| Mol. Mass.: | 85656.87 |
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| Organism: | Homo sapiens (Human) |
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| Description: | P04150 |
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| Residue: | 777 |
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| Sequence: | MDSKESLTPGREENPSSVLAQERGDVMDFYKTLRGGATVKVSASSPSLAVASQSDSKQRR
LLVDFPKGSVSNAQQPDLSKAVSLSMGLYMGETETKVMGNDLGFPQQGQISLSSGETDLK
LLEESIANLNRSTSVPENPKSSASTAVSAAPTEKEFPKTHSDVSSEQQHLKGQTGTNGGN
VKLYTTDQSTFDILQDLEFSSGSPGKETNESPWRSDLLIDENCLLSPLAGEDDSFLLEGN
SNEDCKPLILPDTKPKIKDNGDLVLSSPSNVTLPQVKTEKEDFIELCTPGVIKQEKLGTV
YCQASFPGANIIGNKMSAISVHGVSTSGGQMYHYDMNTASLSQQQDQKPIFNVIPPIPVG
SENWNRCQGSGDDNLTSLGTLNFPGRTVFSNGYSSPSMRPDVSSPPSSSSTATTGPPPKL
CLVCSDEASGCHYGVLTCGSCKVFFKRAVEGQHNYLCAGRNDCIIDKIRRKNCPACRYRK
CLQAGMNLEARKTKKKIKGIQQATTGVSQETSENPGNKTIVPATLPQLTPTLVSLLEVIE
PEVLYAGYDSSVPDSTWRIMTTLNMLGGRQVIAAVKWAKAIPGFRNLHLDDQMTLLQYSW
MFLMAFALGWRSYRQSSANLLCFAPDLIINEQRMTLPCMYDQCKHMLYVSSELHRLQVSY
EEYLCMKTLLLLSSVPKDGLKSQELFDEIRMTYIKELGKAIVKREGNSSQNWQRFYQLTK
LLDSMHEVVENLLNYCFQTFLDKTMSIEFPEMLAEIITNQIPKYSNGNIKKLLFHQK
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| BDBM19192 |
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| BDBM18207 |
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| Name | BDBM19192 |
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| Synonyms: | (R)-[(4aR,5S)-1-(4-fluorophenyl)-4a-methyl-1H,4H,4aH,5H,6H,7H,8H-cyclohexa[f]indazol-5-yl](4-fluorophenyl)methanol | BMCL173354 benzo[f]indazole, 6 | CHEMBL79807 | N-Arylpyrazolo[3,2-c]-Based Ligand, 11 |
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| Type | Small organic molecule |
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| Emp. Form. | C25H24F2N2O |
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| Mol. Mass. | 406.4677 |
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| SMILES | [H][C@@]1(CCCC2=Cc3c(C[C@]12C)cnn3-c1ccc(F)cc1)[C@@H](O)c1ccc(F)cc1 |r,t:5| |
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| Structure | 
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