Reaction Details |
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Target | Glucocorticoid receptor |
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Ligand | BDBM18746 |
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Substrate/Competitor | BDBM18207 |
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Meas. Tech. | Fluorescence Polarization Competitive Binding Assay. |
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pH | 7.4±n/a |
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Temperature | 295.15±n/a K |
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IC50 | 34±n/a nM |
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Citation | Takahashi, H; Bekkali, Y; Capolino, AJ; Gilmore, T; Goldrick, SE; Kaplita, PV; Liu, L; Nelson, RM; Terenzio, D; Wang, J; Zuvela-Jelaska, L; Proudfoot, J; Nabozny, G; Thomson, D Discovery and SAR study of novel dihydroquinoline-containing glucocorticoid receptor agonists. Bioorg Med Chem Lett17:5091-5 (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 |
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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BDBM18746 |
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BDBM18207 |
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Name | BDBM18746 |
Synonyms: | 6-(5-fluoro-2-methoxyphenyl)-2,2-dimethyl-4-[1-(prop-2-en-1-yloxy)ethyl]-1,2-dihydroquinoline | dihydroquinoline-based ligand, 38 |
Type | Small organic molecule |
Emp. Form. | C23H26FNO2 |
Mol. Mass. | 367.4564 |
SMILES | COc1ccc(F)cc1-c1ccc2NC(C)(C)C=C(C(C)OCC=C)c2c1 |t:18| |
Structure |
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