Reaction Details |
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Target | Glucocorticoid receptor |
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Ligand | BDBM50228078 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_452393 (CHEMBL902629) |
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Ki | 8.9±n/a nM |
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Citation | Bell, MG; Gernert, DL; Grese, TA; Belvo, MD; Borromeo, PS; Kelley, SA; Kennedy, JH; Kolis, SP; Lander, PA; Richey, R; Sharp, VS; Stephenson, GA; Williams, JD; Yu, H; Zimmerman, KM; Steinberg, MI; Jadhav, PK (S)-N-{3-[1-cyclopropyl-1-(2,4-difluoro-phenyl)-ethyl]-1H-indol-7-yl}-methanesulfonamide: a potent, nonsteroidal, functional antagonist of the mineralocorticoid receptor. J Med Chem50:6443-5 (2007) [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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BDBM50228078 |
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n/a |
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Name | BDBM50228078 |
Synonyms: | (S)-N-(3-(1-cyclopropyl-1-(2,4-difluorophenyl)ethyl)-1H-indol-7-yl)methanesulfonamide | CHEMBL235206 |
Type | Small organic molecule |
Emp. Form. | C20H20F2N2O2S |
Mol. Mass. | 390.447 |
SMILES | C[C@](C1CC1)(c1c[nH]c2c(NS(C)(=O)=O)cccc12)c1ccc(F)cc1F |
Structure |
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