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TargetGlucocorticoid receptor
LigandBDBM50417606
Substrate/Competitorn/a
Meas. Tech.ChEMBL_698229 (CHEMBL1646699)
EC50 25.12±n/a nM
Citation Brown, ARBosies, MCameron, HClark, JCowley, ACraighead, MElmore, MAFirth, AGoodwin, RGoutcher, SGrant, EGrassie, MGrove, SJHamilton, NMHampson, HHillier, AHo, KKKiczun, MKingsbury, CKultgen, SGLittlewood, PTLusher, SJMacdonald, SMcIntosh, LMcIntyre, TMistry, AMorphy, JRNimz, OOhlmeyer, MPick, JRankovic, ZSherborne, BSmith, ASpeake, MSpinks, GThomson, FWatson, LWeston, M Discovery and optimisation of a selective non-steroidal glucocorticoid receptor antagonist. Bioorg Med Chem Lett21:137-40 (2010) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Glucocorticoid receptor
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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  Blast E-value cutoff:
BDBM50417606
n/a
NameBDBM50417606
Synonyms:CHEMBL1645398
TypeSmall organic molecule
Emp. Form.C19H21N3O4S
Mol. Mass.387.453
SMILESCOc1ncccc1-c1ccc(cc1)[C@@H](C)NS(=O)(=O)c1c(C)noc1C |r|
Structure
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