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Target
Glucocorticoid receptor
Ligand
BDBM18627
Substrate
BDBM18207
Meas. Tech.
GR Binding Assay and GRAF Assay
pH
8±n/a
Temperature
277.15±n/a K
IC50
1.1±n/a nM
EC50
4.8±n/a nM
Comments
VP16 agonism = 59 %.
Citation
 Link, JT; Sorensen, B; Patel, J; Grynfarb, M; Goos-Nilsson, A; Wang, J; Fung, S; Wilcox, D; Zinker, B; Nguyen, P; Hickman, B; Schmidt, JM; Swanson, S; Tian, Z; Reisch, TJ; Rotert, G; Du, J; Lane, B; von Geldern, TW; Jacobson, PB Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators. J Med Chem 48:5295-304 (2005) [PubMed]  Article 
Target
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:
MDSKESLTPGREENPSSVLAQERGDVMDFYKTLRGGATVKVSASSPSLAVASQSDSKQRRLLVDFPKGSVSNAQQPDLSKAVSLSMGLYMGETETKVMGNDLGFPQQGQISLSSGETDLKLLEESIANLNRSTSVPENPKSSASTAVSAAPTEKEFPKTHSDVSSEQQHLKGQTGTNGGNVKLYTTDQSTFDILQDLEFSSGSPGKETNESPWRSDLLIDENCLLSPLAGEDDSFLLEGNSNEDCKPLILPDTKPKIKDNGDLVLSSPSNVTLPQVKTEKEDFIELCTPGVIKQEKLGTVYCQASFPGANIIGNKMSAISVHGVSTSGGQMYHYDMNTASLSQQQDQKPIFNVIPPIPVGSENWNRCQGSGDDNLTSLGTLNFPGRTVFSNGYSSPSMRPDVSSPPSSSSTATTGPPPKLCLVCSDEASGCHYGVLTCGSCKVFFKRAVEGQHNYLCAGRNDCIIDKIRRKNCPACRYRKCLQAGMNLEARKTKKKIKGIQQATTGVSQETSENPGNKTIVPATLPQLTPTLVSLLEVIEPEVLYAGYDSSVPDSTWRIMTTLNMLGGRQVIAAVKWAKAIPGFRNLHLDDQMTLLQYSWMFLMAFALGWRSYRQSSANLLCFAPDLIINEQRMTLPCMYDQCKHMLYVSSELHRLQVSYEEYLCMKTLLLLSSVPKDGLKSQELFDEIRMTYIKELGKAIVKREGNSSQNWQRFYQLTKLLDSMHEVVENLLNYCFQTFLDKTMSIEFPEMLAEIITNQIPKYSNGNIKKLLFHQK
  
Inhibitor
Name:
BDBM18627
Synonyms:
(10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]-14-hydroxy-15-methyl-14-(prop-1-yn-1-yl)tetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-1,6-dien-5-one | Mifeprex | Mifepristone | RU-486 | RU486 (tetramethyl-rhodamine conjugated)
Type:
Small organic molecule
Emp. Form.:
C29H35NO2
Mol. Mass.:
429.5937
SMILES:
[H][C@@]12CC[C@@](O)(C#CC)[C@@]1(C)C[C@@H](C1=C3CCC(=O)C=C3CC[C@@]21[H])c1ccc(cc1)N(C)C |r,c:14,20|
Structure:
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Substrate
Name:
BDBM18207
Synonyms:
(1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dihydroxy-14-(2-hydroxyacetyl)-2,13,15-trimethyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-3,6-dien-5-one | US10869929, Compound Dexamethasone | US11554172, Compound Dexamethasone | dexamethasone | dexamethasone (tetramethyl-rhodamine conjugated )
Type:
Steroid
Emp. Form.:
C22H29FO5
Mol. Mass.:
392.4611
SMILES:
[H][C@@]12C[C@@H](C)[C@](O)(C(=O)CO)[C@@]1(C)C[C@H](O)[C@@]1(F)[C@@]2([H])CCC2=CC(=O)C=C[C@]12C |c:28,t:24|
Structure:
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