Reaction Details |
| Report a problem with these data |
Target | Glucocorticoid receptor |
---|
Ligand | BDBM19207 |
---|
Substrate/Competitor | BDBM18207 |
---|
Meas. Tech. | GR Binding Assay and Human IL-6 Assay |
---|
pH | 7.5±n/a |
---|
Temperature | 277.15±n/a K |
---|
IC50 | 1.1±n/a nM |
---|
EC50 | 4.4±n/a nM |
---|
Citation | Ali, A; Thompson, CF; Balkovec, JM; Graham, DW; Hammond, ML; Quraishi, N; Tata, JR; Einstein, M; Ge, L; Harris, G; Kelly, TM; Mazur, P; Pandit, S; Santoro, J; Sitlani, A; Wang, C; Williamson, J; Miller, DK; Thompson, CM; Zaller, DM; Forrest, MJ; Carballo-Jane, E; Luell, S Novel N-arylpyrazolo[3,2-c]-based ligands for the glucocorticoid receptor: receptor binding and in vivo activity. J Med Chem47:2441-52 (2004) [PubMed] Article |
---|
More Info.: | Get all data from this article, Inhibition_Run data, Solution Info, 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
|
|
|
BDBM19207 |
---|
BDBM18207 |
---|
Name | BDBM19207 |
Synonyms: | (1S)-1-[(4aR,5S)-1-(4-fluorophenyl)-4a-methyl-1H,4H,4aH,5H,6H,7H,8H-cyclohexa[f]indazol-5-yl]pent-4-en-1-ol | N-Arylpyrazolo[3,2-c]-Based Ligand, 31 |
Type | Small organic molecule |
Emp. Form. | C23H27FN2O |
Mol. Mass. | 366.4717 |
SMILES | [H][C@@]1(CCCC2=Cc3c(C[C@]12C)cnn3-c1ccc(F)cc1)[C@@H](O)CCC=C |r,t:5| |
Structure |
|