| Reaction Details |
|---|
 | Report a problem with these data |
| Target | Glucocorticoid receptor |
|---|
| Ligand | BDBM50319665 |
|---|
| Substrate/Competitor | n/a |
|---|
| Meas. Tech. | ChEMBL_634660 (CHEMBL1118533) |
|---|
| IC50 | >10000±n/a nM |
|---|
| Citation |  Véniant, MM; Hale, C; Hungate, RW; Gahm, K; Emery, MG; Jona, J; Joseph, S; Adams, J; Hague, A; Moniz, G; Zhang, J; Bartberger, MD; Li, V; Syed, R; Jordan, S; Komorowski, R; Chen, MM; Cupples, R; Kim, KW; St Jean, DJ; Johansson, L; Henriksson, MA; Williams, M; Vallgårda, J; Fotsch, C; Wang, M Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221). J Med Chem53:4481-7 (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
|
|
|
|---|
| BDBM50319665 |
|---|
| n/a |
|---|
| Name | BDBM50319665 |
|---|
| Synonyms: | (S)-2-((1S,2S,4R)-Bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one | AMG-221 | CHEMBL1085107 |
|---|
| Type | Small organic molecule |
|---|
| Emp. Form. | C14H22N2OS |
|---|
| Mol. Mass. | 266.402 |
|---|
| SMILES | CC(C)[C@]1(C)SC(N[C@H]2C[C@@H]3CC[C@H]2C3)=NC1=O |r,c:16| |
|---|
| Structure | 
|
|---|
Search and Browse
