| Reaction Details |
|---|
 | Report a problem with these data |
| Target | 11-beta-hydroxysteroid dehydrogenase 1 |
|---|
| Ligand | BDBM22471 |
|---|
| Substrate/Competitor | BDBM13739 |
|---|
| Meas. Tech. | Human 11beta-HSD1 Scintillation Proximity Assay (SPA) |
|---|
| pH | 7.2±n/a |
|---|
| Temperature | 295.15±n/a K |
|---|
| Ki | 14±3 nM |
|---|
| Citation |  Johansson, L; Fotsch, C; Bartberger, MD; Castro, VM; Chen, M; Emery, M; Gustafsson, S; Hale, C; Hickman, D; Homan, E; Jordan, SR; Komorowski, R; Li, A; McRae, K; Moniz, G; Matsumoto, G; Orihuela, C; Palm, G; Veniant, M; Wang, M; Williams, M; Zhang, J 2-Amino-1,3-thiazol-4(5H)-ones as Potent and Selective 11beta-Hydroxysteroid Dehydrogenase Type 1 Inhibitors: Enzyme-Ligand Co-Crystal Structure and Demonstration of Pharmacodynamic Effects in C57Bl/6 Mice. J Med Chem51:2933-43 (2008) [PubMed] Article |
|---|
| More Info.: | Get all data from this article, Inhibition_Run data, Solution Info, Assay Method |
|---|
| |
| 11-beta-hydroxysteroid dehydrogenase 1 |
|---|
| Name: | 11-beta-hydroxysteroid dehydrogenase 1 |
|---|
| Synonyms: | 11-DH | 11-beta-HSD1 | 11-beta-Hydroxysteroid Dehydrogenase 1 (11-beta-HSD1) | 11-beta-hydroxysteroid dehydrogenase | 11-beta-hydroxysteroid dehydrogenase 1 (11HSD1) | Corticosteroid 11-beta-dehydrogenase isozyme 1 | Corticosteroid 11-beta-dehydrogenase isozyme 1 (11-beta-HSD-1) | Corticosteroid 11-beta-dehydrogenase isozyme 1 (11-beta-HSD1) | Corticosteroid 11-beta-dehydrogenase isozyme 1 (11beta-HSD1) | DHI1_HUMAN | HSD11 | HSD11B1 | HSD11L | SDR26C1 |
|---|
| Type: | Enzyme |
|---|
| Mol. Mass.: | 32409.16 |
|---|
| Organism: | Homo sapiens (Human) |
|---|
| Description: | P28845 |
|---|
| Residue: | 292 |
|---|
| Sequence: | MAFMKKYLLPILGLFMAYYYYSANEEFRPEMLQGKKVIVTGASKGIGREMAYHLAKMGAH
VVVTARSKETLQKVVSHCLELGAASAHYIAGTMEDMTFAEQFVAQAGKLMGGLDMLILNH
ITNTSLNLFHDDIHHVRKSMEVNFLSYVVLTVAALPMLKQSNGSIVVVSSLAGKVAYPMV
AAYSASKFALDGFFSSIRKEYSVSRVNVSITLCVLGLIDTETAMKAVSGIVHMQAAPKEE
CALEIIKGGALRQEEVYYDSSLWTTLLIRNPCRKILEFLYSTSYNMDRFINK
|
|
|
|---|
| BDBM22471 |
|---|
| BDBM13739 |
|---|
| Name | BDBM22471 |
|---|
| Synonyms: | 2-(cyclooctylamino)-1-thia-3-azaspiro[4.4]non-2-en-4-one | 2-Amino-1,3-thiazol-4(5H)-one, 8a |
|---|
| Type | Small organic molecule |
|---|
| Emp. Form. | C15H24N2OS |
|---|
| Mol. Mass. | 280.429 |
|---|
| SMILES | O=C1N=C(NC2CCCCCCC2)SC11CCCC1 |t:2| |
|---|
| Structure | 
|
|---|
Search and Browse
