| Reaction Details |
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 | Report a problem with these data |
| Target | 11-beta-hydroxysteroid dehydrogenase 1 |
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| Ligand | BDBM22473 |
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| Substrate/Competitor | BDBM13739 |
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| Meas. Tech. | Mouse and Rat 11beta-HSD1 SPA Assay |
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| pH | 7.2±n/a |
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| Temperature | 295.15±n/a K |
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| Ki | 180±33 nM |
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| 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 |
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| More Info.: | Get all data from this article, Inhibition_Run data, Solution Info, Assay Method |
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| 11-beta-hydroxysteroid dehydrogenase 1 |
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| Name: | 11-beta-hydroxysteroid dehydrogenase 1 |
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| Synonyms: | 11-DH | 11-beta-HSD1 | 11-beta-Hydroxysteroid Dehydrogenase 1 (11-beta-HSD1) | 11-beta-hydroxysteroid dehydrogenase 1 | Corticosteroid 11-beta-dehydrogenase isozyme 1 | Corticosteroid 11-beta-dehydrogenase isozyme 1 (11-beta-HSD-1) | DHI1_RAT | Hsd11 | Hsd11b1 |
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| Type: | Enzyme |
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| Mol. Mass.: | 31889.48 |
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| Organism: | Rattus norvegicus (rat) |
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| Description: | P16232 |
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| Residue: | 288 |
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| Sequence: | MKKYLLPVLVLCLGYYYSTNEEFRPEMLQGKKVIVTGASKGIGREMAYHLSKMGAHVVLT
ARSEEGLQKVVSRCLELGAASAHYIAGTMEDMAFAERFVVEAGKLLGGLDMLILNHITQT
TMSLFHDDIHSVRRSMEVNFLSYVVLSTAALPMLKQSNGSIAIISSMAGKMTQPLIASYS
ASKFALDGFFSTIRKEHLMTKVNVSITLCVLGFIDTETALKETSGIILSQAAPKEECALE
IIKGTVLRKDEVYYDKSSWTPLLLGNPGRRIMEFLSLRSYNRDLFVSN
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| BDBM22473 |
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| BDBM13739 |
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| Name | BDBM22473 |
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| Synonyms: | 2-(hexahydro-2,5-methanopentalen-3a(1H)-ylamino)-1-thia-3-azaspiro[4.4]non-2-en-4-one | 2-Amino-1,3-thiazol-4(5H)-one, 8b | 2-{tricyclo[3.3.1.0^{3,7}]nonan-3-ylamino}-1-thia-3-azaspiro[4.4]non-2-en-4-one |
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| Type | Small organic molecule |
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| Emp. Form. | C16H22N2OS |
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| Mol. Mass. | 290.424 |
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| SMILES | O=C1N=C(NC23CC4CC2CC(C3)C4)SC11CCCC1 |t:2,TLB:12:11:5.6:8,4:5:8:11.10.13,4:5:10:7.8.13,THB:6:5:10:7.8.13,6:7:5.12:10,12:5:8:11.10.13| |
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| Structure | 
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