| Reaction Details |
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 | Report a problem with these data |
| Target | 11-beta-hydroxysteroid dehydrogenase 1 |
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| Ligand | BDBM22468 |
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| Substrate/Competitor | BDBM13739 |
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| Meas. Tech. | Human 11beta-HSD1 Scintillation Proximity Assay (SPA) |
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| pH | 7.2±n/a |
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| Temperature | 295.15±n/a K |
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| Ki | 24±5 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 | 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 |
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| Type: | Enzyme |
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| Mol. Mass.: | 32409.16 |
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| Organism: | Homo sapiens (Human) |
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| Description: | P28845 |
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| Residue: | 292 |
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| Sequence: | MAFMKKYLLPILGLFMAYYYYSANEEFRPEMLQGKKVIVTGASKGIGREMAYHLAKMGAH
VVVTARSKETLQKVVSHCLELGAASAHYIAGTMEDMTFAEQFVAQAGKLMGGLDMLILNH
ITNTSLNLFHDDIHHVRKSMEVNFLSYVVLTVAALPMLKQSNGSIVVVSSLAGKVAYPMV
AAYSASKFALDGFFSSIRKEYSVSRVNVSITLCVLGLIDTETAMKAVSGIVHMQAAPKEE
CALEIIKGGALRQEEVYYDSSLWTTLLIRNPCRKILEFLYSTSYNMDRFINK
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| BDBM22468 |
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| BDBM13739 |
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| Name | BDBM22468 |
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| Synonyms: | 2-(adamantan-1-ylamino)-5-ethyl-5-methyl-4,5-dihydro-1,3-thiazol-4-one | 2-Amino-1,3-thiazol-4(5H)-one, 5i |
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| Type | Small organic molecule |
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| Emp. Form. | C16H24N2OS |
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| Mol. Mass. | 292.44 |
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| SMILES | CCC1(C)SC(NC23CC4CC(CC(C4)C2)C3)=NC1=O |c:19,TLB:16:7:14:10.11.12,THB:16:11:14:8.7.15,15:7:10:14.13.12,15:13:10:8.7.16,6:7:14:10.11.12| |
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| Structure | 
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