Reaction Details |
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Target | 11-beta-hydroxysteroid dehydrogenase type 2 |
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Ligand | BDBM22457 |
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Substrate/Competitor | BDBM13775 |
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Meas. Tech. | Human 11beta-HSD1 Scintillation Proximity Assay (SPA) |
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IC50 | >10000±n/a 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, Solution Info, Assay Method |
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11-beta-hydroxysteroid dehydrogenase type 2 |
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Name: | 11-beta-hydroxysteroid dehydrogenase type 2 |
Synonyms: | 11-DH2 | 11-beta-HSD2 | 11-beta-Hydroxysteroid Dehydrogenase 2 (11-beta-HSD2) | 11-beta-hydroxysteroid dehydrogenase | 11-beta-hydroxysteroid dehydrogenase 2 | 11-beta-hydroxysteroid dehydrogenase type 2 | 11-beta-hydroxysteroid dehydrogenase type 2 (11-beta-HSD2) | Corticosteroid 11-beta-dehydrogenase isozyme 2 | DHI2_HUMAN | HSD11B2 | HSD11K | NAD-dependent 11-beta-hydroxysteroid dehydrogenase | SDR9C3 |
Type: | Enzyme |
Mol. Mass.: | 44141.72 |
Organism: | Homo sapiens (Human) |
Description: | Purified recombinant human 11beta-HSD2. |
Residue: | 405 |
Sequence: | MERWPWPSGGAWLLVAARALLQLLRSDLRLGRPLLAALALLAALDWLCQRLLPPPAALAV
LAAAGWIALSRLARPQRLPVATRAVLITGCDSGFGKETAKKLDSMGFTVLATVLELNSPG
AIELRTCCSPRLRLLQMDLTKPGDISRVLEFTKAHTTSTGLWGLVNNAGHNEVVADAELS
PVATFRSCMEVNFFGALELTKGLLPLLRSSRGRIVTVGSPAGDMPYPCLGAYGTSKAAVA
LLMDTFSCELLPWGVKVSIIQPGCFKTESVRNVGQWEKRKQLLLANLPQELLQAYGKDYI
EHLHGQFLHSLRLAMSDLTPVVDAITDALLAARPRRRYYPGQGLGLMYFIHYYLPEGLRR
RFLQAFFISHCLPRALQPGQPGTTPPQDAAQDPNLSPGPSPAVAR
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BDBM22457 |
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BDBM13775 |
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Name | BDBM22457 |
Synonyms: | 2-(cycloheptylamino)-5-methyl-5-propyl-4,5-dihydro-1,3-thiazol-4-one | 2-Amino-1,3-thiazol-4(5H)-one, 6c |
Type | Small organic molecule |
Emp. Form. | C14H24N2OS |
Mol. Mass. | 268.418 |
SMILES | CCCC1(C)SC(NC2CCCCCC2)=NC1=O |c:15| |
Structure |
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