Reaction Details |
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Target | 11-beta-hydroxysteroid dehydrogenase 1 |
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Ligand | BDBM50174284 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_326694 (CHEMBL868713) |
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IC50 | 1.8±n/a nM |
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Citation | Gu, X; Dragovic, J; Koo, GC; Koprak, SL; LeGrand, C; Mundt, SS; Shah, K; Springer, MS; Tan, EY; Thieringer, R; Hermanowski-Vosatka, A; Zokian, HJ; Balkovec, JM; Waddell, ST Discovery of 4-heteroarylbicyclo[2.2.2]octyltriazoles as potent and selective inhibitors of 11beta-HSD1: novel therapeutic agents for the treatment of metabolic syndrome. Bioorg Med Chem Lett15:5266-9 (2005) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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11-beta-hydroxysteroid dehydrogenase 1 |
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Name: | 11-beta-hydroxysteroid dehydrogenase 1 |
Synonyms: | 11-DH | 11-beta-HSD1 | 11-beta-Hydroxysteroid Dehydrogenase 1 (11-beta-HSD1) | 11-beta-hydroxysteroid dehydrogenase 1 | 11beta-HSD1A | Corticosteroid 11-beta-dehydrogenase isozyme 1 | Corticosteroid 11-beta-dehydrogenase isozyme 1 (11-beta-HSD-1) | DHI1_MOUSE | Hsd11 | Hsd11b1 |
Type: | Enzyme |
Mol. Mass.: | 32369.70 |
Organism: | Mus musculus (mouse) |
Description: | P50172 |
Residue: | 292 |
Sequence: | MAVMKNYLLPILVLFLAYYYYSTNEEFRPEMLQGKKVIVTGASKGIGREMAYHLSKMGAH
VVLTARSEEGLQKVVSRCLELGAASAHYIAGTMEDMTFAEQFIVKAGKLMGGLDMLILNH
ITQTSLSLFHDDIHSVRRVMEVNFLSYVVMSTAALPMLKQSNGSIAVISSLAGKMTQPMI
APYSASKFALDGFFSTIRTELYITKVNVSITLCVLGLIDTETAMKEISGIINAQASPKEE
CALEIIKGTALRKSEVYYDKSPLTPILLGNPGRKIMEFFSLRYYNKDMFVSN
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BDBM50174284 |
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n/a |
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Name | BDBM50174284 |
Synonyms: | 4-methyl-3-(4-(3-(4-(methylsulfonyl)phenyl)-1,2,4-oxadiazol-5-yl)bicyclo[2.2.2]octan-1-yl)-5-(2-(trifluoromethyl)phenyl)-4H-1,2,4-triazole | CHEMBL197220 |
Type | Small organic molecule |
Emp. Form. | C27H26F3N5O3S |
Mol. Mass. | 557.587 |
SMILES | Cn1c(nnc1C12CCC(CC1)(CC2)c1nc(no1)-c1ccc(cc1)S(C)(=O)=O)-c1ccccc1C(F)(F)F |
Structure |
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