Reaction Details |
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Target | 11-beta-hydroxysteroid dehydrogenase 1 |
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Ligand | BDBM50273458 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_561241 (CHEMBL1013596) |
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Ki | 300±n/a nM |
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Citation | Fotsch, C; Bartberger, MD; Bercot, EA; Chen, M; Cupples, R; Emery, M; Fretland, J; Guram, A; Hale, C; Han, N; Hickman, D; Hungate, RW; Hayashi, M; Komorowski, R; Liu, Q; Matsumoto, G; St Jean, DJ; Ursu, S; Véniant, M; Xu, G; Ye, Q; Yuan, C; Zhang, J; Zhang, X; Tu, H; Wang, M Further studies with the 2-amino-1,3-thiazol-4(5H)-one class of 11beta-hydroxysteroid dehydrogenase type 1 inhibitors: reducing pregnane X receptor activity and exploring activity in a monkey pharmacodynamic model. J Med Chem51:7953-67 (2008) [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 | Corticosteroid 11-beta-dehydrogenase isozyme 1 | Corticosteroid 11-beta-dehydrogenase isozyme 1 (11-beta-HSD-1) | DHI1_RAT | Hsd11 | Hsd11b1 |
Type: | Enzyme |
Mol. Mass.: | 31889.48 |
Organism: | Rattus norvegicus (rat) |
Description: | P16232 |
Residue: | 288 |
Sequence: | MKKYLLPVLVLCLGYYYSTNEEFRPEMLQGKKVIVTGASKGIGREMAYHLSKMGAHVVLT
ARSEEGLQKVVSRCLELGAASAHYIAGTMEDMAFAERFVVEAGKLLGGLDMLILNHITQT
TMSLFHDDIHSVRRSMEVNFLSYVVLSTAALPMLKQSNGSIAIISSMAGKMTQPLIASYS
ASKFALDGFFSTIRKEHLMTKVNVSITLCVLGFIDTETALKETSGIILSQAAPKEECALE
IIKGTVLRKDEVYYDKSSWTPLLLGNPGRRIMEFLSLRSYNRDLFVSN
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BDBM50273458 |
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n/a |
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Name | BDBM50273458 |
Synonyms: | (5S)-2-{[(1S)-1-(4-fluorophenyl)ethyl]amino}-5-(1-hydroxy-1-methylethyl)-5-methyl-1,3-thiazol-4(5H)-one | (S)-2-[(S)-1-(4-Fluorophenyl)ethylamino]-5-(2-hydroxypropan-2-yl)-5-methylthiazol-4(5H)-one | CHEMBL455907 |
Type | Small organic molecule |
Emp. Form. | C15H19FN2O2S |
Mol. Mass. | 310.387 |
SMILES | C[C@H](NC1=NC(=O)[C@@](C)(S1)C(C)(C)O)c1ccc(F)cc1 |r,t:3| |
Structure |
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