5CGJ
 
 | | Crystal structure of murine Keap1 in complex with RA839, a non-covalent small-molecule binder to Keap1 and selective activator of Nrf2 signalling. | | 分子名称: | (3S)-1-(4-{[(2,3,5,6-tetramethylphenyl)sulfonyl]amino}naphthalen-1-yl)pyrrolidine-3-carboxylic acid, Kelch-like ECH-associated protein 1, SULFATE ION | | 著者 | Schimanski-Breves, S, Loenze, P, Engel, C.K. | | 登録日 | 2015-07-09 | | 公開日 | 2015-10-21 | | 最終更新日 | 2024-05-08 | | 実験手法 | X-RAY DIFFRACTION (3.36 Å) | | 主引用文献 | Characterization of RA839, a Noncovalent Small Molecule Binder to Keap1 and Selective Activator of Nrf2 Signaling.
J.Biol.Chem., 290, 2015
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3QQP
 | | Crystal Structure of 11beta-Hydroxysteroid Dehydrogenase 1 (11b-HSD1) in Complex with Urea Inhibitor | | 分子名称: | 3,4-dihydroquinolin-1(2H)-yl[4-(1H-imidazol-5-yl)piperidin-1-yl]methanone, Corticosteroid 11-beta-dehydrogenase isozyme 1, NADPH DIHYDRO-NICOTINAMIDE-ADENINE-DINUCLEOTIDE PHOSPHATE | | 著者 | Loenze, P, Schimanski-Breves, S, Engel, C.K. | | 登録日 | 2011-02-16 | | 公開日 | 2012-02-22 | | 最終更新日 | 2024-02-21 | | 実験手法 | X-RAY DIFFRACTION (2.72 Å) | | 主引用文献 | Pyrrolidine-pyrazole ureas as potent and selective inhibitors of 11beta-hydroxysteroid-dehydrogenase type 1.
Bioorg.Med.Chem.Lett., 21, 2011
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4K26
 | | 4,4-Dioxo-5,6-dihydro-[1,4,3]oxathiazines, a novel class of 11 -HSD1 inhibitors for the treatment of diabetes | | 分子名称: | (4aS,8aR)-N-cyclohexyl-4a,5,6,7,8,8a-hexahydro-4,1,2-benzoxathiazin-3-amine 1,1-dioxide, Corticosteroid 11-beta-dehydrogenase isozyme 1, NADPH DIHYDRO-NICOTINAMIDE-ADENINE-DINUCLEOTIDE PHOSPHATE, ... | | 著者 | Loenze, P, Schimanski-Breves, S, Vonderheyden, C, Engel, C.K. | | 登録日 | 2013-04-08 | | 公開日 | 2014-04-09 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (2.21 Å) | | 主引用文献 | 1,1-Dioxo-5,6-dihydro-[4,1,2]oxathiazines, a novel class of 11-HSD1 inhibitors for the treatment of diabetes.
Bioorg.Med.Chem.Lett., 23, 2013
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3LFS
 | | Crystal structure of CDK2 with SAR37, an aminoindazole type inhibitor | | 分子名称: | Cell division protein kinase 2, N-(6-chloro-5-phenyl-1H-indazol-3-yl)butanamide | | 著者 | Dreyer, M.K, Wendt, K.U, Schimanski-Breves, S, Loenze, P. | | 登録日 | 2010-01-18 | | 公開日 | 2010-03-02 | | 最終更新日 | 2024-02-21 | | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | | 主引用文献 | Rational design of potent GSK3beta inhibitors with selectivity for Cdk1 and Cdk2.
Bioorg.Med.Chem.Lett., 20, 2010
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4K1L
 | | 4,4-Dioxo-5,6-dihydro-[1,4,3]oxathiazines, a novel class of 11 beta-HSD1 inhibitors for the treatment of diabetes | | 分子名称: | (4aS,8aR)-N-cyclohexyl-4a,5,6,7,8,8a-hexahydro-4,1,2-benzoxathiazin-3-amine 1,1-dioxide, Corticosteroid 11-beta-dehydrogenase isozyme 1, NADPH DIHYDRO-NICOTINAMIDE-ADENINE-DINUCLEOTIDE PHOSPHATE | | 著者 | Loenze, P, Schimanski-Breves, S, Von der Heyden, C, Engel, C.K. | | 登録日 | 2013-04-05 | | 公開日 | 2014-04-09 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (1.96 Å) | | 主引用文献 | 1,1-Dioxo-5,6-dihydro-[4,1,2]oxathiazines, a novel class of 11-HSD1 inhibitors for the treatment of diabetes.
Bioorg.Med.Chem.Lett., 23, 2013
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3LFQ
 | | Crystal structure of CDK2 with SAR60, an aminoindazole type inhibitor | | 分子名称: | Cell division protein kinase 2, N-(6,7-difluoro-5-phenyl-1H-indazol-3-yl)butanamide | | 著者 | Dreyer, M.K, Wendt, K.U, Schimanski-Breves, S, Loenze, P. | | 登録日 | 2010-01-18 | | 公開日 | 2010-03-02 | | 最終更新日 | 2024-02-21 | | 実験手法 | X-RAY DIFFRACTION (2.03 Å) | | 主引用文献 | Rational design of potent GSK3beta inhibitors with selectivity for Cdk1 and Cdk2.
Bioorg.Med.Chem.Lett., 20, 2010
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3LFN
 | | Crystal structure of CDK2 with SAR57, an aminoindazole type inhibitor | | 分子名称: | Cell division protein kinase 2, N-[6-(4-hydroxyphenyl)-5-phenyl-1H-indazol-3-yl]butanamide | | 著者 | Dreyer, M.K, Wendt, K.U, Schimanski-Breves, S, Loenze, P. | | 登録日 | 2010-01-18 | | 公開日 | 2010-03-02 | | 最終更新日 | 2024-02-21 | | 実験手法 | X-RAY DIFFRACTION (2.28 Å) | | 主引用文献 | Rational design of potent GSK3beta inhibitors with selectivity for Cdk1 and Cdk2.
Bioorg.Med.Chem.Lett., 20, 2010
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4HX5
 | | Crystal structure of 11 beta-HSD1 in complex with SAR184841 | | 分子名称: | 4-[5-(4-tert-butylpiperazin-1-yl)pyridin-2-yl]-N-[(1R,2S,3S,5S,7s)-5-carbamoyltricyclo[3.3.1.1~3,7~]dec-2-yl]-3,4-dihydroquinoxaline-1(2H)-carboxamide, Corticosteroid 11-beta-dehydrogenase isozyme 1, NADPH DIHYDRO-NICOTINAMIDE-ADENINE-DINUCLEOTIDE PHOSPHATE | | 著者 | Loenze, P, Schimanski-Breves, S, Engel, C.K. | | 登録日 | 2012-11-09 | | 公開日 | 2013-05-08 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (2.19 Å) | | 主引用文献 | Discovery of SAR184841, a potent and long-lasting inhibitor of 11beta-hydroxysteroid dehydrogenase type 1, active in a physiopathological animal model of T2D
Bioorg.Med.Chem.Lett., 23, 2013
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