4NMH
| 11-beta-HSD1 in complex with a 3,3-Di-methyl-azetidin-2-one | Descriptor: | (4S)-4-(2-methoxyphenyl)-3,3-dimethyl-1-[3-(methylsulfonyl)phenyl]azetidin-2-one, Corticosteroid 11-beta-dehydrogenase isozyme 1, NADPH DIHYDRO-NICOTINAMIDE-ADENINE-DINUCLEOTIDE PHOSPHATE, ... | Authors: | McCoull, W, Augustin, M, Blake, C, Ertan, A, Kilgour, E.K, Krapp, S, Moore, J.E, Newcombe, N.J, Packer, M.J, Rees, A, Revill, J, Scott, J.S, Selmi, N, Gerhardt, S, Ogg, D.J, Steinbacher, S, Whittamore, P.R.O. | Deposit date: | 2013-11-15 | Release date: | 2014-03-26 | Last modified: | 2024-02-28 | Method: | X-RAY DIFFRACTION (2.9 Å) | Cite: | Identification and optimisation of 3,3-dimethyl-azetidin-2-ones as potent and selective inhibitors of 11 beta-hydroxysteroid dehydrogenase type 1 (11-beta-HSD1) TO BE PUBLISHED
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2W05
| Structure of CDK2 in complex with an imidazolyl pyrimidine, compound 5b | Descriptor: | CELL DIVISION PROTEIN KINASE 2, N-(2-METHOXYETHYL)-4-({4-[2-METHYL-1-(1-METHYLETHYL)-1H-IMIDAZOL-5-YL]PYRIMIDIN-2-YL}AMINO)BENZENESULFONAMIDE | Authors: | Anderson, M, Andrews, D.M, Barker, A.J, Brassington, C.A, Breed, J, Byth, K.F, Culshaw, J.D, Finlay, M.R, Fisher, E, Green, C.P, Heaton, D.W, Nash, I.A, Newcombe, N.J, Oakes, S.E, Pauptit, R.A, Roberts, A, Stanway, J.J, Thomas, A.P, Tucker, J.A, Weir, H.M. | Deposit date: | 2008-08-08 | Release date: | 2008-10-14 | Last modified: | 2024-05-01 | Method: | X-RAY DIFFRACTION (1.9 Å) | Cite: | Imidazoles: Sar and Development of a Potent Class of Cyclin-Dependent Kinase Inhibitors. Bioorg.Med.Chem.Lett., 18, 2008
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2W06
| Structure of CDK2 in complex with an imidazolyl pyrimidine, compound 5c | Descriptor: | 4-{[4-(1-CYCLOPROPYL-2-METHYL-1H-IMIDAZOL-5-YL)PYRIMIDIN-2-YL]AMINO}-N-METHYLBENZENESULFONAMIDE, CELL DIVISION PROTEIN KINASE 2 | Authors: | Anderson, M, Andrews, D.M, Barker, A.J, Brassington, C.A, Byth, K.F, Culshaw, J.D, Finlay, M.R.V, Fisher, E, Mcmiken, H.H.J, Green, C.P, Heaton, D.W, Nash, I.A, Newcombe, N.J, Oakes, S.E, Roberts, A, Stanway, J.J, Thomas, A.P, Tucker, J.A, Weir, H.M. | Deposit date: | 2008-08-08 | Release date: | 2008-09-23 | Last modified: | 2024-05-01 | Method: | X-RAY DIFFRACTION (2.04 Å) | Cite: | Imidazoles: Sar and Development of a Potent Class of Cyclin-Dependent Kinase Inhibitors Bioorg.Med.Chem.Lett., 18, 2008
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4HFR
| Human 11beta-Hydroxysteroid Dehydrogenase Type 1 in complex with an orally bioavailable acidic inhibitor AZD4017. | Descriptor: | Corticosteroid 11-beta-dehydrogenase isozyme 1, NADP NICOTINAMIDE-ADENINE-DINUCLEOTIDE PHOSPHATE, {(3S)-1-[5-(cyclohexylcarbamoyl)-6-(propylsulfanyl)pyridin-2-yl]piperidin-3-yl}acetic acid | Authors: | Ogg, D.J, Gerhardt, S, Hargreaves, D. | Deposit date: | 2012-10-05 | Release date: | 2012-10-17 | Last modified: | 2023-09-20 | Method: | X-RAY DIFFRACTION (2.73 Å) | Cite: | Discovery of a Potent, Selective, and Orally Bioavailable Acidic 11 -Hydroxysteroid Dehydrogenase Type 1 (11 -HSD1) Inhibitor: Discovery of 2-[(3S)-1-[5-(Cyclohexylcarbamoyl)-6-propylsulfanylpyridin-2-yl]-3-piperidyl]acetic Acid (AZD4017) J.Med.Chem., 55, 2012
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