5MAG
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![BU of 5mag by Molmil](/molmil-images/mine/5mag) | Crystal structure of MELK in complex with an inhibitor | 分子名称: | DIMETHYL SULFOXIDE, GLYCEROL, Maternal embryonic leucine zipper kinase, ... | 著者 | Canevari, G, Re Depaolini, S, Casale, E, Felder, E, Kuster, B, Heinzlmeir, S. | 登録日 | 2016-11-03 | 公開日 | 2017-12-06 | 最終更新日 | 2024-05-01 | 実験手法 | X-RAY DIFFRACTION (2.35 Å) | 主引用文献 | The target landscape of clinical kinase drugs. Science, 358, 2017
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5TQW
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![BU of 5tqw by Molmil](/molmil-images/mine/5tqw) | CryoEM reconstruction of human IKK1, open conformation 1 | 分子名称: | Inhibitor of nuclear factor kappa-B kinase subunit alpha | 著者 | Lyumkis, D, Ghosh, G, Polley, S, Biswath, T, Huang, D, Passos, D.O. | 登録日 | 2016-10-24 | 公開日 | 2016-11-09 | 最終更新日 | 2024-03-13 | 実験手法 | ELECTRON MICROSCOPY (5.6 Å) | 主引用文献 | Structural Basis for the Activation of IKK1/ alpha. Cell Rep, 17, 2016
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5TVT
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![BU of 5tvt by Molmil](/molmil-images/mine/5tvt) | Structure of Maternal Embryonic Leucine Zipper Kinase | 分子名称: | 9-(3,5-dichloro-4-hydroxyphenyl)-1-{trans-4-[(dimethylamino)methyl]cyclohexyl}-3-methyl-3,4-dihydropyrimido[5,4-c][1,5]naphthyridin-2(1H)-one, Maternal embryonic leucine zipper kinase | 著者 | Seo, H.-Y, Huang, H, Gray, N.S, Dhe-Paganon, S. | 登録日 | 2016-11-10 | 公開日 | 2017-11-15 | 最終更新日 | 2024-03-06 | 実験手法 | X-RAY DIFFRACTION (2.28 Å) | 主引用文献 | Structure of Maternal Embryonic Leucine Zipper Kinase To Be Published
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5U6Y
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![BU of 5u6y by Molmil](/molmil-images/mine/5u6y) | |
5TQX
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![BU of 5tqx by Molmil](/molmil-images/mine/5tqx) | CryoEM reconstruction of human IKK1, intermediate conformation 2 | 分子名称: | Inhibitor of nuclear factor kappa-B kinase subunit alpha | 著者 | Lyumkis, D, Ghosh, G, Polley, S, Biswath, T, Huang, D, Passos, D.O. | 登録日 | 2016-10-24 | 公開日 | 2016-11-09 | 最終更新日 | 2024-03-13 | 実験手法 | ELECTRON MICROSCOPY (5.4 Å) | 主引用文献 | Structural Basis for the Activation of IKK1/ alpha. Cell Rep, 17, 2016
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5TX3
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![BU of 5tx3 by Molmil](/molmil-images/mine/5tx3) | Structure of Maternal Embryonic Leucine Zipper Kinase | 分子名称: | 7-[(1S)-4-hydroxy-2,3-dihydro-1H-inden-1-yl]-5,5-dimethyl-2-({3-[(pyrrolidin-1-yl)methyl]phenyl}amino)-5,7-dihydro-6H-pyrrolo[2,3-d]pyrimidin-6-one, Maternal embryonic leucine zipper kinase | 著者 | Li, Q, Seo, H.-S, Huang, H.-T, Gray, N.S, Dhe-Paganon, S, Eck, M.J. | 登録日 | 2016-11-15 | 公開日 | 2017-11-22 | 最終更新日 | 2024-03-06 | 実験手法 | X-RAY DIFFRACTION (2.9 Å) | 主引用文献 | MELK is not necessary for the proliferation of basal-like breast cancer cells. Elife, 6, 2017
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5NCL
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![BU of 5ncl by Molmil](/molmil-images/mine/5ncl) | Crystal structure of the Cbk1-Mob2 kinase-coactivator complex with an SSD1 peptide | 分子名称: | CBK1 kinase activator protein MOB2, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER, Protein SSD1, ... | 著者 | Gogl, G, Remenyi, A, Parker, B, Weiss, E. | 登録日 | 2017-03-06 | 公開日 | 2018-05-16 | 最終更新日 | 2024-01-17 | 実験手法 | X-RAY DIFFRACTION (3.15 Å) | 主引用文献 | Ndr/Lats Kinases Bind Specific Mob-Family Coactivators through a Conserved and Modular Interface. Biochemistry, 2020
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5NZZ
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5M5A
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![BU of 5m5a by Molmil](/molmil-images/mine/5m5a) | Crystal structure of MELK in complex with an inhibitor | 分子名称: | CHLORIDE ION, K-252A, Maternal embryonic leucine zipper kinase, ... | 著者 | Canevari, G, Re Depaolini, S, Casale, E, Felder, E, Kuster, B, Heinzlmeir, S. | 登録日 | 2016-10-21 | 公開日 | 2017-12-06 | 最終更新日 | 2024-05-01 | 実験手法 | X-RAY DIFFRACTION (1.9 Å) | 主引用文献 | The target landscape of clinical kinase drugs. Science, 358, 2017
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5MAH
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![BU of 5mah by Molmil](/molmil-images/mine/5mah) | Crystal structure of MELK in complex with an inhibitor | 分子名称: | CHLORIDE ION, GLYCEROL, Maternal embryonic leucine zipper kinase, ... | 著者 | Canevari, G, Re Depaolini, S, Casale, E, Felder, E, Kuster, B, Heinzlmeir, S. | 登録日 | 2016-11-03 | 公開日 | 2017-12-06 | 最終更新日 | 2024-05-01 | 実験手法 | X-RAY DIFFRACTION (2 Å) | 主引用文献 | The target landscape of clinical kinase drugs. Science, 358, 2017
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5MAF
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![BU of 5maf by Molmil](/molmil-images/mine/5maf) | Crystal structure of MELK in complex with an inhibitor | 分子名称: | CHLORIDE ION, DIMETHYL SULFOXIDE, Maternal embryonic leucine zipper kinase, ... | 著者 | Canevari, G, Re Depaolini, S, Casale, E, Felder, E, Kuster, B, Heinzlmeir, S. | 登録日 | 2016-11-03 | 公開日 | 2017-12-06 | 最終更新日 | 2024-05-01 | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | 主引用文献 | The target landscape of clinical kinase drugs. Science, 358, 2017
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5O2C
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![BU of 5o2c by Molmil](/molmil-images/mine/5o2c) | Crystal structure of WNK3 kinase and CCT1 didomain in a unphosphorylated state | 分子名称: | DI(HYDROXYETHYL)ETHER, GLYCEROL, Serine/threonine-protein kinase WNK3 | 著者 | Bartual, S.G, Pinkas, D.M, Bufton, J.C, Kupinska, K, Wang, D, Chalk, R, Berridge, G, Burgess-Brown, N.A, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Bullock, A, Structural Genomics Consortium (SGC) | 登録日 | 2017-05-19 | 公開日 | 2017-06-28 | 最終更新日 | 2024-05-08 | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | 主引用文献 | Crystal structure of WNK3 kinase and CCT1 didomain in a unphosphorylated state To Be Published
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5MAI
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![BU of 5mai by Molmil](/molmil-images/mine/5mai) | Crystal structure of MELK in complex with an inhibitor | 分子名称: | 3-[(3~{Z})-3-[[[4-[(dimethylamino)methyl]phenyl]amino]-phenyl-methylidene]-2-oxidanylidene-1~{H}-indol-6-yl]-~{N}-ethyl-prop-2-ynamide, DIMETHYL SULFOXIDE, Maternal embryonic leucine zipper kinase | 著者 | Canevari, G, Re Depaolini, S, Casale, E, Felder, E, Kuster, B, Heinzlmeir, S. | 登録日 | 2016-11-03 | 公開日 | 2017-12-06 | 最終更新日 | 2024-05-01 | 実験手法 | X-RAY DIFFRACTION (2.15 Å) | 主引用文献 | The target landscape of clinical kinase drugs. Science, 358, 2017
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5T5T
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![BU of 5t5t by Molmil](/molmil-images/mine/5t5t) | AMPK bound to allosteric activator | 分子名称: | 5'-AMP-activated protein kinase catalytic subunit alpha-1, 5'-AMP-activated protein kinase subunit beta-1, 5'-AMP-activated protein kinase subunit gamma-1, ... | 著者 | Calabrese, M.F, Kurumbail, R.G. | 登録日 | 2016-08-31 | 公開日 | 2017-03-29 | 最終更新日 | 2023-10-04 | 実験手法 | X-RAY DIFFRACTION (3.46 Å) | 主引用文献 | Selective Activation of AMPK beta 1-Containing Isoforms Improves Kidney Function in a Rat Model of Diabetic Nephropathy. J. Pharmacol. Exp. Ther., 361, 2017
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5UKM
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![BU of 5ukm by Molmil](/molmil-images/mine/5ukm) | bovine GRK2 in complex with human Gbetagamma subunits and CCG258208 (14as) | 分子名称: | 5-[(3S,4R)-3-{[(2H-1,3-benzodioxol-5-yl)oxy]methyl}piperidin-4-yl]-2-fluoro-N-[(1H-pyrazol-5-yl)methyl]benzamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | 著者 | Cruz-Rodriguez, O, Tesmer, J.J.G. | 登録日 | 2017-01-23 | 公開日 | 2017-04-12 | 最終更新日 | 2023-10-04 | 実験手法 | X-RAY DIFFRACTION (3.03 Å) | 主引用文献 | Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors Based on Paroxetine. J. Med. Chem., 60, 2017
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5NEV
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![BU of 5nev by Molmil](/molmil-images/mine/5nev) | CDK2/Cyclin A in complex with compound 73 | 分子名称: | 4-[[6-(3-phenylphenyl)-7~{H}-purin-2-yl]amino]benzenesulfonamide, Cyclin-A2, Cyclin-dependent kinase 2 | 著者 | Coxon, C.R, Anscombe, E, Harnor, S.J, Martin, M.P, Carbain, B, Hardcastle, I.R, Harlow, L.K, Korolchuk, S, Matheson, C.J, Noble, M.E.M, Newell, D.R, Turner, D, Sivaprakasam, M, Wang, L.Z, Wong, C, Golding, B.T, Griffin, R.J, Cano, G. | 登録日 | 2017-03-12 | 公開日 | 2017-03-29 | 最終更新日 | 2024-01-17 | 実験手法 | X-RAY DIFFRACTION (2.97 Å) | 主引用文献 | Cyclin-Dependent Kinase (CDK) Inhibitors: Structure-Activity Relationships and Insights into the CDK-2 Selectivity of 6-Substituted 2-Arylaminopurines. J. Med. Chem., 60, 2017
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5UQ2
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5UVC
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![BU of 5uvc by Molmil](/molmil-images/mine/5uvc) | Design, Synthesis, and Evaluation of the First Selective and Potent G-protein-Coupled Receptor Kinase 2 (GRK2) Inhibitor for the Potential Treatment of Heart Failure | 分子名称: | Beta-adrenergic receptor kinase 1, N-benzyl-3-({[5-(pyridin-4-yl)-4H-1,2,4-triazol-3-yl]methyl}amino)benzamide, SULFATE ION | 著者 | Hoffman, I.D, Lawson, J.D. | 登録日 | 2017-02-20 | 公開日 | 2017-07-26 | 最終更新日 | 2024-03-06 | 実験手法 | X-RAY DIFFRACTION (2.65 Å) | 主引用文献 | Design, Synthesis, and Evaluation of the Highly Selective and Potent G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitor for the Potential Treatment of Heart Failure. J. Med. Chem., 60, 2017
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5LIH
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![BU of 5lih by Molmil](/molmil-images/mine/5lih) | Structure of a peptide-substrate bound to PKCiota core kinase domain | 分子名称: | ADENOSINE-5'-DIPHOSPHATE, ALUMINUM FLUORIDE, MANGANESE (II) ION, ... | 著者 | Soriano, E.V, Purkiss, A.G, McDonald, N.Q. | 登録日 | 2016-07-14 | 公開日 | 2016-09-14 | 最終更新日 | 2024-01-10 | 実験手法 | X-RAY DIFFRACTION (3.25 Å) | 主引用文献 | aPKC Inhibition by Par3 CR3 Flanking Regions Controls Substrate Access and Underpins Apical-Junctional Polarization. Dev.Cell, 38, 2016
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5UKK
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![BU of 5ukk by Molmil](/molmil-images/mine/5ukk) | Human GRK2 in complex with human G-beta-gamma subunits and CCG211998 (14ak) | 分子名称: | 5-[(3S,4R)-3-{[(2H-1,3-benzodioxol-5-yl)oxy]methyl}piperidin-4-yl]-2-fluoro-N-[(pyridin-2-yl)methyl]benzamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | 著者 | Cato, M.C, Homan, K.T, Tesmer, J.J.G. | 登録日 | 2017-01-23 | 公開日 | 2017-04-05 | 最終更新日 | 2023-10-04 | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | 主引用文献 | Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors Based on Paroxetine. J. Med. Chem., 60, 2017
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5UPL
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5UKL
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![BU of 5ukl by Molmil](/molmil-images/mine/5ukl) | Human GRK2 in complex with Gbetagamma subunits and CCG222886 (14bd) | 分子名称: | 2-{5-[(3S,4R)-3-{[(2H-1,3-benzodioxol-5-yl)oxy]methyl}piperidin-4-yl]-2-fluorophenyl}-N-[2-(1H-pyrazol-4-yl)ethyl]acetamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | 著者 | Cato, M.C, Homan, K.T, Tesmer, J.J.G. | 登録日 | 2017-01-23 | 公開日 | 2017-04-05 | 最終更新日 | 2023-10-04 | 実験手法 | X-RAY DIFFRACTION (2.15 Å) | 主引用文献 | Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors Based on Paroxetine. J. Med. Chem., 60, 2017
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5UFU
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![BU of 5ufu by Molmil](/molmil-images/mine/5ufu) | Structure of AMPK bound to activator | 分子名称: | 1,4:3,6-dianhydro-2-O-(6-chloro-5-{4-[1-(hydroxymethyl)cyclopropyl]phenyl}-1H-benzimidazol-2-yl)-D-mannitol, 5'-AMP-activated protein kinase catalytic subunit alpha-1, 5'-AMP-activated protein kinase subunit beta-1, ... | 著者 | Calabrese, M.F, Kurumbail, R.G. | 登録日 | 2017-01-05 | 公開日 | 2017-05-17 | 実験手法 | X-RAY DIFFRACTION (3.45 Å) | 主引用文献 | Activation of Skeletal Muscle AMPK Promotes Glucose Disposal and Glucose Lowering in Non-human Primates and Mice. Cell Metab., 25, 2017
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5UQ3
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5UPK
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![BU of 5upk by Molmil](/molmil-images/mine/5upk) | CDC42 binds PAK4 via an extended GTPase-effector interface - 3 peptide: PAK4cat, PAK4-N45, CDC42 | 分子名称: | Cell division control protein 42 homolog, MAGNESIUM ION, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER, ... | 著者 | Ha, B.H, Boggon, T.J. | 登録日 | 2017-02-03 | 公開日 | 2017-12-27 | 最終更新日 | 2023-10-04 | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | 主引用文献 | CDC42 binds PAK4 via an extended GTPase-effector interface. Proc. Natl. Acad. Sci. U.S.A., 115, 2018
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