3V5W
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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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5WG4
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![BU of 5wg4 by Molmil](/molmil-images/mine/5wg4) | Human GRK2 in complex with Gbetagamma subunits and CCG257284 | 分子名称: | 2-fluoro-5-[(3S,4R)-3-{[(1H-indazol-5-yl)oxy]methyl}piperidin-4-yl]-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 | Bouley, R, Tesmer, J.J.G. | 登録日 | 2017-07-13 | 公開日 | 2017-12-27 | 最終更新日 | 2023-10-04 | 実験手法 | X-RAY DIFFRACTION (2.31 Å) | 主引用文献 | Structural Determinants Influencing the Potency and Selectivity of Indazole-Paroxetine Hybrid G Protein-Coupled Receptor Kinase 2 Inhibitors. Mol. Pharmacol., 92, 2017
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4MK0
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6U7C
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![BU of 6u7c by Molmil](/molmil-images/mine/6u7c) | Human GRK2 in complex with Gbetagamma subunits and CCG258747 | 分子名称: | 5-[(3S,4R)-3-{[(2H-1,3-benzodioxol-5-yl)oxy]methyl}piperidin-4-yl]-2-fluoro-N-[(2H-indazol-3-yl)methyl]benzamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | 著者 | Bouley, R, Tesmer, J.J.G. | 登録日 | 2019-09-02 | 公開日 | 2020-04-15 | 最終更新日 | 2023-10-11 | 実験手法 | X-RAY DIFFRACTION (2.44 Å) | 主引用文献 | A New Paroxetine-Based GRK2 Inhibitor Reduces Internalization of themu-Opioid Receptor. Mol.Pharmacol., 97, 2020
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7K7L
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4PNK
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![BU of 4pnk by Molmil](/molmil-images/mine/4pnk) | G protein-coupled receptor kinase 2 in complex with GSK180736A | 分子名称: | (4S)-4-(4-fluorophenyl)-N-(2H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | 著者 | Homan, K.T, Larimore, K.M, Elkins, J, Knapp, S, Tesmer, J.J.G. | 登録日 | 2014-05-23 | 公開日 | 2014-10-08 | 最終更新日 | 2023-12-27 | 実験手法 | X-RAY DIFFRACTION (2.56 Å) | 主引用文献 | Identification and structure-function analysis of subfamily selective g protein-coupled receptor kinase inhibitors. Acs Chem.Biol., 10, 2015
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7PWD
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![BU of 7pwd by Molmil](/molmil-images/mine/7pwd) | Structure of an inhibited GRK2-G-beta and G-gamma complex | 分子名称: | 4-chloranyl-N-[2-(4-chlorophenyl)ethyl]thieno[2,3-c]pyridine-2-carboxamide, Beta-adrenergic receptor kinase 1, CHLORIDE ION, ... | 著者 | Faucher, N, Tauchert, M.J, Konz Makino, D.L, Vuillard, L.M. | 登録日 | 2021-10-06 | 公開日 | 2021-10-20 | 最終更新日 | 2024-06-19 | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | 主引用文献 | Synthesis of thieno[2,3-c]pyridine derived GRK2 inhibitors Monatsh Chem, 2022
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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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7K7Z
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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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5UUU
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![BU of 5uuu by Molmil](/molmil-images/mine/5uuu) | 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: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, 3-({[4-methyl-5-(pyridin-4-yl)-4H-1,2,4-triazol-3-yl]methyl}amino)-N-[2-(trifluoromethyl)benzyl]benzamide, Beta-adrenergic receptor kinase 1, ... | 著者 | Hoffman, I.D, Lawson, J.D. | 登録日 | 2017-02-17 | 公開日 | 2017-07-26 | 最終更新日 | 2024-03-06 | 実験手法 | X-RAY DIFFRACTION (2.7 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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6C2Y
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![BU of 6c2y by Molmil](/molmil-images/mine/6c2y) | Human GRK2 in complex with Gbetagamma subunits and CCG257142 | 分子名称: | (4R,5R,6S)-4-[4-fluoro-3-({[3-(methoxymethyl)-1,2,4-oxadiazol-5-yl]methyl}carbamoyl)phenyl]-N-(2H-indazol-5-yl)-6-methyl-2-oxohexahydropyrimidine-5-carboxamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | 著者 | Bouley, R, Tesmer, J.J.G. | 登録日 | 2018-01-09 | 公開日 | 2018-04-25 | 最終更新日 | 2023-10-04 | 実験手法 | X-RAY DIFFRACTION (2.74 Å) | 主引用文献 | Utilizing a structure-based docking approach to develop potent G protein-coupled receptor kinase (GRK) 2 and 5 inhibitors. Bioorg. Med. Chem. Lett., 28, 2018
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3CIK
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![BU of 3cik by Molmil](/molmil-images/mine/3cik) | Human GRK2 in Complex with Gbetagamma subunits | 分子名称: | Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, ... | 著者 | Tesmer, J.J.G, Lodowski, D.T. | 登録日 | 2008-03-11 | 公開日 | 2009-02-17 | 最終更新日 | 2012-03-07 | 実験手法 | X-RAY DIFFRACTION (2.75 Å) | 主引用文献 | Structure of human G protein-coupled receptor kinase 2 in complex with the kinase inhibitor balanol. J.Med.Chem., 53, 2010
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5WG3
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![BU of 5wg3 by Molmil](/molmil-images/mine/5wg3) | Human GRK2 in complex with Gbetagamma subunits and CCG258748 | 分子名称: | 2-fluoro-5-[(3S,4R)-3-{[(1H-indazol-5-yl)oxy]methyl}piperidin-4-yl]-N-[(1H-pyrazol-3-yl)methyl]benzamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | 著者 | Bouley, R, Tesmer, J.J.G. | 登録日 | 2017-07-13 | 公開日 | 2017-12-27 | 最終更新日 | 2023-10-04 | 実験手法 | X-RAY DIFFRACTION (2.896 Å) | 主引用文献 | Structural Determinants Influencing the Potency and Selectivity of Indazole-Paroxetine Hybrid G Protein-Coupled Receptor Kinase 2 Inhibitors. Mol. Pharmacol., 92, 2017
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3KRW
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5WG5
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![BU of 5wg5 by Molmil](/molmil-images/mine/5wg5) | Human GRK2 in complex with Gbetagamma subunits and CCG224061 | 分子名称: | 5-{[(3S,4R)-4-(4-fluorophenyl)piperidin-3-yl]methoxy}-2H-indazole, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | 著者 | Bouley, R, Tesmer, J.J.G. | 登録日 | 2017-07-13 | 公開日 | 2017-12-27 | 最終更新日 | 2023-10-04 | 実験手法 | X-RAY DIFFRACTION (3.1 Å) | 主引用文献 | Structural Determinants Influencing the Potency and Selectivity of Indazole-Paroxetine Hybrid G Protein-Coupled Receptor Kinase 2 Inhibitors. Mol. Pharmacol., 92, 2017
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3KRX
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5HE1
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![BU of 5he1 by Molmil](/molmil-images/mine/5he1) | Human GRK2 in complex with Gbetagamma subunits and CCG224062 | 分子名称: | (4~{S})-4-[4-fluoranyl-3-(isoquinolin-1-ylmethylcarbamoyl)phenyl]-~{N}-(1~{H}-indazol-5-yl)-6-methyl-2-oxidanylidene-3,4-dihydro-1~{H}-pyrimidine-5-carboxamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | 著者 | Cato, M.C, Tesmer, J.J.G. | 登録日 | 2016-01-05 | 公開日 | 2016-05-11 | 最終更新日 | 2024-03-06 | 実験手法 | X-RAY DIFFRACTION (3.15 Å) | 主引用文献 | Structure-Based Design, Synthesis, and Biological Evaluation of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors. J.Med.Chem., 59, 2016
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1BAK
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![BU of 1bak by Molmil](/molmil-images/mine/1bak) | |