3CD8
 
 | | X-ray Structure of c-Met with triazolopyridazine Inhibitor. | | 分子名称: | 7-methoxy-4-[(6-phenyl[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methoxy]quinoline, Hepatocyte growth factor receptor | | 著者 | Bellon, S.F, Albrecht, B.K, Harmange, J.-C, Bauer, D, Choquette, D, Dussault, I. | | 登録日 | 2008-02-26 | | 公開日 | 2008-04-29 | | 最終更新日 | 2023-08-30 | | 実験手法 | X-RAY DIFFRACTION (2 Å) | | 主引用文献 | Discovery and Optimization of Triazolopyridazines as Potent and Selective Inhibitors of the c-Met Kinase.
J.Med.Chem., 51, 2008
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5EYC
 | | Crystal structure of c-Met in complex with naphthyridinone inhibitor 5 | | 分子名称: | 6-[(1~{R})-1-[8-fluoranyl-6-(3-methyl-1,2-oxazol-5-yl)-[1,2,4]triazolo[4,3-a]pyridin-3-yl]ethyl]-1,6-naphthyridin-5-one, Hepatocyte growth factor receptor | | 著者 | Whittington, D.A, Long, A.M. | | 登録日 | 2015-11-24 | | 公開日 | 2016-02-10 | | 最終更新日 | 2023-09-27 | | 実験手法 | X-RAY DIFFRACTION (1.8 Å) | | 主引用文献 | Discovery of (R)-6-(1-(8-Fluoro-6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)ethyl)-3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)-one (AMG 337), a Potent and Selective Inhibitor of MET with High Unbound Target Coverage and Robust In Vivo Antitumor Activity.
J.Med.Chem., 59, 2016
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5EYD
 | | Crystal structure of c-Met in complex with AMG 337 | | 分子名称: | 6-[(1~{R})-1-[8-fluoranyl-6-(1-methylpyrazol-4-yl)-[1,2,4]triazolo[4,3-a]pyridin-3-yl]ethyl]-3-(2-methoxyethoxy)-1,6-naphthyridin-5-one, Hepatocyte growth factor receptor | | 著者 | Whittington, D.A, Long, A.M. | | 登録日 | 2015-11-24 | | 公開日 | 2016-02-10 | | 最終更新日 | 2023-09-27 | | 実験手法 | X-RAY DIFFRACTION (1.85 Å) | | 主引用文献 | Discovery of (R)-6-(1-(8-Fluoro-6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)ethyl)-3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)-one (AMG 337), a Potent and Selective Inhibitor of MET with High Unbound Target Coverage and Robust In Vivo Antitumor Activity.
J.Med.Chem., 59, 2016
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4FJY
 | | Crystal structure of PI3K-gamma in complex with quinoline-indoline inhibitor 24f | | 分子名称: | 4-[3,3-dimethyl-6-(morpholin-4-yl)-2,3-dihydro-1H-indol-1-yl]-7-fluoro-3-methyl-2-(pyridin-3-yl)quinoline, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform, SULFATE ION | | 著者 | Whittington, D.A, Tang, J, Yakowec, P. | | 登録日 | 2012-06-12 | | 公開日 | 2012-10-24 | | 最終更新日 | 2024-02-28 | | 実験手法 | X-RAY DIFFRACTION (2.9 Å) | | 主引用文献 | Discovery and in Vivo Evaluation of Dual PI3K-beta/delta inhibitors
J.Med.Chem., 55, 2012
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4FJZ
 | | Crystal structure of PI3K-gamma in complex with pyrrolo-pyridine inhibitor 63 | | 分子名称: | 1'-[7-fluoro-3-methyl-2-(pyridin-2-yl)quinolin-4-yl]-6'-(morpholin-4-yl)-1',2,2',3,5,6-hexahydrospiro[pyran-4,3'-pyrrolo[3,2-b]pyridine], Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform, SULFATE ION | | 著者 | Whittington, D.A, Tang, J, Yakowec, P. | | 登録日 | 2012-06-12 | | 公開日 | 2012-10-24 | | 最終更新日 | 2024-02-28 | | 実験手法 | X-RAY DIFFRACTION (3 Å) | | 主引用文献 | Discovery and in Vivo Evaluation of Dual PI3K-beta/delta inhibitors
J.Med.Chem., 55, 2012
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3I5N
 | | Crystal structure of c-Met with triazolopyridazine inhibitor 13 | | 分子名称: | 7-methoxy-N-[(6-phenyl[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methyl]-1,5-naphthyridin-4-amine, Hepatocyte growth factor receptor | | 著者 | Bellon, S.F, Whittington, D.A, Long, A.M, Boezio, A.A. | | 登録日 | 2009-07-06 | | 公開日 | 2010-01-12 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (2 Å) | | 主引用文献 | Discovery and optimization of potent and selective triazolopyridazine series of c-Met inhibitors
Bioorg.Med.Chem.Lett., 19, 2009
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6SKV
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6SKS
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6SKT
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5NK2
 | | Crystal Structure of Ephrin A2 (EphA2) Receptor Protein Kinase with Compound 2b | | 分子名称: | 1,2-ETHANEDIOL, Ephrin type-A receptor 2, ~{N}-(2-chloranyl-6-methyl-phenyl)-2-[[3-[[(3~{R},4~{R})-3-fluoranylpiperidin-4-yl]carbamoyl]phenyl]amino]-1,3-thiazole-5-carboxamide | | 著者 | Kudlinzki, D, Linhard, V.L, Witt, K, Gande, S.L, Saxena, K, Heinzlmeir, S, Medard, G, Kuester, B, Schwalbe, H. | | 登録日 | 2017-03-31 | | 公開日 | 2017-06-07 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (1.649 Å) | | 主引用文献 | Chemoproteomics-Aided Medicinal Chemistry for the Discovery of EPHA2 Inhibitors.
ChemMedChem, 12, 2017
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5NJZ
 | | Crystal Structure of Ephrin A2 (EphA2) Receptor Protein Kinase with Compound 1g | | 分子名称: | Ephrin type-A receptor 2, ~{N}-(2-chloranyl-6-methyl-phenyl)-2-[[3-(piperidin-4-ylcarbamoyl)phenyl]amino]-1,3-thiazole-5-carboxamide | | 著者 | Kudlinzki, D, Linhard, V.L, Witt, K, Gande, S.L, Saxena, K, Heinzlmeir, S, Medard, G, Kuester, B, Schwalbe, H. | | 登録日 | 2017-03-31 | | 公開日 | 2017-06-07 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (1.768 Å) | | 主引用文献 | Chemoproteomics-Aided Medicinal Chemistry for the Discovery of EPHA2 Inhibitors.
ChemMedChem, 12, 2017
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5NKA
 | | Crystal Structure of Ephrin A2 (EphA2) Receptor Protein Kinase with Compound 2g | | 分子名称: | 1,2-ETHANEDIOL, 4-[[3-[[5-[(2-chloranyl-6-methyl-phenyl)carbamoyl]-1,3-thiazol-2-yl]amino]phenyl]carbonylamino]cyclohexane-1-carboxylic acid, Ephrin type-A receptor 2 | | 著者 | Kudlinzki, D, Linhard, V.L, Witt, K, Gande, S.L, Saxena, K, Heinzlmeir, S, Medard, G, Kuester, B, Schwalbe, H. | | 登録日 | 2017-03-31 | | 公開日 | 2017-06-07 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (1.377 Å) | | 主引用文献 | Chemoproteomics-Aided Medicinal Chemistry for the Discovery of EPHA2 Inhibitors.
ChemMedChem, 12, 2017
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5NK1
 | | Crystal Structure of Ephrin A2 (EphA2) Receptor Protein Kinase with Compound 1k | | 分子名称: | 2-[[3-[(4-azanyl-6-methyl-1,3,5-triazin-2-yl)carbamoyl]phenyl]amino]-~{N}-(2-chloranyl-6-methyl-phenyl)-1,3-thiazole-5-carboxamide, Ephrin type-A receptor 2 | | 著者 | Kudlinzki, D, Linhard, V.L, Witt, K, Gande, S.L, Saxena, K, Heinzlmeir, S, Medard, G, Kuester, B, Schwalbe, H. | | 登録日 | 2017-03-31 | | 公開日 | 2017-06-07 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (1.548 Å) | | 主引用文献 | Chemoproteomics-Aided Medicinal Chemistry for the Discovery of EPHA2 Inhibitors.
ChemMedChem, 12, 2017
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5NK6
 | | Crystal Structure of Ephrin A2 (EphA2) Receptor Protein Kinase with Compound 2d | | 分子名称: | Ephrin type-A receptor 2, ~{N}-(2-chloranyl-6-methyl-phenyl)-2-[[3-[(4-oxidanylcyclohexyl)carbamoyl]phenyl]amino]-1,3-thiazole-5-carboxamide | | 著者 | Kudlinzki, D, Linhard, V.L, Witt, K, Gande, S.L, Saxena, K, Heinzlmeir, S, Medard, G, Kuester, B, Schwalbe, H. | | 登録日 | 2017-03-31 | | 公開日 | 2017-06-07 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (1.267 Å) | | 主引用文献 | Chemoproteomics-Aided Medicinal Chemistry for the Discovery of EPHA2 Inhibitors.
ChemMedChem, 12, 2017
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5NK5
 | | Crystal Structure of Ephrin A2 (EphA2) Receptor Protein Kinase with Compound 1m | | 分子名称: | 2-[[3-[(3-aminophenyl)carbamoyl]phenyl]amino]-~{N}-(2-chloranyl-6-methyl-phenyl)-1,3-thiazole-5-carboxamide, Ephrin type-A receptor 2 | | 著者 | Kudlinzki, D, Linhard, V.L, Witt, K, Gande, S.L, Saxena, K, Heinzlmeir, S, Medard, G, Kuester, B, Schwalbe, H. | | 登録日 | 2017-03-31 | | 公開日 | 2017-06-07 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (1.329 Å) | | 主引用文献 | Chemoproteomics-Aided Medicinal Chemistry for the Discovery of EPHA2 Inhibitors.
ChemMedChem, 12, 2017
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5NKD
 | | Crystal Structure of Ephrin A2 (EphA2) Receptor Protein Kinase with Compound 2i | | 分子名称: | 1,2-ETHANEDIOL, 2-[(3~{R})-1-[3-[[5-[(2-chloranyl-6-methyl-phenyl)carbamoyl]-1,3-thiazol-2-yl]amino]phenyl]carbonylpyrrolidin-3-yl]ethanoic acid, Ephrin type-A receptor 2 | | 著者 | Kudlinzki, D, Linhard, V.L, Witt, K, Gande, S.L, Saxena, K, Heinzlmeir, S, Medard, G, Kuester, B, Schwalbe, H. | | 登録日 | 2017-03-31 | | 公開日 | 2017-06-07 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (1.408 Å) | | 主引用文献 | Chemoproteomics-Aided Medicinal Chemistry for the Discovery of EPHA2 Inhibitors.
ChemMedChem, 12, 2017
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5NK0
 | | Crystal Structure of Ephrin A2 (EphA2) Receptor Protein Kinase with Compound 1j | | 分子名称: | 2-[[3-[(3-azanyl-2,2-dimethyl-propyl)carbamoyl]phenyl]amino]-~{N}-(2-chloranyl-6-methyl-phenyl)-1,3-thiazole-5-carboxamide, Ephrin type-A receptor 2 | | 著者 | Kudlinzki, D, Linhard, V.L, Witt, K, Gande, S.L, Saxena, K, Heinzlmeir, S, Medard, G, Kuester, B, Schwalbe, H. | | 登録日 | 2017-03-31 | | 公開日 | 2017-06-07 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (1.597 Å) | | 主引用文献 | Chemoproteomics-Aided Medicinal Chemistry for the Discovery of EPHA2 Inhibitors.
ChemMedChem, 12, 2017
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5NK4
 | | Crystal Structure of Ephrin A2 (EphA2) Receptor Protein Kinase with Compound 2c | | 分子名称: | 1,2-ETHANEDIOL, 2-[[3-[[(4~{R})-3,3-bis(fluoranyl)piperidin-4-yl]carbamoyl]phenyl]amino]-~{N}-(2-chloranyl-6-methyl-phenyl)-1,3-thiazole-5-carboxamide, Ephrin type-A receptor 2 | | 著者 | Kudlinzki, D, Linhard, V.L, Witt, K, Gande, S.L, Saxena, K, Heinzlmeir, S, Medard, G, Kuester, B, Schwalbe, H. | | 登録日 | 2017-03-31 | | 公開日 | 2017-06-07 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (1.45 Å) | | 主引用文献 | Chemoproteomics-Aided Medicinal Chemistry for the Discovery of EPHA2 Inhibitors.
ChemMedChem, 12, 2017
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5NKB
 | | Crystal Structure of Ephrin A2 (EphA2) Receptor Protein Kinase with Compound 4a | | 分子名称: | 1,2-ETHANEDIOL, Ephrin type-A receptor 2, ~{N}-(2-chloranyl-6-methyl-phenyl)-2-[(3,5-dimorpholin-4-ylphenyl)amino]-1,3-thiazole-5-carboxamide | | 著者 | Kudlinzki, D, Linhard, V.L, Witt, K, Gande, S.L, Saxena, K, Heinzlmeir, S, Medard, G, Kuester, B, Schwalbe, H. | | 登録日 | 2017-03-31 | | 公開日 | 2017-06-07 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (1.5 Å) | | 主引用文献 | Chemoproteomics-Aided Medicinal Chemistry for the Discovery of EPHA2 Inhibitors.
ChemMedChem, 12, 2017
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5NKH
 | | Crystal Structure of Ephrin A2 (EphA2) Receptor Protein Kinase with Compound 3e | | 分子名称: | 2-[[3-(2-aminophenyl)-5-(piperidin-4-ylcarbamoyl)phenyl]amino]-~{N}-(2-chloranyl-6-methyl-phenyl)-1,3-thiazole-5-carboxamide, Ephrin type-A receptor 2 | | 著者 | Kudlinzki, D, Linhard, V.L, Witt, K, Gande, S.L, Saxena, K, Heinzlmeir, S, Medard, G, Kuester, B, Schwalbe, H. | | 登録日 | 2017-03-31 | | 公開日 | 2017-06-07 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (1.29 Å) | | 主引用文献 | Chemoproteomics-Aided Medicinal Chemistry for the Discovery of EPHA2 Inhibitors.
ChemMedChem, 12, 2017
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5NKE
 | | Crystal Structure of Ephrin A2 (EphA2) Receptor Protein Kinase with Compound 3a | | 分子名称: | 2-[[3-bromanyl-5-(piperidin-4-ylcarbamoyl)phenyl]amino]-~{N}-(2-chloranyl-6-methyl-phenyl)-1,3-thiazole-5-carboxamide, Ephrin type-A receptor 2 | | 著者 | Kudlinzki, D, Linhard, V.L, Witt, K, Gande, S.L, Saxena, K, Heinzlmeir, S, Medard, G, Kuester, B, Schwalbe, H. | | 登録日 | 2017-03-31 | | 公開日 | 2017-06-07 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (1.39 Å) | | 主引用文献 | Chemoproteomics-Aided Medicinal Chemistry for the Discovery of EPHA2 Inhibitors.
ChemMedChem, 12, 2017
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5NK8
 | | Crystal Structure of Ephrin A2 (EphA2) Receptor Protein Kinase with Compound 2f | | 分子名称: | Ephrin type-A receptor 2, ~{N}-(2-chloranyl-6-methyl-phenyl)-2-[[3-[(2,2,6,6-tetramethyl-1-oxidanyl-piperidin-4-yl)carbamoyl]phenyl]amino]-1,3-thiazole-5-carboxamide | | 著者 | Kudlinzki, D, Linhard, V.L, Witt, K, Gande, S.L, Saxena, K, Heinzlmeir, S, Medard, G, Kuester, B, Schwalbe, H. | | 登録日 | 2017-03-31 | | 公開日 | 2017-06-07 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (1.761 Å) | | 主引用文献 | Chemoproteomics-Aided Medicinal Chemistry for the Discovery of EPHA2 Inhibitors.
ChemMedChem, 12, 2017
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5NKG
 | | Crystal Structure of Ephrin A2 (EphA2) Receptor Protein Kinase with Compound 3d | | 分子名称: | Ephrin type-A receptor 2, ~{N}-(2-chloranyl-6-methyl-phenyl)-2-[[3-ethyl-5-(piperidin-4-ylcarbamoyl)phenyl]amino]-1,3-thiazole-5-carboxamide | | 著者 | Kudlinzki, D, Linhard, V.L, Witt, K, Gande, S.L, Saxena, K, Heinzlmeir, S, Medard, G, Kuester, B, Schwalbe, H. | | 登録日 | 2017-03-31 | | 公開日 | 2017-06-07 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (1.1 Å) | | 主引用文献 | Chemoproteomics-Aided Medicinal Chemistry for the Discovery of EPHA2 Inhibitors.
ChemMedChem, 12, 2017
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5NK9
 | | Crystal Structure of Ephrin A2 (EphA2) Receptor Protein Kinase with Compound 2e | | 分子名称: | (2~{Z})-~{N}-(2-chloranyl-6-methyl-phenyl)-2-[3-[(4-methyl-4-oxidanyl-cyclohexyl)carbamoyl]phenyl]imino-1,3-thiazolidine-5-carboxamide, Ephrin type-A receptor 2 | | 著者 | Kudlinzki, D, Linhard, V.L, Witt, K, Gande, S.L, Saxena, K, Heinzlmeir, S, Medard, G, Kuester, B, Schwalbe, H. | | 登録日 | 2017-03-31 | | 公開日 | 2017-06-07 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (1.588 Å) | | 主引用文献 | Chemoproteomics-Aided Medicinal Chemistry for the Discovery of EPHA2 Inhibitors.
ChemMedChem, 12, 2017
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5NKI
 | | Crystal Structure of Ephrin A2 (EphA2) Receptor Protein Kinase with Compound 4b | | 分子名称: | Ephrin type-A receptor 2, ~{N}-(2-chloranyl-6-methyl-phenyl)-2-[(3-methylsulfonyl-5-morpholin-4-yl-phenyl)amino]-1,3-thiazole-5-carboxamide | | 著者 | Kudlinzki, D, Linhard, V.L, Witt, K, Gande, S.L, Saxena, K, Heinzlmeir, S, Medard, G, Kuester, B, Schwalbe, H. | | 登録日 | 2017-03-31 | | 公開日 | 2017-06-07 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (1.675 Å) | | 主引用文献 | Chemoproteomics-Aided Medicinal Chemistry for the Discovery of EPHA2 Inhibitors.
ChemMedChem, 12, 2017
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