8ROX
 
 | | Structure of the human DDB1-DDA1-DCAF15 E3 ubiquitin ligase bound to compound furan 12 | | 分子名称: | 5-[[3,4-bis(chloranyl)-1~{H}-indol-7-yl]sulfamoyl]-~{N},~{N},3-trimethyl-furan-2-carboxamide;ethane, DDB1- and CUL4-associated factor 15, DET1- and DDB1-associated protein 1, ... | | 著者 | Shilliday, F, Lucas, S.C.C, Richter, M, Michaelides, I.N, Fusani, L. | | 登録日 | 2024-01-12 | | 公開日 | 2024-04-03 | | 最終更新日 | 2024-05-22 | | 実験手法 | ELECTRON MICROSCOPY (3.3 Å) | | 主引用文献 | Optimization of Potent Ligands for the E3 Ligase DCAF15 and Evaluation of Their Use in Heterobifunctional Degraders.
J.Med.Chem., 67, 2024
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8ROY
 | | Structure of the human DDB1-DDA1-DCAF15 E3 ubiquitin ligase bound to compound furan 24 | | 分子名称: | 1-[5-[[3,4-bis(chloranyl)-1~{H}-indol-7-yl]sulfamoyl]-3-methyl-furan-2-yl]carbonyl-~{N}-methyl-piperidine-4-carboxamide, DDB1- and CUL4-associated factor 15, DET1- and DDB1-associated protein 1, ... | | 著者 | Shilliday, F, Lucas, S.C.C, Richter, M, Michaelides, I.N, Fusani, L. | | 登録日 | 2024-01-12 | | 公開日 | 2024-04-03 | | 最終更新日 | 2024-04-24 | | 実験手法 | ELECTRON MICROSCOPY (3.1 Å) | | 主引用文献 | Optimization of Potent Ligands for the E3 Ligase DCAF15 and Evaluation of Their Use in Heterobifunctional Degraders.
J.Med.Chem., 67, 2024
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8OUU
 | | Crystal structure of D1228V c-MET bound by compound 29 | | 分子名称: | 1,2-ETHANEDIOL, 5-(3-ethynyl-5-fluoranyl-1H-indazol-7-yl)-1-[(1S)-1-phenylethyl]pyrimidine-2,4-dione, FORMIC ACID, ... | | 著者 | Collie, G.W. | | 登録日 | 2023-04-24 | | 公開日 | 2023-07-05 | | 最終更新日 | 2023-07-26 | | 実験手法 | X-RAY DIFFRACTION (1.77 Å) | | 主引用文献 | Discovery and Optimization of the First ATP Competitive Type-III c-MET Inhibitor.
J.Med.Chem., 66, 2023
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8OUV
 | | Crystal structure of D1228V c-MET bound by compound 15 | | 分子名称: | 5-(1H-indazol-7-yl)-1-[(1S)-1-phenylethyl]pyrimidine-2,4-dione, CHLORIDE ION, Hepatocyte growth factor receptor | | 著者 | Collie, G.W. | | 登録日 | 2023-04-24 | | 公開日 | 2023-07-05 | | 最終更新日 | 2023-07-26 | | 実験手法 | X-RAY DIFFRACTION (1.783 Å) | | 主引用文献 | Discovery and Optimization of the First ATP Competitive Type-III c-MET Inhibitor.
J.Med.Chem., 66, 2023
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8OV7
 | | Crystal structure of D1228V c-MET bound by compound 10 | | 分子名称: | 5-[3,5-bis(fluoranyl)phenyl]-1-[(1S)-1-[3-(1H-imidazol-5-yl)phenyl]ethyl]pyrimidine-2,4-dione, Hepatocyte growth factor receptor | | 著者 | Collie, G.W. | | 登録日 | 2023-04-25 | | 公開日 | 2023-07-05 | | 最終更新日 | 2023-07-26 | | 実験手法 | X-RAY DIFFRACTION (1.95 Å) | | 主引用文献 | Discovery and Optimization of the First ATP Competitive Type-III c-MET Inhibitor.
J.Med.Chem., 66, 2023
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8OVZ
 | | Crystal structure of D1228V c-MET bound by compound 16 | | 分子名称: | 1-[(1S)-1-[3-(1H-imidazol-4-yl)phenyl]ethyl]-5-(1H-indazol-7-yl)pyrimidine-2,4-dione, Hepatocyte growth factor receptor, IODIDE ION | | 著者 | Collie, G.W. | | 登録日 | 2023-04-26 | | 公開日 | 2023-07-05 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (2.206 Å) | | 主引用文献 | Discovery and Optimization of the First ATP Competitive Type-III c-MET Inhibitor.
J.Med.Chem., 66, 2023
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8OW3
 | | Crystal structure of wild-type c-MET bound by compound 2 | | 分子名称: | 5-[3,5-bis(fluoranyl)phenyl]-1-[(1S)-1-phenylethyl]pyrimidine-2,4-dione, Hepatocyte growth factor receptor | | 著者 | Collie, G.W. | | 登録日 | 2023-04-26 | | 公開日 | 2023-07-05 | | 最終更新日 | 2023-07-26 | | 実験手法 | X-RAY DIFFRACTION (2.27 Å) | | 主引用文献 | Discovery and Optimization of the First ATP Competitive Type-III c-MET Inhibitor.
J.Med.Chem., 66, 2023
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8OWG
 | | Crystal structure of D1228V c-MET bound by compound 2 | | 分子名称: | 5-[3,5-bis(fluoranyl)phenyl]-1-[(1S)-1-phenylethyl]pyrimidine-2,4-dione, Hepatocyte growth factor receptor | | 著者 | Collie, G.W. | | 登録日 | 2023-04-27 | | 公開日 | 2023-07-05 | | 最終更新日 | 2023-07-26 | | 実験手法 | X-RAY DIFFRACTION (2.631 Å) | | 主引用文献 | Discovery and Optimization of the First ATP Competitive Type-III c-MET Inhibitor.
J.Med.Chem., 66, 2023
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8ANS
 | | Crystal structure of D1228V c-MET bound by compound 1. | | 分子名称: | 3-[bis(fluoranyl)methyl]-~{N}-methyl-~{N}-[(1~{R})-8-methyl-5-(3-methyl-1~{H}-indazol-6-yl)-1,2,3,4-tetrahydronaphthalen-1-yl]pyridine-2-carboxamide, GLYCEROL, Hepatocyte growth factor receptor | | 著者 | Collie, G.W. | | 登録日 | 2022-08-05 | | 公開日 | 2022-08-31 | | 最終更新日 | 2024-01-31 | | 実験手法 | X-RAY DIFFRACTION (2.01 Å) | | 主引用文献 | Discovery of a selective c-MET inhibitor with a novel binding mode.
Bioorg.Med.Chem.Lett., 75, 2022
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8AN8
 | | Crystal structure of wild-type c-MET bound by compound 7. | | 分子名称: | 3-[bis(fluoranyl)methyl]-~{N}-methyl-~{N}-[(1~{R})-8-methyl-5-(3-methyl-1~{H}-indazol-6-yl)-1,2,3,4-tetrahydronaphthalen-1-yl]pyridine-2-carboxamide, Hepatocyte growth factor receptor, SULFATE ION | | 著者 | Collie, G.W. | | 登録日 | 2022-08-04 | | 公開日 | 2022-08-31 | | 最終更新日 | 2024-05-01 | | 実験手法 | X-RAY DIFFRACTION (2.394 Å) | | 主引用文献 | Discovery of a selective c-MET inhibitor with a novel binding mode.
Bioorg.Med.Chem.Lett., 75, 2022
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7B42
 | | Crystal structure of c-MET bound by compound 8 | | 分子名称: | 3-[(3-fluorophenyl)methyl]-5-(1-piperidin-4-ylpyrazol-4-yl)-1~{H}-pyrrolo[2,3-b]pyridine, Hepatocyte growth factor receptor | | 著者 | Collie, G.W. | | 登録日 | 2020-12-02 | | 公開日 | 2020-12-09 | | 最終更新日 | 2024-05-01 | | 実験手法 | X-RAY DIFFRACTION (1.8 Å) | | 主引用文献 | Structural Basis for Targeting the Folded P-Loop Conformation of c-MET.
Acs Med.Chem.Lett., 12, 2021
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7B3W
 | | Crystal structure of c-MET bound by compound 4 | | 分子名称: | 1,2-ETHANEDIOL, 3-(6-fluoranyl-1~{H}-indazol-4-yl)-4,5-dihydro-1~{H}-pyrrolo[3,4-b]pyrrol-6-one, Hepatocyte growth factor receptor | | 著者 | Collie, G.W. | | 登録日 | 2020-12-01 | | 公開日 | 2020-12-09 | | 最終更新日 | 2024-05-01 | | 実験手法 | X-RAY DIFFRACTION (2.02 Å) | | 主引用文献 | Structural Basis for Targeting the Folded P-Loop Conformation of c-MET.
Acs Med.Chem.Lett., 12, 2021
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7B43
 | | Crystal structure of c-MET bound by compound 9 | | 分子名称: | 3-[(4-fluorophenyl)methyl]-5-(1-piperidin-4-ylpyrazol-4-yl)-1~{H}-pyrrolo[2,3-b]pyridine, Hepatocyte growth factor receptor | | 著者 | Collie, G.W. | | 登録日 | 2020-12-02 | | 公開日 | 2020-12-09 | | 最終更新日 | 2024-05-01 | | 実験手法 | X-RAY DIFFRACTION (1.87 Å) | | 主引用文献 | Structural Basis for Targeting the Folded P-Loop Conformation of c-MET.
Acs Med.Chem.Lett., 12, 2021
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7B3Q
 | | Crystal structure of c-MET bound by compound 1 | | 分子名称: | 1-(phenylmethyl)-5~{H}-pyrrolo[3,2-c]pyridin-4-one, Hepatocyte growth factor receptor, SULFATE ION | | 著者 | Collie, G.W. | | 登録日 | 2020-12-01 | | 公開日 | 2020-12-09 | | 最終更新日 | 2024-05-01 | | 実験手法 | X-RAY DIFFRACTION (1.75 Å) | | 主引用文献 | Structural Basis for Targeting the Folded P-Loop Conformation of c-MET.
Acs Med.Chem.Lett., 12, 2021
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7B40
 | | Crystal structure of c-MET bound by compound 6 | | 分子名称: | 3-(phenylmethyl)-5-(1-piperidin-4-ylpyrazol-4-yl)-1~{H}-pyrrolo[2,3-b]pyridine, Hepatocyte growth factor receptor | | 著者 | Collie, G.W. | | 登録日 | 2020-12-01 | | 公開日 | 2020-12-09 | | 最終更新日 | 2024-05-01 | | 実験手法 | X-RAY DIFFRACTION (1.76 Å) | | 主引用文献 | Structural Basis for Targeting the Folded P-Loop Conformation of c-MET.
Acs Med.Chem.Lett., 12, 2021
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7B3Z
 | | Crystal structure of c-MET bound by compound 5 | | 分子名称: | 3-[3-(phenylmethyl)-1~{H}-pyrrolo[2,3-b]pyridin-5-yl]-4,5-dihydro-1~{H}-pyrrolo[3,4-b]pyrrol-6-one, DIMETHYL SULFOXIDE, Hepatocyte growth factor receptor | | 著者 | Collie, G.W. | | 登録日 | 2020-12-01 | | 公開日 | 2020-12-09 | | 最終更新日 | 2024-05-01 | | 実験手法 | X-RAY DIFFRACTION (1.8 Å) | | 主引用文献 | Structural Basis for Targeting the Folded P-Loop Conformation of c-MET.
Acs Med.Chem.Lett., 12, 2021
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7B3V
 | | Crystal structure of c-MET bound by compound 3 | | 分子名称: | 3-(3-methyl-1~{H}-pyrrolo[2,3-b]pyridin-5-yl)-1~{H}-pyrrolo[3,4-b]pyrrol-6-one, Hepatocyte growth factor receptor | | 著者 | Collie, G.W. | | 登録日 | 2020-12-01 | | 公開日 | 2020-12-09 | | 最終更新日 | 2024-05-01 | | 実験手法 | X-RAY DIFFRACTION (1.93 Å) | | 主引用文献 | Structural Basis for Targeting the Folded P-Loop Conformation of c-MET.
Acs Med.Chem.Lett., 12, 2021
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7B44
 | | Crystal structure of c-MET bound by compound S1 | | 分子名称: | 5-methoxy-1~{H}-indazole, DIMETHYL SULFOXIDE, Hepatocyte growth factor receptor, ... | | 著者 | Collie, G.W. | | 登録日 | 2020-12-02 | | 公開日 | 2020-12-09 | | 最終更新日 | 2024-05-01 | | 実験手法 | X-RAY DIFFRACTION (1.76 Å) | | 主引用文献 | Structural Basis for Targeting the Folded P-Loop Conformation of c-MET.
Acs Med.Chem.Lett., 12, 2021
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7B3T
 | | Crystal structure of c-MET bound by compound 2 | | 分子名称: | 3-(phenylmethyl)-1~{H}-pyrrolo[2,3-b]pyridine, CHLORIDE ION, Hepatocyte growth factor receptor, ... | | 著者 | Collie, G.W. | | 登録日 | 2020-12-01 | | 公開日 | 2020-12-09 | | 最終更新日 | 2024-05-01 | | 実験手法 | X-RAY DIFFRACTION (2.23 Å) | | 主引用文献 | Structural Basis for Targeting the Folded P-Loop Conformation of c-MET.
Acs Med.Chem.Lett., 12, 2021
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7B41
 | | Crystal structure of c-MET bound by compound 7 | | 分子名称: | 3-[(2-fluorophenyl)methyl]-5-(1-piperidin-4-ylpyrazol-4-yl)-1~{H}-pyrrolo[2,3-b]pyridine, Hepatocyte growth factor receptor | | 著者 | Collie, G.W. | | 登録日 | 2020-12-02 | | 公開日 | 2020-12-09 | | 最終更新日 | 2024-05-01 | | 実験手法 | X-RAY DIFFRACTION (1.97 Å) | | 主引用文献 | Structural Basis for Targeting the Folded P-Loop Conformation of c-MET.
Acs Med.Chem.Lett., 12, 2021
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