2BPM
| STRUCTURE OF CDK2-CYCLIN A WITH PHA-630529 | Descriptor: | (2S)-N-[(3Z)-5-CYCLOPROPYL-3H-PYRAZOL-3-YLIDENE]-2-[4-(2-OXOIMIDAZOLIDIN-1-YL)PHENYL]PROPANAMIDE, CELL DIVISION PROTEIN KINASE 2, CYCLIN A2, ... | Authors: | Cameron, A, Fogliatto, G, Pevarello, P, Brasca, M.G, Orsini, P, Traquandi, G, Longo, A, Nesi, M, Orzi, F, Piutti, C, Sansonna, P, Varasi, M, Vulpetti, A, Roletto, F, Alzani, R, Ciomei, M, Albanese, C, Pastori, W, Marsiglio, A, Pesenti, E, Fiorentini, F, Bischoff, J.R, Mercurio, C. | Deposit date: | 2005-04-21 | Release date: | 2005-12-08 | Last modified: | 2023-12-13 | Method: | X-RAY DIFFRACTION (2.4 Å) | Cite: | 3-Aminopyrazole Inhibitors of Cdk2-Cyclin a as Antitumor Agents. 2. Lead Optimization J.Med.Chem., 48, 2005
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2C4G
| STRUCTURE OF CDK2-CYCLIN A WITH PHA-533514 | Descriptor: | (3Z)-5-ACETYL-3-(BENZOYLIMINO)-3,6-DIHYDROPYRROLO[3,4-C]PYRAZOL-5-IUM, CELL DIVISION PROTEIN KINASE 2, CYCLIN A2, ... | Authors: | Cameron, A, Fogliatto, G, Pevarello, P, Fancelli, D, Vulpetti, A, Amici, R, Villa, M, Pittala, V, Ciomei, M, Mercurio, C, Bischoff, J.R, Roletto, F, Varasi, M, Brasca, M.G. | Deposit date: | 2005-10-19 | Release date: | 2005-11-23 | Last modified: | 2023-12-13 | Method: | X-RAY DIFFRACTION (2.7 Å) | Cite: | 3-Amino-1,4,5,6-Tetrahydropyrrolo[3,4-C]Pyrazoles: A New Class of Cdk2 Inhibitors. Bioorg.Med.Chem.Lett., 16, 2006
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8A2A
| EGFR kinase domain in complex with 2-(6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-1-yl)-2-[6-[2-[4-[[4-(hydroxymethyl)-1-piperidyl]methyl]phenyl]ethynyl]-1-oxo-4-(trifluoromethyl)isoindolin-2-yl]-N-thiazol-2-yl-acetamide (form 2) | Descriptor: | (2R)-2-(6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-1-yl)-2-[5-[2-[4-[[4-(hydroxymethyl)piperidin-1-yl]methyl]phenyl]ethynyl]-3-oxidanylidene-7-(trifluoromethyl)-1H-isoindol-2-yl]-N-(1,3-thiazol-2-yl)ethanamide, Epidermal growth factor receptor, SULFATE ION | Authors: | Kuglstatter, A, Ehler, A. | Deposit date: | 2022-06-03 | Release date: | 2022-10-19 | Last modified: | 2024-01-31 | Method: | X-RAY DIFFRACTION (1.43 Å) | Cite: | Discovery of Novel Allosteric EGFR L858R Inhibitors for the Treatment of Non-Small-Cell Lung Cancer as a Single Agent or in Combination with Osimertinib. J.Med.Chem., 65, 2022
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8A2B
| EGFR kinase domain (L858R/V948R) in complex with 2-(6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-1-yl)-2-[6-[2-[4-[[4-(hydroxymethyl)-1-piperidyl]methyl]phenyl]ethynyl]-1-oxo-4-(trifluoromethyl)isoindolin-2-yl]-N-thiazol-2-yl-acetamide | Descriptor: | (2R)-2-(6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-1-yl)-2-[5-[2-[4-[[4-(hydroxymethyl)piperidin-1-yl]methyl]phenyl]ethynyl]-3-oxidanylidene-7-(trifluoromethyl)-1H-isoindol-2-yl]-N-(1,3-thiazol-2-yl)ethanamide, Epidermal growth factor receptor | Authors: | Kuglstatter, A, Ehler, A. | Deposit date: | 2022-06-03 | Release date: | 2022-10-19 | Last modified: | 2024-01-31 | Method: | X-RAY DIFFRACTION (1.69 Å) | Cite: | Discovery of Novel Allosteric EGFR L858R Inhibitors for the Treatment of Non-Small-Cell Lung Cancer as a Single Agent or in Combination with Osimertinib. J.Med.Chem., 65, 2022
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8A27
| EGFR kinase domain in complex with 2-(6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-1-yl)-2-[6-[2-[4-[[4-(hydroxymethyl)-1-piperidyl]methyl]phenyl]ethynyl]-1-oxo-4-(trifluoromethyl)isoindolin-2-yl]-N-thiazol-2-yl-acetamide | Descriptor: | (2R)-2-(6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-1-yl)-2-[5-[2-[4-[[4-(hydroxymethyl)piperidin-1-yl]methyl]phenyl]ethynyl]-3-oxidanylidene-7-(trifluoromethyl)-1H-isoindol-2-yl]-N-(1,3-thiazol-2-yl)ethanamide, 1,2-ETHANEDIOL, Epidermal growth factor receptor, ... | Authors: | Kuglstatter, A, Ehler, A. | Deposit date: | 2022-06-02 | Release date: | 2022-10-19 | Last modified: | 2024-01-31 | Method: | X-RAY DIFFRACTION (1.07 Å) | Cite: | Discovery of Novel Allosteric EGFR L858R Inhibitors for the Treatment of Non-Small-Cell Lung Cancer as a Single Agent or in Combination with Osimertinib. J.Med.Chem., 65, 2022
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8A2D
| EGFR kinase domain (L858R/V948R) in complex with 2-[4-(difluoromethyl)-6-[2-[4-[[4-(hydroxymethyl)-1-piperidyl]methyl]phenyl]ethynyl]-7-methyl-indazol-2-yl]-2-spiro[6,7-dihydropyrrolo[1,2-c]imidazole-5,1'-cyclopropane]-1-yl-N-thiazol-2-yl-acetamide | Descriptor: | (2R)-2-[4-[bis(fluoranyl)methyl]-6-[2-[4-[[4-(hydroxymethyl)piperidin-1-yl]methyl]phenyl]ethynyl]-7-methyl-indazol-2-yl]-2-spiro[6,7-dihydropyrrolo[1,2-c]imidazole-5,1'-cyclopropane]-1-yl-N-(1,3-thiazol-2-yl)ethanamide, 1,2-ETHANEDIOL, 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, ... | Authors: | Kuglstatter, A, Ehler, A. | Deposit date: | 2022-06-03 | Release date: | 2022-10-19 | Last modified: | 2024-01-31 | Method: | X-RAY DIFFRACTION (1.11 Å) | Cite: | Discovery of Novel Allosteric EGFR L858R Inhibitors for the Treatment of Non-Small-Cell Lung Cancer as a Single Agent or in Combination with Osimertinib. J.Med.Chem., 65, 2022
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2RGF
| RBD OF RAL GUANOSINE-NUCLEOTIDE EXCHANGE FACTOR (PROTEIN), NMR, 10 STRUCTURES | Descriptor: | RALGEF-RBD | Authors: | Geyer, M, Herrmann, C, Wittinghofer, A, Kalbitzer, H.R. | Deposit date: | 1997-02-13 | Release date: | 1998-03-04 | Last modified: | 2024-05-22 | Method: | SOLUTION NMR | Cite: | Structure of the Ras-binding domain of RalGEF and implications for Ras binding and signalling. Nat.Struct.Biol., 4, 1997
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1RAX
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