4CQE
| B-Raf Kinase V600E mutant in complex with a diarylthiazole B-Raf Inhibitor | Descriptor: | N-{4-[2-(1-cyclopropylpiperidin-4-yl)-4-(3-{[(2,5-difluorophenyl)sulfonyl]amino}-2-fluorophenyl)-1,3-thiazol-5-yl]pyridin-2-yl}acetamide, SLC45A3-BRAF FUSION PROTEIN | Authors: | Casale, E, Fasolini, M, Pulici, M, Traquandi, G, Marchionni, C, Modugno, M, Lupi, R, Amboldi, N, Colombo, N, Corti, L, Gasparri, F, Pastori, W, Scolaro, A, Donati, D, Felder, E, Galvani, A, Isacchi, A, Pesenti, E, Ciomei, M. | Deposit date: | 2014-02-14 | Release date: | 2014-12-10 | Last modified: | 2023-12-20 | Method: | X-RAY DIFFRACTION (2.3 Å) | Cite: | Optimization of Diarylthiazole B-Raf Inhibitors: Identification of a Compound Endowed with High Oral Antitumor Activity, Mitigated Herg Inhibition, and Low Paradoxical Effect. Chemmedchem, 10, 2015
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2XRU
| AURORA-A T288E COMPLEXED WITH PHA-828300 | Descriptor: | 3-({[4-(4-METHYLPIPERAZIN-1-YL)PHENYL]CARBONYL}AMINO)-N-[(1R)-1-PHENYLPROPYL]-1H-THIENO[3,2-C]PYRAZOLE-5-CARBOXAMIDE, SERINE/THREONINE-PROTEIN KINASE 6 | Authors: | Bindi, S, Fancelli, D, Alli, C, Berta, D, Bertrand, J.A, Cameron, A.D, Cappella, P, Carpinelli, P, Cervi, G, Croci, W, D'Anello, M, Forte, B, LauraGiorgini, M, Marsiglio, A, Moll, J, Pesenti, E, Pittala, V, Pulici, M, Riccardi-Sirtori, F, Roletto, F, Soncini, C, Storici, P, Varasi, M, Volpi, D, Zugnoni, P, Vianello, P. | Deposit date: | 2010-09-22 | Release date: | 2010-09-29 | Last modified: | 2024-05-08 | Method: | X-RAY DIFFRACTION (2.9 Å) | Cite: | Thieno[3,2-C]Pyrazoles: A Novel Class of Aurora Inhibitors with Favorable Antitumor Activity. Bioorg.Med.Chem., 18, 2010
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1VYZ
| Structure of CDK2 complexed with PNU-181227 | Descriptor: | CELL DIVISION PROTEIN KINASE 2, N-(5-CYCLOPROPYL-1H-PYRAZOL-3-YL)BENZAMIDE | Authors: | Pevarello, P, Brasca, M.G, Amici, R, Orsini, P, Traquandi, G, Corti, L, Piutti, C, Sansonna, P, Villa, M, Pierce, B.S, Pulici, M, Giordano, G, Martina, K, Lfritzen, E, Nugent, R.A, Casale, E, Cameron, A, Ciomei, M, Roletto, F, Isacchi, A, Fogliatto, G, Pesenti, E, Pastori, W, Marsiglio, W, Leach, K.L, Clare, P.M, Fiorentini, F, Varasi, M, Vulpetti, A, Warpehoski, M.A. | Deposit date: | 2004-05-07 | Release date: | 2004-06-17 | Last modified: | 2024-05-08 | Method: | X-RAY DIFFRACTION (2.21 Å) | Cite: | 3-Aminopyrazole Inhibitors of Cdk2/Cyclin a as Antitumor Agents. 1. Lead Finding J.Med.Chem., 47, 2004
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1VYW
| Structure of CDK2/Cyclin A with PNU-292137 | Descriptor: | CELL DIVISION PROTEIN KINASE 2, CYCLIN A2, N-(3-CYCLOPROPYL-1H-PYRAZOL-5-YL)-2-(2-NAPHTHYL)ACETAMIDE, ... | Authors: | Pevarello, P, Brasca, M.G, Amici, R, Orsini, P, Traquandi, G, Corti, L, Piutti, C, Sansonna, P, Villa, M, Pierce, B.S, Pulici, M, Giordano, P, Martina, K, Fritzen, E.L, Nugent, R.A, Casale, E, Cameron, A, Ciomei, M, Roletto, F, Isacchi, A, Fogliatto, G, Pesenti, E, Pastori, W, Marsiglio, A, Leach, K.L, Clare, P.M, Fiorentini, F, Varasi, M, Vulpetti, A, Warpehoski, M.A. | Deposit date: | 2004-05-07 | Release date: | 2004-06-10 | Last modified: | 2024-05-08 | Method: | X-RAY DIFFRACTION (2.3 Å) | Cite: | 3-Aminopyrazole Inhibitors of Cdk2/Cyclin a as Antitumor Agents. Part 1. Lead Finding J.Med.Chem., 47, 2004
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