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2WIH
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STRUCTURE OF CDK2-CYCLIN A WITH PHA-848125
分子名称:CELL DIVISION PROTEIN KINASE 2, CYCLIN-A2, N,1,4,4-TETRAMETHYL-8-{[4-(4-METHYLPIPERAZIN-1-YL)PHENYL]AMINO}-4,5-DIHYDRO-1H-PYRAZOLO[4,3-H]QUINAZOLINE-3-CARBOXAMIDE, ...
著者Brasca, M.G., Amboldi, N., Ballinari, D., Cameron, A.D., Casale, E., Cervi, G., Colombo, M., Colotta, F., Croci, V., Dalessio, R., Fiorentini, F., Isacchi, A., Mercurio, C., Moretti, W., Panzeri, A., Pastori, W., Pevarello, P., Quartieri, F., Roletto, F., Traquandi, G., Vianello, P., Vulpetti, A., Ciomei, M.
登録日2009-05-13
公開日2009-07-28
最終更新日2019-04-03
実験手法X-RAY DIFFRACTION (2.5 Å)
主引用文献Identification of N,1,4,4-Tetramethyl-8-{[4-(4-Methylpiperazin-1-Yl)Phenyl]Amino}-4,5-Dihydro-1H-Pyrazolo[4,3-H]Quinazoline-3-Carboxamide (Pha-848125), a Potent, Orally Available Cyclin Dependent Kinase Inhibitor.
J.Med.Chem., 52, 2009
2WIP
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STRUCTURE OF CDK2-CYCLIN A COMPLEXED WITH 8-ANILINO-1-METHYL-4,5-DIHYDRO- 1H-PYRAZOLO[4,3-H] QUINAZOLINE-3-CARBOXYLIC ACID
分子名称:CELL DIVISION PROTEIN KINASE 2, CYCLIN-A2, 1-methyl-8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxylic acid, ...
著者Brasca, M.G., Amboldi, N., Ballinari, D., Cameron, A.D., Casale, E., Cervi, G., Colombo, M., Colotta, F., Croci, V., Dalessio, R., Fiorentini, F., Isacchi, A., Mercurio, C., Moretti, W., Panzeri, A., Pastori, W., Pevarello, P., Quartieri, F., Roletto, F., Traquandi, G., Vianello, P., Vulpetti, A., Ciomei, M.
登録日2009-05-14
公開日2009-07-28
最終更新日2019-04-03
実験手法X-RAY DIFFRACTION (2.8 Å)
主引用文献Identification of N,1,4,4-Tetramethyl-8-{[4-(4-Methylpiperazin-1-Yl)Phenyl]Amino}-4,5-Dihydro-1H-Pyrazolo[4,3-H]Quinazoline-3-Carboxamide (Pha-848125), a Potent, Orally Available Cyclin Dependent Kinase Inhibitor.
J.Med.Chem., 52, 2009
2WXV
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STRUCTURE OF CDK2-CYCLIN A WITH A PYRAZOLO(4,3-H) QUINAZOLINE-3- CARBOXAMIDE INHIBITOR
分子名称:CELL DIVISION PROTEIN KINASE 2, CYCLIN-A2, N,1-DIMETHYL-8-{[1-(METHYLSULFONYL)PIPERIDIN-4-YL]AMINO}-1H-PYRAZOLO[4,3-H]QUINAZOLINE-3-CARBOXAMIDE, ...
著者Traquandi, G., Ciomei, M., Ballinari, D., Casale, E., Colombo, N., Croci, V., Fiorentini, F., Isacchi, A., Longo, A., Mercurio, C., Panzeri, A., Pastori, W., Pevarello, P., Volpi, D., Roussel, P., Vulpetti, A., Brasca, M.G.
登録日2009-11-10
公開日2010-02-23
最終更新日2019-04-03
実験手法X-RAY DIFFRACTION (2.6 Å)
主引用文献Identification of Potent Pyrazolo[4,3-H]Quinazoline-3-Carboxamides as Multi-Cyclin-Dependent Kinase Inhibitors.
J.Med.Chem., 53, 2010
4D0W
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PYRROLE-3-CARBOXAMIDES AS POTENT AND SELECTIVE JAK2 INHIBITORS
分子名称:TYROSINE-PROTEIN KINASE JAK2, GLYCEROL, 5-(2-aminopyrimidin-4-yl)-2-(5-chloro-2-methylphenyl)-1H-pyrrole-3-carboxamide
著者Bertrand, J., Canevari, G., Fasolini, M., Brasca, M.G., Nesi, M., Avanzi, N., Ballinari, D., Bandiera, T., Bindi, S., Carenzi, D., Casero, D., Ceriani, L., Ciomei, M., Cirla, A., Colombo, M., Cribioli, S., Cristiani, C., Della Vedova, F., Fachin, G., Felder, E.R., Galvani, A., Isacchi, A., Mirizzi, D., Motto, I., Panzeri, A., Pesenti, E., Vianello, P., Gnocchi, P., Donati, D.
登録日2014-04-30
公開日2014-07-23
最終更新日2019-04-24
実験手法X-RAY DIFFRACTION (1.77 Å)
主引用文献Pyrrole-3-Carboxamides as Potent and Selective Jak2 Inhibitors.
Bioorg.Med.Chem., 22, 2014
4D0X
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PYRROLE-3-CARBOXAMIDES AS POTENT AND SELECTIVE JAK2 INHIBITORS
分子名称:TYROSINE-PROTEIN KINASE JAK2, 5-(2-aminopyrimidin-4-yl)-2-[2-chloro-5-(trifluoromethyl)phenyl]-1H-pyrrole-3-carboxamide, GLYCEROL
著者Canevari, G., Fasolini, M., Bertrand, J., Brasca, M.G., Nesi, M., Avanzi, N., Ballinari, D., Bandiera, T., Bindi, S., Carenzi, D., Casero, D., Ceriani, L., Ciomei, M., Cirla, A., Colombo, M., Cribioli, S., Cristiani, C., Della Vedova, F., Fachin, G., Felder, E.R., Galvani, A., Isacchi, A., Mirizzi, D., Motto, I., Panzeri, A., Pesenti, E., Vianello, P., Gnocchi, P., Donati, D.
登録日2014-04-30
公開日2014-07-23
最終更新日2019-04-24
実験手法X-RAY DIFFRACTION (1.82 Å)
主引用文献Pyrrole-3-Carboxamides as Potent and Selective Jak2 Inhibitors.
Bioorg.Med.Chem., 22, 2014
4D1S
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PYRROLE-3-CARBOXAMIDES AS POTENT AND SELECTIVE JAK2 INHIBITORS
分子名称:TYROSINE-PROTEIN KINASE JAK2, 2-(5-chloro-2-methylphenyl)-1-methyl-5-(2-{[4-(4-methylpiperazin-1-yl)phenyl]amino}pyrimidin-4-yl)-1H-pyrrole-3-carboxamide
著者Bertrand, J., Canevari, G., Fasolini, M., Brasca, M.G., Nesi, M., Avanzi, N., Ballinari, D., Bandiera, T., Bindi, S., Carenzi, D., Casero, D., Ceriani, L., Ciomei, M., Cirla, A., Colombo, M., Cribioli, S., Cristiani, C., Della Vedova, F., Fachin, G., Felder, E.R., Galvani, A., Isacchi, A., Mirizzi, D., Motto, I., Panzeri, A., Pesenti, E., Vianello, P., Gnocchi, P., Donati, D.
登録日2014-05-05
公開日2014-07-23
最終更新日2019-04-24
実験手法X-RAY DIFFRACTION (1.66 Å)
主引用文献Pyrrole-3-Carboxamides as Potent and Selective Jak2 Inhibitors.
Bioorg.Med.Chem., 22, 2014
5AEP
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NOVEL PYRROLE CARBOXAMIDE INHIBITORS OF JAK2 AS POTENTIAL TREATMENT OF MYELOPROLIFERATIVE DISORDERS
分子名称:TYROSINE-PROTEIN KINASE JAK2, 1-(5-chloro-2-methylphenyl)-4-(pyrrolo[2,1-f][1,2,4]triazin-4-yl)-1H-pyrrole-2-carboxamide
著者Canevari, G., Bertrand, J., Brasca, M.G., Nesi, M., Amboldi, N., Avanzi, N., Bindi, S., Casero, D., Ciomei, M., Colombo, N., Cribioli, S., Fachin, G., Felder, E.R., Galvani, A., Isacchi, A., Motto, I., Panzeri, A., Gnocchi, P., Donati, D.
登録日2015-01-08
公開日2015-04-29
最終更新日2019-05-08
実験手法X-RAY DIFFRACTION (1.95 Å)
主引用文献Novel Pyrrole Carboxamide Inhibitors of Jak2 as Potential Treatment of Myeloproliferative Disorders.
Bioorg.Med.Chem., 23, 2015
5FTO
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CRYSTAL STRUCTURE OF THE ALK KINASE DOMAIN IN COMPLEX WITH ENTRECTINIB
分子名称:ALK TYROSINE KINASE RECEPTOR, Entrectinib
著者Bossi, R., Canevari, G., Fasolini, M., Menichincheri, M., Ardini, E., Magnaghi, P., Avanzi, N., Banfi, P., Buffa, L., Ceriani, L., Colombo, M., Corti, L., Donati, D., Felder, E., Fiorelli, C., Fiorentini, F., Galvani, A., Isacchi, A., Lombardi Borgia, A., Marchionni, C., Nesi, M., Orrenius, C., Panzeri, A., Perrone, E., Pesenti, E., Rusconi, L., Saccardo, M.B., Vanotti, E., Orsini, P.
登録日2016-01-14
公開日2016-04-06
最終更新日2016-04-27
実験手法X-RAY DIFFRACTION (2.22 Å)
主引用文献Discovery of Entrectinib: A New 3-Aminoindazole as a Potent Anaplastic Lymphoma Kinase (Alk), C-Ros Oncogene 1 Kinase (Ros1), and Pan-Tropomyosin Receptor Kinases (Pan-Trks) Inhibitor.
J.Med.Chem., 59, 2016
5FTQ
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CRYSTAL STRUCTURE OF THE ALK KINASE DOMAIN IN COMPLEX WITH CMPD 17
分子名称:ALK TYROSINE KINASE RECEPTOR, N-[5-(3,5-DIFLUOROBENZYL)-1H-INDAZOL-3-YL]-2-[(4-HYDROXYCYCLOHEXYL)AMINO]-4-(4-METHYLPIPERAZIN-1-YL) BENZAMIDE, GLYCEROL
著者Bossi, R., Canevari, G., Fasolini, M., Menichincheri, M., Ardini, E., Magnaghi, P., Avanzi, N., Banfi, P., Buffa, L., Ceriani, L., Colombo, M., Corti, L., Donati, D., Felder, E., Fiorelli, C., Fiorentini, F., Galvani, A., Isacchi, A., Lombardi Borgia, A., Marchionni, C., Nesi, M., Orrenius, C., Panzeri, A., Perrone, E., Pesenti, E., Rusconi, L., Saccardo, M.B., Vanotti, E., Orsini, P.
登録日2016-01-14
公開日2016-04-06
最終更新日2016-04-27
実験手法X-RAY DIFFRACTION (1.7 Å)
主引用文献Discovery of Entrectinib: A New 3-Aminoindazole as a Potent Anaplastic Lymphoma Kinase (Alk), C-Ros Oncogene 1 Kinase (Ros1), and Pan-Tropomyosin Receptor Kinases (Pan-Trks) Inhibitor.
J.Med.Chem., 59, 2016