Author results

2XRU
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AURORA-A T288E COMPLEXED WITH PHA-828300
分子名称:SERINE/THREONINE-PROTEIN KINASE 6, 3-({[4-(4-METHYLPIPERAZIN-1-YL)PHENYL]CARBONYL}AMINO)-N-[(1R)-1-PHENYLPROPYL]-1H-THIENO[3,2-C]PYRAZOLE-5-CARBOXAMIDE
著者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.
登録日2010-09-22
公開日2010-09-29
最終更新日2019-04-03
実験手法X-RAY DIFFRACTION (2.9 Å)
主引用文献Thieno[3,2-C]Pyrazoles: A Novel Class of Aurora Inhibitors with Favorable Antitumor Activity.
Bioorg.Med.Chem., 18, 2010
2BMC
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AURORA-2 T287D T288D COMPLEXED WITH PHA-680632
分子名称:SERINE THREONINE-PROTEIN KINASE 6, (3E)-N-(2,6-DIETHYLPHENYL)-3-{[4-(4-METHYLPIPERAZIN-1-YL)BENZOYL]IMINO}PYRROLO[3,4-C]PYRAZOLE-5(3H)-CARBOXAMIDE
著者Cameron, A.D., Izzo, G., Sagliano, A., Rusconi, L., Storici, P., Fancelli, D., Berta, D., Bindi, S., Catana, C., Forte, B., Giordano, P., Mantegani, S., Meroni, M., Moll, J., Pittala, V., Severino, D., Tonani, R., Varasi, M., Vulpetti, A., Vianello, P.
登録日2005-03-11
公開日2005-03-17
最終更新日2019-04-03
実験手法X-RAY DIFFRACTION (2.6 Å)
主引用文献Potent and Selective Aurora Inhibitors Identified by the Expansion of a Novel Scaffold for Protein Kinase Inhibition.
J.Med.Chem., 48, 2005
4BQG
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STRUCTURE OF HSP90 WITH AN INHIBITOR BOUND
分子名称:HSP90AA1 PROTEIN, 5-(3,4-dichloro-phenoxy)-benzene-1,3-diol
著者Casale, E., Brasca, M.G., Mantegani, S., Amboldi, N., Bindi, S., Caronni, D., Ceccarelli, W., Colombo, N., DePonti, A., Donati, D., Ermoli, A., Fachin, G., Felder, E.R., Ferguson, R.D., Fiorelli, C., Guanci, M., Isacchi, A., Pesenti, E., Polucci, P., Riceputi, L., Sola, F., Visco, C., Zuccotto, F., Fogliatto, G.
登録日2013-05-30
公開日2013-10-23
最終更新日2017-06-28
実験手法X-RAY DIFFRACTION (1.9 Å)
主引用文献Discovery of Nms-E973 as Novel, Selective and Potent Inhibitor of Heat Shock Protein 90 (Hsp90).
Bioorg.Med.Chem., 21, 2013
4BQJ
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STRUCTURE OF HSP90 WITH AN INHIBITOR BOUND
分子名称:HEAT SHOCK PROTEIN HSP 90-ALPHA, 5-[2,4-dihydroxy-6-(4-nitrophenoxy)phenyl]-N-ethyl-1,2-oxazole-3-carboxamide
著者Casale, E., Brasca, M.G., Mantegani, S., Amboldi, N., Bindi, S., Caronni, D., Ceccarelli, W., Colombo, N., DePonti, A., Donati, D., Ermoli, A., Fachin, G., Felder, E.R., Ferguson, R.D., Fiorelli, C., Guanci, M., Isacchi, A., Pesenti, E., Polucci, P., Riceputi, L., Sola, F., Visco, C., Zuccotto, F., Fogliatto, G.
登録日2013-05-30
公開日2013-10-23
最終更新日2017-06-28
実験手法X-RAY DIFFRACTION (2 Å)
主引用文献Discovery of Nms-E973 as Novel, Selective and Potent Inhibitor of Heat Shock Protein 90 (Hsp90).
Bioorg.Med.Chem., 21, 2013
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
2J4Z
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STRUCTURE OF AURORA-2 IN COMPLEX WITH PHA-680626
分子名称:SERINE THREONINE-PROTEIN KINASE 6, 4-(4-METHYLPIPERAZIN-1-YL)-N-[5-(2-THIENYLACETYL)-1,5-DIHYDROPYRROLO[3,4-C]PYRAZOL-3-YL]BENZAMIDE, ARSENIC
著者Cameron, A.D., Izzo, G., Storici, P., Rusconi, L., Fancelli, D., Varasi, M., Berta, D., Bindi, S., Forte, B., Severino, D., Tonani, R., Vianello, P.
登録日2006-09-08
公開日2006-11-06
最終更新日2019-04-03
実験手法X-RAY DIFFRACTION (2 Å)
主引用文献1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: identification of a potent Aurora kinase inhibitor with a favorable antitumor kinase inhibition profile.
J. Med. Chem., 49, 2006
2J50
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STRUCTURE OF AURORA-2 IN COMPLEX WITH PHA-739358
分子名称:SERINE/THREONINE-PROTEIN KINASE 6, N-[(3E)-5-[(2R)-2-METHOXY-2-PHENYLACETYL]PYRROLO[3,4-C]PYRAZOL-3(5H)-YLIDENE]-4-(4-METHYLPIPERAZIN-1-YL)BENZAMIDE, SULFATE ION
著者Cameron, A.D., Izzo, G., Storici, P., Rusconi, L., Fancelli, D., Varasi, M., Berta, D., Bindi, S., Forte, B., Severino, D., Tonani, R., Vianello, P.
登録日2006-09-08
公開日2006-11-06
最終更新日2019-04-03
実験手法X-RAY DIFFRACTION (3 Å)
主引用文献1,4,5,6-Tetrahydropyrrolo[3,4-C]Pyrazoles: Identification of a Potent Aurora Kinase Inhibitor with a Favorable Antitumor Kinase Inhibition Profile.
J.Med.Chem., 49, 2006