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2BKZ
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STRUCTURE OF CDK2-CYCLIN A WITH PHA-404611
分子名称:CELL DIVISION PROTEIN KINASE 2, CYCLIN A2, 1-[4-(AMINOSULFONYL)PHENYL]-1,6-DIHYDROPYRAZOLO[3,4-E]INDAZOLE-3-CARBOXAMIDE, ...
著者DAlessio, R., Bargiottia, A., Metz, S., Brasca, M.G., Cameron, A., Ermoli, A., Marsiglio, A., Polucci, P., Roletto, F., Tibolla, M., Vazquez, M.L., Vulpetti, A., Pevarello, P.
登録日2005-02-23
公開日2006-03-08
最終更新日2019-04-03
実験手法X-RAY DIFFRACTION (2.6 Å)
主引用文献Benzodipyrazoles: A New Class of Potent Cdk2 Inhibitors
Bioorg.Med.Chem.Lett., 15, 2005
1VYW
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STRUCTURE OF CDK2/CYCLIN A WITH PNU-292137
分子名称:CELL DIVISION PROTEIN KINASE 2, CYCLIN A2, SULFATE ION, ...
著者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.
登録日2004-05-07
公開日2004-06-10
最終更新日2019-04-03
実験手法X-RAY DIFFRACTION (2.3 Å)
主引用文献3-Aminopyrazole Inhibitors of Cdk2/Cyclin a as Antitumor Agents. Part 1. Lead Finding
J.Med.Chem., 47, 2004
2BPM
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STRUCTURE OF CDK2-CYCLIN A WITH PHA-630529
分子名称:CELL DIVISION PROTEIN KINASE 2, CYCLIN A2, (2S)-N-[(3Z)-5-CYCLOPROPYL-3H-PYRAZOL-3-YLIDENE]-2-[4-(2-OXOIMIDAZOLIDIN-1-YL)PHENYL]PROPANAMIDE, ...
著者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.
登録日2005-04-21
公開日2005-12-08
最終更新日2019-04-03
実験手法X-RAY DIFFRACTION (2.4 Å)
主引用文献3-Aminopyrazole Inhibitors of Cdk2-Cyclin a as Antitumor Agents. 2. Lead Optimization
J.Med.Chem., 48, 2005
4BZN
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CRYSTAL STRUCTURE OF PIM1 IN COMPLEX WITH A PYRROLO(1,2-A)PYRAZINONE INHIBITOR
分子名称:SERINE/THREONINE-PROTEIN KINASE PIM-1, N-(2,2-dimethylpropyl)-2-[1-oxo-7-(thiophen-3-yl)-1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazin-4-yl]acetamide
著者Casale, E., Casuscelli, F., Ardini, E., Avanzi, N., Cervi, G., D'Anello, M., Donati, D., Faiardi, D., Ferguson, R.D., Fogliatto, G., Galvani, A., Marsiglio, A., Mirizzi, D.G., Montemartini, M., Orrenius, C., Papeo, G., Piutti, C., Salom, B., Felder, E.R.
登録日2013-07-29
公開日2013-10-30
最終更新日2013-11-13
実験手法X-RAY DIFFRACTION (1.9 Å)
主引用文献Discovery and Optimization of Pyrrolo[1,2-A]Pyrazinones Leads to Novel and Selective Inhibitors of Pim Kinases.
Bioorg.Med.Chem., 21, 2013
4BZO
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CRYSTAL STRUCTURE OF PIM1 IN COMPLEX WITH A PYRROLO-PYRAZINONE INHIBITOR
分子名称:SERINE/THREONINE-PROTEIN KINASE PIM-1, N-[(1S)-2-AMINO-1-PHENYLETHYL]-2-[(4S)-7-(2-FLUORO-4-PYRIDINYL)-1-OXO-1,2,3,4-TETRAHYDROPYRROLO[1,2-A]PYRAZIN-4-YL]ACETAMIDE
著者Casale, E., Casuscelli, F., Ardini, E., Avanzi, N., Cervi, G., D'Anello, M., Donati, D., Faiardi, D., Ferguson, R.D., Fogliatto, G., Galvani, A., Marsiglio, A., Mirizzi, D.G., Montemartini, M., Orrenius, C., Papeo, G., Piutti, C., Salom, B., Felder, E.R.
登録日2013-07-29
公開日2013-10-30
最終更新日2013-11-13
実験手法X-RAY DIFFRACTION (2.1 Å)
主引用文献Discovery and Optimization of Pyrrolo[1,2-A]Pyrazinones Leads to Novel and Selective Inhibitors of Pim Kinases.
Bioorg.Med.Chem., 21, 2013
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
1VYZ
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STRUCTURE OF CDK2 COMPLEXED WITH PNU-181227
分子名称:CELL DIVISION PROTEIN KINASE 2, N-(5-CYCLOPROPYL-1H-PYRAZOL-3-YL)BENZAMIDE
著者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.
登録日2004-05-07
公開日2004-06-17
最終更新日2019-04-03
実験手法X-RAY DIFFRACTION (2.21 Å)
主引用文献3-Aminopyrazole Inhibitors of Cdk2/Cyclin a as Antitumor Agents. 1. Lead Finding
J.Med.Chem., 47, 2004
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
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