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4BZN
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CRYSTAL STRUCTURE OF PIM1 IN COMPLEX WITH A PYRROLO(1,2-A)PYRAZINONE INHIBITOR
Descriptor: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
Authors: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.
Deposit date:2013-07-29
Release date:2013-10-30
Last modified:2013-11-13
Method:X-RAY DIFFRACTION (1.9 Å)
Cite: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
Descriptor: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
Authors: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.
Deposit date:2013-07-29
Release date:2013-10-30
Last modified:2013-11-13
Method:X-RAY DIFFRACTION (2.1 Å)
Cite:Discovery and Optimization of Pyrrolo[1,2-A]Pyrazinones Leads to Novel and Selective Inhibitors of Pim Kinases.
Bioorg.Med.Chem., 21, 2013
2WIH
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STRUCTURE OF CDK2-CYCLIN A WITH PHA-848125
Descriptor: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, ...
Authors: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.
Deposit date:2009-05-13
Release date:2009-07-28
Last modified:2019-04-03
Method:X-RAY DIFFRACTION (2.5 Å)
Cite: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
Descriptor:CELL DIVISION PROTEIN KINASE 2, CYCLIN-A2, 1-methyl-8-(phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxylic acid, ...
Authors: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.
Deposit date:2009-05-14
Release date:2009-07-28
Last modified:2019-04-03
Method:X-RAY DIFFRACTION (2.8 Å)
Cite: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
2XRU
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AURORA-A T288E COMPLEXED WITH PHA-828300
Descriptor: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
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:2019-04-03
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