6DCG
 
 | | Discovery of MK-8353: An Orally Bioavailable Dual Mechanism ERK Inhibitor for Oncology | | 分子名称: | (3S)-3-(methylsulfanyl)-1-(2-{4-[4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl]-3,6-dihydropyridin-1(2H)-yl}-2-oxoethyl)-N-(3-{6-[(propan-2-yl)oxy]pyridin-3-yl}-1H-indazol-5-yl)pyrrolidine-3-carboxamide, Mitogen-activated protein kinase 1, SULFATE ION | | 著者 | Boga, S.B, Deng, Y, Zhu, L, Nan, Y, Cooper, A, Shipps Jr, G.W, Doll, R, Shih, N, Zhu, H, Sun, R, Wang, T, Paliwal, S, Tsui, H, Gao, X, Yao, X, Desai, J, Wang, J, Alhassan, A.B, Kelly, J, Patel, M, Muppalla, K, Gudipati, S, Zhang, L, Buevich, A, Hesk, D, Carr, D, Dayananth, P, Mei, H, Cox, K, Sherborne, B, Hruza, A.W, Xiao, L, Jin, W, Long, B, Liu, G, Taylor, S.A, Kirschmeier, P, Windsor, W.T, Bishop, R, Samatar, A.A. | | 登録日 | 2018-05-06 | | 公開日 | 2018-08-08 | | 最終更新日 | 2023-10-11 | | 実験手法 | X-RAY DIFFRACTION (1.45 Å) | | 主引用文献 | MK-8353: Discovery of an Orally Bioavailable Dual Mechanism ERK Inhibitor for Oncology.
ACS Med Chem Lett, 9, 2018
|
|
1QBQ
 | | STRUCTURE OF RAT FARNESYL PROTEIN TRANSFERASE COMPLEXED WITH A CVIM PEPTIDE AND ALPHA-HYDROXYFARNESYLPHOSPHONIC ACID. | | 分子名称: | ACETATE ION, ACETYL-CYS-VAL-ILE-SELENOMET-COOH PEPTIDE, ALPHA-HYDROXYFARNESYLPHOSPHONIC ACID, ... | | 著者 | Strickland, C.L, Windsor, W.T, Syto, R, Wang, L, Bond, R, Wu, Z, Schwartz, J, Le, H.V, Beese, L.S, Weber, P.C. | | 登録日 | 1999-04-27 | | 公開日 | 1999-06-18 | | 最終更新日 | 2024-03-13 | | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | | 主引用文献 | Crystal structure of farnesyl protein transferase complexed with a CaaX peptide and farnesyl diphosphate analogue
Biochemistry, 37, 1998
|
|
4QYY
 | | Discovery of Novel, Dual Mechanism ERK Inhibitors by Affinity Selection Screening of an Inactive Kinase State | | 分子名称: | (3R)-1-{2-[4-(4-acetylphenyl)piperazin-1-yl]-2-oxoethyl}-N-(3-chloro-4-hydroxyphenyl)pyrrolidine-3-carboxamide, Mitogen-activated protein kinase 1, SULFATE ION | | 著者 | Deng, Y, Shipps, G.W, Cooper, A, English, J.M, Annis, D.A, Carr, D, Nan, Y, Wang, T, Zhu, Y.H, Chuang, C, Dayananth, P, Hruza, A.W, Xiao, L, Jin, W, Kirschmeier, P, Windsor, W.T, Samatar, A.A. | | 登録日 | 2014-07-26 | | 公開日 | 2014-11-12 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (1.65 Å) | | 主引用文献 | Discovery of Novel, Dual Mechanism ERK Inhibitors by Affinity Selection Screening of an Inactive Kinase.
J.Med.Chem., 57, 2014
|
|
4NJ3
 | |
1O5M
 | | Structure of FPT bound to the inhibitor SCH66336 | | 分子名称: | 4-{2-[4-(3,10-DIBROMO-8-CHLORO-6,11-DIHYDRO-5H-BENZO[5,6]CYCLOHEPTA[1,2-B]PYRIDIN-11-YL)PIPERIDIN-1-YL]-2-OXOETHYL}PIPERIDINE-1-CARBOXAMIDE, FARNESYL DIPHOSPHATE, Protein farnesyltransferase alpha subunit, ... | | 著者 | Strickland, C.L, Weber, P.C, Ganguly, A.K. | | 登録日 | 2003-09-26 | | 公開日 | 2003-10-21 | | 最終更新日 | 2023-12-27 | | 実験手法 | X-RAY DIFFRACTION (2.3 Å) | | 主引用文献 | Tricyclic Farnesyl Protein Transferase Inhibitors: Crystallographic and Calorimetric Studies of Structure-Activity Relationships
J.Med.Chem., 42, 1999
|
|
1INR
 | | CYTOKINE SYNTHESIS | | 分子名称: | INTERLEUKIN-10 | | 著者 | Walter, M.R. | | 登録日 | 1995-07-31 | | 公開日 | 1996-10-14 | | 最終更新日 | 2011-07-13 | | 実験手法 | X-RAY DIFFRACTION (2 Å) | | 主引用文献 | Crystal structure of interleukin 10 reveals an interferon gamma-like fold.
Biochemistry, 34, 1995
|
|
2R3P
 | | Crystal Structure of Cyclin-Dependent Kinase 2 with inhibitor | | 分子名称: | 5-(2,3-dichlorophenyl)-N-(pyridin-4-ylmethyl)-3-thiocyanatopyrazolo[1,5-a]pyrimidin-7-amine, Cell division protein kinase 2 | | 著者 | Fischmann, T.O, Hruza, A.W, Madison, V.M, Duca, J.S. | | 登録日 | 2007-08-29 | | 公開日 | 2008-01-22 | | 最終更新日 | 2011-07-13 | | 実験手法 | X-RAY DIFFRACTION (1.66 Å) | | 主引用文献 | Structure-guided discovery of cyclin-dependent kinase inhibitors.
Biopolymers, 89, 2008
|
|
2R3K
 | | Crystal Structure of Cyclin-Dependent Kinase 2 with inhibitor | | 分子名称: | 3-bromo-5-phenyl-N-(pyrimidin-5-ylmethyl)pyrazolo[1,5-a]pyridin-7-amine, Cell division protein kinase 2 | | 著者 | Fischmann, T.O, Hruza, A.W, Madison, V.M, Duca, J.S. | | 登録日 | 2007-08-29 | | 公開日 | 2008-01-22 | | 最終更新日 | 2011-07-13 | | 実験手法 | X-RAY DIFFRACTION (1.7 Å) | | 主引用文献 | Structure-guided discovery of cyclin-dependent kinase inhibitors.
Biopolymers, 89, 2008
|
|
2R3N
 | | Crystal Structure of Cyclin-Dependent Kinase 2 with inhibitor | | 分子名称: | 3-cyclopropyl-5-phenyl-N-(pyridin-3-ylmethyl)pyrazolo[1,5-a]pyrimidin-7-amine, Cell division protein kinase 2 | | 著者 | Fischmann, T.O, Hruza, A.W, Madison, V.M, Duca, J.S. | | 登録日 | 2007-08-29 | | 公開日 | 2008-01-22 | | 最終更新日 | 2011-07-13 | | 実験手法 | X-RAY DIFFRACTION (1.63 Å) | | 主引用文献 | Structure-guided discovery of cyclin-dependent kinase inhibitors.
Biopolymers, 89, 2008
|
|
2R3G
 | | Crystal Structure of Cyclin-Dependent Kinase 2 with inhibitor | | 分子名称: | 6-(2-fluorophenyl)-N-(pyridin-3-ylmethyl)imidazo[1,2-a]pyrazin-8-amine, Cell division protein kinase 2 | | 著者 | Fischmann, T.O, Hruza, A.W, Madison, V.M, Duca, J.S. | | 登録日 | 2007-08-29 | | 公開日 | 2008-01-22 | | 最終更新日 | 2011-07-13 | | 実験手法 | X-RAY DIFFRACTION (1.55 Å) | | 主引用文献 | Structure-guided discovery of cyclin-dependent kinase inhibitors.
Biopolymers, 89, 2008
|
|
2R3R
 | | Crystal Structure of Cyclin-Dependent Kinase 2 with inhibitor | | 分子名称: | 3-bromo-5-phenyl-N-(pyridin-4-ylmethyl)pyrazolo[1,5-a]pyrimidin-7-amine, Cell division protein kinase 2 | | 著者 | Fischmann, T.O, Hruza, A.W, Madison, V.M, Duca, J.S. | | 登録日 | 2007-08-29 | | 公開日 | 2008-01-22 | | 最終更新日 | 2021-07-28 | | 実験手法 | X-RAY DIFFRACTION (1.47 Å) | | 主引用文献 | Structure-guided discovery of cyclin-dependent kinase inhibitors.
Biopolymers, 89, 2008
|
|
2R3L
 | | Crystal Structure of Cyclin-Dependent Kinase 2 with inhibitor | | 分子名称: | 3-bromo-6-phenyl-N-(pyrimidin-5-ylmethyl)imidazo[1,2-a]pyridin-8-amine, Cell division protein kinase 2 | | 著者 | Fischmann, T.O, Hruza, A.W, Madison, V.M, Duca, J.S. | | 登録日 | 2007-08-29 | | 公開日 | 2008-01-22 | | 最終更新日 | 2011-07-13 | | 実験手法 | X-RAY DIFFRACTION (1.65 Å) | | 主引用文献 | Structure-guided discovery of cyclin-dependent kinase inhibitors.
Biopolymers, 89, 2008
|
|
2R3O
 | | Crystal Structure of Cyclin-Dependent Kinase 2 with inhibitor | | 分子名称: | (5-phenyl-7-(pyridin-3-ylmethylamino)pyrazolo[1,5-a]pyrimidin-3-yl)methanol, Cell division protein kinase 2 | | 著者 | Fischmann, T.O, Hruza, A.W, Madison, V.M, Duca, J.S. | | 登録日 | 2007-08-29 | | 公開日 | 2008-01-22 | | 最終更新日 | 2011-07-13 | | 実験手法 | X-RAY DIFFRACTION (1.8 Å) | | 主引用文献 | Structure-guided discovery of cyclin-dependent kinase inhibitors.
Biopolymers, 89, 2008
|
|
2R3I
 | | Crystal Structure of Cyclin-Dependent Kinase 2 with inhibitor | | 分子名称: | 5-(2-fluorophenyl)-N-(pyridin-4-ylmethyl)pyrazolo[1,5-a]pyrimidin-7-amine, Cell division protein kinase 2 | | 著者 | Fischmann, T.O, Hruza, A.W, Madison, V.M, Duca, J.S. | | 登録日 | 2007-08-29 | | 公開日 | 2008-01-22 | | 最終更新日 | 2011-07-13 | | 実験手法 | X-RAY DIFFRACTION (1.28 Å) | | 主引用文献 | Structure-guided discovery of cyclin-dependent kinase inhibitors.
Biopolymers, 89, 2008
|
|
2R3M
 | | Crystal Structure of Cyclin-Dependent Kinase 2 with inhibitor | | 分子名称: | Cell division protein kinase 2, N-((2-aminopyrimidin-5-yl)methyl)-5-(2,6-difluorophenyl)-3-ethylpyrazolo[1,5-a]pyrimidin-7-amine | | 著者 | Fischmann, T.O, Hruza, A.W, Madison, V.M, Duca, J.S. | | 登録日 | 2007-08-29 | | 公開日 | 2008-01-22 | | 最終更新日 | 2024-04-03 | | 実験手法 | X-RAY DIFFRACTION (1.7 Å) | | 主引用文献 | Structure-guided discovery of cyclin-dependent kinase inhibitors.
Biopolymers, 89, 2008
|
|
2R3F
 | | Crystal Structure of Cyclin-Dependent Kinase 2 with inhibitor | | 分子名称: | 5-(2,3-dichlorophenyl)-N-(pyridin-4-ylmethyl)pyrazolo[1,5-a]pyrimidin-7-amine, Cell division protein kinase 2 | | 著者 | Fischmann, T.O, Hruza, A.W, Madison, V.M, Duca, J.S. | | 登録日 | 2007-08-29 | | 公開日 | 2008-01-22 | | 最終更新日 | 2011-07-13 | | 実験手法 | X-RAY DIFFRACTION (1.5 Å) | | 主引用文献 | Structure-guided discovery of cyclin-dependent kinase inhibitors.
Biopolymers, 89, 2008
|
|
2R3Q
 | | Crystal Structure of Cyclin-Dependent Kinase 2 with inhibitor | | 分子名称: | 3-((3-bromo-5-o-tolylpyrazolo[1,5-a]pyrimidin-7-ylamino)methyl)pyridine 1-oxide, Cell division protein kinase 2 | | 著者 | Fischmann, T.O, Hruza, A.W, Madison, V.M, Duca, J.S. | | 登録日 | 2007-08-29 | | 公開日 | 2008-01-22 | | 最終更新日 | 2011-07-13 | | 実験手法 | X-RAY DIFFRACTION (1.35 Å) | | 主引用文献 | Structure-guided discovery of cyclin-dependent kinase inhibitors.
Biopolymers, 89, 2008
|
|
2R3H
 | | Crystal Structure of Cyclin-Dependent Kinase 2 with inhibitor | | 分子名称: | 3-methyl-N-(pyridin-4-ylmethyl)imidazo[1,2-a]pyrazin-8-amine, Cell division protein kinase 2 | | 著者 | Fischmann, T.O, Hruza, A.W, Madison, V.M, Duca, J.S. | | 登録日 | 2007-08-29 | | 公開日 | 2008-01-22 | | 最終更新日 | 2011-07-13 | | 実験手法 | X-RAY DIFFRACTION (1.5 Å) | | 主引用文献 | Structure-guided discovery of cyclin-dependent kinase inhibitors.
Biopolymers, 89, 2008
|
|
2R3J
 | | Crystal Structure of Cyclin-Dependent Kinase 2 with inhibitor | | 分子名称: | 3-bromo-5-phenyl-N-(pyridin-3-ylmethyl)pyrazolo[1,5-a]pyrimidin-7-amine, Cell division protein kinase 2 | | 著者 | Fischmann, T.O, Hruza, A.W, Madison, V.M, Duca, J.S. | | 登録日 | 2007-08-29 | | 公開日 | 2008-01-22 | | 最終更新日 | 2011-07-13 | | 実験手法 | X-RAY DIFFRACTION (1.65 Å) | | 主引用文献 | Structure-guided discovery of cyclin-dependent kinase inhibitors.
Biopolymers, 89, 2008
|
|
