4W4W
 
 | | JNK2/3 in complex with N-(2-methylpyridin-4-yl)-3-{4-[(phenylcarbamoyl)amino]-1H-pyrazol-1-yl}benzamide | | 分子名称: | N-(2-methylpyridin-4-yl)-3-{4-[(phenylcarbamoyl)amino]-1H-pyrazol-1-yl}benzamide, c-Jun N-terminal kinase 3 | | 著者 | Park, H, Iqbal, S, Hernandez, P, Mora, R, Zheng, K, Feng, Y, LoGrasso, P. | | 登録日 | 2014-08-15 | | 公開日 | 2015-02-11 | | 最終更新日 | 2023-12-27 | | 実験手法 | X-RAY DIFFRACTION (1.9 Å) | | 主引用文献 | Structural Basis and Biological Consequences for JNK2/3 Isoform Selective Aminopyrazoles.
Sci Rep, 5, 2015
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4UYN
 | | SAR156497 an exquisitely selective inhibitor of Aurora kinases | | 分子名称: | AURORA KINASE A, ethyl (9S)-9-[5-(1H-benzimidazol-2-ylsulfanyl)furan-2-yl]-8-hydroxy-5,6,7,9-tetrahydro-2H-pyrrolo[3,4-b]quinoline-3-carboxylate | | 著者 | Carry, J.C, Clerc, F, Minoux, H, Schio, L, Mauger, J, Nair, A, Parmantier, E, Lemoigne, R, Delorme, C, Nicolas, J.P, Krick, A, Abecassis, P.Y, Crocq-Stuerga, V, Pouzieux, S, Delarbre, L, Maignan, S, Bertrand, T, Bjergarde, K, Ma, N, Lachaud, S, Guizani, H, Lebel, R, Doerflinger, G, Monget, S, Perron, S, Gasse, F, Angouillant-Boniface, O, Filoche-Romme, B, Murer, M, Gontier, S, Prevost, C, Monteiro, M.L, Combeau, C. | | 登録日 | 2014-09-02 | | 公開日 | 2014-11-19 | | 最終更新日 | 2024-05-08 | | 実験手法 | X-RAY DIFFRACTION (1.9 Å) | | 主引用文献 | Sar156497, an Exquisitely Selective Inhibitor of Aurora Kinases.
J.Med.Chem., 58, 2015
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4WB5
 | | Crystal structure of human cAMP-dependent protein kinase A (catalytic alpha subunit) | | 分子名称: | ADENOSINE-5'-TRIPHOSPHATE, MAGNESIUM ION, PKI (5-24), ... | | 著者 | Cheung, J, Ginter, C, Cassidy, M, Franklin, M.C, Rudolph, M.J, Hendrickson, W.A. | | 登録日 | 2014-09-02 | | 公開日 | 2015-01-21 | | 最終更新日 | 2023-09-27 | | 実験手法 | X-RAY DIFFRACTION (1.641 Å) | | 主引用文献 | Structural insights into mis-regulation of protein kinase A in human tumors.
Proc.Natl.Acad.Sci.USA, 112, 2015
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4UY9
 | | Structure of MLK1 kinase domain with leucine zipper 1 | | 分子名称: | MITOGEN-ACTIVATED PROTEIN KINASE KINASE KINASE 9 | | 著者 | Read, J.A, Brassington, C, Pollard, H.K, Phillips, C, Green, I, Overmann, R, Collier, M. | | 登録日 | 2014-08-29 | | 公開日 | 2015-09-30 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (2.81 Å) | | 主引用文献 | Recurrent Mlk4 Loss-of-Function Mutations Suppress Jnk Signaling to Promote Colon Tumorigenesis.
Cancer Res., 76, 2016
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4W9X
 | | Crystal Structure of BMP-2-inducible kinase in complex with baricitinib | | 分子名称: | 1,2-ETHANEDIOL, BMP-2-inducible protein kinase, Baricitinib | | 著者 | Sorrell, F.J, Elkins, J.M, Krojer, T, Williams, E, Savitsky, P, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Knapp, S, Structural Genomics Consortium (SGC) | | 登録日 | 2014-08-28 | | 公開日 | 2014-09-10 | | 最終更新日 | 2024-05-08 | | 実験手法 | X-RAY DIFFRACTION (2.14 Å) | | 主引用文献 | Family-wide Structural Analysis of Human Numb-Associated Protein Kinases.
Structure, 24, 2016
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4UZH
 | | SAR156497 an exquisitely selective inhibitor of Aurora kinases | | 分子名称: | (4S)-4-(2-fluorophenyl)-2,4,6,7,8,9-hexahydro-5H-pyrazolo[3,4-b][1,7]naphthyridin-5-one, AURORA 2 KINASE DOMAIN | | 著者 | Pouzieux, S, Maignan, S, Crenne, J.Y. | | 登録日 | 2014-09-05 | | 公開日 | 2014-11-19 | | 最終更新日 | 2024-05-08 | | 実験手法 | X-RAY DIFFRACTION (2 Å) | | 主引用文献 | Sar156497 an Exquisitely Selective Inhibitor of Aurora Kinases.
J.Med.Chem., 58, 2015
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4USF
 | | Human SLK with SB-440719 | | 分子名称: | 4-[4-(6-methoxynaphthalen-2-yl)-1H-imidazol-5-yl]pyridine, STE20-LIKE SERINE/THREONINE-PROTEIN KINASE | | 著者 | Elkins, J.M, Salah, E, Szklarz, M, von Delft, F, Bountra, C, Edwards, A.M, Knapp, S. | | 登録日 | 2014-07-07 | | 公開日 | 2015-07-22 | | 最終更新日 | 2024-05-08 | | 実験手法 | X-RAY DIFFRACTION (1.75 Å) | | 主引用文献 | Comprehensive Characterization of the Published Kinase Inhibitor Set.
Nat.Biotechnol., 34, 2016
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4USD
 | | Human STK10 (LOK) with SB-633825 | | 分子名称: | 4-{5-(6-methoxynaphthalen-2-yl)-1-methyl-2-[2-methyl-4-(methylsulfonyl)phenyl]-1H-imidazol-4-yl}pyridine, SERINE/THREONINE-PROTEIN KINASE 10 | | 著者 | Elkins, J.M, Salah, E, Szklarz, M, von Delft, F, Canning, P, Raynor, J, Bountra, C, Edwards, A.M, Knapp, S. | | 登録日 | 2014-07-07 | | 公開日 | 2015-07-22 | | 最終更新日 | 2024-05-08 | | 実験手法 | X-RAY DIFFRACTION (3.05 Å) | | 主引用文献 | Comprehensive Characterization of the Published Kinase Inhibitor Set.
Nat.Biotechnol., 34, 2016
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4UZD
 | | SAR156497 an exquisitely selective inhibitor of Aurora kinases | | 分子名称: | AURORA KINASE A, ethyl (9S)-9-[3-(1H-benzimidazol-2-yloxy)phenyl]-8-oxo-4,5,6,7,8,9-hexahydro-2H-pyrrolo[3,4-b]quinoline-3-carboxylate | | 著者 | Pouzieux, S, Delarbre, L, Crenne, J.Y. | | 登録日 | 2014-09-05 | | 公開日 | 2014-11-19 | | 最終更新日 | 2024-05-08 | | 実験手法 | X-RAY DIFFRACTION (3.2 Å) | | 主引用文献 | Sar156497 an Exquisitely Selective Inhibitor of Aurora Kinases.
J.Med.Chem., 58, 2015
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4WHZ
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4WIH
 | | Crystal structure of cAMP-dependent Protein Kinase A from Cricetulus griseus | | 分子名称: | cAMP Dependent Protein Kinase Inhibitor PKI-tide, cAMP-dependent protein kinase catalytic subunit alpha | | 著者 | Kudlinzki, D, Linhard, V.L, Saxena, K, Dreyer, M, Schwalbe, H. | | 登録日 | 2014-09-25 | | 公開日 | 2014-10-22 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (1.139 Å) | | 主引用文献 | High-resolution crystal structure of cAMP-dependent protein kinase from Cricetulus griseus.
Acta Crystallogr.,Sect.F, 71, 2015
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4WNP
 | | Structure of ULK1 bound to a potent inhibitor | | 分子名称: | GLYCEROL, N~2~-(1H-benzimidazol-6-yl)-N~4~-(5-cyclobutyl-1H-pyrazol-3-yl)quinazoline-2,4-diamine, Serine/threonine-protein kinase ULK1 | | 著者 | Lazarus, M.B, Novotny, C.J, Shokat, K.M. | | 登録日 | 2014-10-14 | | 公開日 | 2015-01-14 | | 最終更新日 | 2023-12-27 | | 実験手法 | X-RAY DIFFRACTION (1.88 Å) | | 主引用文献 | Structure of the Human Autophagy Initiating Kinase ULK1 in Complex with Potent Inhibitors.
Acs Chem.Biol., 10, 2015
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4WOT
 | | ROCK2 IN COMPLEX WITH 1426382-07-1 | | 分子名称: | Rho-associated protein kinase 2, methyl 3-[({2'-(aminomethyl)-5'-[(3-fluoropyridin-4-yl)carbamoyl]biphenyl-3-yl}carbonyl)amino]-4-fluorobenzoate | | 著者 | Augustin, M, Krapp, S, Boland, S, Defert, O, Bourin, A, Alen, J, Leysen, D. | | 登録日 | 2014-10-16 | | 公開日 | 2015-05-06 | | 最終更新日 | 2024-05-08 | | 実験手法 | X-RAY DIFFRACTION (2.93 Å) | | 主引用文献 | Design, synthesis, and biological evaluation of novel, highly active soft ROCK inhibitors.
J. Med. Chem., 58, 2015
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4X7N
 | | Co-crystal Structure of PERK bound to 4-[2-amino-4-methyl-3-(2-methylquinolin-6-yl)benzoyl]-1-methyl-2,5-diphenyl-1,2-dihydro-3H-pyrazol-3-one inhibitor | | 分子名称: | 4-[2-amino-4-methyl-3-(2-methylquinolin-6-yl)benzoyl]-1-methyl-2,5-diphenyl-1,2-dihydro-3H-pyrazol-3-one, Eukaryotic translation initiation factor 2-alpha kinase 3,Eukaryotic translation initiation factor 2-alpha kinase 3, L(+)-TARTARIC ACID | | 著者 | Shaffer, P.L, Long, A.M, Chen, H. | | 登録日 | 2014-12-09 | | 公開日 | 2015-01-28 | | 最終更新日 | 2023-09-27 | | 実験手法 | X-RAY DIFFRACTION (2.35 Å) | | 主引用文献 | Discovery of 1H-Pyrazol-3(2H)-ones as Potent and Selective Inhibitors of Protein Kinase R-like Endoplasmic Reticulum Kinase (PERK).
J.Med.Chem., 58, 2015
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4X21
 | | The MAP kinase JNK3 as target for halogen bonding | | 分子名称: | CHLORIDE ION, Mitogen-activated protein kinase 10, N-ethyl-4-{[4-(1H-indol-3-yl)-5-iodopyrimidin-2-yl]amino}piperidine-1-carboxamide | | 著者 | Lange, A, Buettner, F.M, Guenther, M.B, Zimmermann, M.O, Hennig, S, Laufer, S.A, Stehle, T, Boeckler, F. | | 登録日 | 2014-11-25 | | 公開日 | 2015-11-11 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (1.95 Å) | | 主引用文献 | Targeting the Gatekeeper MET146 of C-Jun N-Terminal Kinase 3 Induces a Bivalent Halogen/Chalcogen Bond.
J.Am.Chem.Soc., 137, 2015
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4WSQ
 | | Crystal Structure of Adaptor Protein 2 Associated Kinase (AAK1) in complex with small molecule inhibitor | | 分子名称: | 1,2-ETHANEDIOL, AP2-associated protein kinase 1, K-252A, ... | | 著者 | Sorrell, F.J, Elkins, J.M, Krojer, T, Williams, E, Abdul, K, Gileadi, O, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Knapp, S, Structural Genomics Consortium (SGC) | | 登録日 | 2014-10-28 | | 公開日 | 2014-11-05 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (1.95 Å) | | 主引用文献 | Family-wide Structural Analysis of Human Numb-Associated Protein Kinases.
Structure, 24, 2016
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4WSY
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4WT6
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4X2K
 | | Selection of fragments for kinase inhibitor design: decoration is key | | 分子名称: | 4-[(3-aminophenyl)amino]pyrido[2,3-d]pyrimidin-5(6H)-one, SULFATE ION, TGF-beta receptor type-1 | | 著者 | Czodrowski, P, Hoelzemann, G, Barnickel, G, Greiner, H, Musil, D. | | 登録日 | 2014-11-26 | | 公開日 | 2014-12-24 | | 最終更新日 | 2024-05-08 | | 実験手法 | X-RAY DIFFRACTION (1.69 Å) | | 主引用文献 | Selection of fragments for kinase inhibitor design: decoration is key.
J.Med.Chem., 58, 2015
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4X7J
 | | Co-crystal Structure of PERK with 2-amino-N-[4-methoxy-3-(trifluoromethyl)phenyl]-4-methyl-3-[2-(methylamino)quinazolin-6-yl]benzamide inhibitor | | 分子名称: | 2-amino-N-[4-methoxy-3-(trifluoromethyl)phenyl]-4-methyl-3-[2-(methylamino)quinazolin-6-yl]benzamide, Eukaryotic translation initiation factor 2-alpha kinase 3,Eukaryotic translation initiation factor 2-alpha kinase 3, L(+)-TARTARIC ACID | | 著者 | Shaffer, P.L, Long, A.M, Chen, H. | | 登録日 | 2014-12-09 | | 公開日 | 2015-01-28 | | 最終更新日 | 2023-09-27 | | 実験手法 | X-RAY DIFFRACTION (2.3 Å) | | 主引用文献 | Discovery of 1H-Pyrazol-3(2H)-ones as Potent and Selective Inhibitors of Protein Kinase R-like Endoplasmic Reticulum Kinase (PERK).
J.Med.Chem., 58, 2015
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4WNO
 | | Structure of ULK1 bound to an inhibitor | | 分子名称: | N~2~-(4-aminophenyl)-N~4~-(5-cyclopropyl-1H-pyrazol-3-yl)quinazoline-2,4-diamine, Serine/threonine-protein kinase ULK1 | | 著者 | Lazarus, M.B, Novotny, C.J, Shokat, K.M. | | 登録日 | 2014-10-14 | | 公開日 | 2015-01-14 | | 最終更新日 | 2023-09-27 | | 実験手法 | X-RAY DIFFRACTION (1.56 Å) | | 主引用文献 | Structure of the Human Autophagy Initiating Kinase ULK1 in Complex with Potent Inhibitors.
Acs Chem.Biol., 10, 2015
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4WRS
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4WUA
 | | Crystal structure of human SRPK1 complexed to an inhibitor SRPIN340 | | 分子名称: | CITRIC ACID, N-[2-(1-piperidinyl)-5-(trifluoromethyl)phenyl]-4-pyridinecarboxamide, SRSF protein kinase 1, ... | | 著者 | Hoshina, M, Ikura, T, Hosoya, T, Hagiwara, M, Ito, N. | | 登録日 | 2014-10-31 | | 公開日 | 2015-09-16 | | 最終更新日 | 2023-11-08 | | 実験手法 | X-RAY DIFFRACTION (2 Å) | | 主引用文献 | Identification of a Dual Inhibitor of SRPK1 and CK2 That Attenuates Pathological Angiogenesis of Macular Degeneration in Mice
Mol.Pharmacol., 88, 2015
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4X7K
 | | Co-crystal Structure of PERK bound to 4-{2-amino-3-[5-fluoro-2-(methylamino)quinazolin-6-yl]-4-methylbenzoyl}-1-methyl-2,5-diphenyl-1,2-dihydro-3H-pyrazol-3-one inhibitor | | 分子名称: | 4-{2-amino-3-[5-fluoro-2-(methylamino)quinazolin-6-yl]-4-methylbenzoyl}-1-methyl-2,5-diphenyl-1,2-dihydro-3H-pyrazol-3-one, Eukaryotic translation initiation factor 2-alpha kinase 3,Eukaryotic translation initiation factor 2-alpha kinase 3, GLYCEROL, ... | | 著者 | Shaffer, P.L, Long, A.M, Chen, H. | | 登録日 | 2014-12-09 | | 公開日 | 2015-01-28 | | 最終更新日 | 2023-09-27 | | 実験手法 | X-RAY DIFFRACTION (1.8 Å) | | 主引用文献 | Discovery of 1H-Pyrazol-3(2H)-ones as Potent and Selective Inhibitors of Protein Kinase R-like Endoplasmic Reticulum Kinase (PERK).
J.Med.Chem., 58, 2015
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4X7Q
 | | PIM2 kinase in complex with Compound 1s | | 分子名称: | 2-(2,6-difluorophenyl)-N-{4-[(3S)-pyrrolidin-3-yloxy]pyridin-3-yl}-1,3-thiazole-4-carboxamide, PHOSPHATE ION, Serine/threonine-protein kinase pim-2 | | 著者 | Marcotte, D.J, Silvian, L.F. | | 登録日 | 2014-12-09 | | 公開日 | 2015-02-11 | | 最終更新日 | 2023-09-27 | | 実験手法 | X-RAY DIFFRACTION (2.33 Å) | | 主引用文献 | Structure-based design of low-nanomolar PIM kinase inhibitors.
Bioorg.Med.Chem.Lett., 25, 2015
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