3RVG
 
 | | Crystals structure of Jak2 with a 1-amino-5H-pyrido[4,3-b]indol-4-carboxamide inhibitor | | 分子名称: | 1-(cyclohexylamino)-7-(1-methyl-1H-pyrazol-4-yl)-5H-pyrido[4,3-b]indole-4-carboxamide, Tyrosine-protein kinase JAK2 | | 著者 | Lim, J, Taoka, B, Otte, R.D, Spencer, K, Dinsmore, C.J, Altman, M.D, Chan, G, Rosenstein, C, Sharma, S, Su, H.P, Szewczak, A.A, Xu, L, Yin, H, Zugay-Murphy, J, Marshall, C.G, Young, J.R. | | 登録日 | 2011-05-06 | | 公開日 | 2012-03-21 | | 最終更新日 | 2017-11-08 | | 実験手法 | X-RAY DIFFRACTION (2.498 Å) | | 主引用文献 | Discovery of 1-amino-5H-pyrido[4,3-b]indol-4-carboxamide inhibitors of Janus kinase 2 (JAK2) for the treatment of myeloproliferative disorders.
J.Med.Chem., 54, 2011
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5WO4
 | | JAK1 complexed with compound 28 | | 分子名称: | 3-[(4-chloro-3-methoxyphenyl)amino]-1-[(3R,4S)-4-cyanooxan-3-yl]-1H-pyrazole-4-carboxamide, Tyrosine-protein kinase JAK1 | | 著者 | Lesburg, C.A, Patel, S.B. | | 登録日 | 2017-08-01 | | 公開日 | 2017-12-06 | | 最終更新日 | 2024-03-06 | | 実験手法 | X-RAY DIFFRACTION (1.84 Å) | | 主引用文献 | The Discovery of 3-((4-Chloro-3-methoxyphenyl)amino)-1-((3R,4S)-4-cyanotetrahydro-2H-pyran-3-yl)-1H-pyrazole-4-carboxamide, a Highly Ligand Efficient and Efficacious Janus Kinase 1 Selective Inhibitor with Favorable Pharmacokinetic Properties.
J. Med. Chem., 60, 2017
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5HX8
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3Q6W
 | | Structure of dually-phosphorylated MET receptor kinase in complex with an MK-2461 analog with specificity for the activated receptor | | 分子名称: | 3-{5-oxo-3-[1-(piperidin-4-yl)-1H-pyrazol-4-yl]-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl}-N-(pyridin-2-ylmethyl)propanamide, Hepatocyte growth factor receptor | | 著者 | Soisson, S.M, Rickert, K.W, Patel, S.B, Lumb, K.J. | | 登録日 | 2011-01-03 | | 公開日 | 2011-01-19 | | 最終更新日 | 2017-11-08 | | 実験手法 | X-RAY DIFFRACTION (1.75 Å) | | 主引用文献 | Structural basis for selective small molecule kinase inhibition of activated c-Met.
J.Biol.Chem., 286, 2011
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3Q6U
 | | Structure of the apo MET receptor kinase in the dually-phosphorylated, activated state | | 分子名称: | Hepatocyte growth factor receptor | | 著者 | Soisson, S.M, Rickert, K.W, Patel, S.B, Allison, T, Lumb, K.J. | | 登録日 | 2011-01-03 | | 公開日 | 2011-01-19 | | 最終更新日 | 2011-07-13 | | 実験手法 | X-RAY DIFFRACTION (1.6 Å) | | 主引用文献 | Structural basis for selective small molecule kinase inhibition of activated c-Met.
J.Biol.Chem., 286, 2011
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3R7O
 | | Structure of dually phosphorylated c-MET receptor kinase in complex with an MK-2461 analog | | 分子名称: | Hepatocyte growth factor receptor, N-[(2R)-1,4-dioxan-2-ylmethyl]-N-methyl-N'-{5-oxo-3-[1-(piperidin-4-yl)-1H-pyrazol-4-yl]-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl}sulfuric diamide | | 著者 | Soisson, S.M, Rickert, K, Patel, S.B, Munshi, S, Lumb, K.J. | | 登録日 | 2011-03-22 | | 公開日 | 2012-02-01 | | 最終更新日 | 2017-11-08 | | 実験手法 | X-RAY DIFFRACTION (2.3 Å) | | 主引用文献 | Structural basis for selective small molecule kinase inhibition of activated c-Met.
J.Biol.Chem., 286, 2011
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4IWD
 | | Structure of dually phosphorylated c-MET receptor kinase in complex with an MK-8033 analog | | 分子名称: | 1-{5-oxo-3-[1-(piperidin-4-yl)-1H-pyrazol-4-yl]-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl}-N-(pyridin-2-ylmethyl)methanesulfonamide, Hepatocyte growth factor receptor | | 著者 | Soisson, S.M, Northrup, A, Rickert, K, Patel, S, Allison, T. | | 登録日 | 2013-01-23 | | 公開日 | 2013-12-11 | | 最終更新日 | 2017-11-15 | | 実験手法 | X-RAY DIFFRACTION (1.99 Å) | | 主引用文献 | Discovery of 1-[3-(1-methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl]-N-(pyridin-2-ylmethyl)methanesulfonamide (MK-8033): A Specific c-Met/Ron dual kinase inhibitor with preferential affinity for the activated state of c-Met.
J.Med.Chem., 56, 2013
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