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PDB: 36 件

4MHA
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Crystal structure of the catalytic domain of the proto-oncogene tyrosine-protein kinase MER in complex with inhibitor UNC1817
分子名称: 2-(butylamino)-4-[(trans-4-hydroxycyclohexyl)amino]-N-(4-sulfamoylbenzyl)pyrimidine-5-carboxamide, CHLORIDE ION, MAGNESIUM ION, ...
著者Zhang, W, Mciver, A, Stashko, M.A, Deryckere, D, Branchford, B.R, Hunter, D, Kireev, D.B, Miley, D.B.M, Norris-Drouin, J, Stewart, W.M, Lee, M, Sather, S, Zhou, Y, Dipaola, J.A, Machius, M, Janzen, W.P, Earp, H.S, Graham, D.K, Frye, S, Wang, X.
登録日2013-08-29
公開日2014-05-21
最終更新日2023-09-20
実験手法X-RAY DIFFRACTION (2.59 Å)
主引用文献Discovery of Mer specific tyrosine kinase inhibitors for the treatment and prevention of thrombosis.
J.Med.Chem., 56, 2013
7OAM
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Kinase domain of MERTK in complex with compound 8
分子名称: 1,2-ETHANEDIOL, 2-[[2,5-bis(fluoranyl)phenyl]methylamino]-4-(cyclopentylamino)-N-[3-(2-oxidanylidenepyrrolidin-1-yl)propyl]pyrimidine-5-carboxamide, Tyrosine-protein kinase Mer
著者Schroeder, M, Russ, N, Knapp, S, Structural Genomics Consortium (SGC)
登録日2021-04-19
公開日2021-05-19
最終更新日2024-01-31
実験手法X-RAY DIFFRACTION (2.65 Å)
主引用文献Design and Development of a Chemical Probe for Pseudokinase Ca 2+ /calmodulin-Dependent Ser/Thr Kinase.
J.Med.Chem., 64, 2021
5TD2
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Structure-based optimization of 1H-imidazole-2-carboxamides as Axl kinase inhibitors utilizing a Mer mutant surrogate
分子名称: N-[2-{4-[(2S)-4-(methylsulfonyl)morpholin-2-yl]-1,3-thiazol-2-yl}-4-(morpholin-4-yl)phenyl]-1H-imidazole-2-carboxamide, Tyrosine-protein kinase Mer
著者Hoffman, I.D, Lawson, J.D.
登録日2016-09-16
公開日2017-01-25
最終更新日2024-03-06
実験手法X-RAY DIFFRACTION (2.68 Å)
主引用文献Structure-based optimization of 1H-imidazole-2-carboxamides as Axl kinase inhibitors utilizing a Mer mutant surrogate.
Bioorg. Med. Chem. Lett., 27, 2017
7CQE
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Crystal structure of the catalytic domain of the proto-oncogene tyrosine-protein kinase MER in complex with AZD-7762
分子名称: 5-(3-fluorophenyl)-N-[(3S)-3-piperidyl]-3-ureido-thiophene-2-carboxamide, CHLORIDE ION, Tyrosine-protein kinase Mer
著者Park, T.H, Lee, B.I.
登録日2020-08-10
公開日2020-11-04
最終更新日2023-11-29
実験手法X-RAY DIFFRACTION (2.69 Å)
主引用文献Crystal Structure of the Kinase Domain of MerTK in Complex with AZD7762 Provides Clues for Structure-Based Drug Development.
Int J Mol Sci, 21, 2020
3TCP
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BU of 3tcp by Molmil
Crystal structure of the catalytic domain of the proto-oncogene tyrosine-protein kinase MER in complex with inhibitor UNC569
分子名称: 1-[(trans-4-aminocyclohexyl)methyl]-N-butyl-3-(4-fluorophenyl)-1H-pyrazolo[3,4-d]pyrimidin-6-amine, CALCIUM ION, CHLORIDE ION, ...
著者Liu, J, Yang, C, Simpson, C, DeRyckere, D, Van Deusen, A, Miley, M, Kireev, D.B, Norris-Drouin, J, Sather, S, Hunter, D, Patel, H.S, Janzen, W.P, Machius, M, Johnson, G, Earp, H.S, Graham, D.K, Frye, S, Wang, X.
登録日2011-08-09
公開日2012-06-20
最終更新日2023-09-13
実験手法X-RAY DIFFRACTION (2.69 Å)
主引用文献Discovery of Novel Small Molecule Mer Kinase Inhibitors for the Treatment of Pediatric Acute Lymphoblastic Leukemia.
ACS Med Chem Lett, 3, 2012
4M3Q
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Crystal structure of the catalytic domain of the proto-oncogene tyrosine-protein kinase MER in complex with inhibitor UNC1917
分子名称: CHLORIDE ION, MAGNESIUM ION, Tyrosine-protein kinase Mer, ...
著者Zhang, W, Zhang, D, Stashko, M.A, DeRyckere, D, Hunter, D, Kireev, D.B, Miley, M, Cummings, C, Lee, M, Norris-Drouin, J, Stewart, W.M, Sather, S, Zhou, Y, Kirkpatrick, G, Machius, M, Janzen, W.P, Earp, H.S, Graham, D.K, Frye, S, Wang, X.
登録日2013-08-06
公開日2013-11-27
最終更新日2023-09-20
実験手法X-RAY DIFFRACTION (2.718 Å)
主引用文献Pseudo-Cyclization through Intramolecular Hydrogen Bond Enables Discovery of Pyridine Substituted Pyrimidines as New Mer Kinase Inhibitors.
J.Med.Chem., 56, 2013
3BPR
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BU of 3bpr by Molmil
Crystal structure of catalytic domain of the proto-oncogene tyrosine-protein kinase MER in complex with inhibitor C52
分子名称: 2-(2-HYDROXYETHYLAMINO)-6-(3-CHLOROANILINO)-9-ISOPROPYLPURINE, CHLORIDE ION, Proto-oncogene tyrosine-protein kinase MER, ...
著者Walker, J.R, Huang, X, Finerty Jr, P.J, Weigelt, J, Arrowsmith, C.H, Edwards, A.M, Bochkarev, A, Dhe-Paganon, S, Structural Genomics Consortium (SGC)
登録日2007-12-19
公開日2008-01-29
最終更新日2023-08-30
実験手法X-RAY DIFFRACTION (2.8 Å)
主引用文献Structural insights into the inhibited states of the Mer receptor tyrosine kinase.
J.Struct.Biol., 165, 2009
6MEP
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Crystal structure of the catalytic domain of the proto-oncogene tyrosine-protein kinase MER in complex with inhibitor UNC3437
分子名称: CHLORIDE ION, MAGNESIUM ION, Tyrosine-protein kinase Mer, ...
著者Da, C, Zhang, D, Stashko, M.A, Cheng, A, Hunter, D, Norris-Drouin, J, Graves, L, Machius, M, Miley, M.J, DeRyckere, D, Earp, H.S, Graham, D.K, Frye, S.V, Wang, X, Kireev, D.
登録日2018-09-06
公開日2019-09-11
最終更新日2024-03-13
実験手法X-RAY DIFFRACTION (2.893 Å)
主引用文献Data-Driven Construction of Antitumor Agents with Controlled Polypharmacology.
J.Am.Chem.Soc., 141, 2019
7M5Z
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Crystal Structure of the MerTK Kinase Domain in Complex with Inhibitor MIPS15692
分子名称: 2-(butylamino)-N-[1-(3-fluoropropyl)piperidin-4-yl]-4-{[(1r,4r)-4-hydroxycyclohexyl]amino}pyrimidine-5-carboxamide, Tyrosine-protein kinase Mer
著者Hermans, S.J, Hancock, N.C, Baell, J.B, Parker, M.W.
登録日2021-03-25
公開日2021-10-06
最終更新日2023-10-18
実験手法X-RAY DIFFRACTION (3.06 Å)
主引用文献Development of [ 18 F]MIPS15692, a radiotracer with in vitro proof-of-concept for the imaging of MER tyrosine kinase (MERTK) in neuroinflammatory disease.
Eur.J.Med.Chem., 226, 2021
7DXL
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Fragment-based Lead Discovery of Indazole-based Compounds as AXL Kinase Inhibitors
分子名称: 3-[4-[6-chloranyl-5-[[(3R)-pyrrolidin-3-yl]amino]-1H-indazol-3-yl]pyrazol-1-yl]benzenecarbonitrile, Tyrosine-protein kinase Mer
著者Anantharajan, J, Baburajendran, N.
登録日2021-01-19
公開日2021-10-13
最終更新日2023-11-29
実験手法X-RAY DIFFRACTION (3.146 Å)
主引用文献Fragment-based lead discovery of indazole-based compounds as AXL kinase inhibitors.
Bioorg.Med.Chem., 49, 2021
2DBJ
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BU of 2dbj by Molmil
Solution structures of the fn3 domain of human Proto-oncogene tyrosine-protein kinase MER precursor
分子名称: Proto-oncogene tyrosine-protein kinase MER precursor
著者Sato, M, Tochio, N, Koshiba, S, Inoue, M, Kigawa, T, Yokoyama, S, RIKEN Structural Genomics/Proteomics Initiative (RSGI)
登録日2005-12-15
公開日2006-12-19
最終更新日2024-05-29
実験手法SOLUTION NMR
主引用文献Solution structures of the fn3 domain of human Proto-oncogene tyrosine-protein kinase MER precursor
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件を2024-07-10に公開中

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