5VND
 
 | | Crystal structure of FGFR1-Y563C (FGFR4 surrogate) covalently bound to H3B-6527 | | 分子名称: | 1,2-ETHANEDIOL, Fibroblast growth factor receptor 1, N-{2-[(6-{[(2,6-dichloro-3,5-dimethoxyphenyl)carbamoyl](methyl)amino}pyrimidin-4-yl)amino]-5-(4-ethylpiperazin-1-yl)phenyl}propanamide, ... | | 著者 | Tsai, J.H.C, Reynolds, D, Fekkes, P, Smith, P, Larsen, N.A. | | 登録日 | 2017-04-30 | | 公開日 | 2017-05-24 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | | 主引用文献 | H3B-6527 Is a Potent and Selective Inhibitor of FGFR4 in FGF19-Driven Hepatocellular Carcinoma.
Cancer Res., 77, 2017
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3PD8
 | | X-ray structure of the ligand-binding core of GluA2 in complex with (S)-7-HPCA at 2.5 A resolution | | 分子名称: | (7S)-3-hydroxy-4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridine-7-carboxylic acid, ACETIC ACID, CACODYLATE ION, ... | | 著者 | Frydenvang, K, Kastrup, J.S. | | 登録日 | 2010-10-22 | | 公開日 | 2010-12-29 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (2.476 Å) | | 主引用文献 | Biostructural and pharmacological studies of bicyclic analogues of the 3-isoxazolol glutamate receptor agonist ibotenic acid.
J. Med. Chem., 53, 2010
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3PD9
 | | X-ray structure of the ligand-binding core of GluA2 in complex with (R)-5-HPCA at 2.1 A resolution | | 分子名称: | (5R)-3-hydroxy-4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridine-5-carboxylic acid, CHLORIDE ION, GLYCEROL, ... | | 著者 | Frydenvang, K, Kastrup, J.S. | | 登録日 | 2010-10-22 | | 公開日 | 2010-12-29 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (2.1 Å) | | 主引用文献 | Biostructural and pharmacological studies of bicyclic analogues of the 3-isoxazolol glutamate receptor agonist ibotenic acid.
J. Med. Chem., 53, 2010
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6CHW
 | | Estrogen Receptor Alpha Y537S covalently bound to antagonist H3B-5942. | | 分子名称: | 1,2-ETHANEDIOL, 4-[(2-{4-[(1E)-1-(1H-indazol-5-yl)-2-phenylbut-1-en-1-yl]phenoxy}ethyl)amino]-N,N-dimethylbutanamide, DIMETHYL SULFOXIDE, ... | | 著者 | Larsen, N.A. | | 登録日 | 2018-02-23 | | 公開日 | 2018-03-21 | | 最終更新日 | 2020-02-26 | | 実験手法 | X-RAY DIFFRACTION (1.89 Å) | | 主引用文献 | Discovery of Selective Estrogen Receptor Covalent Antagonists for the Treatment of ER alphaWTand ER alphaMUTBreast Cancer.
Cancer Discov, 8, 2018
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6CHZ
 | | Estrogen Receptor Alpha Y537S bound to antagonist H3B-9224. | | 分子名称: | 1,2-ETHANEDIOL, 4-[(2-{4-[(1E)-1-(1H-indazol-5-yl)-2-phenylbut-1-en-1-yl]phenoxy}ethyl)amino]-N,N-dimethylbutanamide, Estrogen receptor | | 著者 | Larsen, N.A. | | 登録日 | 2018-02-23 | | 公開日 | 2018-03-21 | | 最終更新日 | 2024-03-13 | | 実験手法 | X-RAY DIFFRACTION (1.68 Å) | | 主引用文献 | Discovery of Selective Estrogen Receptor Covalent Antagonists for the Treatment of ER alphaWTand ER alphaMUTBreast Cancer.
Cancer Discov, 8, 2018
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4YMA
 | | Structure of the ligand-binding domain of GluA2 in complex with the antagonist CNG10109 | | 分子名称: | (3R)-3-(3-carboxy-5-hydroxyphenyl)-L-proline, 1,2-ETHANEDIOL, ACETATE ION, ... | | 著者 | Moller, C, Tapken, D, Kastrup, J.S, Frydenvang, K. | | 登録日 | 2015-03-06 | | 公開日 | 2015-08-05 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (1.895 Å) | | 主引用文献 | Structure-Activity Relationship Study of Ionotropic Glutamate Receptor Antagonist (2S,3R)-3-(3-Carboxyphenyl)pyrrolidine-2-carboxylic Acid.
J.Med.Chem., 58, 2015
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4YMB
 | | Structure of the ligand-binding domain of GluK1 in complex with the antagonist CNG10111 | | 分子名称: | (3R,4S)-3-(3-carboxyphenyl)-4-propyl-L-proline, 1,2-ETHANEDIOL, ACETATE ION, ... | | 著者 | Moller, C, Tapken, D, Kastrup, J.S, Frydenvang, K. | | 登録日 | 2015-03-06 | | 公開日 | 2015-08-05 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (1.93 Å) | | 主引用文献 | Structure-Activity Relationship Study of Ionotropic Glutamate Receptor Antagonist (2S,3R)-3-(3-Carboxyphenyl)pyrrolidine-2-carboxylic Acid.
J.Med.Chem., 58, 2015
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5SYB
 | | Crystal structure of human PHF5A | | 分子名称: | 1,2-ETHANEDIOL, PHD finger-like domain-containing protein 5A, ZINC ION | | 著者 | Tsai, J.H.C, Teng, T, Zhu, P, Fekkes, P, Larsen, N.A. | | 登録日 | 2016-08-10 | | 公開日 | 2016-09-07 | | 最終更新日 | 2024-03-06 | | 実験手法 | X-RAY DIFFRACTION (1.82 Å) | | 主引用文献 | Splicing modulators act at the branch point adenosine binding pocket defined by the PHF5A-SF3b complex.
Nat Commun, 8, 2017
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5M2V
 | | Structure of GluK1 ligand-binding domain (S1S2) in complex with (2S,4R)-4-(2-carboxyphenoxy)pyrrolidine-2-carboxylic acid at 3.18 A resolution | | 分子名称: | (2~{S},4~{R})-4-(2-carboxyphenoxy)pyrrolidine-2-carboxylic acid, CHLORIDE ION, Glutamate receptor ionotropic, ... | | 著者 | Frydenvang, K, Kastrup, J.S, Kristensen, C.M. | | 登録日 | 2016-10-13 | | 公開日 | 2017-01-11 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (3.18 Å) | | 主引用文献 | Design and Synthesis of a Series of l-trans-4-Substituted Prolines as Selective Antagonists for the Ionotropic Glutamate Receptors Including Functional and X-ray Crystallographic Studies of New Subtype Selective Kainic Acid Receptor Subtype 1 (GluK1) Antagonist (2S,4R)-4-(2-Carboxyphenoxy)pyrrolidine-2-carboxylic Acid.
J. Med. Chem., 60, 2017
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4HEJ
 | | Discovery of Selective and Potent Inhibitors of Gram-positive Bacterial Thymidylate Kinase (TMK): Compund 16 | | 分子名称: | 5-methyl-1-[(3S)-1-{3-[3-(trifluoromethyl)phenoxy]benzyl}piperidin-3-yl]pyrimidine-2,4(1H,3H)-dione, Thymidylate kinase | | 著者 | Martinez-Botella, G, Breen, J, Duffy, J, Dumas, J, Geng, B, Gowers, I, Green, O, Guler, S, Hentemann, M, Hernandez-Juan, F, Joseph-McCarthy, D, Kawatkar, S, Larsen, N, Lazari, O, Loch, J, Macritchie, J. | | 登録日 | 2012-10-03 | | 公開日 | 2012-10-24 | | 最終更新日 | 2024-02-28 | | 実験手法 | X-RAY DIFFRACTION (2 Å) | | 主引用文献 | Discovery of Selective and Potent Inhibitors of Gram-Positive Bacterial Thymidylate Kinase (TMK).
J.Med.Chem., 55, 2012
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6EN4
 | | SF3b core in complex with a splicing modulator | | 分子名称: | PHD finger-like domain-containing protein 5A, Splicing factor 3B subunit 1, Splicing factor 3B subunit 3, ... | | 著者 | Cretu, C, Pena, V. | | 登録日 | 2017-10-04 | | 公開日 | 2018-06-20 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (3.08 Å) | | 主引用文献 | Structural Basis of Splicing Modulation by Antitumor Macrolide Compounds.
Mol. Cell, 70, 2018
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