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 | 2024-10-30 | | 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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8S99
 | | Crystal structure of the TYK2 pseudokinase domain in complex with compound 11 | | 分子名称: | (8S)-N-[(1R,2S)-2-fluorocyclopropyl]-5-{[(1M,2'M)-3'-fluoro-2-oxo-2H-[1,2'-bipyridin]-3-yl]amino}-7-(methylamino)pyrazolo[1,5-a]pyrimidine-3-carboxamide, 1,2-ETHANEDIOL, ACETATE ION, ... | | 著者 | Toms, A.V, Leit, S, Greenwood, J.R, Carriero, S, Mondal, S, Abel, R, Ashwell, M, Blanchette, H, Boyles, N, Cartwright, M, Collis, A, Feng, S, Ghanakota, P, Harriman, G.C, Hosagrahara, V, Kaila, N, Kapeller, R, Rafi, S, Romero, D.L, Tarantino, P, Timaniya, J, Wester, R.T, Westlin, W, Srivastava, B, Miao, W, Tummino, P, McElwee, J.J, Edmondson, S.D, Massee, C.E. | | 登録日 | 2023-03-27 | | 公開日 | 2023-07-26 | | 最終更新日 | 2023-08-23 | | 実験手法 | X-RAY DIFFRACTION (1.71 Å) | | 主引用文献 | Discovery of a Potent and Selective Tyrosine Kinase 2 Inhibitor: TAK-279.
J.Med.Chem., 66, 2023
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8S9A
 | | Crystal structure of the TYK2 pseudokinase domain in complex with TAK-279 | | 分子名称: | (8S)-N-[(1R,2R)-2-methoxycyclobutyl]-7-(methylamino)-5-{[(1P,2'P)-2-oxo-2H-[1,2'-bipyridin]-3-yl]amino}pyrazolo[1,5-a]pyrimidine-3-carboxamide, 1,2-ETHANEDIOL, ACETATE ION, ... | | 著者 | Toms, A.V, Leit, S, Greenwood, J.R, Carriero, S, Mondal, S, Abel, R, Ashwell, M, Blanchette, H, Boyles, N, Cartwright, M, Collis, A, Feng, S, Ghanakota, P, Harriman, G.C, Hosagrahara, V, Kaila, N, Kapeller, R, Rafi, S, Romero, D.L, Tarantino, P, Timaniya, J, Wester, R.T, Westlin, W, Srivastava, B, Miao, W, Tummino, P, McElwee, J.J, Edmondson, S.D, Massee, C.E. | | 登録日 | 2023-03-27 | | 公開日 | 2023-07-26 | | 最終更新日 | 2023-08-23 | | 実験手法 | X-RAY DIFFRACTION (1.83 Å) | | 主引用文献 | Discovery of a Potent and Selective Tyrosine Kinase 2 Inhibitor: TAK-279.
J.Med.Chem., 66, 2023
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8S98
 | | Crystal structure of the TYK2 pseudokinase domain in complex with compound 8 | | 分子名称: | (8S)-N-cyclopropyl-5-[(2-methoxypyridin-3-yl)amino]-7-(methylamino)pyrazolo[1,5-a]pyrimidine-3-carboxamide, Non-receptor tyrosine-protein kinase TYK2 | | 著者 | Toms, A.V, Leit, S, Greenwood, J.R, Carriero, S, Mondal, S, Abel, R, Ashwell, M, Blanchette, H, Boyles, N, Cartwright, M, Collis, A, Feng, S, Ghanakota, P, Harriman, G.C, Hosagrahara, V, Kaila, N, Kapeller, R, Rafi, S, Romero, D.L, Tarantino, P, Timaniya, J, Wester, R.T, Westlin, W, Srivastava, B, Miao, W, Tummino, P, McElwee, J.J, Edmondson, S.D, Massee, C.E. | | 登録日 | 2023-03-27 | | 公開日 | 2023-07-26 | | 最終更新日 | 2024-10-09 | | 実験手法 | X-RAY DIFFRACTION (1.87 Å) | | 主引用文献 | Discovery of a Potent and Selective Tyrosine Kinase 2 Inhibitor: TAK-279.
J.Med.Chem., 66, 2023
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2ANJ
 | | Crystal Structure of the Glur2 Ligand Binding Core (S1S2J-Y450W) Mutant in Complex With the Partial Agonist Kainic Acid at 2.1 A Resolution | | 分子名称: | 3-(CARBOXYMETHYL)-4-ISOPROPENYLPROLINE, Glutamate receptor 2 | | 著者 | Holm, M.M, Naur, P, Vestergaard, B, Geballe, M.T, Gajhede, M, Kastrup, J.S, Traynelis, S.F, Egebjerg, J. | | 登録日 | 2005-08-11 | | 公開日 | 2005-08-30 | | 最終更新日 | 2024-11-06 | | 実験手法 | X-RAY DIFFRACTION (2.1 Å) | | 主引用文献 | A Binding Site Tyrosine Shapes Desensitization Kinetics and Agonist Potency at GluR2: a mutagenic, kinetic, and crystallographic study
J.Biol.Chem., 280, 2005
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5FHO
 | | Crystal structure of the GluA2 ligand-binding domain (S1S2J) in complex with (S)-2-Amino-3-(5-(2-(3-chlorobenzyl)-2H-tetrazol-5-yl)-3-hydroxyisoxazol-4-yl)propanoic acid at 2.3 A resolution | | 分子名称: | (1S)-1-carboxy-2-(5-{2-[(3-chlorophenyl)methyl]-2H-tetrazol-5-yl}-3-oxo-2,3-dihydro-1,2-oxazol-4-yl)ethan-1-aminium, 1,2-ETHANEDIOL, CHLORIDE ION, ... | | 著者 | Frydenvang, K, Kastrup, J.S. | | 登録日 | 2015-12-22 | | 公開日 | 2016-03-02 | | 最終更新日 | 2024-11-13 | | 実験手法 | X-RAY DIFFRACTION (2.3 Å) | | 主引用文献 | Tweaking Subtype Selectivity and Agonist Efficacy at (S)-2-Amino-3-(3-hydroxy-5-methyl-isoxazol-4-yl)propionic acid (AMPA) Receptors in a Small Series of BnTetAMPA Analogues.
J.Med.Chem., 59, 2016
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5FHM
 | | Crystal structure of the GluA2 ligand-binding domain (S1S2J) in complex with (S)-2-Amino-3-(5-(2-(3-(aminomethyl)benzyl)-2H-tetrazol-5-yl)-3-hydroxyisoxazol-4-yl)propanoic acid at resolution 1.55 A resolution | | 分子名称: | (2~{S})-3-[5-[2-[[3-(aminomethyl)phenyl]methyl]-1,2,3,4-tetrazol-5-yl]-3-oxidanyl-1,2-oxazol-4-yl]-2-azanyl-propanoic acid, 1,2-ETHANEDIOL, ACETATE ION, ... | | 著者 | Kastrup, J.S, Frydenvang, K, Al-musaed, A. | | 登録日 | 2015-12-22 | | 公開日 | 2016-03-02 | | 最終更新日 | 2024-11-06 | | 実験手法 | X-RAY DIFFRACTION (1.55 Å) | | 主引用文献 | Tweaking Subtype Selectivity and Agonist Efficacy at (S)-2-Amino-3-(3-hydroxy-5-methyl-isoxazol-4-yl)propionic acid (AMPA) Receptors in a Small Series of BnTetAMPA Analogues.
J.Med.Chem., 59, 2016
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5FHN
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