7SR8
 
 | | Molecular mechanism of the the wake-promoting agent TAK-925 | | 分子名称: | Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, Hypocretin receptor type 2, ... | | 著者 | Yin, J, Chapman, K, Lian, P, De Brabander, J.K, Rosenbaum, D.M. | | 登録日 | 2021-11-08 | | 公開日 | 2022-06-08 | | 実験手法 | ELECTRON MICROSCOPY (3.3 Å) | | 主引用文献 | Molecular mechanism of the wake-promoting agent TAK-925.
Nat Commun, 13, 2022
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4RVM
 | | CHK1 kinase domain with diazacarbazole compound 19 | | 分子名称: | 3-[4-(piperidin-1-ylmethyl)phenyl]-9H-pyrrolo[2,3-b:5,4-c']dipyridine-6-carbonitrile, Serine/threonine-protein kinase Chk1 | | 著者 | Gazzard, L, Blackwood, E, Burton, B, Chapman, K, Chen, H, Crackett, P, Drobnick, J, Ellwood, C, Epler, J, Flagella, M, Goodacre, S, Halladay, J, Hunt, H, Kintz, S, Lyssikatos, J, MacLeod, C, Ramiscal, S, Schmidt, S, Seward, E, Wiesmann, C, Williams, K, Wu, P, Yee, S, Yen, I, Malek, S. | | 登録日 | 2014-11-26 | | 公開日 | 2015-06-03 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (1.86 Å) | | 主引用文献 | Mitigation of Acetylcholine Esterase Activity in the 1,7-Diazacarbazole Series of Inhibitors of Checkpoint Kinase 1.
J.Med.Chem., 58, 2015
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8EIT
 | | Structure of FFAR1-Gq complex bound to DHA | | 分子名称: | A modified Guanine nucleotide-binding protein G(q) subunit alpha, DOCOSA-4,7,10,13,16,19-HEXAENOIC ACID, Free fatty acid receptor 1, ... | | 著者 | Kumari, P, Inoue, A, Chapman, K, Lian, P, Rosenbaum, D.M. | | 登録日 | 2022-09-15 | | 公開日 | 2023-05-24 | | 最終更新日 | 2023-05-31 | | 実験手法 | ELECTRON MICROSCOPY (2.8 Å) | | 主引用文献 | Molecular mechanism of fatty acid activation of FFAR1.
Proc.Natl.Acad.Sci.USA, 120, 2023
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8EJK
 | | Structure of FFAR1-Gq complex bound to TAK-875 in a lipid nanodisc | | 分子名称: | A modified Guanine nucleotide-binding protein G(q) subunit alpha, Free fatty acid receptor 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | 著者 | Kumari, P, Inoue, A, Chapman, K, Lian, P, Rosenbaum, D.M. | | 登録日 | 2022-09-17 | | 公開日 | 2023-05-24 | | 最終更新日 | 2023-05-31 | | 実験手法 | ELECTRON MICROSCOPY (3.4 Å) | | 主引用文献 | Molecular mechanism of fatty acid activation of FFAR1.
Proc.Natl.Acad.Sci.USA, 120, 2023
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8EJC
 | | Structure of FFAR1-Gq complex bound to TAK-875 | | 分子名称: | A modified Guanine nucleotide-binding protein G(q) subunit alpha, Free fatty acid receptor 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | 著者 | Kumari, P, Inoue, A, Chapman, K, Lian, P, Rosenbaum, D.M. | | 登録日 | 2022-09-16 | | 公開日 | 2023-05-24 | | 最終更新日 | 2023-05-31 | | 実験手法 | ELECTRON MICROSCOPY (3 Å) | | 主引用文献 | Molecular mechanism of fatty acid activation of FFAR1.
Proc.Natl.Acad.Sci.USA, 120, 2023
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6E59
 | | Crystal structure of the human NK1 tachykinin receptor | | 分子名称: | 1-(4-{[(2R,3S)-2-{(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy}-3-(4-fluorophenyl)morpholin-4-yl]methyl}-1H-1,2,3-triazol-5-yl)-N,N-dimethylmethanamine, Substance-P receptor, GlgA glycogen synthase, ... | | 著者 | Yin, J, Clark, L, Chapman, K, Shao, Z, Borek, D, Xu, Q, Wang, J, Rosenbaum, D.M. | | 登録日 | 2018-07-19 | | 公開日 | 2018-12-12 | | 最終更新日 | 2023-10-11 | | 実験手法 | X-RAY DIFFRACTION (3.4 Å) | | 主引用文献 | Crystal structure of the human NK1tachykinin receptor.
Proc. Natl. Acad. Sci. U.S.A., 115, 2018
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4QYH
 | | CHK1 kinase domain in complex with diazacarbazole GNE-783 | | 分子名称: | 3-[4-(4-methylpiperazin-1-yl)phenyl]-9H-pyrrolo[2,3-b:5,4-c']dipyridine-6-carbonitrile, Serine/threonine-protein kinase Chk1 | | 著者 | Wiesmann, C, Wu, P. | | 登録日 | 2014-07-24 | | 公開日 | 2014-12-17 | | 最終更新日 | 2024-02-28 | | 実験手法 | X-RAY DIFFRACTION (1.9 Å) | | 主引用文献 | Discovery of the 1,7-diazacarbazole class of inhibitors of checkpoint kinase 1.
Bioorg.Med.Chem.Lett., 24, 2014
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4QYG
 | | CHK1 kinase domain in complex with diazacarbazole compound 14 | | 分子名称: | 3-[4-(4-methylpiperazin-1-yl)phenyl]-9H-pyrrolo[2,3-b:5,4-c']dipyridine-6-carboxylic acid, Serine/threonine-protein kinase Chk1 | | 著者 | Wiesmann, C, Wu, P. | | 登録日 | 2014-07-24 | | 公開日 | 2014-12-17 | | 最終更新日 | 2024-02-28 | | 実験手法 | X-RAY DIFFRACTION (1.75 Å) | | 主引用文献 | Discovery of the 1,7-diazacarbazole class of inhibitors of checkpoint kinase 1.
Bioorg.Med.Chem.Lett., 24, 2014
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4QYF
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4RVK
 | | CHK1 kinase domain with diazacarbazole compound 8: N-[3-(6-cyano-9H-pyrrolo[2,3-b:5,4-c']dipyridin-3-yl)phenyl]acetamide | | 分子名称: | N-[3-(6-cyano-9H-pyrrolo[2,3-b:5,4-c']dipyridin-3-yl)phenyl]acetamide, Serine/threonine-protein kinase Chk1 | | 著者 | Wiesmann, C, Wu, P. | | 登録日 | 2014-11-26 | | 公開日 | 2015-06-03 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (1.85 Å) | | 主引用文献 | Mitigation of Acetylcholine Esterase Activity in the 1,7-Diazacarbazole Series of Inhibitors of Checkpoint Kinase 1.
J.Med.Chem., 58, 2015
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7SQO
 | | Structure of the orexin-2 receptor(OX2R) bound to TAK-925, Gi and scFv16 | | 分子名称: | Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, Guanine nucleotide-binding protein G(i) subunit alpha-1, ... | | 著者 | McGrath, A.P, Kang, Y, Flinspach, M. | | 登録日 | 2021-11-05 | | 公開日 | 2022-05-25 | | 最終更新日 | 2022-07-06 | | 実験手法 | ELECTRON MICROSCOPY (3.17 Å) | | 主引用文献 | Molecular mechanism of the wake-promoting agent TAK-925.
Nat Commun, 13, 2022
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4RVL
 | | CHK1 kinase domain with diazacarbazole compound 7: 3-(2-hydroxyphenyl)-9H-pyrrolo[2,3-b:5,4-c']dipyridine-6-carbonitrile | | 分子名称: | 3-(2-hydroxyphenyl)-9H-pyrrolo[2,3-b:5,4-c']dipyridine-6-carbonitrile, Serine/threonine-protein kinase Chk1 | | 著者 | Wiesmann, C, Wu, P. | | 登録日 | 2014-11-26 | | 公開日 | 2015-06-03 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (1.85 Å) | | 主引用文献 | Mitigation of Acetylcholine Esterase Activity in the 1,7-Diazacarbazole Series of Inhibitors of Checkpoint Kinase 1.
J.Med.Chem., 58, 2015
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6KQI
 | | Structure of an allosteric modulator bound to the CB1 cannabinoid receptor | | 分子名称: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, 2-[(1R,2R,5R)-5-hydroxy-2-(3-hydroxypropyl)cyclohexyl]-5-(2-methyloctan-2-yl)phenol, 5-chloro-3-ethyl-N-{2-[4-(piperidin-1-yl)phenyl]ethyl}-1H-indole-2-carboxamide, ... | | 著者 | Shao, Z.H, Yan, W. | | 登録日 | 2019-08-17 | | 公開日 | 2019-10-23 | | 最終更新日 | 2023-11-22 | | 実験手法 | X-RAY DIFFRACTION (3.245 Å) | | 主引用文献 | Structure of an allosteric modulator bound to the CB1 cannabinoid receptor.
Nat.Chem.Biol., 15, 2019
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5U09
 | | High-resolution crystal structure of the human CB1 cannabinoid receptor | | 分子名称: | Cannabinoid receptor 1,GlgA glycogen synthase, DI(HYDROXYETHYL)ETHER, N-[(2S,3S)-4-(4-chlorophenyl)-3-(3-cyanophenyl)butan-2-yl]-2-methyl-2-{[5-(trifluoromethyl)pyridin-2-yl]oxy}propanamide, ... | | 著者 | Shao, Z.H, Yin, J, Rosenbaum, D. | | 登録日 | 2016-11-23 | | 公開日 | 2016-12-07 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | | 主引用文献 | High-resolution crystal structure of the human CB1 cannabinoid receptor.
Nature, 2016
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4QYE
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1WUT
 | | Acyl Ureas as Human Liver Glycogen Phosphorylase Inhibitors for the Treatment of Type 2 Diabetes | | 分子名称: | 7-[2,6-DICHLORO-4-({[(2-CHLOROBENZOYL)AMINO]CARBONYL}AMINO)PHENOXY]HEPTANOIC ACID, Glycogen phosphorylase, muscle form, ... | | 著者 | Klabunde, T, Wendt, K.U, Kadereit, D, Brachvogel, V, Burger, H.-J, Herling, A.W, Oikonomakos, N.G, Kosmopoulou, M.N, Schmoll, D, Sarubbi, E, von Roedern, E, Schonafinger, K, Defossa, E. | | 登録日 | 2004-12-08 | | 公開日 | 2005-12-08 | | 最終更新日 | 2011-07-13 | | 実験手法 | X-RAY DIFFRACTION (2.26 Å) | | 主引用文献 | Crystallographic studies on acyl ureas, a new class of glycogen phosphorylase inhibitors, as potential antidiabetic drugs
Protein Sci., 14, 2005
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