3V4A
 
 | | Structure of ar lbd with activator peptide and sarm inhibitor 2 | | 分子名称: | (5R)-3-(3,4-dichlorophenyl)-5-(4-hydroxyphenyl)-1,5-dimethyl-2-thioxoimidazolidin-4-one, Androgen receptor, SULFATE ION | | 著者 | Nique, F, Hebbe, S, Peixoto, C, Annoot, D, Lefrancois, J.-M, Duval, E, Michoux, L, Triballeau, N, Lemoullec, J.M, Mollat, P, Thauvin, M, Prange, T, Minet, D, Clement-Lacroix, P, Robin-Jagerschmidt, C, Fleury, D, Guedin, D, Deprez, P. | | 登録日 | 2011-12-14 | | 公開日 | 2012-09-05 | | 最終更新日 | 2023-09-13 | | 実験手法 | X-RAY DIFFRACTION (1.95 Å) | | 主引用文献 | Discovery of diarylhydantoins as new selective androgen receptor modulators.
J.Med.Chem., 55, 2012
|
|
3V49
 | | Structure of ar lbd with activator peptide and sarm inhibitor 1 | | 分子名称: | 4-[(4R)-4-(4-hydroxyphenyl)-3,4-dimethyl-2,5-dioxoimidazolidin-1-yl]-2-(trifluoromethyl)benzonitrile, Androgen receptor, activator peptide, ... | | 著者 | Nique, F, Hebbe, S, Peixoto, C, Annoot, D, Lefrancois, J.-M, Duval, E, Michoux, L, Triballeau, N, Lemoullec, J.-M, Mollat, P, Thauvin, M, Prange, T, Minet, D, Clement-Lacroix, P, Robin-Jagerschmidt, C, Fleury, D, Guedin, D, Deprez, P. | | 登録日 | 2011-12-14 | | 公開日 | 2012-09-05 | | 最終更新日 | 2023-09-13 | | 実験手法 | X-RAY DIFFRACTION (1.7 Å) | | 主引用文献 | Discovery of diarylhydantoins as new selective androgen receptor modulators.
J.Med.Chem., 55, 2012
|
|
2J5W
 | | Ceruloplasmin revisited: structural and functional roles of various metal cation binding sites | | 分子名称: | 2-acetamido-2-deoxy-beta-D-glucopyranose, CALCIUM ION, CERULOPLASMIN, ... | | 著者 | Bento, I, Peixoto, C, Zaitsev, V.N, Lindley, P.F. | | 登録日 | 2006-09-19 | | 公開日 | 2007-02-06 | | 最終更新日 | 2023-12-13 | | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | | 主引用文献 | Ceruloplasmin Revisited: Structural and Functional Roles of Various Metal Cation-Binding Sites.
Acta Crystallogr.,Sect.D, 63, 2007
|
|
1E3G
 | | Human Androgen Receptor Ligand Binding in complex with the ligand metribolone (R1881) | | 分子名称: | (17BETA)-17-HYDROXY-17-METHYLESTRA-4,9,11-TRIEN-3-ONE, ANDROGEN RECEPTOR | | 著者 | Matias, P.M, Donner, P, Coelho, R, Thomaz, M, Peixoto, C, Macedo, S, Otto, N, Joschko, S, Scholz, P, Wegg, A, Basler, S, Schafer, M, Ruff, M, Egner, U, Carrondo, M.A. | | 登録日 | 2000-06-14 | | 公開日 | 2001-06-14 | | 最終更新日 | 2023-12-13 | | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | | 主引用文献 | Structural evidence for ligand specificity in the binding domain of the human androgen receptor. Implications for pathogenic gene mutations.
J. Biol. Chem., 275, 2000
|
|
1E3K
 | | Human Progesteron Receptor Ligand Binding Domain in complex with the ligand metribolone (R1881) | | 分子名称: | (17BETA)-17-HYDROXY-17-METHYLESTRA-4,9,11-TRIEN-3-ONE, PROGESTERONE RECEPTOR | | 著者 | Matias, P.M, Donner, P, Coelho, R, Thomaz, M, Peixoto, C, Macedo, S, Otto, N, Joschko, S, Scholz, P, Wegg, A, Basler, S, Schafer, M, Egner, U, Carrondo, M.A. | | 登録日 | 2000-06-19 | | 公開日 | 2001-06-14 | | 最終更新日 | 2023-12-13 | | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | | 主引用文献 | Structural evidence for ligand specificity in the binding domain of the human androgen receptor. Implications for pathogenic gene mutations.
J. Biol. Chem., 275, 2000
|
|
6YJM
 | | Crystal Structure of the Catalytic Domain of ADAMTS-5 in Complex with the Inhibitor GLPG1972 | | 分子名称: | (5~{S})-5-[3-[(3~{S})-4-[3,5-bis(fluoranyl)phenyl]-3-methyl-piperazin-1-yl]-3-oxidanylidene-propyl]-5-cyclopropyl-imidazolidine-2,4-dione, A disintegrin and metalloproteinase with thrombospondin motifs 5, CALCIUM ION, ... | | 著者 | Goepfert, A, Leonard, P, Triballeau, N, Fleury, D, Mollat, P, Lamers, M. | | 登録日 | 2020-04-03 | | 公開日 | 2021-04-14 | | 最終更新日 | 2024-01-24 | | 実験手法 | X-RAY DIFFRACTION (2.25 Å) | | 主引用文献 | Discovery of GLPG1972/S201086, a Potent, Selective, and Orally Bioavailable ADAMTS-5 Inhibitor for the Treatment of Osteoarthritis.
J.Med.Chem., 64, 2021
|
|
5M7M
 | | Novel Imidazo[1,2-a]pyridine Derivatives with Potent Autotaxin/ENPP2 Inhibitor Activity | | 分子名称: | CHLORIDE ION, Ectonucleotide pyrophosphatase/phosphodiesterase family member 2, IODIDE ION, ... | | 著者 | Wolhkoning, A, Fleury, D, Leonard, P, Triballeau, N, Mollat, P, Vercheval, L. | | 登録日 | 2016-10-28 | | 公開日 | 2017-08-30 | | 最終更新日 | 2020-07-29 | | 実験手法 | X-RAY DIFFRACTION (2.7 Å) | | 主引用文献 | Discovery, Structure-Activity Relationship, and Binding Mode of an Imidazo[1,2-a]pyridine Series of Autotaxin Inhibitors.
J. Med. Chem., 60, 2017
|
|
5MHP
 | | Novel Imidazo[1,2-a]pyridine Derivatives with Potent Autotaxin/ENPP2 Inhibitor Activity | | 分子名称: | 2-[[2-ethyl-8-methyl-6-[4-[2-(3-oxidanylazetidin-1-yl)-2-oxidanylidene-ethyl]piperazin-1-yl]imidazo[1,2-a]pyridin-3-yl]-methyl-amino]-4-(4-fluorophenyl)-1,3-thiazole-5-carbonitrile, 2-acetamido-2-deoxy-beta-D-glucopyranose, CALCIUM ION, ... | | 著者 | Fleury, D, Mueller, I, Lamers, M, Triballeau, N, Mollat, P, Vercheval, L. | | 登録日 | 2016-11-25 | | 公開日 | 2017-08-30 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (2.43 Å) | | 主引用文献 | Discovery of 2-[[2-Ethyl-6-[4-[2-(3-hydroxyazetidin-1-yl)-2-oxoethyl]piperazin-1-yl]-8-methylimidazo[1,2-a]pyridin-3-yl]methylamino]-4-(4-fluorophenyl)thiazole-5-carbonitrile (GLPG1690), a First-in-Class Autotaxin Inhibitor Undergoing Clinical Evaluation for the Treatment of Idiopathic Pulmonary Fibrosis.
J. Med. Chem., 60, 2017
|
|
8OKU
 | | Salt-Inducible Kinase 3 in complex with an inhibitor | | 分子名称: | Serine/threonine-protein kinase SIK3, ~{N}-ethyl-4-[5-[1-(2-hydroxyethyl)pyrazol-4-yl]benzimidazol-1-yl]-2,6-dimethoxy-benzamide | | 著者 | Flower, T.G, Leonard, P.M, Lamers, M.B.A.C, Mollat, P. | | 登録日 | 2023-03-29 | | 公開日 | 2024-01-10 | | 最終更新日 | 2024-01-24 | | 実験手法 | X-RAY DIFFRACTION (3.1 Å) | | 主引用文献 | Optimization of Selectivity and Pharmacokinetic Properties of Salt-Inducible Kinase Inhibitors that Led to the Discovery of Pan-SIK Inhibitor GLPG3312.
J.Med.Chem., 67, 2024
|
|
