1QE6
| INTERLEUKIN-8 WITH AN ADDED DISULFIDE BETWEEN RESIDUES 5 AND 33 (L5C/H33C) | 分子名称: | INTERLEUKIN-8 VARIANT, SULFATE ION | 著者 | Gerber, N, Lowman, H, Artis, D.R, Eigenbrot, C. | 登録日 | 1999-07-13 | 公開日 | 2000-03-22 | 最終更新日 | 2018-01-31 | 実験手法 | X-RAY DIFFRACTION (2.35 Å) | 主引用文献 | Receptor-binding conformation of the "ELR" motif of IL-8: X-ray structure of the L5C/H33C variant at 2.35 A resolution. Proteins, 38, 2000
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3RTP
| Design and synthesis of brain penetrant selective JNK inhibitors with improved pharmacokinetic properties for the prevention of neurodegeneration | 分子名称: | Mitogen-activated protein kinase 10, N-[4-cyano-3-(1H-1,2,4-triazol-5-yl)thiophen-2-yl]-2-(2-oxo-3,4-dihydroquinolin-1(2H)-yl)acetamide | 著者 | Bowers, S, Truong, A.P, Neitz, R.J, Hom, R.K, Sealy, J.M, Probst, G.D, Quincy, Q, Peterson, B, Chan, W, Galemmo Jr, R.A, Konradi, A.W, Sham, H.L, Pan, H, Lin, M, Yao, N, Artis, D.R, Zhang, H, Chen, L, Dryer, M, Samant, B, Zmolek, W, Wong, K, Lorentzen, C, Goldbach, E, Tonn, G, Quinn, K.P, Sauer, J, Wright, S, Powell, K, Ruslim, L, Ren, Z, Bard, F, Yednock, T.A, Griswold-Prenne, I. | 登録日 | 2011-05-03 | 公開日 | 2013-05-08 | 最終更新日 | 2024-02-28 | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | 主引用文献 | Design and synthesis of brain penetrant selective JNK inhibitors with improved pharmacokinetic properties for the prevention of neurodegeneration. Bioorg.Med.Chem.Lett., 21, 2011
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1ICW
| INTERLEUKIN-8, MUTANT WITH GLU 38 REPLACED BY CYS AND CYS 50 REPLACED BY ALA | 分子名称: | INTERLEUKIN-8 | 著者 | Eigenbrot, C, Lowman, H.B, Chee, L, Artis, D.R. | 登録日 | 1996-09-18 | 公開日 | 1997-03-12 | 最終更新日 | 2021-11-03 | 実験手法 | X-RAY DIFFRACTION (2.01 Å) | 主引用文献 | Structural change and receptor binding in a chemokine mutant with a rearranged disulfide: X-ray structure of E38C/C50AIL-8 at 2 A resolution. Proteins, 27, 1997
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1TBF
| Catalytic Domain Of Human Phosphodiesterase 5A in Complex with Sildenafil | 分子名称: | 5-{2-ETHOXY-5-[(4-METHYLPIPERAZIN-1-YL)SULFONYL]PHENYL}-1-METHYL-3-PROPYL-1H,6H,7H-PYRAZOLO[4,3-D]PYRIMIDIN-7-ONE, GLYCEROL, MAGNESIUM ION, ... | 著者 | Zhang, K.Y.J, Card, G.L, Suzuki, Y, Artis, D.R, Fong, D, Gillette, S, Hsieh, D, Neiman, J, West, B.L, Zhang, C, Milburn, M.V, Kim, S.-H, Schlessinger, J, Bollag, G. | 登録日 | 2004-05-20 | 公開日 | 2004-08-03 | 最終更新日 | 2023-08-23 | 実験手法 | X-RAY DIFFRACTION (1.3 Å) | 主引用文献 | A Glutamine Switch Mechanism for Nucleotide Selectivity by Phosphodiesterases Mol.Cell, 15, 2004
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1TB7
| Catalytic Domain Of Human Phosphodiesterase 4D In Complex With AMP | 分子名称: | 1,2-ETHANEDIOL, 2-[3-(2-HYDROXY-1,1-DIHYDROXYMETHYL-ETHYLAMINO)-PROPYLAMINO]-2-HYDROXYMETHYL-PROPANE-1,3-DIOL, ADENOSINE MONOPHOSPHATE, ... | 著者 | Zhang, K.Y.J, Card, G.L, Suzuki, Y, Artis, D.R, Fong, D, Gillette, S, Hsieh, D, Neiman, J, West, B.L, Zhang, C, Milburn, M.V, Kim, S.-H, Schlessinger, J, Bollag, G. | 登録日 | 2004-05-19 | 公開日 | 2004-08-03 | 最終更新日 | 2024-02-14 | 実験手法 | X-RAY DIFFRACTION (1.63 Å) | 主引用文献 | A Glutamine Switch Mechanism for Nucleotide Selectivity by Phosphodiesterases Mol.Cell, 15, 2004
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1T9S
| Catalytic Domain Of Human Phosphodiesterase 5A in Complex with GMP | 分子名称: | GUANOSINE-5'-MONOPHOSPHATE, MAGNESIUM ION, ZINC ION, ... | 著者 | Zhang, K.Y.J, Card, G.L, Suzuki, Y, Artis, D.R, Fong, D, Gillette, S, Hsieh, D, Neiman, J, West, B.L, Zhang, C, Milburn, M.V, Kim, S.-H, Schlessinger, J, Bollag, G. | 登録日 | 2004-05-18 | 公開日 | 2004-08-03 | 最終更新日 | 2023-08-23 | 実験手法 | X-RAY DIFFRACTION (2 Å) | 主引用文献 | A Glutamine Switch Mechanism for Nucleotide Selectivity by Phosphodiesterases Mol.Cell, 15, 2004
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1TBB
| Catalytic Domain Of Human Phosphodiesterase 4D In Complex With Rolipram | 分子名称: | 1,2-ETHANEDIOL, MAGNESIUM ION, ROLIPRAM, ... | 著者 | Zhang, K.Y.J, Card, G.L, Suzuki, Y, Artis, D.R, Fong, D, Gillette, S, Hsieh, D, Neiman, J, West, B.L, Zhang, C, Milburn, M.V, Kim, S.-H, Schlessinger, J, Bollag, G. | 登録日 | 2004-05-19 | 公開日 | 2004-08-03 | 最終更新日 | 2024-02-14 | 実験手法 | X-RAY DIFFRACTION (1.6 Å) | 主引用文献 | A Glutamine Switch Mechanism for Nucleotide Selectivity by Phosphodiesterases Mol.Cell, 15, 2004
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1TAZ
| Catalytic Domain Of Human Phosphodiesterase 1B | 分子名称: | Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1B, MAGNESIUM ION, ZINC ION | 著者 | Zhang, K.Y.J, Card, G.L, Suzuki, Y, Artis, D.R, Fong, D, Gillette, S, Hsieh, D, Neiman, J, West, B.L, Zhang, C, Milburn, M.V, Kim, S.-H, Schlessinger, J, Bollag, G. | 登録日 | 2004-05-19 | 公開日 | 2004-08-03 | 最終更新日 | 2011-07-13 | 実験手法 | X-RAY DIFFRACTION (1.77 Å) | 主引用文献 | A Glutamine Switch Mechanism for Nucleotide Selectivity by Phosphodiesterases Mol.Cell, 15, 2004
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1TB5
| Catalytic Domain Of Human Phosphodiesterase 4B In Complex With AMP | 分子名称: | ADENOSINE MONOPHOSPHATE, MAGNESIUM ION, ZINC ION, ... | 著者 | Zhang, K.Y.J, Card, G.L, Suzuki, Y, Artis, D.R, Fong, D, Gillette, S, Hsieh, D, Neiman, J, West, B.L, Zhang, C, Milburn, M.V, Kim, S.-H, Schlessinger, J, Bollag, G. | 登録日 | 2004-05-19 | 公開日 | 2004-08-03 | 最終更新日 | 2024-02-14 | 実験手法 | X-RAY DIFFRACTION (2.15 Å) | 主引用文献 | A Glutamine Switch Mechanism for Nucleotide Selectivity by Phosphodiesterases Mol.Cell, 15, 2004
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1T9R
| Catalytic Domain Of Human Phosphodiesterase 5A | 分子名称: | CITRIC ACID, PHOSPHATE ION, ZINC ION, ... | 著者 | Zhang, K.Y.J, Card, G.L, Suzuki, Y, Artis, D.R, Fong, D, Gillette, S, Hsieh, D, Neiman, J, West, B.L, Zhang, C, Milburn, M.V, Kim, S.-H, Schlessinger, J, Bollag, G. | 登録日 | 2004-05-18 | 公開日 | 2004-08-03 | 最終更新日 | 2024-02-14 | 実験手法 | X-RAY DIFFRACTION (2.1 Å) | 主引用文献 | A Glutamine Switch Mechanism for Nucleotide Selectivity by Phosphodiesterases Mol.Cell, 15, 2004
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1XM4
| Catalytic Domain Of Human Phosphodiesterase 4B In Complex With Piclamilast | 分子名称: | 3-(CYCLOPENTYLOXY)-N-(3,5-DICHLOROPYRIDIN-4-YL)-4-METHOXYBENZAMIDE, MAGNESIUM ION, ZINC ION, ... | 著者 | Card, G.L, England, B.P, Suzuki, Y, Fong, D, Powell, B, Lee, B, Luu, C, Tabrizizad, M, Gillette, S, Ibrahim, P.N, Artis, D.R, Bollag, G, Milburn, M.V, Kim, S.-H, Schlessinger, J, Zhang, K.Y.J. | 登録日 | 2004-10-01 | 公開日 | 2004-12-14 | 最終更新日 | 2011-07-13 | 実験手法 | X-RAY DIFFRACTION (2.31 Å) | 主引用文献 | Structural Basis for the Activity of Drugs that Inhibit Phosphodiesterases. STRUCTURE, 12, 2004
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1XLX
| Catalytic Domain Of Human Phosphodiesterase 4B In Complex With Cilomilast | 分子名称: | CILOMILAST, MAGNESIUM ION, ZINC ION, ... | 著者 | Card, G.L, England, B.P, Suzuki, Y, Fong, D, Powell, B, Lee, B, Luu, C, Tabrizizad, M, Gillette, S, Ibrahim, P.N, Artis, D.R, Bollag, G, Milburn, M.V, Kim, S.-H, Schlessinger, J, Zhang, K.Y.J. | 登録日 | 2004-09-30 | 公開日 | 2004-12-14 | 最終更新日 | 2011-07-13 | 実験手法 | X-RAY DIFFRACTION (2.19 Å) | 主引用文献 | Structural Basis for the Activity of Drugs that Inhibit Phosphodiesterases. Structure, 12, 2004
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1XM6
| Catalytic Domain Of Human Phosphodiesterase 4B In Complex With (R)-Mesopram | 分子名称: | (5R)-5-(4-methoxy-3-propoxyphenyl)-5-methyl-1,3-oxazolidin-2-one, MAGNESIUM ION, ZINC ION, ... | 著者 | Card, G.L, England, B.P, Suzuki, Y, Fong, D, Powell, B, Lee, B, Luu, C, Tabrizizad, M, Gillette, S, Ibrahim, P.N, Artis, D.R, Bollag, G, Milburn, M.V, Kim, S.-H, Schlessinger, J, Zhang, K.Y.J. | 登録日 | 2004-10-01 | 公開日 | 2004-12-14 | 最終更新日 | 2011-07-13 | 実験手法 | X-RAY DIFFRACTION (1.92 Å) | 主引用文献 | Structural Basis for the Activity of Drugs that Inhibit Phosphodiesterases. STRUCTURE, 12, 2004
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1YXT
| Crystal Structure of Kinase Pim1 in complex with AMPPNP | 分子名称: | PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER, Proto-oncogene serine/threonine-protein kinase Pim-1 | 著者 | Kumar, A, Mandiyan, V, Suzuki, Y, Zhang, C, Rice, J, Tsai, J, Artis, D.R, Ibrahim, P, Bremer, R. | 登録日 | 2005-02-22 | 公開日 | 2005-04-26 | 最終更新日 | 2024-02-14 | 実験手法 | X-RAY DIFFRACTION (2 Å) | 主引用文献 | Crystal structures of proto-oncogene kinase Pim1: a target of aberrant somatic hypermutations in diffuse large cell lymphoma. J.Mol.Biol., 348, 2005
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1Y2D
| Catalytic Domain Of Human Phosphodiesterase 4D In Complex With 1-(4-methoxy-phenyl)-3,5-dimethyl-1H-pyrazole-4-carboxylic acid ethyl ester | 分子名称: | 1,2-ETHANEDIOL, 1-(4-METHOXYPHENYL)-3,5-DIMETHYL-1H-PYRAZOLE-4-CARBOXYLIC ACID ETHYL ESTER, 2-[3-(2-HYDROXY-1,1-DIHYDROXYMETHYL-ETHYLAMINO)-PROPYLAMINO]-2-HYDROXYMETHYL-PROPANE-1,3-DIOL, ... | 著者 | Card, G.L, Blasdel, L, England, B.P, Zhang, C, Suzuki, Y, Gillette, S, Fong, D, Ibrahim, P.N, Artis, D.R, Bollag, G, Milburn, M.V, Kim, S.-H, Schlessinger, J, Zhang, K.Y.J. | 登録日 | 2004-11-22 | 公開日 | 2005-03-01 | 最終更新日 | 2024-02-14 | 実験手法 | X-RAY DIFFRACTION (1.7 Å) | 主引用文献 | A family of phosphodiesterase inhibitors discovered by cocrystallography and scaffold-based drug design Nat.Biotechnol., 23, 2005
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1XOR
| Catalytic Domain Of Human Phosphodiesterase 4D In Complex With Zardaverine | 分子名称: | 6-(4-DIFLUOROMETHOXY-3-METHOXY-PHENYL)-2H-PYRIDAZIN-3-ONE, MAGNESIUM ION, ZINC ION, ... | 著者 | Card, G.L, England, B.P, Suzuki, Y, Fong, D, Powell, B, Lee, B, Luu, C, Tabrizizad, M, Gillette, S, Ibrahim, P.N, Artis, D.R, Bollag, G, Milburn, M.V, Kim, S.-H, Schlessinger, J, Zhang, K.Y.J. | 登録日 | 2004-10-06 | 公開日 | 2004-12-14 | 最終更新日 | 2024-02-14 | 実験手法 | X-RAY DIFFRACTION (1.54 Å) | 主引用文献 | Structural Basis for the Activity of Drugs that Inhibit Phosphodiesterases. STRUCTURE, 12, 2004
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1XOS
| Catalytic Domain Of Human Phosphodiesterase 4B In Complex With Sildenafil | 分子名称: | 5-{2-ETHOXY-5-[(4-METHYLPIPERAZIN-1-YL)SULFONYL]PHENYL}-1-METHYL-3-PROPYL-1H,6H,7H-PYRAZOLO[4,3-D]PYRIMIDIN-7-ONE, MAGNESIUM ION, SULFATE ION, ... | 著者 | Card, G.L, England, B.P, Suzuki, Y, Fong, D, Powell, B, Lee, B, Luu, C, Tabrizizad, M, Gillette, S, Ibrahim, P.N, Artis, D.R, Bollag, G, Milburn, M.V, Kim, S.-H, Schlessinger, J, Zhang, K.Y.J. | 登録日 | 2004-10-06 | 公開日 | 2004-12-14 | 最終更新日 | 2011-07-13 | 実験手法 | X-RAY DIFFRACTION (2.28 Å) | 主引用文献 | Structural Basis for the Activity of Drugs that Inhibit Phosphodiesterases. STRUCTURE, 12, 2004
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1XOZ
| Catalytic Domain Of Human Phosphodiesterase 5A In Complex With Tadalafil | 分子名称: | 6-BENZO[1,3]DIOXOL-5-YL-2-METHYL-2,3,6,7,12,12A-HEXAHYDRO-PYRAZINO[1',2':1,6]PYRIDO[3,4-B]INDOLE-1,4-DIONE, MAGNESIUM ION, ZINC ION, ... | 著者 | Card, G.L, England, B.P, Suzuki, Y, Fong, D, Powell, B, Lee, B, Luu, C, Tabrizizad, M, Gillette, S, Ibrahim, P.N, Artis, D.R, Bollag, G, Milburn, M.V, Kim, S.-H, Schlessinger, J, Zhang, K.Y.J. | 登録日 | 2004-10-07 | 公開日 | 2004-12-14 | 最終更新日 | 2024-02-14 | 実験手法 | X-RAY DIFFRACTION (1.37 Å) | 主引用文献 | Structural Basis for the Activity of Drugs that Inhibit Phosphodiesterases. STRUCTURE, 12, 2004
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1XLZ
| Catalytic Domain Of Human Phosphodiesterase 4B In Complex With Filaminast | 分子名称: | (1E)-1-[3-(CYCLOPENTYLOXY)-4-METHOXYPHENYL]ETHANONE O-(AMINOCARBONYL)OXIME, MAGNESIUM ION, ZINC ION, ... | 著者 | Card, G.L, England, B.P, Suzuki, Y, Fong, D, Powell, B, Lee, B, Luu, C, Tabrizizad, M, Gillette, S, Ibrahim, P.N, Artis, D.R, Bollag, G, Milburn, M.V, Kim, S.-H, Schlessinger, J, Zhang, K.Y.J. | 登録日 | 2004-09-30 | 公開日 | 2004-12-14 | 最終更新日 | 2011-07-13 | 実験手法 | X-RAY DIFFRACTION (2.06 Å) | 主引用文献 | Structural Basis for the Activity of Drugs that Inhibit Phosphodiesterases. STRUCTURE, 12, 2004
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1XON
| Catalytic Domain Of Human Phosphodiesterase 4D In Complex With Piclamilast | 分子名称: | 1,2-ETHANEDIOL, 2-[3-(2-HYDROXY-1,1-DIHYDROXYMETHYL-ETHYLAMINO)-PROPYLAMINO]-2-HYDROXYMETHYL-PROPANE-1,3-DIOL, 3-(CYCLOPENTYLOXY)-N-(3,5-DICHLOROPYRIDIN-4-YL)-4-METHOXYBENZAMIDE, ... | 著者 | Card, G.L, England, B.P, Suzuki, Y, Fong, D, Powell, B, Lee, B, Luu, C, Tabrizizad, M, Gillette, S, Ibrahim, P.N, Artis, D.R, Bollag, G, Milburn, M.V, Kim, S.-H, Schlessinger, J, Zhang, K.Y.J. | 登録日 | 2004-10-06 | 公開日 | 2004-12-14 | 最終更新日 | 2024-02-14 | 実験手法 | X-RAY DIFFRACTION (1.72 Å) | 主引用文献 | Structural Basis for the Activity of Drugs that Inhibit Phosphodiesterases. STRUCTURE, 12, 2004
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1Y2E
| Catalytic Domain Of Human Phosphodiesterase 4D In Complex With 1-(4-amino-phenyl)-3,5-dimethyl-1H-pyrazole-4-carboxylic acid ethyl ester | 分子名称: | 1,2-ETHANEDIOL, 1-(4-AMINOPHENYL)-3,5-DIMETHYL-1H-PYRAZOLE-4-CARBOXYLIC ACID ETHYL ESTER, MAGNESIUM ION, ... | 著者 | Card, G.L, Blasdel, L, England, B.P, Zhang, C, Suzuki, Y, Gillette, S, Fong, D, Ibrahim, P.N, Artis, D.R, Bollag, G, Milburn, M.V, Kim, S.-H, Schlessinger, J, Zhang, K.Y.J. | 登録日 | 2004-11-22 | 公開日 | 2005-03-01 | 最終更新日 | 2024-02-14 | 実験手法 | X-RAY DIFFRACTION (2.1 Å) | 主引用文献 | A family of phosphodiesterase inhibitors discovered by cocrystallography and scaffold-based drug design Nat.Biotechnol., 23, 2005
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1YGC
| Short Factor VIIa with a small molecule inhibitor | 分子名称: | (R)-4-[2-(3-AMINO-BENZENESULFONYLAMINO)-1-(3,5-DIETHOXY-2-FLUOROPHENYL)-2-OXO-ETHYLAMINO]-2-HYDROXY-BENZAMIDINE, CALCIUM ION, Coagulation factor VII, ... | 著者 | Olivero, A.G, Eigenbrot, C, Goldsmith, R, Robarge, K, Artis, D.R, Flygare, J, Rawson, T, Refino, C, Bunting, S, Kirchhofer, D. | 登録日 | 2005-01-04 | 公開日 | 2005-01-18 | 最終更新日 | 2011-07-13 | 実験手法 | X-RAY DIFFRACTION (2 Å) | 主引用文献 | A selective, slow binding inhibitor of factor VIIa binds to a nonstandard active site conformation and attenuates thrombus formation in vivo. J.Biol.Chem., 280, 2005
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1Y2J
| Catalytic Domain Of Human Phosphodiesterase 4B In Complex With 3,5-dimethyl-1-(3-nitro-phenyl)-1H-pyrazole-4-carboxylic acid ethyl ester | 分子名称: | 3,5-DIMETHYL-1-(3-NITROPHENYL)-1H-PYRAZOLE-4-CARBOXYLIC ACID ETHYL ESTER, MAGNESIUM ION, ZINC ION, ... | 著者 | Card, G.L, Blasdel, L, England, B.P, Zhang, C, Suzuki, Y, Gillette, S, Fong, D, Ibrahim, P.N, Artis, D.R, Bollag, G, Milburn, M.V, Kim, S.-H, Schlessinger, J, Zhang, K.Y.J. | 登録日 | 2004-11-22 | 公開日 | 2005-03-01 | 最終更新日 | 2011-07-13 | 実験手法 | X-RAY DIFFRACTION (2.55 Å) | 主引用文献 | A family of phosphodiesterase inhibitors discovered by cocrystallography and scaffold-based drug design Nat.Biotechnol., 23, 2005
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1XOT
| Catalytic Domain Of Human Phosphodiesterase 4B In Complex With Vardenafil | 分子名称: | 2-{2-ETHOXY-5-[(4-ETHYLPIPERAZIN-1-YL)SULFONYL]PHENYL}-5-METHYL-7-PROPYLIMIDAZO[5,1-F][1,2,4]TRIAZIN-4(1H)-ONE, MAGNESIUM ION, ZINC ION, ... | 著者 | Card, G.L, England, B.P, Suzuki, Y, Fong, D, Powell, B, Lee, B, Luu, C, Tabrizizad, M, Gillette, S, Ibrahim, P.N, Artis, D.R, Bollag, G, Milburn, M.V, Kim, S.-H, Schlessinger, J, Zhang, K.Y.J. | 登録日 | 2004-10-06 | 公開日 | 2004-12-14 | 最終更新日 | 2011-07-13 | 実験手法 | X-RAY DIFFRACTION (2.34 Å) | 主引用文献 | Structural Basis for the Activity of Drugs that Inhibit Phosphodiesterases. STRUCTURE, 12, 2004
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1Y2C
| Catalytic Domain Of Human Phosphodiesterase 4D In Complex With 3,5-dimethyl-1-phenyl-1H-pyrazole-4-carboxylic acid ethyl ester | 分子名称: | 1,2-ETHANEDIOL, 3,5-DIMETHYL-1-PHENYL-1H-PYRAZOLE-4-CARBOXYLIC ACID ETHYL ESTER, MAGNESIUM ION, ... | 著者 | Card, G.L, Blasdel, L, England, B.P, Zhang, C, Suzuki, Y, Gillette, S, Fong, D, Ibrahim, P.N, Artis, D.R, Bollag, G, Milburn, M.V, Kim, S.-H, Schlessinger, J, Zhang, K.Y.J. | 登録日 | 2004-11-22 | 公開日 | 2005-03-01 | 最終更新日 | 2024-02-14 | 実験手法 | X-RAY DIFFRACTION (1.67 Å) | 主引用文献 | A family of phosphodiesterase inhibitors discovered by cocrystallography and scaffold-based drug design Nat.Biotechnol., 23, 2005
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