4RL5
 
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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 | | Descriptor: | 1,2-ETHANEDIOL, 1-(4-AMINOPHENYL)-3,5-DIMETHYL-1H-PYRAZOLE-4-CARBOXYLIC ACID ETHYL ESTER, MAGNESIUM ION, ... | | Authors: | 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. | | Deposit date: | 2004-11-22 | | Release date: | 2005-03-01 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | A family of phosphodiesterase inhibitors discovered by cocrystallography and scaffold-based drug design
Nat.Biotechnol., 23, 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 | | Descriptor: | 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, ... | | Authors: | 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. | | Deposit date: | 2004-11-22 | | Release date: | 2005-03-01 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (1.7 Å) | | Cite: | A family of phosphodiesterase inhibitors discovered by cocrystallography and scaffold-based drug design
Nat.Biotechnol., 23, 2005
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1Y2B
 | | Catalytic Domain Of Human Phosphodiesterase 4D In Complex With 3,5-dimethyl-1H-pyrazole-4-carboxylic acid ethyl ester | | Descriptor: | 1,2-ETHANEDIOL, 3,5-DIMETHYL-1H-PYRAZOLE-4-CARBOXYLIC ACID ETHYL ESTER, MAGNESIUM ION, ... | | Authors: | 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. | | Deposit date: | 2004-11-22 | | Release date: | 2005-03-01 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (1.4 Å) | | Cite: | A family of phosphodiesterase inhibitors discovered by cocrystallography and scaffold-based drug design
Nat.Biotechnol., 23, 2005
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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 | | Descriptor: | 1,2-ETHANEDIOL, 3,5-DIMETHYL-1-PHENYL-1H-PYRAZOLE-4-CARBOXYLIC ACID ETHYL ESTER, MAGNESIUM ION, ... | | Authors: | 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. | | Deposit date: | 2004-11-22 | | Release date: | 2005-03-01 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (1.67 Å) | | Cite: | A family of phosphodiesterase inhibitors discovered by cocrystallography and scaffold-based drug design
Nat.Biotechnol., 23, 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 | | Descriptor: | 3,5-DIMETHYL-1-(3-NITROPHENYL)-1H-PYRAZOLE-4-CARBOXYLIC ACID ETHYL ESTER, MAGNESIUM ION, ZINC ION, ... | | Authors: | 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. | | Deposit date: | 2004-11-22 | | Release date: | 2005-03-01 | | Last modified: | 2011-07-13 | | Method: | X-RAY DIFFRACTION (2.55 Å) | | Cite: | A family of phosphodiesterase inhibitors discovered by cocrystallography and scaffold-based drug design
Nat.Biotechnol., 23, 2005
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1Y2K
 | | Catalytic Domain Of Human Phosphodiesterase 4D In Complex With 3,5-dimethyl-1-(3-nitro-phenyl)-1H-pyrazole-4-carboxylic acid ethyl ester | | Descriptor: | 1,2-ETHANEDIOL, 3,5-DIMETHYL-1-(3-NITROPHENYL)-1H-PYRAZOLE-4-CARBOXYLIC ACID ETHYL ESTER, MAGNESIUM ION, ... | | Authors: | 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. | | Deposit date: | 2004-11-22 | | Release date: | 2005-03-01 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (1.36 Å) | | Cite: | A family of phosphodiesterase inhibitors discovered by cocrystallography and scaffold-based drug design
Nat.Biotechnol., 23, 2005
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1Y2H
 | | Catalytic Domain Of Human Phosphodiesterase 4B In Complex With 1-(2-chloro-phenyl)-3,5-dimethyl-1H-pyrazole-4-carboxylic acid ethyl ester | | Descriptor: | 1-(2-CHLOROPHENYL)-3,5-DIMETHYL-1H-PYRAZOLE-4-CARBOXYLIC ACID ETHYL ESTER, MAGNESIUM ION, ZINC ION, ... | | Authors: | 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. | | Deposit date: | 2004-11-22 | | Release date: | 2005-03-01 | | Last modified: | 2011-07-13 | | Method: | X-RAY DIFFRACTION (2.4 Å) | | Cite: | A family of phosphodiesterase inhibitors discovered by cocrystallography and scaffold-based drug design
Nat.Biotechnol., 23, 2005
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4XV3
 | | B-Raf Kinase V600E oncogenic mutant in complex with PLX7922 | | Descriptor: | N'-{3-[5-(2-aminopyrimidin-4-yl)-2-tert-butyl-1,3-thiazol-4-yl]-2-fluorophenyl}-N-ethyl-N-methylsulfuric diamide, Serine/threonine-protein kinase B-raf | | Authors: | Zhang, Y, Zhang, C. | | Deposit date: | 2015-01-26 | | Release date: | 2015-10-28 | | Last modified: | 2024-02-28 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | RAF inhibitors that evade paradoxical MAPK pathway activation.
Nature, 526, 2015
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4XV9
 | | B-Raf Kinase domain in complex with PLX5568 | | Descriptor: | N-{3-[(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)carbonyl]-2,4-difluorophenyl}-4-(trifluoromethyl)benzenesulfonamide, SULFATE ION, Serine/threonine-protein kinase B-raf | | Authors: | zhang, Y, zhang, c, wang, w. | | Deposit date: | 2015-01-26 | | Release date: | 2015-10-28 | | Last modified: | 2024-02-28 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | RAF inhibitors that evade paradoxical MAPK pathway activation.
Nature, 526, 2015
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4XV2
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6PT0
 | | Cryo-EM structure of human cannabinoid receptor 2-Gi protein in complex with agonist WIN 55,212-2 | | Descriptor: | CHOLESTEROL, Cannabinoid receptor 2, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Xu, T.H, Xing, C, Zhuang, Y, Feng, Z, Zhou, X.E, Chen, M, Wang, L, Meng, X, Xue, Y, Wang, J, Liu, H, McGuire, T, Zhao, G, Melcher, K, Zhang, C, Xu, H.E, Xie, X.Q. | | Deposit date: | 2019-07-14 | | Release date: | 2020-02-12 | | Last modified: | 2020-03-04 | | Method: | ELECTRON MICROSCOPY (3.2 Å) | | Cite: | Cryo-EM Structure of the Human Cannabinoid Receptor CB2-GiSignaling Complex.
Cell, 180, 2020
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4XV1
 | | B-Raf Kinase V600E oncogenic mutant in complex with PLX7904 | | Descriptor: | N'-(3-{[5-(2-cyclopropylpyrimidin-5-yl)-1H-pyrrolo[2,3-b]pyridin-3-yl]carbonyl}-2,4-difluorophenyl)-N-ethyl-N-methylsulfuric diamide, Serine/threonine-protein kinase B-raf | | Authors: | Zhang, Y, Zhang, C. | | Deposit date: | 2015-01-26 | | Release date: | 2015-10-28 | | Last modified: | 2024-02-28 | | Method: | X-RAY DIFFRACTION (2.47 Å) | | Cite: | RAF inhibitors that evade paradoxical MAPK pathway activation.
Nature, 526, 2015
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2X4Z
 | | Crystal Structure of the Human p21-Activated Kinase 4 in Complex with PF-03758309 | | Descriptor: | GLYCEROL, PF-3758309, SERINE/THREONINE-PROTEIN KINASE PAK 4 | | Authors: | Knighton, D.R, Deng, Y, Murray, B, Guo, C, Piraino, J, Westwick, J, Zhang, C, Lamerdin, J, Dagostino, E, Loi, C.-M, Zager, M, Kraynov, E, Christensen, J, Martinez, R, Kephart, S, Marakovits, J, Karlicek, S, Bergqvist, S, Smeal, T. | | Deposit date: | 2010-02-03 | | Release date: | 2010-05-19 | | Last modified: | 2019-01-23 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | Small-Molecule P21-Activated Kinase Inhibitor Pf- 3758309 is a Potent Inhibitor of Oncogenic Signaling and Tumor Growth.
Proc.Natl.Acad.Sci.USA, 107, 2010
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4HVS
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4HW7
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1TAZ
 | | Catalytic Domain Of Human Phosphodiesterase 1B | | Descriptor: | Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1B, MAGNESIUM ION, ZINC ION | | Authors: | 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. | | Deposit date: | 2004-05-19 | | Release date: | 2004-08-03 | | Last modified: | 2011-07-13 | | Method: | X-RAY DIFFRACTION (1.77 Å) | | Cite: | A Glutamine Switch Mechanism for Nucleotide Selectivity by Phosphodiesterases
Mol.Cell, 15, 2004
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1TBF
 | | Catalytic Domain Of Human Phosphodiesterase 5A in Complex with Sildenafil | | Descriptor: | 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, ... | | Authors: | 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. | | Deposit date: | 2004-05-20 | | Release date: | 2004-08-03 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (1.3 Å) | | Cite: | 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 | | Descriptor: | ADENOSINE MONOPHOSPHATE, MAGNESIUM ION, ZINC ION, ... | | Authors: | 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. | | Deposit date: | 2004-05-19 | | Release date: | 2004-08-03 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (2.15 Å) | | Cite: | 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 | | Descriptor: | 1,2-ETHANEDIOL, 2-[3-(2-HYDROXY-1,1-DIHYDROXYMETHYL-ETHYLAMINO)-PROPYLAMINO]-2-HYDROXYMETHYL-PROPANE-1,3-DIOL, ADENOSINE MONOPHOSPHATE, ... | | Authors: | 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. | | Deposit date: | 2004-05-19 | | Release date: | 2004-08-03 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (1.63 Å) | | Cite: | A Glutamine Switch Mechanism for Nucleotide Selectivity by Phosphodiesterases
Mol.Cell, 15, 2004
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1T9R
 | | Catalytic Domain Of Human Phosphodiesterase 5A | | Descriptor: | CITRIC ACID, PHOSPHATE ION, ZINC ION, ... | | Authors: | 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. | | Deposit date: | 2004-05-18 | | Release date: | 2004-08-03 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | 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 | | Descriptor: | GUANOSINE-5'-MONOPHOSPHATE, MAGNESIUM ION, ZINC ION, ... | | Authors: | 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. | | Deposit date: | 2004-05-18 | | Release date: | 2004-08-03 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | 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 | | Descriptor: | 1,2-ETHANEDIOL, MAGNESIUM ION, ROLIPRAM, ... | | Authors: | 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. | | Deposit date: | 2004-05-19 | | Release date: | 2004-08-03 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (1.6 Å) | | Cite: | A Glutamine Switch Mechanism for Nucleotide Selectivity by Phosphodiesterases
Mol.Cell, 15, 2004
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2WEI
 | | Crystal structure of the kinase domain of Cryptosporidium parvum calcium dependent protein kinase in complex with 3-MB-PP1 | | Descriptor: | 1-tert-butyl-3-(3-methylbenzyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine, CALMODULIN-DOMAIN PROTEIN KINASE 1, PUTATIVE | | Authors: | Roos, A.K, King, O, Chaikuad, A, Zhang, C, Shokat, K.M, Wernimont, A.K, Artz, J.D, Lin, L, MacKenzie, F.I, Finerty, P.J, Vedadi, M, Schapira, M, Indarte, M, Kozieradzki, I, Pike, A.C.W, Fedorov, O, Doyle, D, Muniz, J, Arrowsmith, C.H, Weigelt, J, Edwards, A, Bountra, C, von Delft, F, Heightman, T, Hui, R. | | Deposit date: | 2009-03-31 | | Release date: | 2009-04-28 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (1.65 Å) | | Cite: | The Cryptosporidium Parvum Kinome.
Bmc Genomics, 12, 2011
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3OG7
 | | B-Raf Kinase V600E oncogenic mutant in complex with PLX4032 | | Descriptor: | AKAP9-BRAF fusion protein, N-(3-{[5-(4-chlorophenyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]carbonyl}-2,4-difluorophenyl)propane-1-sulfonamide | | Authors: | Zhang, Y, Zhang, K.Y, Zhang, C. | | Deposit date: | 2010-08-16 | | Release date: | 2010-09-22 | | Last modified: | 2024-02-21 | | Method: | X-RAY DIFFRACTION (2.45 Å) | | Cite: | Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma.
Nature, 467, 2010
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