3G6G
 
 | | Equally potent inhibition of c-Src and Abl by compounds that recognize inactive kinase conformations | | Descriptor: | GLYCEROL, N-{3-[(3-{4-[(4-methoxyphenyl)amino]-1,3,5-triazin-2-yl}pyridin-2-yl)amino]-4-methylphenyl}-4-[(4-methylpiperazin-1-yl)methyl]benzamide, Proto-oncogene tyrosine-protein kinase Src | | Authors: | Seeliger, M.A, Ranjitkar, P, Kasap, C, Shan, Y, Shaw, D.E, Shah, N.P, Kuriyan, J, Maly, D.J. | | Deposit date: | 2009-02-06 | | Release date: | 2009-03-24 | | Last modified: | 2023-09-06 | | Method: | X-RAY DIFFRACTION (2.31 Å) | | Cite: | Equally potent inhibition of c-Src and Abl by compounds that recognize inactive kinase conformations
Cancer Res., 69, 2009
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3G6H
 | | Src Thr338Ile inhibited in the DFG-Asp-Out conformation | | Descriptor: | N-{4-methyl-3-[(3-{4-[(3,4,5-trimethoxyphenyl)amino]-1,3,5-triazin-2-yl}pyridin-2-yl)amino]phenyl}-3-(trifluoromethyl)benzamide, Proto-oncogene tyrosine-protein kinase Src | | Authors: | Seeliger, M.A, Ranjitkar, P, Kasap, C, Shan, Y, Shaw, D.E, Shah, N.P, Kuriyan, J, Maly, D.J. | | Deposit date: | 2009-02-06 | | Release date: | 2009-03-24 | | Last modified: | 2023-09-06 | | Method: | X-RAY DIFFRACTION (2.35 Å) | | Cite: | Equally potent inhibition of c-Src and Abl by compounds that recognize inactive kinase conformations
Cancer Res., 69, 2009
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2F4J
 | | Structure of the Kinase Domain of an Imatinib-Resistant Abl Mutant in Complex with the Aurora Kinase Inhibitor VX-680 | | Descriptor: | CYCLOPROPANECARBOXYLIC ACID {4-[4-(4-METHYL-PIPERAZIN-1-YL)-6-(5-METHYL-2H-PYRAZOL-3-YLAMINO)-PYRIMIDIN-2-YLSULFANYL]-PHENYL}-AMIDE, Proto-oncogene tyrosine-protein kinase ABL1 | | Authors: | Young, M.A, Shah, N.P, Chao, L.H, Zarrinkar, P, Sawyers, P, Kuriyan, J. | | Deposit date: | 2005-11-23 | | Release date: | 2006-01-24 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (1.91 Å) | | Cite: | Structure of the kinase domain of an imatinib-resistant Abl mutant in complex with the Aurora kinase inhibitor VX-680.
Cancer Res., 66, 2006
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4RT7
 | | Crystal Structure of FLT3 with a small molecule inhibitor | | Descriptor: | 1-(5-tert-butyl-1,2-oxazol-3-yl)-3-(4-{7-[2-(morpholin-4-yl)ethoxy]imidazo[2,1-b][1,3]benzothiazol-2-yl}phenyl)urea, Receptor-type tyrosine-protein kinase FLT3 | | Authors: | Zhang, Y, Zhang, C. | | Deposit date: | 2014-11-13 | | Release date: | 2015-04-22 | | Last modified: | 2015-06-17 | | Method: | X-RAY DIFFRACTION (3.1 Å) | | Cite: | Characterizing and Overriding the Structural Mechanism of the Quizartinib-Resistant FLT3 "Gatekeeper" F691L Mutation with PLX3397.
Cancer Discov, 5, 2015
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4OGI
 | | Crystal Structure of the first bromodomain of human BRD4 in complex with the inhibitor BI-2536 | | Descriptor: | 1,2-ETHANEDIOL, 4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,7,8-tetrahydropteridin-2-yl]amino}-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide, Bromodomain-containing protein 4 | | Authors: | Filippakopoulos, P, Picaud, S, Jose, B, Martin, S, Fedorov, O, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Knapp, S, Structural Genomics Consortium (SGC) | | Deposit date: | 2014-01-16 | | Release date: | 2014-02-26 | | Last modified: | 2023-09-20 | | Method: | X-RAY DIFFRACTION (1.73 Å) | | Cite: | Dual kinase-bromodomain inhibitors for rationally designed polypharmacology.
Nat.Chem.Biol., 10, 2014
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4OGJ
 | | Crystal Structure of the first bromodomain of human BRD4 in complex with the inhibitor TG-101348 | | Descriptor: | 1,2-ETHANEDIOL, Bromodomain-containing protein 4, N-tert-butyl-3-{[5-methyl-2-({4-[2-(pyrrolidin-1-yl)ethoxy]phenyl}amino)pyrimidin-4-yl]amino}benzenesulfonamide | | Authors: | Filippakopoulos, P, Picaud, S, Jose, B, Martin, S, Fedorov, O, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Knapp, S, Structural Genomics Consortium (SGC) | | Deposit date: | 2014-01-16 | | Release date: | 2014-02-26 | | Last modified: | 2023-09-20 | | Method: | X-RAY DIFFRACTION (1.65 Å) | | Cite: | Dual kinase-bromodomain inhibitors for rationally designed polypharmacology.
Nat.Chem.Biol., 10, 2014
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