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PDB: 137 件
3F3U
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BU of 3f3u by Molmil
Kinase domain of cSrc in complex with inhibitor RL37 (Type III)
分子名称: 1-[1-(3-aminophenyl)-3-tert-butyl-1H-pyrazol-5-yl]-3-phenylurea, Proto-oncogene tyrosine-protein kinase Src
著者Gruetter, C, Klueter, S, Getlik, M, Rauh, D.
登録日2008-10-31
公開日2009-03-03
最終更新日2023-11-01
実験手法X-RAY DIFFRACTION (2.5 Å)
主引用文献A new screening assay for allosteric inhibitors of cSrc
Nat.Chem.Biol., 5, 2009
2HWO
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BU of 2hwo by Molmil
Crystal structure of Src kinase domain in complex with covalent inhibitor
分子名称: GLYCEROL, N-(4-PHENYLAMINO-QUINAZOLIN-6-YL)-ACRYLAMIDE, Proto-oncogene tyrosine-protein kinase Src
著者Rauh, D, Blair, J.A, Shokat, K.M.
登録日2006-08-01
公開日2007-02-27
最終更新日2021-10-20
実験手法X-RAY DIFFRACTION (2.5 Å)
主引用文献Structure-guided development of affinity probes for tyrosine kinases using chemical genetics.
Nat.Chem.Biol., 3, 2007
5SWH
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BU of 5swh by Molmil
c-Src V281C kinase domain in complex with Rao-IV-151
分子名称: (2R)-3-[4-amino-5-(4-chlorophenyl)-7-(2-methoxyethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]-2-cyano-N-(propan-2-yl)propanami de, Proto-oncogene tyrosine-protein kinase Src
著者Merritt, E.A, Dieter, E.M.
登録日2016-08-08
公開日2017-08-16
最終更新日2023-10-04
実験手法X-RAY DIFFRACTION (2.5 Å)
主引用文献A combined approach reveals a regulatory mechanism coupling Src's kinase activity, localization, and phosphotransferase-independent functions
Mol.Cell, 2019
5T0P
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BU of 5t0p by Molmil
c-Src kinase domain in complex with Rao-IV-151
分子名称: (2E)-3-[4-amino-5-(4-chlorophenyl)-7-(2-methoxyethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]-2-cyano-N-(propan-2-yl)prop-2-enamide, Proto-oncogene tyrosine-protein kinase Src
著者Dieter, E.M, Merritt, E.A, Maly, D.J.
登録日2016-08-16
公開日2017-08-23
最終更新日2023-10-04
実験手法X-RAY DIFFRACTION (2.5 Å)
主引用文献A chemical genetic method for conformation-selective kinase inhibition
To Be Published
3EN4
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BU of 3en4 by Molmil
Targeted polypharmacology: crystal structure of the c-Src kinase domain in complex with PP121, a multitargeted kinase inhibitor
分子名称: 1-cyclopentyl-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine, Proto-oncogene tyrosine-protein kinase Src
著者Blair, J.A, Apsel, B, Knight, Z.A, Shokat, K.M.
登録日2008-09-25
公開日2008-10-14
最終更新日2023-09-06
実験手法X-RAY DIFFRACTION (2.55 Å)
主引用文献Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.
Nat.Chem.Biol., 4, 2008
3F3V
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BU of 3f3v by Molmil
Kinase domain of cSrc in complex with inhibitor RL45 (Type II)
分子名称: 1-{4-[(6-aminoquinazolin-4-yl)amino]phenyl}-3-[3-tert-butyl-1-(3-methylphenyl)-1H-pyrazol-5-yl]urea, Proto-oncogene tyrosine-protein kinase Src
著者Grutter, C, Kluter, S, Getlik, M, Rauh, D.
登録日2008-10-31
公開日2009-06-02
最終更新日2023-11-01
実験手法X-RAY DIFFRACTION (2.6 Å)
主引用文献Hybrid compound design to overcome the gatekeeper T338M mutation in cSrc
J.Med.Chem., 52, 2009
3F3W
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BU of 3f3w by Molmil
Drug resistant cSrc kinase domain in complex with inhibitor RL45 (Type II)
分子名称: 1-{4-[(6-aminoquinazolin-4-yl)amino]phenyl}-3-[3-tert-butyl-1-(3-methylphenyl)-1H-pyrazol-5-yl]urea, Proto-oncogene tyrosine-protein kinase Src
著者Grutter, C, Kluter, S, Getlik, M, Rauh, D.
登録日2008-10-31
公開日2009-06-02
最終更新日2023-11-01
実験手法X-RAY DIFFRACTION (2.6 Å)
主引用文献Hybrid compound design to overcome the gatekeeper T338M mutation in cSrc
J.Med.Chem., 52, 2009
4AGW
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BU of 4agw by Molmil
Discovery of a small molecule type II inhibitor of wild-type and gatekeeper mutants of BCR-ABL, PDGFRalpha, Kit, and Src kinases
分子名称: 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, 3-{2-[(cyclopropylcarbonyl)amino][1,3]thiazolo[5,4-b]pyridin-5-yl}-N-{4-[(4-ethylpiperazin-1-yl)methyl]-3-(trifluoromet hyl)phenyl}benzamide, GLYCEROL, ...
著者Weisberg, E, Choi, H.G, Seeliger, M, Gray, N, Griffin, J.D.
登録日2012-02-01
公開日2012-02-15
最終更新日2024-05-08
実験手法X-RAY DIFFRACTION (2.6 Å)
主引用文献Discovery of a Small-Molecule Type II Inhibitor of Wild-Type and Gatekeeper Mutants of Bcr-Abl, Pdgfralpha, Kit, and Src Kinases: Novel Type II Inhibitor of Gatekeeper Mutants.
Blood, 115, 2010
4YBJ
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BU of 4ybj by Molmil
Type II Dasatinib Analog Crystallized with c-Src Kinase
分子名称: 2-({6-[4-(2-hydroxyethyl)piperazin-1-yl]-2-methylpyrimidin-4-yl}amino)-N-(3-{[3-(trifluoromethyl)benzoyl]amino}phenyl)-1,3-thiazole-5-carboxamide, Proto-oncogene tyrosine-protein kinase Src
著者Kwarcinski, F.E, Brandvold, K.B, Johnson, T.K, Phadke, S, Meagher, J.L, Seeliger, M.A, Stuckey, J.A, Soellner, M.B.
登録日2015-02-18
公開日2016-03-02
最終更新日2023-09-27
実験手法X-RAY DIFFRACTION (2.61 Å)
主引用文献Conformation-Selective Analogues of Dasatinib Reveal Insight into Kinase Inhibitor Binding and Selectivity.
Acs Chem.Biol., 11, 2016
4DGG
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BU of 4dgg by Molmil
c-SRC kinase domain in complex with RM-1-176
分子名称: 3-{6-[(3-chlorobenzyl)oxy]naphthalen-2-yl}-1-(propan-2-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine, Proto-oncogene tyrosine-protein kinase Src
著者Merritt, E.A, Larson, E.T.
登録日2012-01-25
公開日2012-10-10
最終更新日2024-02-28
実験手法X-RAY DIFFRACTION (2.65 Å)
主引用文献Active site profiling reveals coupling between domains in SRC-family kinases.
Nat.Chem.Biol., 9, 2013
3EN5
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BU of 3en5 by Molmil
Targeted polypharmacology: crystal structure of the c-Src kinase domain in complex with PP494, a multitargeted kinase inhibitor
分子名称: 1-cyclobutyl-3-(3,4-dimethoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine, Proto-oncogene tyrosine-protein kinase Src
著者Blair, J.A, Apsel, B, Knight, Z.A, Shokat, K.M.
登録日2008-09-25
公開日2008-10-14
最終更新日2024-02-21
実験手法X-RAY DIFFRACTION (2.66 Å)
主引用文献Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.
Nat.Chem.Biol., 4, 2008
7D5O
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BU of 7d5o by Molmil
C-Src in complex with TAS-120
分子名称: 1-[(3S)-3-{4-amino-3-[(3,5-dimethoxyphenyl)ethynyl]-1H-pyrazolo[3,4-d]pyrimidin-1-yl}pyrrolidin-1-yl]prop-2-en-1-one, Proto-oncogene tyrosine-protein kinase Src
著者Qu, L.Z, Chen, Y.H.
登録日2020-09-27
公開日2021-12-22
最終更新日2023-11-29
実験手法X-RAY DIFFRACTION (2.69 Å)
主引用文献Structural insights into the potency and selectivity of covalent pan-FGFR inhibitors
Commun Chem, 5, 2022
3OF0
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BU of 3of0 by Molmil
crystal structure of the L317I mutant of the chicken c-Src tyrosine kinase domain
分子名称: Proto-oncogene tyrosine-protein kinase Src
著者Boubeva, R, Pernot, L, Perozzo, R, Scapozza, L.
登録日2010-08-13
公開日2011-08-17
最終更新日2023-09-06
実験手法X-RAY DIFFRACTION (2.7 Å)
主引用文献a single amino-acid dictates the dynamics of the switch between active and inactive C-Src conformation
To be Published
5D10
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BU of 5d10 by Molmil
Kinase domain of cSrc in complex with RL236
分子名称: N-[4-({4-(4-methylpiperazin-1-yl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl}oxy)phenyl]prop-2-enamide, Proto-oncogene tyrosine-protein kinase Src
著者Becker, C, Mayer-Wrangowski, S.C, Julian, E, Rauh, D.
登録日2015-08-03
公開日2015-09-02
最終更新日2024-01-10
実験手法X-RAY DIFFRACTION (2.7 Å)
主引用文献Targeting Drug Resistance in EGFR with Covalent Inhibitors: A Structure-Based Design Approach.
J.Med.Chem., 58, 2015
3TZ8
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BU of 3tz8 by Molmil
Kinase domain of cSrc in complex with RL104
分子名称: N-(4-{[4-({[1-(3-aminophenyl)-3-tert-butyl-1H-pyrazol-5-yl]carbamoyl}amino)phenyl]amino}quinazolin-6-yl)-3-(4-methylpiperazin-1-yl)propanamide, Proto-oncogene tyrosine-protein kinase Src
著者Gruetter, C, Richters, A, Rauh, D.
登録日2011-09-27
公開日2012-10-10
最終更新日2023-11-01
実験手法X-RAY DIFFRACTION (2.7 Å)
主引用文献Overcoming Gatekeeper Mutations in cSrc and Abl by Hybrid Compound Design
To be Published
4MCV
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BU of 4mcv by Molmil
Star 12 bound to analog-sensitive Src kinase
分子名称: (7S)-12-(4-aminobutyl)-7-(2-methylpropyl)-6,7,12,13-tetrahydro-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazol-5-one, Proto-oncogene tyrosine-protein kinase Src
著者Lopez, M.S, Shokat, K.M.
登録日2013-08-21
公開日2013-11-20
最終更新日2024-02-28
実験手法X-RAY DIFFRACTION (2.73 Å)
主引用文献Staurosporine-derived inhibitors broaden the scope of analog-sensitive kinase technology.
J.Am.Chem.Soc., 135, 2013
3QLG
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BU of 3qlg by Molmil
Crystal structure of the L317I mutant of the C-src tyrosine kinase domain complexed with dasatinib
分子名称: N-(2-CHLORO-6-METHYLPHENYL)-2-({6-[4-(2-HYDROXYETHYL)PIPERAZIN-1-YL]-2-METHYLPYRIMIDIN-4-YL}AMINO)-1,3-THIAZOLE-5-CARBOXAMIDE, Proto-oncogene tyrosine-protein kinase Src
著者Boubeva, R, Pernot, L, Perozzo, R, Scapozza, L.
登録日2011-02-02
公開日2012-02-08
最終更新日2023-09-13
実験手法X-RAY DIFFRACTION (2.75 Å)
主引用文献A single amino-acid dictates the dynamics of the switch between active and inactive C-src conformation
To be Published
3QLF
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BU of 3qlf by Molmil
Crystal structure of the L317I mutant of the C-src tyrosine kinase domain complexed with pyrazolopyrimidine 5
分子名称: 1-{4-[4-amino-1-(1-methylethyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl]phenyl}-3-[3-(trifluoromethyl)phenyl]urea, Proto-oncogene tyrosine-protein kinase Src
著者Boubeva, R, Pernot, L, Perozzo, R, Scapozza, L.
登録日2011-02-02
公開日2012-02-08
最終更新日2023-09-13
実験手法X-RAY DIFFRACTION (2.75 Å)
主引用文献A single amino-acid dictates the dynamics of the switch between active and inactive C-src conformation
To be Published
3EL7
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BU of 3el7 by Molmil
Crystal structure of c-Src in complex with pyrazolopyrimidine 3
分子名称: 1-{3-[(4-amino-1-cyclopentyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl)methyl]phenyl}-3-[3-(trifluoromethyl)phenyl]urea, Proto-oncogene tyrosine-protein kinase Src
著者Dar, A.C, Lopez, M.S, Shokat, K.M.
登録日2008-09-20
公開日2008-10-28
最終更新日2023-08-30
実験手法X-RAY DIFFRACTION (2.8 Å)
主引用文献Small molecule recognition of c-Src via the Imatinib-binding conformation.
Chem.Biol., 15, 2008
5SYS
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BU of 5sys by Molmil
c-Src V281C bound to N-[3-({6-[(1E)-2-cyano-3-(methylamino)-3-oxoprop-1-en-1-yl]-7-(2-methoxyethyl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl}ethynyl)-4-methylphenyl]-3-(trifluoromethyl)benzamide inhibitor
分子名称: N-[3-({6-[(2S)-2-cyano-3-(methylamino)-3-oxopropyl]-7-(2-methoxyethyl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl}ethynyl)-4-methylphenyl]-3-(trifluoromethyl)benzamide, Proto-oncogene tyrosine-protein kinase Src
著者Dieter, E.M, Merritt, E.A, Maly, D.J.
登録日2016-08-11
公開日2017-08-16
最終更新日2023-10-04
実験手法X-RAY DIFFRACTION (2.8 Å)
主引用文献A combined approach reveals a regulatory mechanism coupling Src's kinase activity, localization, and phosphotransferase-independent functions
Mol.Cell, 2019
3EN7
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BU of 3en7 by Molmil
Targeted polypharmacology: crystal structure of the c-Src kinase domain in complex with S1, a multitargeted kinase inhibitor
分子名称: 3-[4-AMINO-1-(1-METHYLETHYL)-1H-PYRAZOLO[3,4-D]PYRIMIDIN-3-YL]PHENOL, Proto-oncogene tyrosine-protein kinase Src
著者Blair, J.A, Apsel, B, Knight, Z.A, Shokat, K.M.
登録日2008-09-25
公開日2008-10-14
最終更新日2024-02-21
実験手法X-RAY DIFFRACTION (2.81 Å)
主引用文献Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.
Nat.Chem.Biol., 4, 2008
4LGH
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BU of 4lgh by Molmil
Crystal structure of 1NM-PP1 bound to analog-sensitive Src kinase
分子名称: 1-tert-butyl-3-(naphthalen-1-ylmethyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine, Proto-oncogene tyrosine-protein kinase Src
著者Lopez, M.S, Dar, A.C, Shokat, K.M.
登録日2013-06-27
公開日2013-08-07
最終更新日2023-09-20
実験手法X-RAY DIFFRACTION (2.84 Å)
主引用文献Structure-guided inhibitor design expands the scope of analog-sensitive kinase technology.
Acs Chem.Biol., 8, 2013
6L8L
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BU of 6l8l by Molmil
C-Src in complex with ibrutinib
分子名称: 1-{(3R)-3-[4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]piperidin-1-yl}prop-2-en-1-one, Proto-oncogene tyrosine-protein kinase Src
著者Guo, M, Dai, S, Chen, L, Chen, Y.
登録日2019-11-06
公開日2020-11-11
最終更新日2023-11-22
実験手法X-RAY DIFFRACTION (2.888 Å)
主引用文献Characterization of ibrutinib as a non-covalent inhibitor of SRC-family kinases.
Bioorg.Med.Chem.Lett., 34, 2020
3D7T
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BU of 3d7t by Molmil
Structural basis for the recognition of c-Src by its inactivator Csk
分子名称: Proto-oncogene tyrosine-protein kinase Src, STAUROSPORINE, Tyrosine-protein kinase CSK
著者Levinson, N.M, Seeliger, M.A, Cole, P.A, Kuriyan, J.
登録日2008-05-21
公開日2008-08-05
最終更新日2021-10-20
実験手法X-RAY DIFFRACTION (2.899 Å)
主引用文献Structural basis for the recognition of c-Src by its inactivator Csk.
Cell(Cambridge,Mass.), 134, 2008
5TEH
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BU of 5teh by Molmil
c-Src V281C kinase domain in complex with Rao-IV-156
分子名称: (2S)-3-[4-amino-7-(2-methoxyethyl)-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]-2-cyano-N-(propan-2-yl)propanamide, Proto-oncogene tyrosine-protein kinase Src
著者Dieter, E.M, Merritt, E.A, Maly, D.J.
登録日2016-09-21
公開日2017-09-27
最終更新日2023-10-04
実験手法X-RAY DIFFRACTION (2.99 Å)
主引用文献A combined approach reveals a regulatory mechanism coupling Src's kinase activity, localization, and phosphotransferase-independent functions
Mol.Cell, 2019

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