4AN2
 
 | | Crystal structures of human MEK1 with carboxamide-based allosteric inhibitor XL518 (GDC-0973), or related analogs. | | Descriptor: | DUAL SPECIFICITY MITOGEN-ACTIVATED PROTEIN KINASE KINASE 1, MAGNESIUM ION, PHOSPHOMETHYLPHOSPHONIC ACID ADENYLATE ESTER, ... | | Authors: | Rice, K.D, Aay, N, Anand, N.K, Blazey, C.M, Bowles, O.J, Bussenius, J, Costanzo, S, Curtis, J.K, Defina, S.C, Dubenko, L, Engst, S, Joshi, A.A, Kennedy, A.R, Kim, A.I, Koltun, E.S, Lougheed, J.C, Manalo, J.C.L, Martini, J.F, Nuss, J.M, Peto, C.J, Tsang, T.H, Yu, P, Johnston, S. | | Deposit date: | 2012-03-14 | | Release date: | 2012-12-19 | | Last modified: | 2014-06-18 | | Method: | X-RAY DIFFRACTION (2.5 Å) | | Cite: | Novel Carboxamide-Based Allosteric Mek Inhibitors: Discovery and Optimization Efforts Toward Xl518 (Gdc-0973)
Acs Med.Chem.Lett., 3, 2012
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4ANB
 | | Crystal structures of human MEK1 with carboxamide-based allosteric inhibitor XL518 (GDC-0973), or related analogs. | | Descriptor: | DUAL SPECIFICITY MITOGEN-ACTIVATED PROTEIN KINASE KINASE 1, MAGNESIUM ION, PHOSPHOMETHYLPHOSPHONIC ACID ADENYLATE ESTER, ... | | Authors: | Rice, K.D, Aay, N, Anand, N.K, Blazey, C.M, Bowles, O.J, Bussenius, J, Costanzo, S, Curtis, J.K, Defina, S.C, Dubenko, L, Engst, S, Joshi, A.A, Kennedy, A.R, Kim, A.I, Koltun, E.S, Lougheed, J.C, Manalo, J.C.L, Martini, J.F, Nuss, J.M, Peto, C.J, Tsang, T.H, Yu, P, Johnston, S. | | Deposit date: | 2012-03-16 | | Release date: | 2012-12-19 | | Last modified: | 2019-05-08 | | Method: | X-RAY DIFFRACTION (2.2 Å) | | Cite: | Novel Carboxamide-Based Allosteric Mek Inhibitors: Discovery and Optimization Efforts Toward Xl518 (Gdc-0973)
Acs Med.Chem.Lett., 3, 2012
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4AN3
 | | Crystal structures of human MEK1 with carboxamide-based allosteric inhibitor XL518 (GDC-0973), or related analogs. | | Descriptor: | ADENOSINE-5'-TRIPHOSPHATE, DUAL SPECIFICITY MITOGEN-ACTIVATED PROTEIN KINASE KINASE 1, MAGNESIUM ION, ... | | Authors: | Rice, K.D, Aay, N, Anand, N.K, Blazey, C.M, Bowles, O.J, Bussenius, J, Costanzo, S, Curtis, J.K, Defina, S.C, Dubenko, L, Engst, S, Joshi, A.A, Kennedy, A.R, Kim, A.I, Koltun, E.S, Lougheed, J.C, Manalo, J.C.L, Martini, J.F, Nuss, J.M, Peto, C.J, Tsang, T.H, Yu, P, Johnston, S. | | Deposit date: | 2012-03-15 | | Release date: | 2012-12-19 | | Last modified: | 2019-05-08 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | Novel Carboxamide-Based Allosteric Mek Inhibitors: Discovery and Optimization Efforts Toward Xl518 (Gdc-0973)
Acs Med.Chem.Lett., 3, 2012
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4AN9
 | | Crystal structures of human MEK1 with carboxamide-based allosteric inhibitor XL518 (GDC-0973), or related analogs. | | Descriptor: | DUAL SPECIFICITY MITOGEN-ACTIVATED PROTEIN KINASE KINASE 1, MAGNESIUM ION, PHOSPHOMETHYLPHOSPHONIC ACID ADENYLATE ESTER, ... | | Authors: | Rice, K.D, Aay, N, Anand, N.K, Blazey, C.M, Bowles, O.J, Bussenius, J, Costanzo, S, Curtis, J.K, Defina, S.C, Dubenko, L, Engst, S, Joshi, A.A, Kennedy, A.R, Kim, A.I, Koltun, E.S, Lougheed, J.C, Manalo, J.C.L, Martini, J.F, Nuss, J.M, Peto, C.J, Tsang, T.H, Yu, P, Johnston, S. | | Deposit date: | 2012-03-16 | | Release date: | 2012-12-19 | | Last modified: | 2019-05-08 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | Novel Carboxamide-Based Allosteric Mek Inhibitors: Discovery and Optimization Efforts Toward Xl518 (Gdc-0973)
Acs Med.Chem.Lett., 3, 2012
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3LQ8
 | | Structure of the kinase domain of c-Met bound to XL880 (GSK1363089) | | Descriptor: | Hepatocyte growth factor receptor, N-(3-fluoro-4-{[6-methoxy-7-(3-morpholin-4-ylpropoxy)quinolin-4-yl]oxy}phenyl)-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide | | Authors: | Lougheed, J.C, Stout, T.J. | | Deposit date: | 2010-02-08 | | Release date: | 2010-05-19 | | Last modified: | 2024-04-03 | | Method: | X-RAY DIFFRACTION (2.02 Å) | | Cite: | Inhibition of tumor cell growth, invasion, and metastasis by EXEL-2880 (XL880, GSK1363089), a novel inhibitor of HGF and VEGF receptor tyrosine kinases.
Cancer Res., 69, 2009
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4ANM
 | | Complex of CK2 with a CDC7 inhibitor | | Descriptor: | 8-BROMANYL-2-[[(3S)-3-OXIDANYLPYRROLIDIN-1-YL]METHYL]-3H-[1]BENZOFURO[3,2-D]PYRIMIDIN-4-ONE, CASEIN KINASE II SUBUNIT ALPHA | | Authors: | Stout, T.J. | | Deposit date: | 2012-03-20 | | Release date: | 2012-05-23 | | Method: | X-RAY DIFFRACTION (1.7 Å) | | Cite: | Discovery of Xl413, a Potent and Selective Cdc7 Inhibitor.
Bioorg.Med.Chem.Lett., 22, 2012
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4ALW
 | | Benzofuropyrimidinone Inhibitors of Pim-1 | | Descriptor: | 8-BROMANYL-2-[(4-METHYLPIPERAZIN-1-YL)METHYL]-3H-[1]BENZOFURO[3,2-D]PYRIMIDIN-4-ONE, IMIDAZOLE, PIM-1 KINASE | | Authors: | Stout, T.J, Adams, L. | | Deposit date: | 2012-03-05 | | Release date: | 2013-01-16 | | Method: | X-RAY DIFFRACTION (1.92 Å) | | Cite: | The Design, Synthesis, and Biological Evaluation of Pim Kinase Inhibitors.
Bioorg.Med.Chem.Lett., 22, 2012
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4ALU
 | | Benzofuropyrimidinone Inhibitors of Pim-1 | | Descriptor: | 8-bromo-2-(2-chlorophenyl)[1]benzofuro[3,2-d]pyrimidin-4(3H)-one, IMIDAZOLE, SERINE/THREONINE-PROTEIN KINASE PIM-1 | | Authors: | Stout, T.J, Adams, L. | | Deposit date: | 2012-03-05 | | Release date: | 2013-01-16 | | Last modified: | 2017-06-28 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | The Design, Synthesis, and Biological Evaluation of Pim Kinase Inhibitors.
Bioorg.Med.Chem.Lett., 22, 2012
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4ALV
 | | Benzofuropyrimidinone Inhibitors of Pim-1 | | Descriptor: | 8-bromo-2-{2-chloro-4-[(piperidin-4-ylmethyl)amino]phenyl}[1]benzofuro[3,2-d]pyrimidin-4(3H)-one, IMIDAZOLE, SERINE/THREONINE-PROTEIN KINASE PIM-1 | | Authors: | Stout, T.J, Adams, L. | | Deposit date: | 2012-03-05 | | Release date: | 2013-01-16 | | Method: | X-RAY DIFFRACTION (2.59 Å) | | Cite: | The Design, Synthesis, and Biological Evaluation of Pim Kinase Inhibitors.
Bioorg.Med.Chem.Lett., 22, 2012
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4BBE
 | | Aminoalkylpyrimidine Inhibitor Complexes with JAK2 | | Descriptor: | N-[4-[2-[(4-morpholin-4-ylphenyl)amino]pyrimidin-4-yl]phenyl]ethanamide, TYROSINE-PROTEIN KINASE JAK2 | | Authors: | Li, J. | | Deposit date: | 2012-09-21 | | Release date: | 2012-11-21 | | Last modified: | 2012-12-19 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Sar and in Vivo Evaluation of 4-Aryl-2-Aminoalkylpyrimidines as Potent and Selective Janus Kinase 2 (Jak2) Inhibitors
Bioorg.Med.Chem.Lett., 22, 2012
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4BBF
 | | Aminoalkylpyrimidine Inhibitor Complexes with JAK2 | | Descriptor: | (2R)-N-[4-[2-[(4-morpholin-4-ylphenyl)amino]pyrimidin-4-yl]phenyl]pyrrolidine-2-carboxamide, TYROSINE-PROTEIN KINASE JAK2 | | Authors: | Li, J. | | Deposit date: | 2012-09-21 | | Release date: | 2012-11-21 | | Last modified: | 2017-06-28 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Sar and in Vivo Evaluation of 4-Aryl-2-Aminoalkylpyrimidines as Potent and Selective Janus Kinase 2 (Jak2) Inhibitors
Bioorg.Med.Chem.Lett., 22, 2012
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4AW5
 | | Complex of the EphB4 kinase domain with an oxindole inhibitor | | Descriptor: | (3Z)-5-[(1-ethylpiperidin-4-yl)amino]-3-[(5-methoxy-1H-benzimidazol-2-yl)(phenyl)methylidene]-1,3-dihydro-2H-indol-2-one, EPHRIN TYPE-B RECEPTOR 4 | | Authors: | Till, J.H, Stout, T.J. | | Deposit date: | 2012-05-31 | | Release date: | 2012-08-01 | | Method: | X-RAY DIFFRACTION (2.33 Å) | | Cite: | The Design, Synthesis, and Biological Evaluation of Potent Receptor Tyrosine Kinase Inhibitors.
Bioorg.Med.Chem.Lett., 22, 2012
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