4PP7
 
 | | Highly Potent and Selective 3-N-methylquinazoline-4(3H)-one Based Inhibitors of B-RafV600E Kinase | | Descriptor: | N-{2,4-difluoro-3-[methyl(3-methyl-4-oxo-3,4-dihydroquinazolin-6-yl)amino]phenyl}propane-1-sulfonamide, Serine/threonine-protein kinase B-raf | | Authors: | Wenglowsky, S, Ren, L, Grina, J, Hansen, J.D, Laird, E.R, Moreno, D, Dinkel, V, Gloor, S.L, Hastings, G, Rana, S, Rasor, K, Sturgis, H.L, Voegtli, W.C, Vigers, G.P.A, Willis, B, Mathieu, S, Rudolph, J. | | Deposit date: | 2014-02-26 | | Release date: | 2014-04-09 | | Last modified: | 2024-02-28 | | Method: | X-RAY DIFFRACTION (3.4 Å) | | Cite: | Highly potent and selective 3-N-methylquinazoline-4(3H)-one based inhibitors of B-Raf(V600E) kinase.
Bioorg.Med.Chem.Lett., 24, 2014
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3SKC
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3TV6
 | | Human B-Raf Kinase Domain in Complex with a Methoxypyrazolopyridinyl Benzamide Inhibitor | | Descriptor: | 2,6-difluoro-N-(3-methoxy-2H-pyrazolo[3,4-b]pyridin-5-yl)-3-[(propylsulfonyl)amino]benzamide, Serine/threonine-protein kinase B-raf | | Authors: | Voegtli, W.C, Sturgis, H.L, Wu, W.-I. | | Deposit date: | 2011-09-19 | | Release date: | 2011-10-05 | | Last modified: | 2024-02-28 | | Method: | X-RAY DIFFRACTION (3.3 Å) | | Cite: | Pyrazolopyridine Inhibitors of B-Raf(V600E). Part 1: The Development of Selective, Orally Bioavailable, and Efficacious Inhibitors.
ACS Med Chem Lett, 2, 2011
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4E4X
 | | Crystal Structure of B-Raf Kinase Domain in Complex with a Dihydropyrido[2,3-d]pyrimidinone-based Inhibitor | | Descriptor: | N-(2,4-difluoro-3-{2-[(3-hydroxypropyl)amino]-8-methyl-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-6-yl}phenyl)propane-1-sulfonamide, Serine/threonine-protein kinase B-raf | | Authors: | Voegtli, W.C, Sturgis, H.L. | | Deposit date: | 2012-03-13 | | Release date: | 2012-05-09 | | Last modified: | 2024-02-28 | | Method: | X-RAY DIFFRACTION (3.6 Å) | | Cite: | The discovery of potent and selective pyridopyrimidin-7-one based inhibitors of B-Raf(V600E) kinase.
Bioorg.Med.Chem.Lett., 22, 2012
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4G9R
 | | B-Raf V600E Kinase Domain Bound to a Type II Dihydroquinazoline Inhibitor | | Descriptor: | 3-(2-cyanopropan-2-yl)-N-{4-methyl-3-[(3-methyl-4-oxo-3,4-dihydroquinazolin-6-yl)amino]phenyl}benzamide, Serine/threonine-protein kinase B-raf | | Authors: | Voegtli, W.C, Sturgis, H.L. | | Deposit date: | 2012-07-24 | | Release date: | 2012-11-14 | | Last modified: | 2024-02-28 | | Method: | X-RAY DIFFRACTION (3.2 Å) | | Cite: | Pyrazolopyridine inhibitors of B-Raf(V600E). Part 4: Rational design and kinase selectivity profile of cell potent type II inhibitors.
Bioorg.Med.Chem.Lett., 22, 2012
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4G9C
 | | Human B-Raf Kinase Domain bound to a Type II Pyrazolopyridine Inhibitor | | Descriptor: | 3-{[3-(2-cyanopropan-2-yl)benzoyl]amino}-2,6-difluoro-N-(3-methoxy-2H-pyrazolo[3,4-b]pyridin-5-yl)benzamide, Serine/threonine-protein kinase B-raf | | Authors: | Voegtli, W.C, Sturgis, H.L. | | Deposit date: | 2012-07-23 | | Release date: | 2012-11-14 | | Last modified: | 2024-02-28 | | Method: | X-RAY DIFFRACTION (3.5 Å) | | Cite: | Pyrazolopyridine inhibitors of B-Raf(V600E). Part 4: Rational design and kinase selectivity profile of cell potent type II inhibitors.
Bioorg.Med.Chem.Lett., 22, 2012
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