6U2H
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![BU of 6u2h by Molmil](/molmil-images/mine/6u2h) | BRAF dimer bound to 14-3-3 | Descriptor: | 14-3-3 protein zeta/delta, 2-{4-[(1E)-1-(hydroxyimino)-2,3-dihydro-1H-inden-5-yl]-3-(pyridin-4-yl)-1H-pyrazol-1-yl}ethanol, Serine/threonine-protein kinase B-raf | Authors: | Liau, N.P.D, Hymowitz, S.G, Sudhamsu, J. | Deposit date: | 2019-08-19 | Release date: | 2019-08-28 | Last modified: | 2023-10-11 | Method: | X-RAY DIFFRACTION (2.5 Å) | Cite: | Negative regulation of RAF kinase activity by ATP is overcome by 14-3-3-induced dimerization. Nat.Struct.Mol.Biol., 27, 2020
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5HID
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![BU of 5hid by Molmil](/molmil-images/mine/5hid) | BRAF Kinase domain b3aC loop deletion mutant in complex with AZ628 | Descriptor: | 3-(2-cyanopropan-2-yl)-N-{4-methyl-3-[(3-methyl-4-oxo-3,4-dihydroquinazolin-6-yl)amino]phenyl}benzamide, DI(HYDROXYETHYL)ETHER, Serine/threonine-protein kinase B-raf | Authors: | Whalen, D.M, Foster, S.A, Ozen, A, Wongchenko, M, Yin, J, Schaefer, G, Mayfield, J, Chmielecki, J, Stephens, P, Albacker, L, Yan, Y, Song, K, Hatzivassiliou, G, Eigenbrot, C, Yu, C, Shaw, A.S, Manning, G, Skelton, N.J, Hymowitz, S.G, Malek, S. | Deposit date: | 2016-01-11 | Release date: | 2016-04-06 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (2.5 Å) | Cite: | Activation Mechanism of Oncogenic Deletion Mutations in BRAF, EGFR, and HER2. Cancer Cell, 29, 2016
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4XV2
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![BU of 4xv2 by Molmil](/molmil-images/mine/4xv2) | |
5CSX
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![BU of 5csx by Molmil](/molmil-images/mine/5csx) | CRYSTAL STRUCTURE OF B-RAF IN COMPLEX WITH BI 882370 | Descriptor: | N-(3-{5-[(1-ethylpiperidin-4-yl)(methyl)amino]-3-(pyrimidin-5-yl)-1H-pyrrolo[3,2-b]pyridin-1-yl}-2,4-difluorophenyl)propane-1-sulfonamide, Serine/threonine-protein kinase B-raf, alpha-D-glucopyranose | Authors: | Bader, G, Stadtmuller, H, Steurer, S. | Deposit date: | 2015-07-23 | Release date: | 2016-03-09 | Last modified: | 2024-01-10 | Method: | X-RAY DIFFRACTION (2.51 Å) | Cite: | A Novel RAF Kinase Inhibitor with DFG-Out-Binding Mode: High Efficacy in BRAF-Mutant Tumor Xenograft Models in the Absence of Normal Tissue Hyperproliferation. Mol.Cancer Ther., 15, 2016
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5HI2
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![BU of 5hi2 by Molmil](/molmil-images/mine/5hi2) | BRAF Kinase domain b3aC loop deletion mutant in complex with sorafenib | Descriptor: | 4-{4-[({[4-CHLORO-3-(TRIFLUOROMETHYL)PHENYL]AMINO}CARBONYL)AMINO]PHENOXY}-N-METHYLPYRIDINE-2-CARBOXAMIDE, Serine/threonine-protein kinase B-raf | Authors: | Whalen, D.M, Foster, S.A, Ozen, A, Wongchenko, M, Yin, J, Schaefer, G, Mayfield, J, Chmielecki, J, Stephens, P, Albacker, L, Yan, Y, Song, K, Hatzivassiliou, G, Eigenbrot, C, Yu, C, Shaw, A.S, Manning, G, Skelton, N.J, Hymowitz, S.G, Malek, S. | Deposit date: | 2016-01-11 | Release date: | 2016-04-06 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (2.512 Å) | Cite: | Activation Mechanism of Oncogenic Deletion Mutations in BRAF, EGFR, and HER2. Cancer Cell, 29, 2016
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4E26
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![BU of 4e26 by Molmil](/molmil-images/mine/4e26) | BRAF in complex with an organic inhibitor 7898734 | Descriptor: | 5-chloro-7-[(R)-furan-2-yl(pyridin-2-ylamino)methyl]quinolin-8-ol, Serine/threonine-protein kinase B-raf | Authors: | Qin, J, Xie, P, Ventocilla, C, Zhou, G, Vultur, A, Chen, Q, Herlyn, M, Winkler, J, Marmorstein, R. | Deposit date: | 2012-03-07 | Release date: | 2012-05-09 | Last modified: | 2024-02-28 | Method: | X-RAY DIFFRACTION (2.55 Å) | Cite: | Identification of a Novel Family of BRAF(V600E) Inhibitors. J.Med.Chem., 55, 2012
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6CAD
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![BU of 6cad by Molmil](/molmil-images/mine/6cad) | Crystal structure of RAF kinase domain bound to the inhibitor 2a | Descriptor: | 1-(propan-2-yl)-3-({3-[3-(trifluoromethyl)phenyl]isoquinolin-8-yl}ethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine, Serine/threonine-protein kinase B-raf | Authors: | Maisonneuve, P, Kurinov, I, Assadieskandar, A, Yu, C, Liu, X, Chen, Y.-C, Prakash, G.K.S, Zhang, C, SIcheri, F. | Deposit date: | 2018-01-30 | Release date: | 2018-02-21 | Last modified: | 2023-10-04 | Method: | X-RAY DIFFRACTION (2.55 Å) | Cite: | Effects of rigidity on the selectivity of protein kinase inhibitors. Eur J Med Chem, 146, 2018
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3C4C
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![BU of 3c4c by Molmil](/molmil-images/mine/3c4c) | B-Raf Kinase in Complex with PLX4720 | Descriptor: | B-Raf proto-oncogene serine/threonine-protein kinase, N-{3-[(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)carbonyl]-2,4-difluorophenyl}propane-1-sulfonamide | Authors: | Zhang, K.Y.J, Wang, W. | Deposit date: | 2008-01-29 | Release date: | 2008-02-26 | Last modified: | 2024-02-21 | Method: | X-RAY DIFFRACTION (2.57 Å) | Cite: | Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity Proc.Natl.Acad.Sci.Usa, 105, 2008
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6PP9
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![BU of 6pp9 by Molmil](/molmil-images/mine/6pp9) | Crystal structure of BRAF:MEK1 complex | Descriptor: | 5-[(2-fluoro-4-iodophenyl)amino]-N-(2-hydroxyethoxy)imidazo[1,5-a]pyridine-6-carboxamide, CHLORIDE ION, Dual specificity mitogen-activated protein kinase kinase 1, ... | Authors: | Li, K, Gonzalez Del-Pino, G, Park, E, Eck, M.J. | Deposit date: | 2019-07-05 | Release date: | 2019-10-09 | Last modified: | 2023-10-11 | Method: | X-RAY DIFFRACTION (2.59 Å) | Cite: | Architecture of autoinhibited and active BRAF-MEK1-14-3-3 complexes. Nature, 575, 2019
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6P7G
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![BU of 6p7g by Molmil](/molmil-images/mine/6p7g) | The co-crystal structure of BRAF(V600E) with PHI1 | Descriptor: | 2-[N-CYCLOHEXYLAMINO]ETHANE SULFONIC ACID, 3-[(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-[4-({[2-(morpholin-4-yl)ethyl]amino}methyl)-3-(trifluoromethyl)phenyl]benzamide, Serine/threonine-protein kinase B-raf | Authors: | Agianian, B, Gavathiotis, E. | Deposit date: | 2019-06-05 | Release date: | 2020-09-23 | Last modified: | 2024-03-13 | Method: | X-RAY DIFFRACTION (2.65 Å) | Cite: | Inhibitors of BRAF dimers using an allosteric site. Nat Commun, 11, 2020
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4FK3
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![BU of 4fk3 by Molmil](/molmil-images/mine/4fk3) | B-Raf Kinase V600E Oncogenic Mutant in Complex with PLX3203 | Descriptor: | N-{2,4-difluoro-3-[(5-pyridin-3-yl-1H-pyrrolo[2,3-b]pyridin-3-yl)carbonyl]phenyl}ethanesulfonamide, Serine/threonine-protein kinase B-raf | Authors: | Zhang, Y, Wang, W, Zhang, K.Y.J. | Deposit date: | 2012-06-12 | Release date: | 2012-08-08 | Last modified: | 2024-02-28 | Method: | X-RAY DIFFRACTION (2.65 Å) | Cite: | Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity. Proc.Natl.Acad.Sci.USA, 105, 2008
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5CSW
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![BU of 5csw by Molmil](/molmil-images/mine/5csw) | B-RAF in complex with Dabrafenib | Descriptor: | CHLORIDE ION, Dabrafenib, Serine/threonine-protein kinase B-raf | Authors: | Bader, G, Stadtmuller, H, Steurer, S. | Deposit date: | 2015-07-23 | Release date: | 2016-03-09 | Last modified: | 2024-01-10 | Method: | X-RAY DIFFRACTION (2.66 Å) | Cite: | A Novel RAF Kinase Inhibitor with DFG-Out-Binding Mode: High Efficacy in BRAF-Mutant Tumor Xenograft Models in the Absence of Normal Tissue Hyperproliferation. Mol.Cancer Ther., 15, 2016
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6B8U
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![BU of 6b8u by Molmil](/molmil-images/mine/6b8u) | Crystals Structure of B-Raf kinase domain in complex with an Imidazopyridinyl benzamide inhibitor | Descriptor: | Serine/threonine-protein kinase B-raf, ~{N}-[3-(2-acetamidoimidazo[1,2-a]pyridin-6-yl)-4-methyl-phenyl]-3-(trifluoromethyl)benzamide | Authors: | Appleton, B.A, Murray, J, Shafer, C.M. | Deposit date: | 2017-10-09 | Release date: | 2017-11-22 | Last modified: | 2023-10-04 | Method: | X-RAY DIFFRACTION (2.68 Å) | Cite: | Imidazo[1,2-a]pyridin-6-yl-benzamide analogs as potent RAF inhibitors. Bioorg. Med. Chem. Lett., 27, 2017
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3IDP
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![BU of 3idp by Molmil](/molmil-images/mine/3idp) | B-Raf V600E kinase domain in complex with an aminoisoquinoline inhibitor | Descriptor: | B-Raf proto-oncogene serine/threonine-protein kinase, N~1~-(4-chlorophenyl)-6-methyl-N~5~-[3-(7H-purin-6-yl)pyridin-2-yl]isoquinoline-1,5-diamine | Authors: | Whittington, D.A, Epstein, L.F. | Deposit date: | 2009-07-21 | Release date: | 2009-10-06 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (2.7 Å) | Cite: | Selective inhibitors of the mutant B-raf pathway: discovery of a potent and orally bioavailable aminoisoquinoline. J.Med.Chem., 52, 2009
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5C9C
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![BU of 5c9c by Molmil](/molmil-images/mine/5c9c) | CRYSTAL STRUCTURE OF BRAF(V600E) IN COMPLEX WITH LY3009120 COMPND | Descriptor: | 1-(3,3-dimethylbutyl)-3-{2-fluoro-4-methyl-5-[7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl]phenyl}urea, CHLORIDE ION, Serine/threonine-protein kinase B-raf | Authors: | Edwards, T, Abendroth, J, Chun, L. | Deposit date: | 2015-06-26 | Release date: | 2015-07-15 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (2.7 Å) | Cite: | Inhibition of RAF Isoforms and Active Dimers by LY3009120 Leads to Anti-tumor Activities in RAS or BRAF Mutant Cancers. Cancer Cell, 28, 2015
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5JT2
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![BU of 5jt2 by Molmil](/molmil-images/mine/5jt2) | BRAFV600E Kinase Domain In Complex with Chemically Linked Vemurafenib Inhibitor VEM-BISAMIDE | Descriptor: | 2,2'-oxybis(N-{[4-(3-{2,6-difluoro-3-[(propane-1-sulfonyl)amino]benzoyl}-1H-pyrrolo[2,3-b]pyridin-5-yl)phenyl]methyl}acetamide), BENZAMIDINE, Serine/threonine-protein kinase B-raf | Authors: | Grasso, M.J, Marmorstein, R. | Deposit date: | 2016-05-09 | Release date: | 2016-09-14 | Last modified: | 2023-10-18 | Method: | X-RAY DIFFRACTION (2.702 Å) | Cite: | Chemically Linked Vemurafenib Inhibitors Promote an Inactive BRAF(V600E) Conformation. Acs Chem.Biol., 11, 2016
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8F7P
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![BU of 8f7p by Molmil](/molmil-images/mine/8f7p) | BRAF kinase in complex with LXH254 (naporafenib) | Descriptor: | N-{3-[2-(2-hydroxyethoxy)-6-(morpholin-4-yl)pyridin-4-yl]-4-methylphenyl}-2-(trifluoromethyl)pyridine-4-carboxamide, Serine/threonine-protein kinase B-raf | Authors: | Tkacik, E, Li, K, Gonzalez Del-Pino, G, Eck, M.J. | Deposit date: | 2022-11-20 | Release date: | 2023-04-12 | Last modified: | 2024-05-22 | Method: | X-RAY DIFFRACTION (2.74 Å) | Cite: | Structure and RAF family kinase isoform selectivity of type II RAF inhibitors tovorafenib and naporafenib. J.Biol.Chem., 299, 2023
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3II5
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![BU of 3ii5 by Molmil](/molmil-images/mine/3ii5) | The Complex of wild-type B-RAF with Pyrazolo pyrimidine inhibitor | Descriptor: | B-Raf proto-oncogene serine/threonine-protein kinase, N-[3-(3-{4-[(dimethylamino)methyl]phenyl}pyrazolo[1,5-a]pyrimidin-7-yl)phenyl]-3-(trifluoromethyl)benzamide, PHOSPHATE ION | Authors: | Xu, W, Breger, D, Torres, N, Dutia, M, Powell, D, Ciszewski, G. | Deposit date: | 2009-07-31 | Release date: | 2009-11-10 | Last modified: | 2024-02-21 | Method: | X-RAY DIFFRACTION (2.79 Å) | Cite: | Non-hinge-binding pyrazolo[1,5-a]pyrimidines as potent B-Raf kinase inhibitors. Bioorg.Med.Chem.Lett., 19, 2009
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3D4Q
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![BU of 3d4q by Molmil](/molmil-images/mine/3d4q) | Pyrazole-based inhibitors of B-Raf kinase | Descriptor: | (1E)-5-(1-piperidin-4-yl-3-pyridin-4-yl-1H-pyrazol-4-yl)-2,3-dihydro-1H-inden-1-one oxime, B-Raf proto-oncogene serine/threonine-protein kinase | Authors: | Morales, T, Vigers, G.P.A, Brandhuber, B.J. | Deposit date: | 2008-05-14 | Release date: | 2008-08-19 | Last modified: | 2024-02-21 | Method: | X-RAY DIFFRACTION (2.8 Å) | Cite: | Potent and selective pyrazole-based inhibitors of B-Raf kinase. Bioorg.Med.Chem.Lett., 18, 2008
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4XV3
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![BU of 4xv3 by Molmil](/molmil-images/mine/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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4MNF
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![BU of 4mnf by Molmil](/molmil-images/mine/4mnf) | Crystal structure of BRAF-V600E bound to GDC0879 | Descriptor: | 2-{4-[(1E)-1-(hydroxyimino)-2,3-dihydro-1H-inden-5-yl]-3-(pyridin-4-yl)-1H-pyrazol-1-yl}ethanol, CHLORIDE ION, Serine/threonine-protein kinase B-raf | Authors: | Sudhamsu, J, Haling, J.R, Morales, T, Brandhuber, B, Hymowitz, S.G. | Deposit date: | 2013-09-10 | Release date: | 2014-06-18 | Last modified: | 2023-09-20 | Method: | X-RAY DIFFRACTION (2.802 Å) | Cite: | Structure of the BRAF-MEK Complex Reveals a Kinase Activity Independent Role for BRAF in MAPK Signaling. Cancer Cell, 26, 2014
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4WO5
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![BU of 4wo5 by Molmil](/molmil-images/mine/4wo5) | Crystal structure of a BRAF kinase domain monomer | Descriptor: | N-{3-[(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)carbonyl]-2,4-difluorophenyl}propane-1-sulfonamide, Serine/threonine-protein kinase B-raf | Authors: | Critton, D.A. | Deposit date: | 2014-10-15 | Release date: | 2014-12-03 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (2.83 Å) | Cite: | Crystal structure of a BRAF kinase domain monomer explains basis for allosteric regulation. Nat.Struct.Mol.Biol., 22, 2015
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4MNE
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![BU of 4mne by Molmil](/molmil-images/mine/4mne) | Crystal structure of the BRAF:MEK1 complex | Descriptor: | 7-fluoro-3-[(2-fluoro-4-iodophenyl)amino]-N-{[(2S)-2-hydroxypropyl]oxy}furo[3,2-c]pyridine-2-carboxamide, CHLORIDE ION, Dual specificity mitogen-activated protein kinase kinase 1, ... | Authors: | Sudhamsu, J, Haling, J.R, Morales, T, Brandhuber, B, Hymowitz, S.G. | Deposit date: | 2013-09-10 | Release date: | 2014-06-18 | Last modified: | 2023-09-20 | Method: | X-RAY DIFFRACTION (2.8483 Å) | Cite: | Structure of the BRAF-MEK Complex Reveals a Kinase Activity Independent Role for BRAF in MAPK Signaling. Cancer Cell, 26, 2014
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7SHV
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![BU of 7shv by Molmil](/molmil-images/mine/7shv) | Crystal structure of BRAF kinase domain bound to GDC0879 | Descriptor: | 2-{4-[(1E)-1-(hydroxyimino)-2,3-dihydro-1H-inden-5-yl]-3-(pyridin-4-yl)-1H-pyrazol-1-yl}ethanol, CHLORIDE ION, Serine/threonine-protein kinase B-raf | Authors: | Kung, J.E, Sudhamsu, J. | Deposit date: | 2021-10-11 | Release date: | 2022-10-26 | Last modified: | 2023-10-18 | Method: | X-RAY DIFFRACTION (2.88 Å) | Cite: | Clearing the Path to Rapid High-Quality Protein Purification To Be Published
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6U2G
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![BU of 6u2g by Molmil](/molmil-images/mine/6u2g) | BRAF-MEK complex with AMP-PCP bound to BRAF | Descriptor: | Dual specificity mitogen-activated protein kinase kinase 1, MAGNESIUM ION, PHOSPHOMETHYLPHOSPHONIC ACID ADENYLATE ESTER, ... | Authors: | Liau, N.P.D, Wendorff, T, Hymowitz, S, Sudhamsu, J. | Deposit date: | 2019-08-19 | Release date: | 2019-08-28 | Last modified: | 2023-10-11 | Method: | X-RAY DIFFRACTION (2.886 Å) | Cite: | Negative regulation of RAF kinase activity by ATP is overcome by 14-3-3-induced dimerization. Nat.Struct.Mol.Biol., 27, 2020
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