3OMV
 
 | | Crystal structure of c-raf (raf-1) | | Descriptor: | (1E)-5-(1-piperidin-4-yl-3-pyridin-4-yl-1H-pyrazol-4-yl)-2,3-dihydro-1H-inden-1-one oxime, RAF proto-oncogene serine/threonine-protein kinase | | Authors: | Hatzivassiliou, G, Song, K, Yen, I, Brandhuber, B.J, Anderson, D.J, Alvarado, R, Ludlam, M.J, Stokoe, D, Gloor, S.L, Vigers, G.P.A, Morales, T, Aliagas, I, Liu, B, Sideris, S, Hoeflich, K.P, Jaiswal, B.S, Seshagiri, S, Koeppen, H, Belvin, M, Friedman, L.S, Malek, S. | | Deposit date: | 2010-08-27 | | Release date: | 2010-09-15 | | Last modified: | 2023-09-06 | | Method: | X-RAY DIFFRACTION (4 Å) | | Cite: | RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth.
Nature, 464, 2010
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3O96
 | | Crystal Structure of Human AKT1 with an Allosteric Inhibitor | | Descriptor: | 1-(1-(4-(7-phenyl-1H-imidazo[4,5-g]quinoxalin-6-yl)benzyl)piperidin-4-yl)-1H-benzo[d]imidazol-2(3H)-one, RAC-alpha serine/threonine-protein kinase | | Authors: | Voegtli, W.C, Wu, W.-I, Lord-Ondash, H.A, Dizon, F.P, Vigers, G.P.A, Brandhuber, B.J. | | Deposit date: | 2010-08-03 | | Release date: | 2010-10-13 | | Last modified: | 2023-09-06 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | Crystal structure of human AKT1 with an allosteric inhibitor reveals a new mode of kinase inhibition.
Plos One, 5, 2010
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3PRF
 | | Crystal Structure of Human B-Raf Kinase Domain in Complex with a Non-Oxime Furopyridine Inhibitor | | Descriptor: | 2-chloro-5-{[2-(pyrimidin-2-yl)furo[2,3-c]pyridin-3-yl]amino}phenol, Serine/threonine-protein kinase B-raf | | Authors: | Voegtli, W.C, Vigers, G.P.A, Morales, T, Brandhuber, B.J. | | Deposit date: | 2010-11-29 | | Release date: | 2011-02-02 | | Last modified: | 2024-02-21 | | Method: | X-RAY DIFFRACTION (2.9 Å) | | Cite: | Non-oxime inhibitors of B-Raf(V600E) kinase.
Bioorg.Med.Chem.Lett., 21, 2011
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3PRI
 | | Crystal Structure of Human B-Raf Kinase in Complex with a Non-Oxime Furopyridine Inhibitor | | Descriptor: | 3-(4-{[2-(pyrimidin-2-yl)furo[2,3-c]pyridin-3-yl]amino}-1H-indazol-3-yl)propan-1-ol, Serine/threonine-protein kinase B-raf | | Authors: | Voegtli, W.C, Vigers, G.P.A, Morales, T, Brandhuber, B.J. | | Deposit date: | 2010-11-29 | | Release date: | 2011-02-02 | | Last modified: | 2024-02-21 | | Method: | X-RAY DIFFRACTION (3.5 Å) | | Cite: | Non-oxime inhibitors of B-Raf(V600E) kinase.
Bioorg.Med.Chem.Lett., 21, 2011
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3PSD
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3PPK
 | | Human B-Raf Kinase in Complex with a Non-Oxime Furopyridine Inhibitor | | Descriptor: | 3-[(5-hydroxynaphthalen-2-yl)amino]-N-(pyrimidin-4-yl)furo[2,3-c]pyridine-2-carboxamide, Serine/threonine-protein kinase B-raf | | Authors: | Voegtli, W.C, Vigers, G.P.A, Morales, T, Brandhuber, B.J. | | Deposit date: | 2010-11-24 | | Release date: | 2011-02-02 | | Last modified: | 2024-02-21 | | Method: | X-RAY DIFFRACTION (3 Å) | | Cite: | Non-oxime inhibitors of B-Raf(V600E) kinase.
Bioorg.Med.Chem.Lett., 21, 2011
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3PPJ
 | | Human B-Raf Kinase in Complex with a Furopyridine Inhibitor | | Descriptor: | Serine/threonine-protein kinase B-raf, methyl 3-{[(5S)-1-(hydroxyamino)-5H-inden-5-yl]amino}furo[2,3-c]pyridine-2-carboxylate | | Authors: | Voegtli, W.C, Vigers, G.P.A, Morales, T, Brandhuber, B.J. | | Deposit date: | 2010-11-24 | | Release date: | 2011-02-02 | | Last modified: | 2024-02-21 | | Method: | X-RAY DIFFRACTION (3.7 Å) | | Cite: | Non-oxime inhibitors of B-Raf(V600E) kinase.
Bioorg.Med.Chem.Lett., 21, 2011
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3PSB
 | | Furo[2,3-c]pyridine-based Indanone Oximes as Potent and Selective B-Raf Inhibitors | | Descriptor: | B-RAF PROTO-ONCOGENE SERINE/THREONINE-PROTEIN KINASE, ethyl 3-{[1-(hydroxyamino)-2H-inden-5-yl]amino}thieno[2,3-c]pyridine-2-carboxylate | | Authors: | Morales, T, Vigers, G.P.A, Brandhuber, B.J. | | Deposit date: | 2010-12-01 | | Release date: | 2011-01-19 | | Last modified: | 2023-09-06 | | Method: | X-RAY DIFFRACTION (3.4 Å) | | Cite: | The Discovery of furo[2,3-c]pyridine-based indanone oximes as potent and selective B-Raf inhibitors.
Bioorg.Med.Chem.Lett., 21, 2011
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3QKL
 | | Spirochromane Akt Inhibitors | | Descriptor: | GSK-3 beta peptide, N-{(2S)-3-[(3S)-8',9'-dihydro-1H,3'H-spiro[piperidine-3,7'-pyrano[3,2-e]indazol]-1-yl]-2-hydroxypropyl}-N-(2-ethoxyethyl)-2,6-dimethylbenzenesulfonamide, RAC-alpha serine/threonine-protein kinase | | Authors: | Kallan, N.C, Spencer, K.L, Blake, J.F, Xu, R, Heizer, J, Bencsik, J.R, Mitchell, I.S, Gloor, S.L, Martinson, M, Risom, T, Gross, S.D, Morales, T, Vigers, G.P.A, Brandhuber, B.J, Skelton, N.J. | | Deposit date: | 2011-02-01 | | Release date: | 2011-03-30 | | Last modified: | 2011-07-13 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Discovery and SAR of spirochromane Akt inhibitors.
Bioorg.Med.Chem.Lett., 21, 2011
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4RCH
 | | Discovery of 2-Pyridyl Ureas as Glucokinase Activators | | Descriptor: | 1-{3-[(2-ethylpyridin-3-yl)oxy]-5-(pyridin-2-ylsulfanyl)pyridin-2-yl}-3-methylurea, Glucokinase, alpha-D-glucopyranose | | Authors: | Voegtli, W, Vigers, G.P.A. | | Deposit date: | 2014-09-16 | | Release date: | 2014-10-08 | | Last modified: | 2023-09-20 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Discovery of 2-pyridylureas as glucokinase activators.
J.Med.Chem., 57, 2014
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