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Nature, ISSN 0028-0836, 03/2010, Volume 464, Issue 7287, pp. 431 - 435
Activating mutations in KRAS and BRAF are found in more than 30% of all human tumours and 40% of melanoma, respectively, thus targeting this pathway could have... 
SELECTIVE INHIBITOR | POTENT | EFFICACY | PHOSPHORYLATION | MULTIDISCIPLINARY SCIENCES | IN-VIVO | C-RAF | HETERODIMERIZATION | B-RAF | PROTEIN-KINASE KINASE | CANCER | Neoplasms - metabolism | ras Proteins - genetics | Proto-Oncogene Proteins p21(ras) | Diphenylamine - pharmacology | raf Kinases - antagonists & inhibitors | Humans | Protein Multimerization | ras Proteins - metabolism | Protein Transport - drug effects | Extracellular Signal-Regulated MAP Kinases - metabolism | raf Kinases - metabolism | Diphenylamine - analogs & derivatives | Mitogen-Activated Protein Kinase Kinases - metabolism | Adenosine Triphosphate - metabolism | Indoles - pharmacology | Benzamides - pharmacology | Cell Membrane - metabolism | raf Kinases - genetics | Cell Membrane - drug effects | Proto-Oncogene Proteins B-raf - metabolism | Proto-Oncogene Proteins B-raf - chemistry | Pyrazoles - pharmacology | Protein Structure, Tertiary | Proto-Oncogene Proteins - metabolism | Cell Line | Indenes - pharmacology | raf Kinases - chemistry | Proto-Oncogene Proteins c-raf - genetics | Mitogen-Activated Protein Kinase Kinases - antagonists & inhibitors | Neoplasms - enzymology | Proto-Oncogene Proteins - genetics | Enzyme Activation - drug effects | Sulfonamides - pharmacology | Proto-Oncogene Proteins c-raf - metabolism | Neoplasms - drug therapy | Proto-Oncogene Proteins B-raf - antagonists & inhibitors | Xenograft Model Antitumor Assays | Animals | MAP Kinase Signaling System - drug effects | Protein Kinase Inhibitors - therapeutic use | Proto-Oncogene Proteins B-raf - genetics | Proto-Oncogene Proteins c-raf - deficiency | Cell Proliferation - drug effects | Mice | Protein Kinase Inhibitors - pharmacology | Neoplasms - pathology | Ras genes | Growth | Physiological aspects | Cellular signal transduction | Genetic aspects | Research | Mitogen-activated protein kinases | Competition | Clinical trials | Enzymes | Kinases | Index Medicus | Proteins | Cellular | Inhibitors | Pathways | Tumours | Signalling | Dimerization
Journal Article
Proceedings of the National Academy of Sciences of the United States of America, ISSN 0027-8424, 07/2017, Volume 114, Issue 30, pp. E6044 - E6053
Journal Article
Journal of Medicinal Chemistry, ISSN 0022-2623, 09/2012, Volume 55, Issue 18, pp. 8110 - 8127
Journal Article
Bioorganic and Medicinal Chemistry Letters, ISSN 0960-894X, 01/2012, Volume 22, Issue 2, pp. 912 - 915
A single crystal was obtained of a lead B-Raf inhibitor with low aqueous solubility. The X-ray crystal structure revealed hydrogen-bonded head-to-tail dimers... 
Single-crystal X-ray | Crystal packing | Aqueous solubility | Crystal lattice energy | B-Raf
Journal Article
Science Signaling, ISSN 1945-0877, 05/2012, Volume 5, Issue 223, pp. ra37 - ra37
Journal Article
Proceedings of the National Academy of Sciences, ISSN 0027-8424, 07/2017, Volume 114, Issue 30, pp. E6044 - E6053
Journal Article
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 10/2012, Volume 22, Issue 19, pp. 6237 - 6241
Cell potent inhibitors of B-Raf that bind to the kinase in the DFG-out conformation are reported. These compounds utilize the hinge-binding group and... 
Inactive conformation | Structure-based design | B-RafV600E | DFG-out | Kinase selectivity | B-Raf | Indexing in process
Journal Article
Bioorganic and Medicinal Chemistry Letters, ISSN 0960-894X, 09/2011, Volume 21, Issue 18, pp. 5533 - 5537
Structure-activity relationships around a novel series of B-Raf inhibitors are reported. The enzymatic and cellular potencies of inhibitors derived from two... 
Pyrrolopyridine | Structure-activity relationship | B-Raf | Pyrazolopyridine
Journal Article
Journal of Medicinal Chemistry, ISSN 0022-2623, 03/2012, Volume 55, Issue 6, pp. 2869 - 2881
Journal Article
Journal Article
Bioorganic and Medicinal Chemistry Letters, ISSN 0960-894X, 01/2012, Volume 22, Issue 2, pp. 1165 - 1168
Herein we describe a novel series of ATP competitive B-Raf inhibitors based on the pyrazolo[1,5-a]pyrimidine scaffold. These inhibitors exhibit both excellent... 
Kinase | B-Raf | Drug discovery | Cancer
Journal Article
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 04/2014, Volume 24, Issue 8, pp. 1923 - 1927
Herein we describe the design of a novel series of ATP competitive B-Raf inhibitors via structure-based methods. These 3- -methylquinazoline-4( )-one based... 
Melonoma | Type IIB inhibitor | B-Raf inhibitors | Kinase drug discovery
Journal Article
Bioorganic and Medicinal Chemistry Letters, ISSN 0960-894X, 04/2014, Volume 24, Issue 8, pp. 1923 - 1927
Herein we describe the design of a novel series of ATP competitive B-Raf inhibitors via structure-based methods. These 3-N-methylquinazoline-4(3H)-one based... 
Journal Article
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 2010, Volume 20, Issue 19, pp. 5607 - 5612
Journal Article
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