タイトル | Discovery and optimization of a potent and selective triazolopyridinone series of c-Met inhibitors. |
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ジャーナル・号・ページ | Bioorg. Med. Chem. Lett., Vol. 22, Page 4089-4093, Year 2012 |
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掲載日 | 2012年1月20日 (構造データの登録日) |
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著者 | Bode, C.M. / Boezio, A.A. / Albrecht, B.K. / Bellon, S.F. / Berry, L. / Broome, M.A. / Choquette, D. / Dussault, I. / Lewis, R.T. / Lin, M.H. ...Bode, C.M. / Boezio, A.A. / Albrecht, B.K. / Bellon, S.F. / Berry, L. / Broome, M.A. / Choquette, D. / Dussault, I. / Lewis, R.T. / Lin, M.H. / Rex, K. / Whittington, D.A. / Yang, Y. / Harmange, J.C. |
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リンク | Bioorg. Med. Chem. Lett. / PubMed:22595176 |
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手法 | X線回折 |
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解像度 | 2 - 2.05 Å |
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構造データ | PDB-4deg: Crystal structure of c-Met in complex with triazolopyridazine inhibitor 2 手法: X-RAY DIFFRACTION / 解像度: 2 Å PDB-4deh: Crystal structure of c-Met in complex with triazolopyridinone inhibitor 3 手法: X-RAY DIFFRACTION / 解像度: 2 Å PDB-4dei: Crystal structure of c-Met in complex with triazolopyridinone inhibitor 24 手法: X-RAY DIFFRACTION / 解像度: 2.05 Å |
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化合物 | ChemComp-0JJ: 7-methoxy-N-{[6-(3-methyl-1,2-thiazol-5-yl)[1,2,4]triazolo[4,3-b]pyridazin-3-yl]methyl}-1,5-naphthyridin-4-amine
ChemComp-0JK: 5-phenyl-3-(quinolin-6-ylmethyl)-3,5,6,7-tetrahydro-4H-[1,2,3]triazolo[4,5-c]pyridin-4-one
ChemComp-0JL: 3-{(1S)-1-[3-(2-methoxyethoxy)quinolin-6-yl]ethyl}-5-(3-methyl-1,2-thiazol-5-yl)-3,5-dihydro-4H-[1,2,3]triazolo[4,5-c]pyridin-4-one
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由来 | ![](img/tx_human.gif) homo sapiens (ヒト)
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キーワード | TRANSFERASE/TRANSFERASE INHIBITOR / proto-oncogene (がん遺伝子) / receptor tyrosine kinase (受容体型チロシンキナーゼ) / RTK / ATP-binding / hepatocyte growth factor/scatter factor / HGF/SF (肝細胞増殖因子) / phosphoprotein / TRANSFERASE-TRANSFERASE INHIBITOR complex / inhibitor (酵素阻害剤) |
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