タイトル | Proline isosteres in a series of 2,4-disubstituted pyrrolo[1,2-f][1,2,4]triazine inhibitors of IGF-1R kinase and IR kinase. |
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ジャーナル・号・ページ | Bioorg. Med. Chem. Lett., Vol. 20, Page 5027-5030, Year 2010 |
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掲載日 | 2010年7月9日 (構造データの登録日) |
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著者 | Sampognaro, A.J. / Wittman, M.D. / Carboni, J.M. / Chang, C. / Greer, A.F. / Hurlburt, W.W. / Sack, J.S. / Vyas, D.M. |
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リンク | Bioorg. Med. Chem. Lett. / PubMed:20675137 |
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手法 | X線回折 |
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解像度 | 2.11 - 2.2 Å |
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構造データ | PDB-3nw5: Crystal structure of insulin-like growth factor 1 receptor (IGF-1R-WT) complex with a carbon-linked proline isostere inhibitor (11B) 手法: X-RAY DIFFRACTION / 解像度: 2.14 Å PDB-3nw6: Crystal structure of insulin-like growth factor 1 receptor (IGF-1R-WT) complex with a carbon-linked proline isostere inhibitor (11A) 手法: X-RAY DIFFRACTION / 解像度: 2.2 Å PDB-3nw7: Crystal structure of insulin-like growth factor 1 receptor (IGF-1R-WT) complex with a carbon-linked proline isostere inhibitor (34) 手法: X-RAY DIFFRACTION / 解像度: 2.11 Å |
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化合物 | ChemComp-LGX: N-(5-cyclopropyl-1H-pyrazol-3-yl)-2-{(2R)-1-[(6-fluoropyridin-3-yl)carbonyl]pyrrolidin-2-yl}pyrrolo[2,1-f][1,2,4]triazin-4-amine
ChemComp-LGW: N-(5-cyclopropyl-1H-pyrazol-3-yl)-2-{(2S)-1-[(6-fluoropyridin-3-yl)carbonyl]pyrrolidin-2-yl}pyrrolo[2,1-f][1,2,4]triazin-4-amine
ChemComp-LGV: N-({4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl}methyl)-6-fluoropyridine-3-carboxamide
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由来 | homo sapiens (ヒト)
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キーワード | TRANSFERASE / HORMONE/GROWTH FACTOR / IGF-1R / KINASE DOMAIN |
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