タイトル | Discovery of triazole aminopyrazines as a highly potent and selective series of PI3K delta inhibitors. |
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ジャーナル・号・ページ | Bioorg. Med. Chem. Lett., Vol. 27, Page 679-687, Year 2017 |
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掲載日 | 2016年8月23日 (構造データの登録日) |
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著者 | Terstiege, I. / Perry, M. / Petersen, J. / Tyrchan, C. / Svensson, T. / Lindmark, H. / Oster, L. |
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リンク | Bioorg. Med. Chem. Lett. / PubMed:28017532 |
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手法 | X線回折 |
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解像度 | 2.3 - 2.9 Å |
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構造データ | PDB-5t23: PI3Kg IN COMPLEX WITH 5d 手法: X-RAY DIFFRACTION / 解像度: 2.78 Å PDB-5t27: mPI3Kd IN COMPLEX WITH 5d 手法: X-RAY DIFFRACTION / 解像度: 2.6 Å PDB-5t28: mPI3Kd IN COMPLEX WITH 5k 手法: X-RAY DIFFRACTION / 解像度: 2.8 Å PDB-5t2b: mPI3Kd IN COMPLEX WITH 5e 手法: X-RAY DIFFRACTION / 解像度: 2.3 Å PDB-5t2d: mPI3Kd IN COMPLEX WITH 7j 手法: X-RAY DIFFRACTION / 解像度: 2.9 Å PDB-5t2g: mPI3Kd IN COMPLEX WITH 7i 手法: X-RAY DIFFRACTION / 解像度: 2.55 Å PDB-5t2i: mPI3Kd IN COMPLEX WITH 7k 手法: X-RAY DIFFRACTION / 解像度: 2.3 Å PDB-5t2l: mPI3Kd IN COMPLEX WITH 7l 手法: X-RAY DIFFRACTION / 解像度: 2.55 Å PDB-5t2m: mPI3Kd IN COMPLEX WITH 7m 手法: X-RAY DIFFRACTION / 解像度: 2.8 Å |
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化合物 | ChemComp-74F: 3-(benzotriazol-1-yl)-5-[1-methyl-5-[(1~{S})-1-morpholin-4-ylethyl]-1,2,4-triazol-3-yl]pyrazin-2-amine
ChemComp-74Q: 3-(benzotriazol-1-yl)-5-[1-methyl-5-(1-phenylcyclopropyl)-1,2,4-triazol-3-yl]pyrazin-2-amine
ChemComp-74O: 5-[1-methyl-5-(1-phenylcyclopropyl)-1,2,4-triazol-3-yl]-3-(1~{H}-pyrazol-4-yl)pyrazin-2-amine
ChemComp-74L: 4-[3-azanyl-6-[1-methyl-5-(1-phenylcyclopropyl)-1,2,4-triazol-3-yl]pyrazin-2-yl]-~{N},~{N}-dimethyl-pyrazole-1-sulfonamide
ChemComp-74K: 4-[3-azanyl-6-[1-methyl-5-(1-phenylcyclopropyl)-1,2,4-triazol-3-yl]pyrazin-2-yl]pyrazole-1-carboxamide
ChemComp-74J: 1-[3-azanyl-6-[1-methyl-5-(1-phenylcyclopropyl)-1,2,4-triazol-3-yl]pyrazin-2-yl]pyrazole-4-carboxamide
ChemComp-74H: 1-[3-azanyl-6-[1-methyl-5-(1-phenylcyclopropyl)-1,2,4-triazol-3-yl]pyrazin-2-yl]pyrazole-3-carboxamide
ChemComp-74N: 4-[3-azanyl-6-[1-methyl-5-(1-phenylcyclopropyl)-1,2,4-triazol-3-yl]pyrazin-2-yl]benzamide
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由来 | homo sapiens (ヒト)![](img/tx_mammal.gif) mus musculus (ハツカネズミ)
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キーワード | TRANSFERASE / PI3Kg / Inhibitor / mI3Kd |
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