タイトル | The Discovery of Pamapimod and R1487 as Orally Bioavailable and Highly Selective Inhibitors of p38 Map Kinase |
---|
ジャーナル・号・ページ | To be Published |
---|
掲載日 | 2008年12月19日 (構造データの登録日) |
---|
著者 | Soth, M. / Kuglstatter, A. / Goldstein, D. |
---|
リンク | PubMedで検索 |
---|
手法 | X線回折 |
---|
解像度 | 1.7 - 2.23 Å |
---|
構造データ | PDB-3flz: P38 kinase crystal structure in complex WITH 8-Methyl-6-phenoxy-2-(tetrahydro-pyran-4-ylamino)-8H-pyrido[2,3-d]pyrimidin-7-one 手法: X-RAY DIFFRACTION / 解像度: 2.23 Å PDB-3fmh: P38 kinase crystal structure in complex with 6-(2,4-Difluoro-phenoxy)-8-methyl-2-((R)-1-methyl-2-tetrazol-2-yl-ethylamino)-8H-pyrido[2,3-d]pyrimidin-7-one 手法: X-RAY DIFFRACTION / 解像度: 1.9 Å PDB-3fmj: P38 kinase crystal structure in complex with 4-(5-Methyl-3-phenyl-isoxazol-4-yl)-pyrimidin-2-ylamine 手法: X-RAY DIFFRACTION / 解像度: 2.0 Å PDB-3fmk: P38 kinase crystal structure in complex with 6-(2,4-Difluoro-phenoxy)-8-methyl-2-((S)-1-methyl-2-tetrazol-2-yl-ethylamino)-8H-pyrido[2,3-d]pyrimidin-7-one 手法: X-RAY DIFFRACTION / 解像度: 1.7 Å PDB-3fsf: P38 kinase crystal structure in complex with 3-(2,6-Dichloro-phenyl)-7-[4-(2-diethylamino-ethoxy)-phenylamino]-1-methyl-3,4-dihydro-1H-pyrimido[4,5-d]pyrimidin-2-one 手法: X-RAY DIFFRACTION / 解像度: 2.1 Å |
---|
化合物 | ChemComp-FLZ: 8-methyl-6-phenoxy-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one
ChemComp-533: 6-(2,4-difluorophenoxy)-8-methyl-2-{[(1R)-1-methyl-2-(2H-tetrazol-2-yl)ethyl]amino}pyrido[2,3-d]pyrimidin-7(8H)-one
ChemComp-FMJ: 4-(5-methyl-3-phenylisoxazol-4-yl)pyrimidin-2-amine
ChemComp-FMK: 6-(2,4-difluorophenoxy)-8-methyl-2-{[(1S)-1-methyl-2-(2H-tetrazol-2-yl)ethyl]amino}pyrido[2,3-d]pyrimidin-7(8H)-one
ChemComp-FSS: 3-(2,6-dichlorophenyl)-7-({4-[(diethylamino)methoxy]phenyl}amino)-1-methyl-3,4-dihydropyrimido[4,5-d]pyrimidin-2(1H)-one
|
---|
由来 | homo sapiens (ヒト)
|
---|
キーワード | SIGNALING PROTEIN / TRANSFERASE / P38; MAP KINASE; SERINE/THREONINE KINASE / ATP-binding / Kinase / Nucleotide-binding / Nucleus / Phosphoprotein / Serine/threonine-protein kinase / Alternative splicing / Cytoplasm / Polymorphism |
---|