タイトル | Discovery and Optimization of Potent, Efficacious and Selective Inhibitors Targeting EGFR Exon20 Insertion Mutations. |
---|
ジャーナル・号・ページ | J. Med. Chem., Vol. 67, Page 8988-9027, Year 2024 |
---|
掲載日 | 2023年7月3日 (構造データの登録日) |
---|
著者 | Thomson, C. / Barton, P. / Braybrooke, E. / Colclough, N. / Dong, Z. / Evans, L. / Floc'h, N. / Guerot, C. / Hargreaves, D. / Khurana, P. ...Thomson, C. / Barton, P. / Braybrooke, E. / Colclough, N. / Dong, Z. / Evans, L. / Floc'h, N. / Guerot, C. / Hargreaves, D. / Khurana, P. / Li, S. / Li, X. / Lister, A. / McCoull, W. / McWilliams, L. / Orme, J.P. / Packer, M.J. / Swaih, A.M. / Ward, R.A. / Winlow, P. / Ye, Y. |
---|
リンク | J. Med. Chem. / PubMed:38770784 |
---|
手法 | X線回折 |
---|
解像度 | 1.621 - 2.523 Å |
---|
構造データ | PDB-8pnz: Discovery and Optimisation of Potent, Efficacious and Selective Inhibitors Targeting EGFR Exon20 Insertion Mutations. Compound 16 bound to EGFR 手法: X-RAY DIFFRACTION / 解像度: 2.51 Å PDB-8po0: Discovery and Optimisation of Potent, Efficacious and Selective Inhibitors Targeting EGFR Exon20 Insertion Mutations. Compound 12 bound to EGFRinsNPG 手法: X-RAY DIFFRACTION / 解像度: 2.523 Å PDB-8po1: Discovery and Optimisation of Potent, Efficacious and Selective Inhibitors Targeting EGFR Exon20 Insertion Mutations. Compound 22 bound to EGFRinsNPG [V948R] 手法: X-RAY DIFFRACTION / 解像度: 2.11 Å PDB-8po2: Discovery and Optimisation of Potent, Efficacious and Selective Inhibitors Targeting EGFR Exon20 Insertion Mutations. Compound 33 bound to EGFRinsNPG [V948R] 手法: X-RAY DIFFRACTION / 解像度: 2.28 Å PDB-8po3: Discovery and Optimisation of Potent, Efficacious and Selective Inhibitors Targeting EGFR Exon20 Insertion Mutations. Compound 18 bound to EGFR[V948R] 手法: X-RAY DIFFRACTION / 解像度: 2.13 Å PDB-8po4: Discovery and Optimisation of Potent, Efficacious and Selective Inhibitors Targeting EGFR Exon20 Insertion Mutations. Compound 33 bound to EGFR[V948R] 手法: X-RAY DIFFRACTION / 解像度: 1.621 Å |
---|
化合物 | |
---|
由来 | homo sapiens (ヒト)
|
---|
キーワード | SIGNALING PROTEIN / EGFR / Exon 20 insertion / non-small cell lung cancer / oncology |
---|