5TC0

Structure-based optimization of 1H-imidazole-2-carboxamides as Axl kinase inhibitors utilizing a Mer mutant surrogate

5TC0 の概要

• エントリーDOI: 10.2210/pdb5tc0/pdb
• 分子名称: Tyrosine-protein kinase Mer, N-(2-{4-[(2S)-4-(methylsulfonyl)morpholin-2-yl]-1,3-thiazol-2-yl}phenyl)-1H-imidazole-2-carboxamide (3 entities in total)
• 機能のキーワード: kinase, inhibitor, surrogate, oncology, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• 由来する生物種: Homo sapiens (Human)
• 細胞内の位置: Membrane ; Single-pass type I membrane protein : Q12866
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 72422.61

構造登録者

Hoffman, I.D.,Lawson, J.D. (登録日: 2016-09-13, 公開日: 2017-01-25, 最終更新日: 2024-03-06)

• 主引用文献: Keung, W.,Boloor, A.,Brown, J.,Kiryanov, A.,Gangloff, A.,Lawson, J.D.,Skene, R.,Hoffman, I.,Atienza, J.,Kahana, J.,De Jong, R.,Farrell, P.,Balakrishna, D.,Halkowycz, P.; Structure-based optimization of 1H-imidazole-2-carboxamides as Axl kinase inhibitors utilizing a Mer mutant surrogate.; Bioorg. Med. Chem. Lett., 27:1099-1104, 2017; PubMed: 28082036; DOI: 10.1016/j.bmcl.2016.12.024

実験手法

X-RAY DIFFRACTION (2.24 Å)