| 标题 |
 Parallel Optimization of Potency and Pharmacokinetics Leading to the Discovery of a Pyrrole Carboxamide ERK5 Kinase Domain Inhibitor 相关领域
激酶
化学
效力
药理学
甲酰胺
MAPK/ERK通路
体内
药代动力学
吡唑
生物利用度
药物发现
蛋白激酶A
生物化学
体外
生物
立体化学
生物技术
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| 网址 | |
| DOI | |
| 其它 |
Abstract Abstract Image The nonclassical extracellular signal-related kinase 5 (ERK5) mitogen-activated protein kinase pathway has been implicated in increased cellular proliferation, migration, survival, and angiogenesis; hence, ERK5 inhibition may be an attractive approach for cancer treatment. However, the development of selective ERK5 inhibitors has been challenging. Previously, we described the development of a pyrrole carboxamide high-throughput screening hit into a selective, submicromolar inhibitor of ERK5 kinase activity. |
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dave 在
2022-05-03 19:08:34 发布，悬赏 10 积分
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