GFB-12811(GFB-12811) - 药物靶点：CDK5_在研适应症：常染色体显性多囊肾病_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

CDK5

作用机制

CDK5抑制剂(细胞周期蛋白依赖性激酶5抑制剂)

治疗领域

遗传病与畸形泌尿生殖系统疾病其他疾病

在研适应症

常染色体显性多囊肾病

非在研适应症-

原研机构

Goldfinch Bio, Inc.初创企业

在研机构

Goldfinch Bio, Inc.初创企业

非在研机构-

最高研发阶段临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

结构

分子式C22H23F4N5O

InChIKeyGHNYLVIESIGHDJ-OAQYLSRUSA-N

CAS号2775311-17-4

关联

100 项与 GFB-12811 相关的临床结果

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100 项与 GFB-12811 相关的转化医学

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100 项与 GFB-12811 相关的专利（医药）

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1

项与 GFB-12811 相关的文献（医药）

2022-02-24·Journal of Medicinal Chemistry1区 · 医学

Discovery and Optimization of Highly Selective Inhibitors of CDK5

1区 · 医学

Article

作者: Williams, Brett ; Coeffet-Le Gal, Marie ; Pan-Zhou, Xin-Ru ; Ledeboer, Mark ; Malojcic, Goran ; Clugston, Susan L. ; Harmange, Jean-Christophe ; Daniels, Matthew H. ; Venkatachalan, Srinivasan

Autosomal dominant polycystic kidney disease (ADPKD) is the most prevalent monogenic human disease, but to date, only one therapy (tolvaptan) is approved to treat kidney cysts in ADPKD patients. Cyclin-dependent kinase 5 (CDK5), an atypical member of the cyclin-dependent kinase family, has been implicated as a target for treating ADPKD. However, no compounds have been disclosed to date that selectively inhibit CDK5 while sparing the broader CDK family members. Herein, we report the discovery of CDK5 inhibitors, including GFB-12811, that are highly selective over the other tested kinases. In cellular assays, our compounds demonstrate CDK5 target engagement while avoiding anti-proliferative effects associated with inhibiting other CDKs. In addition, we show that the compounds in this series exhibit promising in vivo PK profiles, enabling their use as tool compounds for interrogating the role of CDK5 in ADPKD and other diseases.

100 项与 GFB-12811 相关的药物交易

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