{"id":10168,"date":"2022-10-17T09:11:19","date_gmt":"2022-10-17T01:11:19","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=10168"},"modified":"2022-10-17T09:11:19","modified_gmt":"2022-10-17T01:11:19","slug":"daniels-matthew-h-s-team-published-research-in-journal-of-medicinal-chemistry-in-2022-cas-15366-34-4","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=10168","title":{"rendered":"Daniels, Matthew H.&#8217;s team published research in Journal of Medicinal Chemistry in 2022 | CAS: 15366-34-4"},"content":{"rendered":"<p><a href=\"https:\/\/www.ambeed.com\/products\/15366-34-4.html\">Product Details of 15366-34-4<\/a>In 2022 ,\u300aDiscovery and Optimization of Highly Selective Inhibitors of CDK5\u300b was published in Journal of Medicinal Chemistry. The article was written by Daniels, Matthew H.; Malojcic, Goran; Clugston, Susan L.; Williams, Brett; Coeffet-Le Gal, Marie; Pan-Zhou, Xin-Ru; Venkatachalan, Srinivasan; Harmange, Jean-Christophe; Ledeboer, Mark. The article contains the following contents:<\/p>\n<p>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 (I), 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. After reading the article, we found that the author used Methyl 1H-pyrazole-3-carboxylate(cas: 15366-34-4<a href=\"https:\/\/www.ambeed.com\/products\/15366-34-4.html\">Product Details of 15366-34-4<\/a>)<\/p>\n<p>Methyl 1H-pyrazole-3-carboxylate(cas: 15366-34-4) belongs to pyrazoles. Pyrazole derivatives have been reported to exhibit a wide range of applications in medicinal chemistry and pharmacology. A large number of drugs incorporating pyrazole structure have been utilized as partial agonists for nicotinic acid receptors, antidepressants, antimicrobial agents, antiviral agents, and antifungal agents solely or along with the combination of other structural motifs.<a href=\"https:\/\/www.ambeed.com\/products\/15366-34-4.html\">Product Details of 15366-34-4<\/a><\/p>\n<p>Referemce:<br \/><a href=\"https:\/\/en.wikipedia.org\/wiki\/Pyrazole\">Pyrazole &#8211; Wikipedia<\/a>,<br \/><a href=\"https:\/\/www.sciencedirect.com\/topics\/chemistry\/pyrazoles\">Pyrazoles &#8211; an overview | ScienceDirect Topics<\/a><\/p>\n","protected":false},"excerpt":{"rendered":"<p>Methyl 1H-pyrazole-3-carboxylate(cas: 15366-34-4) belongs to pyrazoles. Pyrazole derivatives have been reported to exhibit a wide range of applications in medicinal chemistry and pharmacology. A large number of drugs incorporating pyrazole structure have been utilized as partial agonists for nicotinic acid receptors, antidepressants, antimicrobial agents, antiviral agents, and antifungal agents solely or along with the combination of other structural motifs.<a href=\"https:\/\/www.ambeed.com\/products\/15366-34-4.html\">Product Details of 15366-34-4<\/a><\/p>\n","protected":false},"author":8,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[174,131],"tags":[128],"class_list":["post-10168","post","type-post","status-publish","format-standard","hentry","category-15366-34-4","category-pyrazoles-derivatives","tag-100-200"],"yoast_head":"<!-- This site is optimized with the Yoast SEO plugin v24.9 - https:\/\/yoast.com\/wordpress\/plugins\/seo\/ -->\n<title>Daniels, Matthew H.&#039;s team published research in Journal of Medicinal Chemistry in 2022 | CAS: 15366-34-4 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"Product Details of 15366-34-4In 2022 ,\u300aDiscovery and Optimization of Highly Selective Inhibitors of CDK5\u300b was published in Journal of Medicinal Chemistry. The article was written by Daniels, Matthew H.; Malojcic, Goran; Clugston, Susan L.; Williams, Brett; Coeffet-Le Gal, Marie; Pan-Zhou, Xin-Ru; Venkatachalan, Srinivasan; Harmange, Jean-Christophe; Ledeboer, Mark. The article contains the following contents:\" \/>\n<meta name=\"robots\" content=\"index, follow, max-snippet:-1, max-image-preview:large, max-video-preview:-1\" \/>\n<link rel=\"canonical\" href=\"https:\/\/www.pyrazoles-derivatives.com\/?p=10168\" \/>\n<meta property=\"og:locale\" content=\"en_US\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Daniels, Matthew H.&#039;s team published research in Journal of Medicinal Chemistry in 2022 | CAS: 15366-34-4 | pyrazoles-derivatives\" \/>\n<meta property=\"og:description\" content=\"Product Details of 15366-34-4In 2022 ,\u300aDiscovery and Optimization of Highly Selective Inhibitors of CDK5\u300b was published in Journal of Medicinal Chemistry. 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