{"id":4116,"date":"2024-09-16T15:00:49","date_gmt":"2024-09-16T15:00:49","guid":{"rendered":"https:\/\/www.sygnaturediscovery.com\/poster\/dedicated-dmpk-for-degraders-a-flexible-approach-for-flexible-molecules\/"},"modified":"2026-01-22T15:10:39","modified_gmt":"2026-01-22T15:10:39","slug":"dedicated-dmpk-for-degraders-a-flexible-approach-for-flexible-molecules","status":"publish","type":"poster","link":"https:\/\/www.sygnaturediscovery.com\/fr\/poster\/dedicated-dmpk-for-degraders-a-flexible-approach-for-flexible-molecules\/","title":{"rendered":"Dedicated DMPK for Degraders &#8211; a flexible approach for flexible molecules"},"content":{"rendered":"<p>Bifunctional degraders are compounds that bind to and induce degradation of a target by simultaneously binding to a ubiquitin ligase.<sup>1<\/sup> Despite their size and physical properties lying outside the space usually required for oral absorption (beyond the rule of 5, bRo5) there are many reports of bifunctional degraders with high levels of bioavailability and acceptable oral exposure levels in pre-clinical models.<\/p>\n<p>However, challenges still exist due to the physicochemical space these molecules occupy and how well <em>in vitro<\/em> DMPK assays translate into <em>in vivo<\/em> performance. In this poster, we describe the assays and dedicated expertise at Sygnature Discovery aimed at supporting drug discovery projects involving bifunctional degraders, together with exemplar data for various compounds.<\/p>\n","protected":false},"excerpt":{"rendered":"<p>Bifunctional degraders bind and degrade proteins via ubiquitin ligase, despite breaking bRo5 rules. Translating in vitro DMPK data to in vivo performance remains a challenge. At Sygnature Discovery, we provide tailored assays and expertise to support projects involving these compounds. Read more in the poster.<\/p>\n","protected":false},"featured_media":2841,"template":"","category":[726,720,683,727,686,728,719,722,743],"class_list":["post-4116","poster","type-poster","status-publish","has-post-thumbnail","hentry","category-bioanalysis","category-chemical-metabolic-stability","category-dmpk","category-in-vivo-pk-pd","category-modalities","category-modelling-and-simulation","category-physicochemical-profiling","category-tissue-binding","category-tpd"],"acf":[],"yoast_head":"<!-- This site is optimized with the Yoast SEO plugin v28.5 - https:\/\/yoast.com\/product\/yoast-seo-wordpress\/ -->\n<title>Dedicated DMPK for Bifunctional Degraders | Poster<\/title>\n<meta name=\"description\" content=\"Explore DMPK assays and expertise for bifunctional degraders, including the challenge of translating in vitro data into in vivo performance. View more.\" \/>\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.sygnaturediscovery.com\/fr\/poster\/dedicated-dmpk-for-degraders-a-flexible-approach-for-flexible-molecules\/\" \/>\n<meta property=\"og:locale\" content=\"fr_CA\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Dedicated DMPK for Bifunctional Degraders | Poster\" \/>\n<meta property=\"og:description\" content=\"Explore DMPK assays and expertise for bifunctional degraders, including the challenge of translating in vitro data into in vivo performance. 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