{"id":1268,"date":"2020-07-17T11:04:45","date_gmt":"2020-07-17T11:04:45","guid":{"rendered":"https:\/\/zobio.com\/online\/?page_id=1268"},"modified":"2020-08-14T11:03:28","modified_gmt":"2020-08-14T11:03:28","slug":"medicinal-chemistry","status":"publish","type":"page","link":"https:\/\/zobio.com\/online\/capabilities\/medicinal-chemistry\/","title":{"rendered":"Medicinal Chemistry"},"content":{"rendered":"<div id=\"pl-1268\"  class=\"panel-layout\" ><div id=\"pg-1268-1\"  class=\"panel-grid panel-has-style\" ><div class=\"panel-row-style panel-row-style-for-1268-1\" ><div id=\"pgc-1268-1-0\"  class=\"panel-grid-cell\" ><div id=\"panel-1268-1-0-0\" class=\"so-panel widget widget_sow-editor panel-first-child panel-last-child\" data-index=\"1\" ><div class=\"with-icon panel-widget-style panel-widget-style-for-1268-1-0-0\" ><div\n\t\t\t\n\t\t\tclass=\"so-widget-sow-editor so-widget-sow-editor-base\"\n\t\t\t\n\t\t><h2 class=\"widget-title\">Medicinal Chemistry<\/h2>\n<div class=\"siteorigin-widget-tinymce textwidget\">\n\t<p>Finding fragment hits is ultimately the product of applying optimal screening methods to a diverse, high quality fragment library.<br \/>\nOur dynamic collection of 1,500 \u2013 2,000 fragments is the result of active maintenance focused on:<\/p>\n<ul>\n<li>Maximizing diversity using novel cheminformatic approaches<\/li>\n<li>Assessing of compound properties in relation to assay technology used for screening<\/li>\n<li>QC of the compounds and screening mixes by NMR spectroscopy<\/li>\n<\/ul>\n<p>Building on carefully designed and optimized <a href=\"https:\/\/zobio.com\/online\/online\/capabilities\/fragment-screening-and-compound-profiling\/\">fragment screening and compound profiling<\/a> assays, we take every molecule with a concentration-dependent binding effect very seriously as a potential unique starting point in your drug discovery project. Orthogonal screening maximizes the chances of finding diverse fragment hits, even against poorly ligandable targets, and efficient biophysical validation allows us to work on those chemical series that matter.<\/p>\n<p>Although orthogonally validated, the most promising chemical series are often still weak in affinity. Conversion of those chemical series to functional binders with a cellular readout remains a challenge in drug discovery and is often cited as one of the main deterrents to the use of fragment-based approaches. Our medicinal chemists have learned to tackle this challenge through years of experience and are adept at:<\/p>\n<ul>\n<li>Interpreting biophysical data when early functional assays do not directly show an effect.<\/li>\n<li>Understanding the strengths and weaknesses of each assay in the cascade and integrating this information to gain insight into how the ligands are interacting with the target.<\/li>\n<li>Using a variety of structural information derived from competition binding, binding site mapping (via Chemical Shift Perturbation analysis in NMR), low-resolution NMR structures and high-resolution crystallographic structures to efficiently design new analogs with the desired MoA and properties.<\/li>\n<\/ul>\n<p>This rich information and experience allow us to successfully traverse the gulf between the low affinity of fragment hits and early analogs to the sub-micromolar regime where compounds begin to show activity in more traditional assays. At this point, we can begin to apply assays for target selectivity, early ADME and activity in relevant cell lines.<\/p>\n<p>At ZoBio, fragment evolution develops validated, low affinity binders to sub-micromolar novel lead molecules.<\/p>\n<\/div>\n<\/div><\/div><\/div><\/div><\/div><\/div><div id=\"pg-1268-2\"  class=\"panel-grid panel-no-style\" ><div id=\"pgc-1268-2-0\"  class=\"panel-grid-cell\" ><div id=\"panel-1268-2-0-0\" class=\"so-panel widget widget_ls_content_block panel-first-child panel-last-child\" data-index=\"2\" ><div><div id=\"pl-1245\"  class=\"panel-layout\" ><div id=\"pg-1245-0\"  class=\"panel-grid panel-has-style\" ><div class=\"icons-capabilties panel-row-style panel-row-style-for-1245-0\" ><div id=\"pgc-1245-0-0\"  class=\"panel-grid-cell panel-grid-cell-empty\" ><\/div><div id=\"pgc-1245-0-1\"  class=\"panel-grid-cell\" ><div id=\"panel-1245-0-1-0\" class=\"so-panel widget widget_sow-image panel-first-child\" data-index=\"0\" ><div class=\"icon-circle panel-widget-style panel-widget-style-for-1245-0-1-0\" ><div\n\t\t\t\n\t\t\tclass=\"so-widget-sow-image so-widget-sow-image-default-c67d20f9f743-1245\"\n\t\t\t\n\t\t>\n<div class=\"sow-image-container\">\n\t\t<img \n\tsrc=\"https:\/\/zobio.com\/online\/wp-content\/uploads\/2020\/01\/protein-engineering-and-production@2x.png\" width=\"80\" height=\"80\" sizes=\"(max-width: 80px) 100vw, 80px\" alt=\"\" \t\tclass=\"so-widget-image\"\/>\n\t<\/div>\n\n<\/div><\/div><\/div><div id=\"panel-1245-0-1-1\" class=\"so-panel widget widget_sow-editor panel-last-child\" data-index=\"1\" ><div class=\"panel-widget-style panel-widget-style-for-1245-0-1-1\" ><div\n\t\t\t\n\t\t\tclass=\"so-widget-sow-editor so-widget-sow-editor-base\"\n\t\t\t\n\t\t>\n<div class=\"siteorigin-widget-tinymce textwidget\">\n\t<p style=\"text-align: center;\"><a href=\"\/capabilities\/#protein-science\"><strong>Protein<br \/>\n<\/strong><strong>Sciences<\/strong><\/a><\/p>\n<\/div>\n<\/div><\/div><\/div><\/div><div id=\"pgc-1245-0-2\"  class=\"panel-grid-cell\" ><div id=\"panel-1245-0-2-0\" class=\"so-panel widget widget_sow-image panel-first-child\" data-index=\"2\" ><div class=\"icon-circle panel-widget-style panel-widget-style-for-1245-0-2-0\" ><div\n\t\t\t\n\t\t\tclass=\"so-widget-sow-image so-widget-sow-image-default-c67d20f9f743-1245\"\n\t\t\t\n\t\t>\n<div class=\"sow-image-container\">\n\t\t<img \n\tsrc=\"https:\/\/zobio.com\/online\/wp-content\/uploads\/2020\/01\/assay-development-and-screening@2x.png\" width=\"80\" height=\"80\" sizes=\"(max-width: 80px) 100vw, 80px\" alt=\"\" \t\tclass=\"so-widget-image\"\/>\n\t<\/div>\n\n<\/div><\/div><\/div><div id=\"panel-1245-0-2-1\" class=\"so-panel widget widget_sow-editor panel-last-child\" data-index=\"3\" ><div class=\"panel-widget-style panel-widget-style-for-1245-0-2-1\" ><div\n\t\t\t\n\t\t\tclass=\"so-widget-sow-editor so-widget-sow-editor-base\"\n\t\t\t\n\t\t>\n<div class=\"siteorigin-widget-tinymce textwidget\">\n\t<p style=\"text-align: center;\"><a href=\"\/capabilities\/#fragment-screening\"><strong>Fragment Screening<\/strong><br \/>\n<strong>and Compound Profiling<\/strong><\/a><\/p>\n<\/div>\n<\/div><\/div><\/div><\/div><div id=\"pgc-1245-0-3\"  class=\"panel-grid-cell\" ><div id=\"panel-1245-0-3-0\" class=\"so-panel widget widget_sow-image panel-first-child\" data-index=\"4\" ><div class=\"icon-circle panel-widget-style panel-widget-style-for-1245-0-3-0\" ><div\n\t\t\t\n\t\t\tclass=\"so-widget-sow-image so-widget-sow-image-default-c67d20f9f743-1245\"\n\t\t\t\n\t\t>\n<div class=\"sow-image-container\">\n\t\t<img \n\tsrc=\"https:\/\/zobio.com\/online\/wp-content\/uploads\/2020\/01\/structural-biology@2x.png\" width=\"80\" height=\"80\" sizes=\"(max-width: 80px) 100vw, 80px\" alt=\"\" \t\tclass=\"so-widget-image\"\/>\n\t<\/div>\n\n<\/div><\/div><\/div><div id=\"panel-1245-0-3-1\" class=\"so-panel widget widget_sow-editor panel-last-child\" data-index=\"5\" ><div class=\"panel-widget-style panel-widget-style-for-1245-0-3-1\" ><div\n\t\t\t\n\t\t\tclass=\"so-widget-sow-editor so-widget-sow-editor-base\"\n\t\t\t\n\t\t>\n<div class=\"siteorigin-widget-tinymce textwidget\">\n\t<p style=\"text-align: center;\"><a href=\"\/capabilities\/#structural-biology\"><strong>Structural<\/strong><br \/>\n<strong>Biology<\/strong><\/a><\/p>\n<\/div>\n<\/div><\/div><\/div><\/div><div id=\"pgc-1245-0-4\"  class=\"panel-grid-cell panel-grid-cell-mobile-last\" ><div id=\"panel-1245-0-4-0\" class=\"so-panel widget widget_sow-image panel-first-child\" data-index=\"6\" ><div class=\"icon-circle panel-widget-style panel-widget-style-for-1245-0-4-0\" ><div\n\t\t\t\n\t\t\tclass=\"so-widget-sow-image so-widget-sow-image-default-c67d20f9f743-1245\"\n\t\t\t\n\t\t>\n<div class=\"sow-image-container\">\n\t\t<img \n\tsrc=\"https:\/\/zobio.com\/online\/wp-content\/uploads\/2020\/01\/medicinal-chemistry@2x.png\" width=\"80\" height=\"80\" sizes=\"(max-width: 80px) 100vw, 80px\" alt=\"\" \t\tclass=\"so-widget-image\"\/>\n\t<\/div>\n\n<\/div><\/div><\/div><div id=\"panel-1245-0-4-1\" class=\"so-panel widget widget_sow-editor panel-last-child\" data-index=\"7\" ><div class=\"panel-widget-style panel-widget-style-for-1245-0-4-1\" ><div\n\t\t\t\n\t\t\tclass=\"so-widget-sow-editor so-widget-sow-editor-base\"\n\t\t\t\n\t\t>\n<div class=\"siteorigin-widget-tinymce textwidget\">\n\t<p style=\"text-align: center;\"><a href=\"\/capabilities\/#medical-chemistry\"><strong>Medicinal<\/strong><br \/>\n<strong>Chemistry<\/strong><\/a><\/p>\n<\/div>\n<\/div><\/div><\/div><\/div><div id=\"pgc-1245-0-5\"  class=\"panel-grid-cell panel-grid-cell-empty\" ><\/div><\/div><\/div><div id=\"pg-1245-1\"  class=\"panel-grid panel-no-style\" ><div id=\"pgc-1245-1-0\"  class=\"panel-grid-cell\" ><div id=\"panel-1245-1-0-0\" class=\"so-panel widget widget_sow-editor panel-first-child panel-last-child\" data-index=\"8\" ><div class=\"zobio-links panel-widget-style panel-widget-style-for-1245-1-0-0\" ><div\n\t\t\t\n\t\t\tclass=\"so-widget-sow-editor so-widget-sow-editor-base\"\n\t\t\t\n\t\t>\n<div class=\"siteorigin-widget-tinymce textwidget\">\n\t<p style=\"text-align: center;\"><a href=\"\/capabilities\">ZoBio Capabilities<\/a><\/p>\n<\/div>\n<\/div><\/div><\/div><\/div><\/div><div id=\"pg-1245-2\"  class=\"panel-grid panel-has-style\" ><div class=\"bg-shadow-behind-icons siteorigin-panels-stretch panel-row-style panel-row-style-for-1245-2\" data-stretch-type=\"full-stretched\" ><div id=\"pgc-1245-2-0\"  class=\"panel-grid-cell panel-grid-cell-empty\" ><\/div><\/div><\/div><\/div><\/div><\/div><\/div><\/div><\/div>","protected":false},"excerpt":{"rendered":"<p>Finding fragment hits is ultimately the product of applying optimal screening methods to a diverse, high quality fragment library. Our dynamic collection of 1,500 \u2013 2,000 fragments is the result of active maintenance focused on: Maximizing diversity using novel cheminformatic approaches Assessing of compound properties in relation to assay technology used for screening QC of&#8230;<\/p>\n","protected":false},"author":1,"featured_media":0,"parent":10,"menu_order":0,"comment_status":"closed","ping_status":"closed","template":"page-about.php","meta":{"gpsa_enabled":false,"gpsa_required_form_ids":[],"gpsa_require_unique_form_submission":false,"gpsa_access_behavior":"show_message","gpsa_form_redirect_path":"","gpsa_requires_access_message":"","gpsa_access":[],"gpsa_content_loading_message":"","footnotes":""},"class_list":["post-1268","page","type-page","status-publish","hentry"],"yoast_head":"<!-- This site is optimized with the Yoast SEO plugin v27.1.1 - https:\/\/yoast.com\/product\/yoast-seo-wordpress\/ -->\n<title>Medicinal Chemistry - ZoBio - Drug Discovery Technology<\/title>\n<meta name=\"robots\" content=\"index, follow, max-snippet:-1, max-image-preview:large, max-video-preview:-1\" \/>\n<link rel=\"canonical\" href=\"https:\/\/zobio.com\/online\/capabilities\/medicinal-chemistry\/\" \/>\n<meta property=\"og:locale\" content=\"en_GB\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Medicinal Chemistry - ZoBio - Drug Discovery Technology\" \/>\n<meta property=\"og:description\" content=\"Finding fragment hits is ultimately the product of applying optimal screening methods to a diverse, high quality fragment library. 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