Hit-to-Lead Optimization Strategy in Drug Discovery

In vitro biochemical assays make possible the high throughput screening (HTS) of large compound libraries. A successful HTS campaign is typically viewed as one that identifies large numbers of diverse chemical series hits as potential starting points on the way to a clinical candidate. These hits are typically weakly active in a primary screen and do not necessarily possess drug like characteristics. Hit-to-Lead optimization is now a key process in drug discovery that explores the chemistry and biology of hits to focus efforts on the most promising starting points so that development time and costs are saved.

What makes a promising starting point for a drug discovery program? In this webinar, strategies to triage hits and focus efforts will be discussed.

Speakers

Mark Wolf, Head, Medicinal Chemistry, AMRI

Mark Wolf has 20 years of drug discovery and development experience at AMRI and has held positions of increasing responsibility during that time. He has led interdisciplinary scientific teams to support large pharma, biotech collaborations and AMRI R&D programs. His research has spanned several therapeutic areas including oncology, CNS, pain/inflammation, and respiratory. Wolf has experience establishing practical screening strategies to identify drug candidate compounds with a first-in-class or best-in-class product profile. He has a PhD in organic chemistry from Miami University, and is experienced managing programs from Hit-to-Lead into the clinic.

Message Presenter

Doug Kitchen, Head, CADD, AMRI

Doug Kitchen obtained his Ph.D. from Princeton University (Chemistry). He joined AMRI in 1997 to begin the computational chemistry group. Kitchen’s interests are in compound library design, structure-guided drug design and lead optimization. He is a co-inventor on more than 10 issued patents and author on more than forty refereed articles and book chapters. Two of Kitchen’s inventions are now marketed drugs.

Message Presenter