Biochemical Assays for Screening Workshop Agenda

Introductions

Lecture: Introduction to drug discovery and the design and development of biochemical assays for drug discovery purposes - what can be achieved and learnings from past successes and failures, screening jargon and terms.

Case Study: Biochemical Assay Development and Screening.

Break

Lecture: Reagent characterisation and selection of assays which will ensure translation of Hits between formats.

Overview of practical work for Day 1 and creation of groups for practical work: 1. General concepts for biochemical assays exemplified using kinase, histone deacetylase and protease enzymes. 2. IC₅₀ determination for inhibitor, signal stability, choice of liquid handling and Z' calculation. 3. Application of biochemical assays in drug discovery.

Talk From Vendor (Optional)

Lunch

Experimental Work

Group Dinner

Discuss Results from Day 1

Lecture: Data Analysis and Reduction - Going Beyond the Z'. Discuss methods for analysing in-vitro biological assays data including false positive/negative rates, dose-response curve fitting and correlations.

Break

Overview of Practical Work for Day 2: 1. Screening of biochemical assays against a small molecule library (proof-ofconcept screen).

Lunch

Talk From Vendor (Optional)

Experimental Work

Free Evening

Discuss Results from Day 2

Case Study: Analysis of High Throughput Screening Assay Data.

Talk From Vendor (Optional)

Break

Lecture: Integrating your research program, design of project critical paths which integrate in-vitro, in-vivo and in-silico elements.

Lunch

Each team to compare results and identify learnings from practical course, presentations from each team and wrap up.