SC3: PHARMACOLOGY TRICKS OF THE TRADE: IDENTIFYING HIGHLY ACTIVE COMPOUNDS AND AVOIDING ASSAY ARTIFACTS

MONDAY, AUGUST 24 | 10:00 AM - 1:00 PM

Pharmacology assays for defining structure-activity relationships (SAR) often rely on unstated and untested technical and conceptual assumptions. Considering these assumptions enables discovery of highly active molecules. Not considering them can lead to project failure, owing to distorted SAR, assay ceilings and inability to predict efficacy. Using case studies, this course will inform attendees of the assumptions of in vitro pharmacology and how they impact lead optimization and discovery.

Topics to be Covered:

These pharmacological in vitro assays and their assumptions will be examined:

• Binding kinetics
• Buffer compositions
• Target concentration
• Artificial signaling systems

Instructor:

Sam Hoare, PhD, Founder, Pharmechanics LLC

Sam Hoare is the Founder and Chief Scientist of Pharmechanics LLC, a company dedicated to helping drug discovery scientists analyze pharmacological data. With the advent of new targets, technologies and dimensions of ligand activity, Pharmechanics helps transform raw data into the drug parameters used to drive drug discovery and development. Previously, Sam was with the Discovery Research group at Neurocrine Biosciences, where he was Lead Pharmacologist on multiple GPCR and transporter drug targets. He is particularly known for applying receptor kinetics to CRF1 receptor antagonist development.

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