As a product manager for a range of instruments that serve the drug discovery market, it was a ‘must’ for me to go to San Diego, in January, to attend SLAS2020. It was 40°F warmer than in Massachusetts (where I live) and the conference was fantastic. It had many scientific tracks on most aspects of drug discovery and was attended by many of the world’s leaders in the field, who were happy to discuss their work.
I must admit that I have not been to that many meetings over the past couple of years. This was a great way to get an overview of the current opinions and trends in the field and this is a brief description of my general observations from ‘track hopping’.
High-throughput screening (HTS) is alive and kicking, very important in small molecule drug discovery and dominated by mass spectrometry and its derivatives. CETSA (cellular thermal shift assay) has moved into the high-throughput space with both Astra Zeneca and GSK using it to screen 0.5 million or greater compounds. There is real hope, that by monitoring ‘real’ target engagement in the cell, that attrition in clinical trials can be reduced. Let’s hope that turns out to be true.
Acoustic dispensing is central to many high throughput screening campaigns, and is increasing efficiency and the reduction of waste. Efficiency improvement was the premise of Paul Harper’s (Astra Zeneca) great talk describing their attempts to automate the medicinal chemistry involved in lead optimization. Jarrod Walsh (also Astra Zeneca) described his work to successfully reduce the number of false positives from PAINS (pan-assay interference) compounds.
AI is still in its infancy in drug discovery but is coming up fast.
Data mining and data quality are the first issues to address if we are to unleash the power of AI to develop new and better drugs, more quickly. Viral Vyas from Bristol-Myers Squibb described the complexities behind even finding the appropriate data associated with a project, and efficiently sharing data from the 50-100 vendors they partner in the clinical trial process. They are making progress!
Great talks on AI in image analysis and for Medicinal Chemistry gave a hint as to where this field is heading, and its potential for increasing value from R&D spend.
Drugging RNA had its very own section for the first time. This class of targets is growing in importance because, we were reminded, only 700 of the 3000 druggable protein targets are currently ‘drugged’ and that there are 100,000 RNA transcripts to go after! There are new companies focusing on this area, and 2 drugs already on the market for spinal muscular dystrophy.
New Life Forms?
If all that wasn’t enough, the conference concluded with a fantastic talk by Prof. Lee Cronin, from Glasgow University, on his Chemputer. Briefly, this is a device that his group has made to create new chemicals with no human contact. This is a stepping stone on his journey to develop a new life form. I could not possibly do his work justice here and I recommend you look him up.
I’m very lucky!
- Microcalorimetry as a tool for structural biology
- Size and zeta potential characterization of liposomes using the Zetasizer Nano
- Biophysical characterization of epigenetic interactions and associated drug discovery, using Isothermal Titration Calorimetry
- Addressing the needs of drug discovery with the MicroCal PEAQ-ITC instruments