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Molecules of the Month – April 2024 Find out what compounds made our April 2024 Molecules of the Month list and check out recent articles for each. Article | drughunters.com/3wD1WYB

“How Do You Choose the Molecules?” Molecules of the Month is out again, and it reminded me about a question I hear in pretty much every meeting with new Drug Hunter (@drughuntersite) members: “How do you choose the molecules?” It’s a lot harder than you might think! We start

AZETIDINE AMIDES IN DRUGS Recently, Gilles Ouvry had an insightful post on azetidine amides on LinkedIn (If you’re a med chemist, he is a MUST-follow there). He points out that azetidine amides are unique because they can have a different SAR than other tertiary amides due to

“COMPOUNDS IN VIALS” ARE NOT ENOUGH “Compounds in vials” is a loaded phrase to med chemists. Sometimes, it’s quipped by bosses to imply their teams need to work harder: “We need compounds in vials.” Sometimes, it’s a sarcastic reaction to proposed ideas that are nice on

Cerevance’s CNS-Penetrant KCNK13 Inhibitor Targets Brain-Specific NLRP3-Inflammasome Blockade | drughunters.com/3KMzB5P Our CVN293 article covers how @Cerevance solved clearance liabilities whilst maintaining CNS-exposure in a high polar surface area chemical series.

Really nice explanation of where the target came from, the rationale, and key problems solved with this deceptively simple looking molecule!

What are you getting quoted for SciFinder, Reaxys, and Cortellis this year?

Molecules of the Month – May 2024 | drughunters.com/45jDyYR Read the full article to find out what compounds made our May 2024 Molecules of the Month list and check out recent articles for each. Article | drughunters.com/45jDyYR

On Scaling Mentorship On the drive up to Seattle for the National Med Chem Symposium, I remembered some moments from nearly ten years ago when I was proposing some of my first compounds to synthesize. We were trying to improve the PK of a lead, and I brought my then-manager a

Does Property-Based Drug Design Merit a Nobel Prize? We can all sense that the drugs of today are fundamentally DIFFERENT from the drugs of the 80's, 90's, and 2000's. They're bigger, gnarlier, more complex, and more impactful than ever. Increasingly, clinical candidates are

Targeting the “Impossible” Asp12 of KRAS(G12D)(ON) with an Aziridine-Containing Tri-complex | drughunters.com/3WqUOr2 RMC-9805 is a first-in-class, covalent KRAS(G12D)(ON) molecular glue inhibitor from @Revolution Medicines. Read the full article on Drug Hunter

We are excited to welcome Dr. Dean Brown to the Drug Hunter Scientific Advisory Board! Dr. Brown brings over 25 years of experience in industry in both large pharmaceutical and biotech organizations. Currently, he is Senior Vice President and Head of Discovery Sciences at Jnana

We are thrilled to welcome Dr. Nicholas A. Meanwell, FRSC to the Drug Hunter Scientific Advisory Board! Dr. Meanwell is an esteemed figure in the field of medicinal chemistry, with over four decades of significant contributions to drug discovery, including the advancement of 33

A Potential Best-in-Class HIF-2α Inhibitor Disclosed by Arcus | drughunters.com/4dWF8D8 From the ACS Fall 2024 first-time disclosures, we bring you the structure and discovery of the compound Arcus hopes will go head-to-head with the FDA approved HIF-2α inhibitor, belzutifan.

An Oral Small Molecule PCSK9 Inhibitor with Remarkable Bioavailability | drughunters.com/3TbhMlc As part of our ACS Fall 2024 First-Time Disclosures coverage, we’re excited to share the structure and discovery story of AstraZeneca's oral small molecule PCSK9 inhibitor AZD0780.

A CNS-Penetrant ARα2C Antagonist Demonstrating Efficacy in Preclinical Obstructive Sleep Apnea Models | drughunters.com/4ew8BUP We detail the discovery of BAY 2925976, as highlighted by Michael Hahn at the ACS Fall 2024 First-Time Disclosures session in Denver, CO.

Check out the key SAR observations that led to the invention of this orally bioavailable PROTAC, its performance in a triple-hit, high-grade BCL and R-CHOP-resistant cell line, why sustaining BCL6 knockdown beyond 24 h was critical, and more. Article: drughunters.com/3Blc1eJ

Why Are VAV1 Degraders Such a Big Deal? Earlier this week, Novartis signed a deal for $150M upfront, up to $2.1B, with Monte Rosa Therapeutics. Drug Hunter scientists highlighted VAV1 patents earlier in the year and noted this program from a conference this summer (see link).