Dennis Hu
@DennisWhom
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founder & CEO @drughuntersite after drug discovery in pharma/biotech (Genentech, RAPT Therapeutics) - discover faster in two min at
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Joined April 2018
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2023 Small Molecule Approvals!
@drughuntersite
A lot of fascinating firsts in 2023 including:
-The first FDA-approved oral ER degrader
-The first FDA-approved reversible BTK inhibitor
-The first FDA-approved gamma-secretase inhibitor (not in Alzheimer’s!)
-A reversible
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A lot of cool "firsts" in 2022 including:
-first novel deuterated & pseudokinase-targeting drug
-first kinase activator (not inhibitor)
-first HIV capsid protein-protein interaction accelerator
-first EP2 agonist, bioactivated in the eye
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Small Molecule of the Year, 2020:
The drug discovery community voted on their favorite molecule from 2020, and their 2020 pick is GS-6207,
@GileadSciences
awe-inspiring HIV capsid inhibitor.
Full story at .
#chemtwitter
#biotwitter
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EXPENSIVE THINGS IN DRUG DISCOVERY
$100 per hour a scientist spends in lab
$300 per assay plate (and just the plastic plate!)
$1,000 per team meeting to decide what to do
$3,000 per compound that actually gets made
$10,000 to see if that compound is orally absorbed in
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Small Molecules of the Month - May 2021 |
A mutant PI3Kα degrader in Ph. III, a wild-type CFTR potentiator for COPD, and a surprisingly well-tolerated Ph. III agent from an aerospace compound
#chemtwitter
#biotwitter
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Small Molecules of the Month - Apr. 2021 |
This month:
An inhibitor that "glues" KRAS to cyclophilin A
A targeted protein stabilizer
An RNA-modifying enzyme inhibitor
Wild!
#chemtwitter
#biotwitter
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2019 SM Drug Approvals w/ Indication, Mechanism, and Dosing - - ChemDraw file available for download for our little community of drug hunters. Looking forward to 2020!
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2020 Small Molecule Drug Approvals -
Drug Hunter subscribers can download the full list w/ mechanism of action, route of admin., pivotal trial NCTs, primary endpoints, enrollment at time of approval, etc.
#chemtwitter
#biotwitter
#medtwitter
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Small Molecules of the Month - Apr. 2020 -
Several clinical candidates disclosures and a variety of uncommon chemical motifs in April that will pique chemists' interest.
Full post, links and PDF download at
Enjoy!
#chemtwitter
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The Resurgence of Antibody-Drug Conjugates |
ADCs are roaring back with impressive activities and new classes of warheads like proteins and oligos.
@drughuntersite
put together a visual review of approved ADCs for reference.
#biotwitter
#chemtwitter
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Small Molecules of the Month | Feb. 2021 - PDF @
A Breakthrough EGFR exon 20 mut. inhibitor, multiple protein dimerizers, a substrate-modifying MBI, and a femtomolar inhibitor among the strongest reversible binders ever recorded.
#chemtwitter
#biotwitter
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Small Molecules of the Month | March 2021 - Hi-res PDF @
A molecular glue for a peptide/receptor interaction, a hydantoin zinc binder and numerous other chemistry rule-breakers this month, including an oral compound with 6 HBDs!
#chemtwitter
#biotwitter
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Small Molecules of the Month - August 2020:
A Gilead cmpd w/ twice-a-year(!!) dosing, a non-classical C-H—O bonding kinase inhibitor from Pfizer, and a cool substrate-assisted covalent mechanism from Takeda among others this time
#chemtwitter
#biotwitter
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BIOTECH VS. PHARMA
A biotech is a pharma company that’s “unencumbered” by revenue.
That can mean more focus, greater speed, and more flexibility..
..but it can also mean fewer resources, less institutional knowledge, and more risk.
Our friends in biotech find awe in the
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Small Molecules of the Month - Jun. 2021 |
A natural product-derived RNA splicing modulator, an mTORC1-selective “bi-steric” inhibitor, and several unusual chemical motifs this month.
via
@drughuntersite
#chemtwitter
#biotwitter
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Mechanisms of Approved Covalent Drugs:
Covalent drugs have deep roots in infectious disease research (hard not to think about atm!). A visual summary of all of the unique mechanisms of approved targeted covalents below.
Enjoy and stay safe!
#chemtwitter
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Small Molecules of the Month, Feb. 2020 -
Highlights from SMDD campaigns published online Jan-Feb. Grab a coffee and use this post as a starting point in getting caught up on the literature this year!
PDF and links to articles in the post
#chemtwitter
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What are great examples of academic labs opening doors for industrial small mol drug discovery?
Thinking heterobifunctional degraders (Crews), molecular glues (Schreiber), reversible covalents (Tauton), mutant KRas starting point (Shokat), mRNA display (Szostak)..
Thoughts?
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Small Molecules of the Month, Oct. 2020:
Hope everyone had a great Thanksgiving. Three here from
#Bayer
, a double soft drug, and several from international sites incl. PL, BE, DK, IN, CN. Enjoy!
#chemtwitter
#biotwitter
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Small Molecules of the Month - July 2020:
A cmpd from a DNA-encoded library, some from phenotypic screens, and a featured cryo-EM structure from Novartis, among July's features!
Full post + hi-res PDF @
#chemtwitter
#biotwitter
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Small Molecules of the Month - June 2020:
Summer starts with some natural-product inspired molecules, two metal-binders (including 1 via a ketone!), two transcription factor modulators, a molecular glue degrader, and more!
#chemtwitter
#biotwitter
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"Don't Work on Things That Don't Work" -
When I interviewed at Genentech, I asked Kim Huard, for advice on how to succeed in drug discovery. “Don’t work on things that don’t work!” — she laughed.
Recently I got to interview Kim about this gem!
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Small Molecules of the Month - Sep. 2020 -
A reversible-covalent aldehyde inhibitor and the hot SHP2 inhibitor from Novartis, a Pfizer GLP-1R agonist w/ a cryo-EM structure, and 7 anions this time! More, links + SMILES in site
#chemtwitter
#biotwitter
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2020 Biotech IPOs - Small Molecule R&D |
@drughuntersite
's review of small molecule-focused biotech IPOs of 2020 - a snapshot of what's in small co.'s aggregate pipeline.
Full list + searchable table at
#chemtwitter
#biotwitter
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Small Molecules of the Month - May 2020:
Another group of interesting structures, biological targets, and mechanisms of action!
Full post, links and hi-res PDF download at
Enjoy!
#ChemTwitter
#biotwitter
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0/ Thread: 2019 roundup
Drug Hunter is a site for those working in biopharma, focusing on drug discovery and industry highlights. Highlights below of top content totaling >250k views in 2019. Looking forward to helping more scientists in 2020!
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Liven up your next design meeting by targeting some of these unusual interactions. These and others were identified as statistically significant across X-ray co-crystal structures in PDB in a
@Roche
study in
@JMedChem
.
#medicinalchemistry
#chemtwitter
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Small Molecule Immunomodulators – H1 2021 |
My colleague Christian Gampe put together a summary of small molecule immunomodulators from H1 2021.
For half a year’s worth of science in a few minutes, check out his article!
#chemtwitter
#biotwitter
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Small Molecules of the Month - Nov. 2020:
Hope everyone had a wonderful Christmas weekend. Quite a few of these molecules would've made for a decent synthesis PhD project! Links and PDF at .
#chemtwitter
#biotwitter
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Small Molecules of the Month - Jan. 2021 -
A mouse urine metabolite as a starting point for a diabetes drug, an inducer of integrin lysosomal degradation, and an in vivo tool from virtual screening. Links and PDF in article.
#chemtwitter
#biotwitter
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Small Molecules of the Month, Mar. 2020 -
It's easy to have missed all the non-COVID drug discovery articles that were published in March. Here's some highlights to help your quarantine reading!
PDF and links to articles in the post
#chemtwitter
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Molecules of the Month, Jul 2021 |
An ER degrader in Ph. III, 4(!) neurology candidates from Takeda, two sulfoximines, and molecule gets ubiquitylated to degrade its target
Gradually moving content to team page
@drughuntersite
#chemtwitter
#biotwitter
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[Drug Hunter] ΔLogD Cheat Sheet and Why LogD Matters -
I didn't take lipophilicity seriously enough when I started in
#medchem
. Post on why LogD is critical, some "traps" encountered when ignoring LogD, and a PDF download of this table.
#chemtwitter
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Big Pharma before pandemic:
👎- Evil/less popular than the federal government
👎- Trials watched by MD/PhD analysts
👎 - Profits for greedy shareholders
Big Pharma after pandemic:
🙏 - Our only hope
🙏 - Trials watched by Twitter/Medium
🙏 - What's left of your 401k
#biotwitter
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List of specialist investors backing drug discovery companies -
#biotwitter
am I obviously missing someone here?
Didn't list the big firms like Sequoia, KCPB, GV, etc. that have a small % to DD
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C-H···O bond was first proposed by a woman in 1962.
@Genentech
scientists Naomi Rajapaksa and Callie Bryan describe inhibitors binding w/ a C-H···O bond in this 'Women in Medicinal
#Chemistry
' issue
@ACSMedChemLett
#womeninchemistry
,
#womeninstem
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This made my week!!!
After an exhausting several months getting this feedback from a the leader of one of the top non-profit drug discovery groups in the world and 30-year Merck veteran was a shot in the arm.
No idea if you're on Twitter but thank you Peter for the kind words
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2020 Small Molecules of the Year -
Vote for your favorite in 2020:
In 2020 highlighted >150 "molecules of the month" - so hard to narrow it down, but we all learned from these!
#chemtwitter
#biotwitter
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During the J.P. Morgan Conference, Gilead announced that they planned to file an NDA for approval in the second half of 2021. Congratulations to the Gilead Sciences team on their success so far and we wish Gilead and their enrolled patients the best through the approval process.
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2020 Large Molecule Drug Approvals |
15 new LM in 2020 including an ASO, a double-stranded siRNA, 2 ADCs, and a several mAbs.
Full summaries and PDF download available at
#biotwitter
#chemtwitter
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2019 Biotech IPOs - Small Molecule R&D -
Last year, 25 biotechs focusing on small molecule drug discovery IPO'd on US exchanges. Great to see investors continuing to support highly risky but potentially impactful research.
#chemtwitter
#biotwitter
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TIL from Christina Woo
@drcmwoo
that the molecule sanglifehrin was named after its discoverers Sanglier and Fehr.
When Prof. Woo and I discover a molecule together my life will be complete.
#chemtwitter
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Hands down the most active compound of all time
Molecule of the Day: Curcumin |
Curcumin is a component of tumeric, and is sold as an herbal supplement, cosmetics ingredient, food flavoring, and food coloring.
The molecule is one of the most widely studied therapeutics in history, with papers,
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The new site is finally out! Lots in the pipeline for 2022 :) Thanks to our Drug Hunter team, our community members, and sponsors for their support.
Phase II is Live! -
It’s gotten harder to keep up with everything that’s going on in pharma. Drug Hunter exists to save you time by curating industry science. We hope you love your new site! Some highlights in this thread (1/n)
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Small Molecules of the Month, Dec. 2020:
An oral(!) insulin analog from Novo, a 2:1-binding non-covalent alternative to Voxelotor from Pfizer, two oral TNFa inhibitors, among others in the last SMOTM of 2020.
Link above for post
#chemtwitter
#biotwitter
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Molecules of the Month - March 2023
A low-dose TYK2 inhibitor that covers IC90 at trough among many other notable molecules with updates in March!
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Drug Hunter's 2020 Large Molecule Biotech IPO Review |
Browsing through the pipelines of recent biotech IPOs is great way to catch up on emerging targets and modalities - lots of cool science in 2020!
Full list
@drughuntersite
#biotwitter
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2020 - Year of the Chimera?
Sure feels like Year of the "Rat" the way 2020 is going. Let's celebrate the Chimera instead!
Intro to chimeric mols, co's working on em, 10 “hot” papers, and some predictions for 2020.
#chemtwitter
#biotwitter
#medchem
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How Does This Thing Get in the Brain?? |
At AAPS 2022, I hosted a symposium where Ovoca Bio plc’s Head of Research told us about orenetide. Orenetide is an internationally approved drug for hypoactive sexual desire disorder (HSDD) (think Viagra for ♀️)...
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Topliss Cheat Sheets -
In this guest post by
@CKuttruff
, Christian explains how to use the Topliss Schemes for compound optimization, useful especially during hit triage. PDF of the 3 cheat sheets available at the site!
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This likely megablockbuster for BMS is one of the most anticipated drug launches due to its better safety profile thanks to its allosteric mechanism of action. Also first drug where the deuterated version was developed first!
More context in the team's Premium article
Deucravacitinib (Sotyktu), a First-In-Class Oral, Allosteric Tyrosine Kinase 2 Inhibitor |
In September 2022, the first de novo deuterated drug was approved by the FDA, deucravacitinib, a first-in-class oral, allosteric tyrosine kinase 2 (TYK2) inhibitor
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With explosive growth in biologics, we've decided to discontinue small molecule coverage at
@drughuntersite
and pivot exclusively to molecules that can be represented with squigglier lines.
What is a biologic drug, you ask? Here's a recap:
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Some inspirational books about early days at Amgen, Vertex, and Genentech linked at the bottom of the table here:
Same principles (focusing on high unmet medical need, niche indications, new modalities) seem to work for the fast growers today!
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I remember working at RAPT when this project was getting started and thinking "there's no way that zwitterion is going to be an oral drug."
Ph. II dosed orally once daily, 50-400 mg - boy was I wrong!
@drughuntersite
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A Gram-Daily Aldehyde for Anemia: Voxelotor -
A case study on one of the most interesting 2019 drug approvals, the reversible covalent drug voxelotor. My feelings about aldehydes have definitely done a 360 over time...
#chemtwitter
#biotwitter
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From the free drug hypothesis to relevant assays, understand the essentials of CNS drug discovery in 30 min
How to Get Drugs Into the Brain
Obtaining adequate drug exposure in the brain is key to treating CNS diseases effectively. Recently, Dennis Koester gave us a crash course in CNS drug discovery in a Drug Hunter FlashTalk.
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Finally joining our Drug Hunter team full-time tomorrow!
Staying up-to-date on the industry, researching partners, and learning new areas was always time-consuming for me - my hope is this platform makes it easier for everybody else.
Wife made a present for me to celebrate 😁
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The best part about building Drug Hunter has been getting to work with so many outstanding leaders in pharma and biotech. I learn something new from our team members and readers every day. Looking forward to 2022!
Drug Hunter Reviewers |
Direct feedback and expertise from our community (you!) helps keep Drug Hunter content high quality. We're grateful to have an outstanding group of featured reviewers who share the love of drug discovery with our followers.
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Amgen's sotorasib is notable to chemists as a rare example of a marketed drug that exists as a stable atropisomer - other examples of candidates here:
Stable Atropisomers in Drug Discovery via Catalysis |
Examples of development candidates that are stable atropisomers, synthesis, and a kilo-scale synthesis of a Ph. III candidate using asymmetric catalysis in this article with the team at Sinocompound
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Liver biochemistry is dark magic - even carboxylic acids are structural alerts due to potential conversion to bioreactive acyl glucoronides. Here’s a list of bioactivatable functional groups
#drugdiscovery
#chemistry
#toxicology
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2019 Biologic Drug Approvals -
20 years after the Human Genome Project we have 14 biologics approval in a year including 2 RNA drugs, 3 ADCs, a "nanobody" and all sorts of humanized antibodies. What's in store for this decade?
#drugdiscovery
#biopharma
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Helpful round-up of first-disclosures from AACR's New Drugs on the Horizon session thanks to Chris DeSavi on LinkedIn:
Eager to see whether the Bolt antibody-immune stim. conjugate principle works. What do you find interesting?
#chemtwitter
#biotwitter
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NOTHING REPLACES THE PRIMARY LITERATURE...
..but if you're only reading papers, you're not getting the full story!
Every industry scientist knows that papers are often published 5, 10, or even 20 years after the work was actually done.
There's also negative survivorship bias -
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“SO… HOW DOES DRUG HUNTER MAKE MONEY?” 🤔
Whenever I host an event like a dinner, someone always asks:
“So… how does Drug Hunter make money?”
Sometimes it comes from people who feel sheepish asking but are just curious…
Sometimes it comes with mild suspicion... (somebody’s
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Chris De Savi's tally of approved drugs so far this year:
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See several i like mentioned already (KRAS, Bcl2, BTK, HCV/HIV) but some of my favs..
-oral CGRPs (gepants)
-oral splicing modifiers (risdiplam)
-synthetic lethality POC (PARPi)
-oral complement inhibitors
-orexants
-tissue-agnostic TRK
-allosteric kinase inh.s
-S1P "agonists"
#medchemtwitter
: What are biggest success stories w. approved small molecule drugs in the last 10 or so years? Not in sales but therapeutic breakthrough, maybe even measure of success (money saved or Qualys)? Or personal favourites? Any thoughts e.g.
@HartungIngo
@g_sbardella
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[Drug Hunter] What is a Biologic Drug Anyway? or, How I Learned to Stop Worrying and Love My Own Definition -
Recently I posted on biologic drugs which were approved in 2019. All was well, until I received an email... full story in today's post
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Show a California drug hunter some love by nominating them for the 2021 Pantheon Award for Scientific Advancement:
We'd nominate Dan Erlanson for FBDD, the Celgene IMiDs team, or the Gilead lenacapavir team - who do you think needs a shout-out?
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Is anyone looking for a small molecule drug discovery LEGEND for their Scientific Advisory Board?
A Drug Hunter community member has some newfound free time to commit that anyone would be truly lucky to have.
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The Chugai hit generation team has been on a roll, with remarkable finds for challenging targets, including pan-RAS macrocycles, class B GPCR agonists like orforglipron, and biased agonists like this molecule!
Class B GPCRs like PTHR1, GLP-1R and CGRP are notoriously difficult to drug. This article highlights Chugai’s agonist, PCO371, and why despite no longer being in development, PCO371 scientifically remains a big deal in GPCR drug discovery.
Full article:
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Degraders are different!
For years many were understandably skeptical about whether degraders would differentiate from tried-and-true small molecule antagonists.
However, there are now numerous remarkable examples, including from clinical assets, showing that degradation
Ten Ways Degraders Differentiate from Traditional Small Molecules
Theoretical advantages of targeted protein degradation over traditional inhibition, with specific industry examples of bifunctional degraders demonstrating proof-of-concept for each.
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C4's BRAF(V600)X degrader was one of the most impressive med chem examples at AACR - orally available w/ 9 rings and 20+ N/O atoms!
Bioavailable Degraders Through Conformational Collapse
This single atom change dramatically influenced oral bioavailability. N-containing compound 8 folds over itself, lowering solvent accessible surface area (SASA) despite higher TPSA.
From article:
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Prodrugs are usually intended to be inactive, only to release an active metabolite later. This one has it's own activity contributing to overall pharmacology!
LY03005: An Active Prodrug, Triple Reuptake Inhibitor for Major Depressive Disorder
In contrast to traditional prodrugs, LY03005 is an “active” prodrug with its own activity as a triple-reuptake inhibitor.
Full story:
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How are drug targets identified in practice?
This minireview takes a look at the most commonly-used approaches in industry with a discussion of pros + cons, and provides recent industry examples for the major approaches.
If you have no idea what your drug's target is, where do you start? This minireview with Pelago Bioscience, summarizes available methods for identifying a drug’s target when it is not known at the outset, with a focus on industry examples.
Full article:
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Full summaries in a slide deck here:
Get a sneak preview of what's coming in Drug Hunter 2.0!
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Impressive to see a brain-penetrant AAK1 kinase inhibitor in Ph. II now for neuropathic pain.. other CNS kinase inhibitors have been for serious indications (brain mets, LRRK2, DLK, RIPK1 for PD, ALS)
So much for kinase inhibitors being stuck in oncology!
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In 2019, the FDA granted GS-6207 Breakthrough Therapy Designation, and in 2020 Gilead announced results from the Ph. 2/3 CAPELLA trial showing that 88% of participants with multidrug resistant HIV receiving GS-6207 achieved viral load reduction over 14 days (vs. 17% in placebo).
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Promising data from ARV-766 today, which was intended to have broadened activity against drug-resistant prostate cancers - an interesting proof-of-concept of how degraders can overcome issues with traditional antagonism
ARV-766, Arvinas' 2nd gen CRBN-based AR degrader, aims to tackle drug-resistant prostate cancer. Its simplified glutarimide recruiter & broad-spectrum activity make it unique.
More on ARV-766 & the future of AR degradation in the full article:
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IS YOUR JOURNAL CLUB DEAD YET?
The traditional way we learn about the latest in drug discovery is a conference presentation or a journal club.
You pick a colleague, ask them to spend two weeks researching a topic, and have the whole department sit in a room for an hour while
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Thanks to
@CKuttruff
, Joachim Rudolph, Callie Bryan, and Adi Murthy for their nominees and commentary this month, and Vinicius,
@danielgedder
,
@MariaKoyioni
, and Jes from our team for help prepping this month's article. Hope this is helpful!
Small Molecules of the Month - Oct. 2021 |
Two cardiac muscle modulators from Cytokinetics, an oral macrocyclic peptide, a hydrazine, ... enjoy!
Full summaries, PDF + links at
#chemtwitter
#biotwitter
#medtwitter
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The confidence that you can create new things that didn’t exist before is what makes the PhD experience valuable imo
The comfort in navigating the unknown and knowing that you can survive “wandering in the desert” without knowing what’s next has been priceless
PhD folks: QT this and talk about how your grad school work compares to what you’re doing in your career post-PhD. The same or different or very different? What skills did you take with you from your PhD that were most important to your job today?
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Still can’t believe how fast this actually happened - got my first Moderna mRNA shot Friday.
I thought the mRNA vaccines would never be commercial because you’d never be able to scale up kgs of RNA in time. Glad I was wrong!
Our industry is amazing.
It's now been almost a year since the New York Times put together this technically impressive yet totally wrong interactive article about how long it would take to get a Covid vaccine.
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First program I ever worked on! Crazy how long development takes but glad to see responses in Ph. I/II. Hope the CCR4 molecules help somebody.
Oral CCR4 inhibitor FLX475 shrinks EBV+ tumors as monotherapy and in combination with a PD-1 inhibitor in Ph. I/II clinical trials. This case study reviews the molecule’s interesting indirect mechanism on cancers and notable discovery story.
Full article:
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Thank you
@HartungIngo
for sharing! Though this one didn't make it our team hopes the community benefits by keeping an eye out for Vps34 on other programs.
Structure-based design & optimization of
#Vps34
inhibitors by the drug hunter
@DennisWhom
himself: Don't get carried away by potency when selecting hits & leaving the kinase flatlands opens the door to exquisite selectivity & drug properties
@ACSBioMed
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Oral efficacy w 5 H bond donors and two carboxylic acids 🤯
compound 49 - Calithera Biosciences |
Compound 49 is an unlikely oral candidate for CD73 inhibition in tumor models, but despite its high number of polar and charged groups and HBD/HBA, it has shown promising oral efficacy.
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Beautiful molecule disclosed by
@Boehringer
in a poster - still hope for MDM2-p53 PPI inhibitors? Single agent activity and Fast Track Designation seem to suggest so!
Still Hope for MDM2/p53 in Cancer?
Boehringer's BI 907828 was disclosed in a poster at AACR, is in the same chemical class as the nutlins. While Roche's idasanutlin was discontinued in Ph. III for AML, BI 907828 continues. What's different?
Full article:
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Fantastic visual lesson from experienced drug hunter and Boehringer research site head
@D_B_McConnell
- if you're trying to get better at med chem and aren't following him already, what are you waiting for? 😉
With all the interesting drug candidate examples from
@drughuntersite
to learn from I thought I'd put together the odd SWOD analysis (Strengths & Weakness of Design) at the risk of offending the designers themselves. Here's one for the early menin binder MI-503.
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Molecules of the Month - August |
A dibasic oral kallikrein inhibitor, a spirocyclobutene FXR agonist, a NaV1.6 clinical candidate, a remarkably long acting RIPK2 PROTAC, and several other interesting clinical candidates.
#chemtwitter
#biotwitter
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“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
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You never know, dacarbazine, a standard chemo agent which releases diazomethane in vivo, looks like something that might have come out of your shop! 😁
So a predatory oncology conference just asked me, an explosives chemist, to deliver a plenary lecture. I’m thinking about what the hell I’d say if this were a legit conference. I sincerely doubt anyone would find my methods of fighting cancer to be plausible!
@AcademicChatter
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Folks have been asking us to cover more molecules that have experienced failures - plenty of interesting science behind those too! Three interesting molecules/mechanisms here..
Negative Readouts: Updates on an NMDAR PAM, an MK2 inhibitor, and a Porcupine inhibitor |
Not all molecules make it, but the science behind them remains interesting. A roundup of notable halted, discontinued or altered clinical trials from March 2023
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Nice ongoing compilation of male/female rat PK difference examples in this thread - another one of those drug discovery phenomena everyone sees or hears about but rarely gets published. Thanks
@med_chemist
!
Do others have examples of papers where the rat PK was so drastically different between male/female?
Seems like perhaps the females aren't cleaving the amide as quickly?
From:
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Totally stealing this for SAR
@nathandao1109
Thanks! We like to use this type of figure to concisely illustrate substrate scope. Figure guru
@ScienceBey
was the person in the group to pioneer this type of figure and it has spread like wildfire🔥
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