Enzymlogic

📸 𝗦𝗽𝗲𝗰𝗶𝗮𝗹 𝗺𝗼𝗺𝗲𝗻𝘁 𝗮𝘁 𝗗𝗶𝘀𝗰𝗼𝘃𝗲𝗿𝘆 𝗼𝗻 𝗧𝗮𝗿𝗴𝗲𝘁 𝟮𝟬𝟮𝟰! It’s been amazing to see Patricia Alfonso San-Segundo and Jeremy Hague connecting with some brilliant minds at the conference! From insightful conversations with Peter Tonge (Stony Brook University) to engaging with Adrian Whitty (Boston University), and Maria Esteban Lopez (UCB), they've been exchanging ideas and diving deep into exciting discussions about drug discovery. So proud of the collaboration and energy at our booth! 🙌 👉 Haven’t stopped by yet? There’s still time! Swing by booth #302 to chat with the team, explore more case studies our #kinetic platforms, 𝗞𝗜𝗡𝗘𝗧𝗜𝗖finder® and 𝗖𝗢𝗩𝗔𝗟finder®, and see how we can support your research. 😀 Let’s keep the energy going! Drop a comment, like, or reach out to connect. #DrugDiscovery #Innovation #DOT2024 #KineticProfiling #CovalentInhibitors #MedChem #Drugdesign

🌟 𝗔 𝗕𝗜𝗚 𝗧𝗛𝗔𝗡𝗞 𝗬𝗢𝗨! 🌟 We’re thrilled by the overwhelming interest and participation at our CSO Patricia Alfonso San-Segundo's presentation, "Kinetic Profiling of Covalent Inhibitors using COVALfinder®," at Discovery on Target 2024! 🙌 The session was packed, and the discussions were inspiring! 💡 If you missed it or want to dive deeper into the case studies we presented, don’t hesitate to visit our booth (#302)! Jeremy and Patricia will be there, excited to share insights on how we can help you advance your drug discovery projects. Let’s keep the conversation going! Drop by, ask questions, and discover more about our innovative solutions. We can't wait to see you there! 👉 If you can’t make it, connect with us here: https://lnkd.in/dSj5ATzW #DiscoveryOnTarget #DOT #DrugDiscovery #COVALfinder #drugdesign #MedChem #Medicinalchemistry #kinetics #covalent

🚨 𝗛𝗲𝗮𝗱𝗶𝗻𝗴 𝘁𝗼 𝗗𝗶𝘀𝗰𝗼𝘃𝗲𝗿𝘆 𝗼𝗻 𝗧𝗮𝗿𝗴𝗲𝘁 𝟮𝟬𝟮𝟰 𝗶𝗻 𝗕𝗼𝘀𝘁𝗼𝗻?🚨 Make sure you don't miss our CSO, Patricia Alfonso San-Segundo, presenting "Kinetic Profiling of Covalent Inhibitors using COVALfinder®" on 𝗠𝗼𝗻𝗱𝗮𝘆, 𝗦𝗲𝗽𝘁𝗲𝗺𝗯𝗲𝗿 𝟯𝟬𝘁𝗵 𝗮𝘁 𝟭𝟬:𝟯𝟬 during the Covalent Chemistries and Induced Proximity session! Patricia will showcase multiple case studies, highlighting how to: ✅ leverage inactivation kinetics to optimize covalent drugs. ✅ fine-tune kinetic selectivity for better target specificity. ✅ identify irreversible drugs targeting the inactive form of proteins. Can't make it on time? No worries! Stop by our booth (#302) from September 30 to October 3. See you there! 🤜🤛

🚀 Enzymlogic is proud to sponsor the Emergence of Irreversible Modulation in Drug Discovery meeting in Cambridge, UK, on 16-17 October 2024! 🤔Struggling to balance inactivation efficiency with drug selectivity? Join us as we present Enzymlogic’s cutting-edge tools for decoding irreversible inhibition kinetics. 💡 Learn how COVALfinder® is helping to refine Medicinal Chemistry, bridge PK/PD gaps, and optimise therapeutic windows. 👀 Find out more about the event here: https://lnkd.in/eW4dwG6B 👉 For Enzymlogic’s kinetic profiling services look here: https://lnkd.in/eKTiK_yE

Enzymlogic is proud to support Iambic Therapeutics ground breaking Type II HER2 inhibitor program with cutting edge Inactivation Kinetic profiling to determine KINETIC SELECTIVTY using COVALfinder® More details in this fantastic poster by Svitlana Kulyk and Iambic colleagues recently presented at AACR : https://lnkd.in/edbHz6qU

𝐍𝐚𝐯𝐢𝐠𝐚𝐭𝐢𝐧𝐠 𝐭𝐡𝐞 𝐂𝐨𝐯𝐚𝐥𝐞𝐧𝐭 𝐅𝐫𝐨𝐧𝐭𝐢𝐞𝐫 Discovering new drugs targeting difficult-to-treat diseases like certain types of cancer is always exciting. Recently, two groundbreaking medicines, sotorasib and adagrasib, have been approved, signaling a new chapter in drug discovery. This marks a shift from past approaches, where drugs were often discovered by chance or by modifying existing ones. Traditionally, drugs were designed to bind reversibly to their targets. But for tricky targets like KRASG12C, a different strategy was needed. The "electrophile-first" strategy, initiated by disulfide tethering and library screening, seeks compounds that create lasting covalent bonds with particular parts of the target molecule. Identifying these promising compounds can be tough. There's a risk of false positives, and measuring their effectiveness requires special methods because of how they bind irreversibly. Still, the potential benefits are huge. Covalent drugs could target proteins that were previously thought to be off-limits, opening up new possibilities for treating diseases. 👉 This review explores the latest techniques for finding these covalent drugs. Researchers look at everything from lab-based methods to high-tech screening approaches: https://lnkd.in/gnTw7vvm 😀 It's an exciting time for covalent drug discovery, and we stand ready to provide the necessary tools! Find out more at: https://lnkd.in/eWTbuuAX #drugdiscovery #pharmaceuticals #drugdesign #medchem #medicinalchemistry #covalent #cancerresearch #science

𝐓𝐡𝐢𝐬 𝐢𝐬 𝐚𝐧 𝐞𝐱𝐜𝐢𝐭𝐢𝐧𝐠 𝐭𝐢𝐦𝐞 𝐭𝐨 𝐛𝐞 𝐰𝐨𝐫𝐤𝐢𝐧𝐠 𝐢𝐧 𝐭𝐡𝐞 𝐜𝐨𝐯𝐚𝐥𝐞𝐧𝐭 𝐝𝐫𝐮𝐠 𝐝𝐢𝐬𝐜𝐨𝐯𝐞𝐫𝐲 𝐟𝐢𝐞𝐥𝐝! Over the past decade, perceptions of covalent inhibitors have improved, addressing concerns about selectivity and safety. Once seen as risky for non-cancer uses due to potential toxicities, recent non-oncology successes have changed the game. This positive shift opens up vast opportunities for innovation and success. To help you make the most of these opportunities, we’re excited to share our latest Application Note: "𝐃𝐢𝐬𝐜𝐨𝐯𝐞𝐫𝐢𝐧𝐠 𝐚𝐧𝐝 𝐃𝐞-𝐫𝐢𝐬𝐤𝐢𝐧𝐠 𝐈𝐫𝐫𝐞𝐯𝐞𝐫𝐬𝐢𝐛𝐥𝐞 𝐈𝐧𝐡𝐢𝐛𝐢𝐭𝐨𝐫𝐬". This guide reveals how kinetic characterization can optimize irreversible inhibitors beyond just IC50 values by determining inactivation rate (kinact/KI) and potency (KI). 🎯 Unlock the potential of COVALfinder®: ✅ Modify compound binding (KI) and reactivity (kinact). ✅ Enhance therapeutic index and safety profiles. ✅ Build better PK/PD models. For more information contact us today. Let’s propel irreversible inhibitor research together! #Pharmacology #IrreversibleInhibitors #PharmaceuticalResearch #covalent #Pharmaceutical #medchem #drugdiscovery #drugdesign

Orexin (OxA) is a neuropeptide produced in neurons of the lateral hypothalamus and projects throughout the central nervous system, activating orexin 1 receptor (Ox1R) or orexin 2 receptor (Ox2R). While Ox2R is linked to sleep and targeted for insomnia and narcolepsy, Ox1R is associated with psychiatric disorders and targeted for substance use disorders, binge eating, and anxiety. A recent scientific publication by Takeda showcases the development of CVN766, a compound with over 1000-fold selectivity for Ox1R over Ox2R, designed to avoid Ox2R-mediated sleepiness. Researchers also emphasizes the importance of receptor binding kinetics. 👉 They were concerned with the kinetics of receptor binding as OxA has a long residency time at its receptors. To overcome this obstacle, they aimed to develop an antagonist with long residence time. 🔬 𝗥𝗲𝘀𝗲𝗮𝗿𝗰𝗵 𝗛𝗶𝗴𝗵𝗹𝗶𝗴𝗵𝘁𝘀: ☑ 𝗦𝗲𝗹𝗲𝗰𝘁𝗶𝘃𝗶𝘁𝘆: CVN766 shows impressive selectivity for Ox1R over Ox2R (1000x), minimizing the risk of sleepiness. ☑ 𝗥𝗲𝗹𝗮𝘁𝗶𝗼𝗻𝘀𝗵𝗶𝗽 𝗯𝗲𝘁𝘄𝗲𝗲𝗻 𝗽𝗼𝘁𝗲𝗻𝗰𝘆, 𝗿𝗲𝗰𝗲𝗽𝘁𝗼𝗿 𝗸𝗶𝗻𝗲𝘁𝗶𝗰𝘀 𝗮𝗻𝗱 𝗲𝘅𝗽𝗼𝘀𝘂𝗿𝗲: Studies on rat brain sections revealed that CVN766 (IC50=8 nM, Residence time=120 min) maintains prolonged receptor occupancy in both brain and plasma. Whereas compounds like CVN45502, with similar IC50 (16 nM) but shorter residence time (5.3 min), demonstrated a time-dependent decline in receptor occupancy, aligning closely with their pharmacokinetic profiles. ☑ 𝗣𝗲𝗿𝗺𝗲𝗮𝗯𝗶𝗹𝗶𝘁𝘆: CVN766 exhibited high brain permeability and an ideal pharmacokinetic profile for clinical studies. ☑ 𝗖𝗹𝗶𝗻𝗶𝗰𝗮𝗹 𝗧𝗿𝗶𝗮𝗹𝘀: A recent Phase I clinical trial revealed that CVN766 was well-tolerated with an excellent safety profile across all dose groups. Unlike many orexin receptor antagonists, CVN766 showed no evidence of somnolence. Stay tuned for more updates on #GPCR drug discovery! https://lnkd.in/dQtcNrAF #Neuroscience #OrexinResearch #Pharmacology #DrugDiscovery #MedChem #DrugDesign #Pharmaceuticals

🌟 Yesterday, we organized the workshop "𝐊𝐢𝐧𝐞𝐭𝐢𝐜 𝐒𝐞𝐥𝐞𝐜𝐭𝐢𝐯𝐢𝐭𝐲: 𝐚 𝐌𝐢𝐬𝐬𝐞𝐝 𝐎𝐩𝐩𝐨𝐫𝐭𝐮𝐧𝐢𝐭𝐲 𝐢𝐧 𝐃𝐫𝐮𝐠 𝐃𝐞𝐬𝐢𝐠𝐧?" at the ACS National Medicinal Chemistry Symposium in Seattle! It was an incredible day full of deep discussion and insightful learning. Our workshop focused on maximizing therapeutic windows for reversible and covalent inhibitors using KINETICfinder® and COVALfinder®, and we had the chance to share innovative ideas and cutting-edge approaches in this exciting field. We want to thank all attendees and participants Peter Tonge and Patricia Alfonso San-Segundo for their enthusiasm and valuable contributions. We look forward to seeing you at future editions and continuing to advance drug discovery together! 😀 #ACS #MedChem #Innovation #MedicinalChemistry #Research #KineticSelectivity #DrugDesign #covalentinhibitors

Don't miss our workshop "𝐊𝐢𝐧𝐞𝐭𝐢𝐜 𝐒𝐞𝐥𝐞𝐜𝐭𝐢𝐯𝐢𝐭𝐲: 𝐚 𝐌𝐢𝐬𝐬𝐞𝐝 𝐎𝐩𝐩𝐨𝐫𝐭𝐮𝐧𝐢𝐭𝐲 𝐢𝐧 𝐃𝐫𝐮𝐠 𝐃𝐞𝐬𝐢𝐠𝐧?" at the #ACS National Medicinal Chemistry Symposium. 📅 Date: June 26, 2024, at 12:15 PM. 📍 Location: Session 6 - A Medicinal Chemist’s Toolbox Why you can’t miss our workshop: ✅ Learn how drug safety hinges not only on affinity but also on drug kinetic profiles. ✅ Discover how to maximize therapeutic windows by modifying on- and off-target kinetics earlier, building greater safety margins, and reducing adverse events using KINETICfinder®. ✅ Find out how to simplify and enhance covalent drug design using COVALfinder®. Don’t miss this opportunity to gain valuable insights and enhance your medicinal chemistry toolkit!