The new issue of J. Med. Chem. (https://lnkd.in/dkZcUqN) is out today!! Check out the great content.
Craig Lindsley, Ph.D., FRSC, FASPET, FAAS, FNAI’s Post
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Building Metabolically Stable and Potent Anti-HIV Thioether-Lipid Analogues of Tenofovir Exalidex: A thorough Pharmacological Analysis
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https://lnkd.in/ekXY2-g2 Great Editorial! #JMEDCHEM
Journal of Medicinal Chemistry Collection: Drug Discovery in the UK
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Core Modifications of GSK3335103 toward Orally Bioavailable αvβ6 Inhibitors with Improved Synthetic Tractability
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Our latest collection-drug discovery in the UK https://lnkd.in/e_4ahzMw #JMEDCHEM
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Atypical atoms/functional groups. Do you have a good story with an atypical atom (B, Si, Se, P, etc...) or an atypical functional group (e.g., SF5, SF4 as a linker motif, etc...) and unexpected activity, selectivity or DMPK profile? I would love to feature such work in JMC. #JMEDCHEM
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https://lnkd.in/eH8TXmZX This is a good read and of importance
Classics in Chemical Neuroscience: Medetomidine
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Exo-Cleavable Linkers: Enhanced Stability and Therapeutic Efficacy in Antibody–Drug Conjugates
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Building Metabolically Stable and Potent Anti-HIV Thioether-Lipid Analogues of Tenofovir Exalidex: A thorough Pharmacological Analysis
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Selectivity. What is the right degree of selectivity data to present for a new in vivo tool compound or clinical candidate to feel comfortable with first-in-class target validation and/or safety moving into development? For kinases, we do a full kinome panel, and for GPCRs/ion channels we do a Cerep 44 safety screen and/or a Eurofin 68 target lead profiling panel and a cardiac channel EP panel - in addition to in-house selectivity for key anti-target and close receptor family members. Is this enough? We are only sampling a small portion of pharmacological space. Should metabolites be characterized similarly? Should we be running functional screens versus radioligand binding and only doing functional follow-up for potent binders? Eager to hear folks thoughts and would love to see someone write a Guest Editorial on this topic. #JMEDCHEM
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