
Practical_Fragments
@PracticalFrag
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A blog founded by Teddy Zartler and run by Dan Erlanson for Fragment-based Drug Discovery devotees to discuss non-confidential issues regarding fragments.
Joined February 2019
Upcoming fragment meet-ups: An updated list of conferences for the rest of 2025 and into 2026.@CHI_Healthtech @FBLDconference @novalix_pharma.
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Agonists and inverse agonists for metabolic/diabetes target HNF4 (hepatocyte nuclear factor 4) using cell-based optimization of fragments.@ACSPublications.
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Finding ligands for RNA: the enthalpy, the entropy, & the limited benefits of positivity.@ACSPublications.
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Careful, meticulous work on SARS-CoV-2 RNA finds hits, and suggests just how tough these targets could be.@angew_chem.
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Unknown rings are bioactive - researchers sought out previously unmade fragments and matched them with likely protein targets to find tiny actives. Within chemical space, little gems remain to be mined .@ACSPublications @unibern.
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High-throughput crystallography of >1000 crude reaction mixtures screened against oncology target PHIP(2) takes fragment with no activity to mid-micromolar inhibitor.@FrankvonDelft @philbiggin @DiamondLightSou @BiochemOxford @angew_chem @GrosjeanHarold.
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A macrocyle that prefers active KRAS.Fragment screens against active form of cancer target #KRAS lead to macrocycles that exploit a new pocket near the switch I-II pocket.@CRUKScotland @JMedChem @Novartis.
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NMR for FBLD gets a boost via a clever new pulse sequence. Focusing on ligand protons reveals bound structure for KRAS hits.@stem_univie @ETH_en @ETH_DCHAB @nmr900@ETH@J_A_C_S.
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Protein-detect NMR without isotopic labeling.ECHOS-ID technique from @abbvie sheds burdensome requirement but still finds weak binders.@ACSMedChemLett.
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This year's CHI Drug Discovery Chemistry in San Diego featured a wealth of improved techniques for covalent and non-covalent fragment screens, success stories, and enabling chemistries.@CHI_Healthtech.
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Probing the cysteinome: 47 hinge-binding fragments crossed with 47 protein kinases yields potential drug starting points plus some general wisdom.@uni_tue @angew_chem.
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Affinity vs reactivity: how size matters for finding covalent fragment hits.Analysis by @keserulab @ACSPublications.
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Nanodiscs make membrane proteins available for screening. They also find lots of nonspecific binders.Team @ubleiden explores how to avoid artifacts in fragment screens.
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Fragment-screening and intense biological sleuthing leads to a chemical probe for eIF4E, part of a protein complex for oncogenic protein synthesis.@ICR_London @Astex @NatureComms.
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Synthesis without purification still yields clear fragment hits. 'Direct-to-Biology' screens crude reaction mixtures & yields covalent and noncovalent inhibitors of SARS-CoV-2 main protease.@angew_chem @Jake_T_Bush @GSK.
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New technique, PEARLscreen, shrinks amount of protein required for NMR ligand-detected screens by an order of magnitude.@ETH_DBIOL @nmr900 @angew_chem.
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Efficient search of vast chemical space:.Multimillion fragment docking screen yields submicromolar OGG1 inhibitor after just a few dozen synthesized molecules.@CarlssonLab @NatureComms.
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A pro-prodrug targets glioblastoma, and illustrates advantages of fragment-based drug discovery for CNS drugs.@yujungche @MSKCancerCenter @David_hsieh_23 @hrldelias @TaoWang_Jessica @IyerSwatsv.
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