PracticalFrag's profile picture. A blog founded by Teddy Zartler and run by Dan Erlanson for Fragment-based Drug Discovery devotees to discuss non-confidential issues regarding fragments.

Practical_Fragments

@PracticalFrag

A blog founded by Teddy Zartler and run by Dan Erlanson for Fragment-based Drug Discovery devotees to discuss non-confidential issues regarding fragments.

Computational screening tool FrankenROCS starts with promising pairs of fragments, then hunts for commercially available molecules against @EnamineLtd vast catalog. Two mega screens find non-charged hits against the macrodomain of SARS-CoV-2 practicalfragments.blogspot.com/2025/11/search… @fraser_lab


Fragment screen + fragment growing = the makings of a stereospecific chemical probe for RhoGDI2 ligand, a guanine nucleotide dissociation inhibitor practicalfragments.blogspot.com/2025/11/fragme… @ACSPublications


Metal-chelating fragments in pursuit of synthetic lethality yield a chemical probe inhibitor for the endonuclease FEN1 practicalfragments.blogspot.com/2025/10/fragme… @ACSPublications


Is that halogen bond for real? An analysis of >16,000 structures provides a way to score potential halogen interactions between ligands and proteins practicalfragments.blogspot.com/2025/10/checki…


The PAINS of ivermectin - researchers take a closer look at the assays (and drug concentrations) behind the molecule's apparent antiviral activity  practicalfragments.blogspot.com/2025/10/iverme… @ACSPublications


Avidity advantage: TentaGel beads used to identify fragments binding to multimeric proteins. Nifty tricks allow screens on homodimers, with dozens of fragments at a time @ACSPublications practicalfragments.blogspot.com/2025/10/exploi…


CHI's Discovery on Target meeting featured many approaches to screening for covalent hits. Also, techniques and data infrastructure essential to enable both human and machine learning @CHI_Healthtech @genentech @AstraZeneca @moma_tx @thesgconline practicalfragments.blogspot.com/2025/09/twenti…


Structure-informed fragment merging, without an actual X-ray structure.  A picomolar inhibitor against migraine target CGRP: practicalfragments.blogspot.com/2025/09/fragme… @JMedChem @ACSPublications


Ligand efficiency (LE) is helpful for prioritizing non-covalent fragment hits - but what metrics can help rank irreversible ligands? @sciencedirect tackles the problem practicalfragments.blogspot.com/2025/09/covale…


Bifunctional building blocks built to better build out fragment hits: practicalfragments.blogspot.com/2025/09/fragme… @J_A_C_S @UniOfYork


Cooler simulations, refined docking: Thermal Titration Molecular Dynamics(TTMD) protocol modified for fragments correctly identifies binding modes practicalfragments.blogspot.com/2025/09/keepin… @StefanoMoro1965 @JCIM_JCTC


Nice #fragment-to-lead story for KEAP1-NRF2 protein-protein interaction, starring crystallographic screening, structure-based design, and multiple assays to fill the Kelch pocket practicalfragments.blogspot.com/2025/08/fragme… @angew_chem


"Unexpectedly high occurrence of wrong ligands."  Roche team examines > 200 high quality ligand-bound structures for fatty-acid binding proteins to gain lots of useful data, including sources of error practicalfragments.blogspot.com/2025/08/hundre… @ActaCrystD


Researchers inhibit two Mycobacterium tuberculosis enzymes with one compound using fragment screens and linking/merging to inhibit bacterial cholesterol metabolism practicalfragments.blogspot.com/2025/08/fragme… @mads_chem @ACSPublications


Stay clear of fake biology! The Chemical Probe Portal can alert astute researchers to artifacts. Ten years, >1170 compounds, and counting! practicalfragments.blogspot.com/2025/08/the-ch… @Cancer_Cell


An AI aggregator alert for artifact avoidance shows its work. With MEGAN, forewarned is forearmed: practicalfragments.blogspot.com/2025/07/can-ma… @angew_chem


High-throughput crystallography raise an urgent question of how to host data. Proposals from several luminaries, including head of the Protein Data Bank practicalfragments.blogspot.com/2025/07/how-ca… @NatureComms @ManfredSWeiss @nsakaii @DiamondLightSou @proteindatabank


Covalent inhibitors are characterized by a ratio of two constants. @bharath_IGC  explains that considering both, and how one affects the other, could help advance hits on difficult targets: practicalfragments.blogspot.com/2025/07/the-im… @JMedChem @CR_UK @ACSBioMed


Upcoming fragment meet-ups:  An updated list of conferences for the rest of 2025 and into 2026 practicalfragments.blogspot.com/2025/07/fragme… @CHI_Healthtech @FBLDconference @novalix_pharma


Agonists and inverse agonists for metabolic/diabetes target HNF4 (hepatocyte nuclear factor 4) using cell-based optimization of fragments practicalfragments.blogspot.com/2025/06/fragme… @ACSPublications


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