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Drug Discovery

The identification and development of new therapeutic compounds, including target identification, lead optimization, high-throughput screening, and computational drug design

5 papers

Papers

Scaffold-Conditioned Preference Triplets for Controllable Molecular Optimization with Large Language Models

The paper introduces Scaffold-Conditioned Preference Triplets (SCPT), a novel pipeline that trains large language models (LLMs) to perform molecular optimization. SCPT enables LLMs to make property-improving edits to molecules while preserving their core structural scaffold, a crucial aspect of drug discovery. The method significantly outperforms non-LLM baselines in scaffold preservation and demonstrates strong compositional generalization to unseen multi-property optimization tasks.

Drug Discovery Apr 16, 01:32 PM

From Water Networks to Binding Affinities: Resolving Solvation Dynamics for Accurate Protein-Ligand Predictions

This computational study introduces Lambda-ABF-OPES, a novel enhanced sampling method that accurately models water dynamics to improve protein-ligand binding affinity predictions. The approach, which shows good agreement with experimental data and significantly increases efficiency, could accelerate drug discovery. However, two authors are co-founders of Qubit Pharmaceuticals, which could directly benefit from this technology.

Drug Discovery Oct 22, 04:20 PM

Identification of a Broad-Spectrum Antiviral Small Molecule against Severe Acute Respiratory Syndrome Coronavirus and Ebola, Hendra, and Nipah Viruses by Using a Novel High-Throughput Screening Assay

This in vitro study identified a small molecule, 5705213, and its derivative that inhibit cathepsin L, a protease essential for SARS, Ebola, Hendra, and Nipah virus entry into host cells. The molecules effectively blocked the entry of pseudoviruses carrying viral glycoproteins into mammalian cells, but further research is needed to determine their effectiveness in vivo.

Drug Discovery Sep 12, 05:01 AM