Discovery of Crystallizable Organic Semiconductors with Machine Learning

HM Johnson, F Gusev, JT Dull, Y Seo… - Journal of the …, 2024 - ACS Publications
Crystalline organic semiconductors are known to have improved charge carrier mobility and
exciton diffusion length in comparison to their amorphous counterparts. Certain organic …

CACHE Challenge# 1: targeting the WDR domain of LRRK2, a Parkinson's Disease associated protein

F Li, S Ackloo, CH Arrowsmith, F Ban… - Journal of Chemical …, 2024 - ACS Publications
The CACHE challenges are a series of prospective benchmarking exercises to evaluate
progress in the field of computational hit-finding. Here we report the results of the inaugural …

Combined Usage of Ligand-and Structure-based Virtual Screening in the Artificial Intelligence Era

J Dai, Z Zhou, Y Zhao, F Kong, Z Zhai, Z Zhu… - European Journal of …, 2024 - Elsevier
Drug design has always been pursuing techniques with time-and cost-benefits. Virtual
screening, generally classified as ligand-based (LBVS) and structure-based (SBVS) …

CACHE Challenge# 1: Docking with GNINA Is All You Need

I Dunn, S Pirhadi, Y Wang, S Ravindran… - Journal of Chemical …, 2024 - ACS Publications
We describe our winning submission to the first Critical Assessment of Computational Hit-
Finding Experiments (CACHE) challenge. In this challenge, 23 participants employed a …

Active Learning to Select the Most Suitable Reagents and One-Step Organic Chemistry Reactions for Prioritizing Target-Specific Hits from Ultralarge Chemical Spaces

V Kozyrev, F Sindt, D Rognan - Journal of Chemical Information …, 2025 - ACS Publications
Designing chemically novel and synthesizable ligands from the largest possible chemical
space is a major issue in modern drug discovery to identify early hits that are easily …

Characterization of novel small molecule inhibitors of estrogen receptor-activation function 2 (ER-AF2)

J Foo, F Gentile, S Massah, H Morin, K Singh… - Breast Cancer …, 2024 - Springer
Up to 40% of patients with estrogen receptor (ER)-positive breast cancer will develop
resistance against the majority of current ER-directed therapies. Resistance can arise …

An Automated On-The-Fly Optimization of Resource Allocation for High-Throughput Protein-Ligand Binding Free Energy Simulations

SB Koby, E Gutkin, S Patel, M Kurnikova - 2024 - chemrxiv.org
Molecular dynamics simulations to compute protein to small molecule binding free energies
are becoming a valuable tool in the early stages of drug discovery. However, their cost and …

Active Learning Guided Hit Optimization for the Leucine-Rich Repeat Kinase 2 WDR Domain Based on In Silico Ligand Binding Affinities

F Gusev, E Gutkin, F Gentile, F Ban, SB Koby, F Li… - 2024 - chemrxiv.org
The leucine-rich repeat kinase 2 (LRRK2) is the most mutated gene in familial Parkinson's
disease, whose mutations lead to pathogenic hallmarks of the disease. The LRRK2 WDR …

Computing Ligand Binding Free Energy in a Large Flexible Pocket of a Large Protein

E Gutkin, C Narangoda, M Kurnikova - 2024 - chemrxiv.org
Protein-ligand standard binding free energy (SBFE) calculations based on molecular
dynamics simulations have recently emerged as an efficient tool for computer-aided drug …

[PDF][PDF] Computational Approaches in Drug Design

E Gutkin - 2024 - kilthub.cmu.edu
Drug design is a complex multistage process of finding novel compounds for treatment of a
certain disease based on the knowledge of a biological target. Due to high failure rates …