Integrating QSAR modelling and deep learning in drug discovery: the emergence of deep QSAR

A Tropsha, O Isayev, A Varnek, G Schneider… - Nature Reviews Drug …, 2024 - nature.com
Quantitative structure–activity relationship (QSAR) modelling, an approach that was
introduced 60 years ago, is widely used in computer-aided drug design. In recent years …

[HTML][HTML] Structure-based drug design with geometric deep learning

C Isert, K Atz, G Schneider - Current Opinion in Structural Biology, 2023 - Elsevier
Abstract Structure-based drug design uses three-dimensional geometric information of
macromolecules, such as proteins or nucleic acids, to identify suitable ligands. Geometric …

Hybrid machine learning approach to predict the site selectivity of iridium-catalyzed arene borylation

E Caldeweyher, M Elkin, G Gheibi… - Journal of the …, 2023 - ACS Publications
The borylation of aryl and heteroaryl C–H bonds is valuable for the site-selective
functionalization of C–H bonds in complex molecules. Iridium catalysts ligated by bipyridine …

Dataset design for building models of chemical reactivity

P Raghavan, BC Haas, ME Ruos, J Schleinitz… - ACS Central …, 2023 - ACS Publications
Models can codify our understanding of chemical reactivity and serve a useful purpose in
the development of new synthetic processes via, for example, evaluating hypothetical …

[HTML][HTML] Prospective de novo drug design with deep interactome learning

K Atz, L Cotos, C Isert, M Håkansson, D Focht… - Nature …, 2024 - nature.com
De novo drug design aims to generate molecules from scratch that possess specific
chemical and pharmacological properties. We present a computational approach utilizing …

High-throughput synthesis provides data for predicting molecular properties and reaction success

J Götz, MK Jackl, C Jindakun, AN Marziale, J André… - Science …, 2023 - science.org
The generation of attractive scaffolds for drug discovery efforts requires the expeditious
synthesis of diverse analogues from readily available building blocks. This endeavor …

[HTML][HTML] Predictive Minisci late stage functionalization with transfer learning

E King-Smith, FA Faber, U Reilly, AV Sinitskiy… - Nature …, 2024 - nature.com
Structural diversification of lead molecules is a key component of drug discovery to explore
chemical space. Late-stage functionalizations (LSFs) are versatile methodologies capable of …

[HTML][HTML] Identifying opportunities for late-stage CH alkylation with high-throughput experimentation and in silico reaction screening

DF Nippa, K Atz, AT Müller, J Wolfard, C Isert… - Communications …, 2023 - nature.com
Enhancing the properties of advanced drug candidates is aided by the direct incorporation
of specific chemical groups, avoiding the need to construct the entire compound from the …

A Prompt-Engineered Large Language Model, Deep Learning Workflow for Materials Classification

S Liu, T Wen, ASL Pattamatta, DJ Srolovitz - arXiv preprint arXiv …, 2024 - arxiv.org
With the advent of ChatGPT, large language models (LLMs) have demonstrated
considerable progress across a wide array of domains. Owing to the extensive number of …

[HTML][HTML] Drug discovery and development in the era of artificial intelligence: From machine learning to large language models

S Guan, G Wang - Artificial Intelligence Chemistry, 2024 - Elsevier
Abstract Drug Research and Development (R&D) is a complex and difficult process, and
current drug R&D faces the challenges of long time span, high investment, and high failure …