Machine learning methods for pKa prediction of small molecules: Advances and challenges

J Wu, Y Kang, P Pan, T Hou - Drug Discovery Today, 2022 - Elsevier
The acid–base dissociation constant (pK a) is a fundamental property influencing many
ADMET properties of small molecules. However, rapid and accurate pK a prediction remains …

AI for organic and polymer synthesis

X Hong, Q Yang, K Liao, J Pei, M Chen, F Mo… - Science China …, 2024 - Springer
Recent years have witnessed the transformative impact from the integration of artificial
intelligence with organic and polymer synthesis. This synergy offers innovative and …

Holistic Prediction of the pKa in Diverse Solvents Based on a Machine‐Learning Approach

Q Yang, Y Li, JD Yang, Y Liu, L Zhang… - Angewandte …, 2020 - Wiley Online Library
While many approaches to predict aqueous pKa values exist, the fast and accurate
prediction of non‐aqueous pKa values is still challenging. Based on the iBonD experimental …

On the Accuracy of the Direct Method to Calculate pKa from Electronic Structure Calculations

FR Dutra, CS Silva, R Custodio - The Journal of Physical …, 2020 - ACS Publications
The direct method (HA (soln)⇌ A (soln)–+ H (soln)+) for calculating p K a of monoprotic acids
is as efficient as thermodynamic cycles. A selective adjustment of proton free energy in …

Enhancing water sampling in free energy calculations with grand canonical Monte Carlo

GA Ross, E Russell, Y Deng, C Lu… - Journal of chemical …, 2020 - ACS Publications
The prediction of protein–ligand binding affinities using free energy perturbation (FEP) is
becoming increasingly routine in structure-based drug discovery. Most FEP packages use …

Explainable Graph Neural Networks with Data Augmentation for Predicting pKa of C–H Acids

H An, X Liu, W Cai, X Shao - Journal of Chemical Information and …, 2023 - ACS Publications
The p K a of C–H acids is an important parameter in the fields of organic synthesis, drug
discovery, and materials science. However, the prediction of p K a is still a great challenge …

Rapid evolution of a fragment-like molecule to pan-metallo-beta-lactamase inhibitors: initial leads toward clinical candidates

M Mandal, L Xiao, W Pan, G Scapin, G Li… - Journal of Medicinal …, 2022 - ACS Publications
With the emergence and rapid spreading of NDM-1 and existence of clinically relevant VIM-
1 and IMP-1, discovery of pan inhibitors targeting metallo-beta-lactamases (MBLs) became …

Electrophile–Arene Affinity: An Energy Scale for Evaluating the Thermodynamics of Electrophilic Dearomatization Reactions

WW Zhang, Z Feng, SL You… - The Journal of Organic …, 2024 - ACS Publications
Rational design and development of organic reactions are lofty goals in synthetic chemistry.
Quantitative description of the properties of molecules and reactions by physical organic …

[HTML][HTML] Quantum chemical package Jaguar: A survey of recent developments and unique features

Y Cao, T Balduf, MD Beachy, MC Bennett… - The Journal of …, 2024 - pubs.aip.org
This paper is dedicated to the quantum chemical package Jaguar, which is commercial
software developed and distributed by Schrödinger, Inc. We discuss Jaguar's scientific …

Design, Synthesis, in vitro and in silico Characterization of 2‐Quinolone‐L‐alaninate‐1,2,3‐triazoles as Antimicrobial Agents

O Moussaoui, R Bhadane, R Sghyar, J Ilaš… - …, 2022 - Wiley Online Library
Due to the ever‐increasing antimicrobial resistance there is an urgent need to continuously
design and develop novel antimicrobial agents. Inspired by the broad antibacterial activities …