Artificial intelligence and machine learning approaches for drug design: challenges and opportunities for the pharmaceutical industries

C Selvaraj, I Chandra, SK Singh - Molecular diversity, 2021 - Springer
The global spread of COVID-19 has raised the importance of pharmaceutical drug
development as intractable and hot research. Developing new drug molecules to overcome …

Cell permeability beyond the rule of 5

P Matsson, BC Doak, B Over, J Kihlberg - Advanced drug delivery reviews, 2016 - Elsevier
Drug discovery for difficult targets that have large and flat binding sites is often better suited
to compounds beyond the “rule of 5”(bRo5). However, such compounds carry higher …

ADME properties evaluation in drug discovery: prediction of Caco-2 cell permeability using a combination of NSGA-II and boosting

NN Wang, J Dong, YH Deng, MF Zhu… - Journal of chemical …, 2016 - ACS Publications
The Caco-2 cell monolayer model is a popular surrogate in predicting the in vitro human
intestinal permeability of a drug due to its morphological and functional similarity with human …

Systems pharmacology in drug discovery and therapeutic insight for herbal medicines

C Huang, C Zheng, Y Li, Y Wang, A Lu… - Briefings in …, 2014 - academic.oup.com
Abstract Systems pharmacology is an emerging field that integrates systems biology and
pharmacology to advance the process of drug discovery, development and the …

Drug-permeability and transporter assays in Caco-2 and MDCK cell lines

DA Volpe - Future medicinal chemistry, 2011 - Taylor & Francis
The human colon adenocarcinoma Caco-2 and Madin–Darby canine kidney epithelial cell
lines provide in vitro tools to assess a drug's permeability and transporter interactions during …

Drug Discovery and Regulatory Considerations for Improving In Silico and In Vitro Predictions that Use Caco-2 as a Surrogate for Human Intestinal Permeability …

CA Larregieu, LZ Benet - The AAPS journal, 2013 - Springer
There is a growing need for highly accurate in silico and in vitro predictive models to
facilitate drug discovery and development. Results from in vitro permeation studies across …

The whole is bigger than the sum of its parts: drug transport in the context of two membranes with active efflux

VV Rybenkov, HI Zgurskaya, C Ganguly… - Chemical …, 2021 - ACS Publications
Cell envelope plays a dual role in the life of bacteria by simultaneously protecting it from a
hostile environment and facilitating access to beneficial molecules. At the heart of this ability …

Multivariate analysis in the pharmaceutical industry: enabling process understanding and improvement in the PAT and QbD era

AP Ferreira, M Tobyn - Pharmaceutical development and …, 2015 - Taylor & Francis
In the pharmaceutical industry, chemometrics is rapidly establishing itself as a tool that can
be used at every step of product development and beyond: from early development to …

General theory for multiple input-output perturbations in complex molecular systems. 1. Linear QSPR electronegativity models in physical, organic, and medicinal …

H Gonzalez-Diaz, S Arrasate… - Current topics in …, 2013 - ingentaconnect.com
In general perturbation methods starts with a known exact solution of a problem and add
“small” variation terms in order to approach to a solution for a related problem without known …

Artificial intelligence-based quantitative structure–property relationship model for predicting human intestinal absorption of compounds with serotonergic activity

N Czub, J Szlęk, A Pacławski… - Molecular …, 2023 - ACS Publications
Oral medicines represent the largest pharmaceutical market area. To achieve a therapeutic
effect, a drug must penetrate the intestinal walls, the main absorption site for orally delivered …