Desaphy, J.

Binding mode information improves fragment docking

Docking is commonly used in drug discovery to predict how ligand binds to protein target.

Jacquemard, C.

Structural Insights on Fragment Binding Mode Conservation

Aiming at a deep understanding of fragment binding to ligandable targets, we performed a large scale analysis of the Protein Data Bank.

Drwal, M. N.

IChem: A Versatile Toolkit for Detecting, Comparing, and Predicting Protein–Ligand Interactions

Abstract Structure-based ligand design requires an exact description of the topology of molecular entities under scrutiny.

Da Silva, F.

Do Fragments and Crystallization Additives Bind Similarly to Drug-like Ligands?

The success of fragment-based drug design (FBDD) hinges upon the optimization of low-molecular-weight compounds (MW < 300 Da) with weak binding affinities to lead compounds with …

Drwal, M. N.

IChemPIC: A Random Forest Classifier of Biological and Crystallographic Protein–Protein Interfaces

Protein–protein interactions are becoming a major focus of academic and pharmaceutical research to identify low molecular weight compounds able to modulate oligomeric signaling …

Da Silva, F.

sc-PDB: a 3D-database of ligandable binding sites—10 years on

The sc-PDB database (available at http://bioinfo-pharma.

Desaphy, J.

Beware of Machine Learning-Based Scoring Functions—On the Danger of Developing Black Boxes

Training machine learning algorithms with protein–ligand descriptors has recently gained considerable attention to predict binding constants from atomic coordinates.

Gabel, J.

sc-PDB-Frag: A Database of Protein–Ligand Interaction Patterns for Bioisosteric Replacements

Bioisosteric replacement plays an important role in medicinal chemistry by keeping the biological activity of a molecule while changing either its core scaffold or substituents, …

Desaphy, J.

Encoding Protein–Ligand Interaction Patterns in Fingerprints and Graphs

We herewith present a novel and universal method to convert protein–ligand coordinates into a simple fingerprint of 210 integers registering the corresponding molecular interaction …

Desaphy, J.

Structural Insights into the Molecular Basis of the Ligand Promiscuity

Selectivity is a key factor in drug development.

Sturm, N.