Dataset for quantum-mechanical exploration of conformers and solvent effects in large drug-like molecules.


Journal

Scientific data
ISSN: 2052-4463
Titre abrégé: Sci Data
Pays: England
ID NLM: 101640192

Informations de publication

Date de publication:
07 Jul 2024
Historique:
received: 18 03 2024
accepted: 13 06 2024
medline: 8 7 2024
pubmed: 8 7 2024
entrez: 7 7 2024
Statut: epublish

Résumé

We here introduce the Aquamarine (AQM) dataset, an extensive quantum-mechanical (QM) dataset that contains the structural and electronic information of 59,783 low-and high-energy conformers of 1,653 molecules with a total number of atoms ranging from 2 to 92 (mean: 50.9), and containing up to 54 (mean: 28.2) non-hydrogen atoms. To gain insights into the solvent effects as well as collective dispersion interactions for drug-like molecules, we have performed QM calculations supplemented with a treatment of many-body dispersion (MBD) interactions of structures and properties in the gas phase and implicit water. Thus, AQM contains over 40 global and local physicochemical properties (including ground-state and response properties) per conformer computed at the tightly converged PBE0+MBD level of theory for gas-phase molecules, whereas PBE0+MBD with the modified Poisson-Boltzmann (MPB) model of water was used for solvated molecules. By addressing both molecule-solvent and dispersion interactions, AQM dataset can serve as a challenging benchmark for state-of-the-art machine learning methods for property modeling and de novo generation of large (solvated) molecules with pharmaceutical and biological relevance.

Identifiants

pubmed: 38972891
doi: 10.1038/s41597-024-03521-8
pii: 10.1038/s41597-024-03521-8
doi:

Substances chimiques

Solvents 0
Pharmaceutical Preparations 0
Water 059QF0KO0R

Types de publication

Journal Article Dataset

Langues

eng

Sous-ensembles de citation

IM

Pagination

742

Subventions

Organisme : Janssen Pharmaceuticals (Janssen Pharmaceuticals, Inc.)
ID : Aquamarine
Organisme : Janssen Pharmaceuticals (Janssen Pharmaceuticals, Inc.)
ID : Aquamarine
Organisme : EC | Horizon 2020 Framework Programme (EU Framework Programme for Research and Innovation H2020)
ID : 956832
Organisme : EC | Horizon 2020 Framework Programme (EU Framework Programme for Research and Innovation H2020)
ID : 956832
Organisme : Janssen Pharmaceuticals (Janssen Pharmaceuticals, Inc.)
ID : Aquamarine
Organisme : Janssen Pharmaceuticals (Janssen Pharmaceuticals, Inc.)
ID : Aquamarine
Organisme : Janssen Pharmaceuticals (Janssen Pharmaceuticals, Inc.)
ID : Aquamarine
Organisme : Janssen Pharmaceuticals (Janssen Pharmaceuticals, Inc.)
ID : Aquamarine
Organisme : Janssen Pharmaceuticals (Janssen Pharmaceuticals, Inc.)
ID : Aquamarine
Organisme : Janssen Pharmaceuticals (Janssen Pharmaceuticals, Inc.)
ID : Aquamarine
Organisme : Janssen Pharmaceuticals (Janssen Pharmaceuticals, Inc.)
ID : Aquamarine

Informations de copyright

© 2024. The Author(s).

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Fallani, A., Medrano Sandonas, L. & Tkatchenko, A. Enabling inverse design in chemical compound space: Mapping quantum properties to structures for small organic molecules. ArXiv https://doi.org/10.48550/arXiv.2309.00506 (2023).

Auteurs

Leonardo Medrano Sandonas (L)

Department of Physics and Materials Science, University of Luxembourg, L-1511, Luxembourg City, Luxembourg. leonardo.medrano@tu-dresden.de.
Institute for Materials Science and Max Bergmann Center of Biomaterials, TU Dresden, 01062, Dresden, Germany. leonardo.medrano@tu-dresden.de.

Dries Van Rompaey (D)

Drug Discovery Data Sciences (D3S), Janssen Pharmaceutica NV, Turnhoutseweg 30, 2340, Beerse, Belgium. dvanrom1@its.jnj.com.

Alessio Fallani (A)

Department of Physics and Materials Science, University of Luxembourg, L-1511, Luxembourg City, Luxembourg.
Drug Discovery Data Sciences (D3S), Janssen Pharmaceutica NV, Turnhoutseweg 30, 2340, Beerse, Belgium.

Mathias Hilfiker (M)

Department of Physics and Materials Science, University of Luxembourg, L-1511, Luxembourg City, Luxembourg.

David Hahn (D)

Computational Chemistry, Janssen Pharmaceutica NV, Turnhoutseweg 30, 2340, Beerse, Belgium.

Laura Perez-Benito (L)

Computational Chemistry, Janssen Pharmaceutica NV, Turnhoutseweg 30, 2340, Beerse, Belgium.

Jonas Verhoeven (J)

Drug Discovery Data Sciences (D3S), Janssen Pharmaceutica NV, Turnhoutseweg 30, 2340, Beerse, Belgium.

Gary Tresadern (G)

Computational Chemistry, Janssen Pharmaceutica NV, Turnhoutseweg 30, 2340, Beerse, Belgium.

Joerg Kurt Wegner (J)

Drug Discovery Data Sciences (D3S), Janssen Pharmaceutica NV, Turnhoutseweg 30, 2340, Beerse, Belgium.
Drug Discovery Data Sciences (D3S), Johnson & Johnson Innovative Medicine, 301 Binney Street, MA 02142, Cambridge, USA.

Hugo Ceulemans (H)

Drug Discovery Data Sciences (D3S), Janssen Pharmaceutica NV, Turnhoutseweg 30, 2340, Beerse, Belgium.

Alexandre Tkatchenko (A)

Department of Physics and Materials Science, University of Luxembourg, L-1511, Luxembourg City, Luxembourg. alexandre.tkatchenko@uni.lu.

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