Computer-Assisted Selective Optimization of Side-Activities-from Cinalukast to a PPARα Modulator.


Journal

ChemMedChem
ISSN: 1860-7187
Titre abrégé: ChemMedChem
Pays: Germany
ID NLM: 101259013

Informations de publication

Date de publication:
17 07 2019
Historique:
received: 10 05 2019
pubmed: 30 5 2019
medline: 7 7 2020
entrez: 30 5 2019
Statut: ppublish

Résumé

Automated computational analogue design and scoring can speed up hit-to-lead optimization and appears particularly promising in selective optimization of side-activities (SOSA) where possible analogue diversity is confined. Probing this concept, we employed the cysteinyl leukotriene receptor 1 (CysLT

Identifiants

pubmed: 31141287
doi: 10.1002/cmdc.201900286
doi:

Substances chimiques

Leukotriene Antagonists 0
Ligands 0
PPAR alpha 0
Receptors, Leukotriene 0
Small Molecule Libraries 0
Thiazoles 0
cinalukast 5E1O433QAI
leukotriene D4 receptor LRF7RW46ID

Types de publication

Journal Article Research Support, N.I.H., Extramural

Langues

eng

Sous-ensembles de citation

IM

Pagination

1343-1348

Subventions

Organisme : NIGMS NIH HHS
ID : P41 GM103311
Pays : United States

Informations de copyright

© 2019 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.

Auteurs

Julius Pollinger (J)

Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Str. 9, 60438, Frankfurt, Germany.

Simone Schierle (S)

Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Str. 9, 60438, Frankfurt, Germany.

Sebastian Neumann (S)

Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Str. 9, 60438, Frankfurt, Germany.

Julia Ohrndorf (J)

Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Str. 9, 60438, Frankfurt, Germany.

Astrid Kaiser (A)

Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Str. 9, 60438, Frankfurt, Germany.

Daniel Merk (D)

Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Str. 9, 60438, Frankfurt, Germany.

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Classifications MeSH