ArticleJournal of medicinal chemistry2023
Structure-Guided Design and Synthesis of a Pyridazinone Series of
Abstract read
In one paragraph
Article in Journal of medicinal chemistry, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
0numbers the graph read from it
0cells of the map it votes in
11citing papers in PubMed
–field-weighted citation impact
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
11 citing papers in PubMed.
- IID432, a parasite-selective topoisomerase II inhibitor, achieves rapid single-dose parasite clearance in a murine chronic Chagas model.Proceedings of the National Academy of Sciences of the United States of America · 2026Article
- Structure-Guided Optimization of Novel Inhibitors ofJournal of medicinal chemistry · 2026Article
- FMOPhore for hotspot identification and efficient fragment-to-lead growth strategies.Nature communications · 2026Article
- Decoding efficacy and resistance space at a drug binding site.Nature communications · 2026Article
- Article
- Optimization of Species-Selective Reversible Proteasome Inhibitors for the Treatment of Malaria.Journal of medicinal chemistry · 2025Article
- Computationally guided optimization of the antimalarial activity and physicochemical properties of 2,4-diaminopyrimidines.RSC medicinal chemistry · 2025Article
- Structure-activity relationships of 1,5-dihydro-2RSC medicinal chemistry · 2025Article
- Carmaphycin B-Based Proteasome Inhibitors to Treat Human African Trypanosomiasis: Structure-Activity Relationship andACS infectious diseases · 2024Article
- Identification of potent and reversible piperidine carboxamides that are species-selective orally active proteasome inhibitors to treat malaria.Cell chemical biology · 2024Article
- The proteasome as a drug target for treatment of parasitic diseases.Advances in parasitology · 2024Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
41 authors.
Michael G ThomasDrug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH.ORCID 0000-0003-0377-0281
Kate McGonagleDrug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH.ORCID 0000-0001-8485-7180
Paul RowlandGlaxoSmithKline, Chemistry, Medicines Research Centre, Gunnels Wood Road, Stevenage, U.K., SG1 2NY.
David A RobinsonDrug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH.
Peter G DoddDrug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH.
Isabel Camino-DíazGlaxoSmithKline, Discovery DMPK, IVIVT, Severo Ochoa 2, PTM, Tres Cantos, Madrid ES 28760, Spain.
Lorna CampbellDrug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH.
Juan CantizaniGlaxoSmithKline, Global Health R&D, Severo Ochoa 2, PTM, Tres Cantos, Madrid ES 28760, Spain.
Pablo CastañedaGlaxoSmithKline, Discovery DMPK, IVIVT, Severo Ochoa 2, PTM, Tres Cantos, Madrid ES 28760, Spain.
Daniel ConnGlaxoSmithKline, Chemistry, Medicines Research Centre, Gunnels Wood Road, Stevenage, U.K., SG1 2NY.
Peter D CraggsGlaxoSmithKline, Chemistry, Medicines Research Centre, Gunnels Wood Road, Stevenage, U.K., SG1 2NY.
Darren EdwardsDrug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH.
Liam FergusonDrug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH.
Andrew FosberryGlaxoSmithKline, Chemistry, Medicines Research Centre, Gunnels Wood Road, Stevenage, U.K., SG1 2NY.
Laura FrameDrug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH.
Panchali GoswamiGlaxoSmithKline, Chemistry, Medicines Research Centre, Gunnels Wood Road, Stevenage, U.K., SG1 2NY.
Xiao HuDrug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH.
Justyna KorczynskaGlaxoSmithKline, Chemistry, Medicines Research Centre, Gunnels Wood Road, Stevenage, U.K., SG1 2NY.
Lorna MacLeanDrug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH.
Julio MartinGlaxoSmithKline, Global Health R&D, Severo Ochoa 2, PTM, Tres Cantos, Madrid ES 28760, Spain.ORCID 0000-0003-1887-0859
Nicole MutterDrug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH.
Maria Osuna-CabelloDrug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH.
Christy PatersonDrug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH.
Imanol PeñaGlaxoSmithKline, Global Health R&D, Severo Ochoa 2, PTM, Tres Cantos, Madrid ES 28760, Spain.
Erika G PintoDrug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH.
Caterina PontDrug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH.
Jennifer RileyDrug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH.
Yoko ShishikuraDrug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH.
Frederick R C SimeonsDrug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH.
Laste StojanovskiDrug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH.
John ThomasDrug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH.
Karolina WrobelDrug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH.
Robert J YoungBlue Burgundy Ltd, Ampthill, Bedfordshire, U.K., MK45 2AD.
Filip ZmudaDrug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH.ORCID 0000-0003-3710-0622
Fabio ZuccottoDrug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH.
Kevin D ReadDrug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH.ORCID 0000-0002-8536-0130
Ian H GilbertDrug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH.ORCID 0000-0002-5238-1314
Maria MarcoGlaxoSmithKline, Global Health R&D, Severo Ochoa 2, PTM, Tres Cantos, Madrid ES 28760, Spain.ORCID 0000-0002-2442-0021
Timothy J MilesGlaxoSmithKline, Global Health R&D, Severo Ochoa 2, PTM, Tres Cantos, Madrid ES 28760, Spain.ORCID 0000-0001-7407-7404
Pilar ManzanoGlaxoSmithKline, Global Health R&D, Severo Ochoa 2, PTM, Tres Cantos, Madrid ES 28760, Spain.
Manu De RyckerDrug Discovery Unit, University of Dundee, School of Life Sciences, Dow Street, Dundee, U.K., DD1 5EH.ORCID 0000-0002-3171-3519
Funding
Wellcome TrustWellcome Trust 204672/Z/16/ZWellcome Trust 224024/Z/21/Z
Abstract
There is an urgent need for new treatments for Chagas disease, a parasitic infection which mostly impacts South and Central America. We previously reported on the discovery of GSK3494245/DDD01305143, a preclinical candidate for visceral leishmaniasis which acted through inhibition of the
Indexed as
Chagas DiseaseLeishmaniasis, VisceralTrypanocidal AgentsTrypanosoma cruziAnimalsMiceProteasome Endopeptidase ComplexProteasome InhibitorsProteasome Endopeptidase ComplexProteasome InhibitorsTrypanocidal Agents
Identifiers
What OpenQuestion holds
Textmetadata
LicenceCC BY
Read underepoch 390
Registered trials
None linked
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.