Evidence map›Paper›PMID 37859710›Full record

ArticleRSC medicinal chemistry2023

The rational design of ARUK2007145, a dual inhibitor of the α and γ isoforms of the lipid kinase phosphatidylinositol 5-phosphate 4-kinase (PI5P4K).

Gregory G Aldred, Timothy P C Rooney, Henriette M G Willems, Helen K Boffey, Christopher Green, David Winpenny, John Skidmore, Jonathan H Clarke, Stephen P Andrews

Open access · hybridAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in RSC medicinal chemistry, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing papers in PubMed
0.2field-weighted citation impact, top 42% of its field
1 · What the graph read from it

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.

2 · The registry

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.

3 · Its place in the literature

Who cites it

1 citing paper in PubMed, 1 citations in OpenAlex.

  1. Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

9 authors at 1 institution in 1 country.

Gregory G AldredThe ALBORADA Drug Discovery Institute, University of Cambridge Island Research Building, Cambridge Biomedical Campus, Hills Road Cambridge CB2 0AH UK spa26@cam.ac.uk.ORCID https://orcid.org/0009-0007-4974-0818
Timothy P C RooneyThe ALBORADA Drug Discovery Institute, University of Cambridge Island Research Building, Cambridge Biomedical Campus, Hills Road Cambridge CB2 0AH UK spa26@cam.ac.uk.ORCID https://orcid.org/0000-0001-6788-5526
Henriette M G WillemsThe ALBORADA Drug Discovery Institute, University of Cambridge Island Research Building, Cambridge Biomedical Campus, Hills Road Cambridge CB2 0AH UK spa26@cam.ac.uk.ORCID https://orcid.org/0000-0001-7196-5975
Helen K BoffeyThe ALBORADA Drug Discovery Institute, University of Cambridge Island Research Building, Cambridge Biomedical Campus, Hills Road Cambridge CB2 0AH UK spa26@cam.ac.uk.ORCID https://orcid.org/0000-0001-5088-4615
Christopher GreenThe ALBORADA Drug Discovery Institute, University of Cambridge Island Research Building, Cambridge Biomedical Campus, Hills Road Cambridge CB2 0AH UK spa26@cam.ac.uk.ORCID https://orcid.org/0000-0002-4690-7594
David WinpennyThe ALBORADA Drug Discovery Institute, University of Cambridge Island Research Building, Cambridge Biomedical Campus, Hills Road Cambridge CB2 0AH UK spa26@cam.ac.uk.
John SkidmoreThe ALBORADA Drug Discovery Institute, University of Cambridge Island Research Building, Cambridge Biomedical Campus, Hills Road Cambridge CB2 0AH UK spa26@cam.ac.uk.ORCID https://orcid.org/0000-0001-9108-7858
Jonathan H ClarkeThe ALBORADA Drug Discovery Institute, University of Cambridge Island Research Building, Cambridge Biomedical Campus, Hills Road Cambridge CB2 0AH UK spa26@cam.ac.uk.ORCID https://orcid.org/0000-0002-4079-5333
Stephen P AndrewsThe ALBORADA Drug Discovery Institute, University of Cambridge Island Research Building, Cambridge Biomedical Campus, Hills Road Cambridge CB2 0AH UK spa26@cam.ac.uk.ORCID https://orcid.org/0000-0001-6021-6899
University of Cambridge · GB

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

The phosphatidylinositol 5-phosphate 4-kinases (PI5P4Ks) are therapeutic targets for diseases such as cancer, neurodegeneration and immunological disorders as they are key components in regulating cell signalling pathways. In an effort to make probe molecules available for further exploring these targets, we have previously reported PI5P4Kα-selective and PI5P4Kγ-selective ligands. Herein we report the rational design of PI5P4Kα/γ dual inhibitors, using knowledge gained during the development of selective inhibitors for these proteins. ARUK2007145 (39) is disclosed as a potent, cell-active probe molecule with ADMET properties amenable to conducting experiments in cells.

Identifiers

PMID37859710
PMCPMC10583824
OpenAlexW4386107538

What Socratic 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 Socratic graph.