Evidence map›Paper›PMID 38116421›Full record

ArticleACS medicinal chemistry letters2023

Fragment-Based Screening Identifies New Quinazolinone-Based Inositol Hexakisphosphate Kinase (IP6K) Inhibitors.

Tyler Heitmann, Gangling Liao, Pablo de León, Glen Ernst, Ingrid Buchler, Huijun Wei, Evgeny Shlevkov, Dean Brown, Martina Fitzek, Matthew Collier and 2 more

Open access · greenAbstract read
In one paragraph

Article in ACS medicinal chemistry letters, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing papers in PubMed
1.1field-weighted citation impact, top 22% 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

4 citing papers in PubMed, 7 citations in OpenAlex.

  1. Review
  2. Review
  3. Article
  4. Enabling Technologies for the Dissection of Inositol Pyrophosphate Physiology.Methods in molecular biology (Clifton, N.J.) · 2025
    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

12 authors at 5 institutions in 3 countries.

Tyler HeitmannLieber Institute for Brain Development, 855 North Wolfe Street, Baltimore, Maryland 21205, United States.
Gangling LiaoLieber Institute for Brain Development, 855 North Wolfe Street, Baltimore, Maryland 21205, United States.
Pablo de LeónLieber Institute for Brain Development, 855 North Wolfe Street, Baltimore, Maryland 21205, United States.
Glen ErnstLieber Institute for Brain Development, 855 North Wolfe Street, Baltimore, Maryland 21205, United States.
Ingrid BuchlerLieber Institute for Brain Development, 855 North Wolfe Street, Baltimore, Maryland 21205, United States.
Huijun WeiLieber Institute for Brain Development, 855 North Wolfe Street, Baltimore, Maryland 21205, United States.
Evgeny ShlevkovLieber Institute for Brain Development, 855 North Wolfe Street, Baltimore, Maryland 21205, United States.
Dean BrownHit Discovery, Discovery Sciences, R&D, AstraZeneca, Boston, Massachusetts 02451, United States.ORCID https://orcid.org/0000-0002-7130-3928
Martina FitzekHit Discovery, Discovery Sciences, R&D, AstraZeneca, Alderley Park, Macclesfield SK10 4TG, U.K.
Matthew CollierHit Discovery, Discovery Sciences, R&D, AstraZeneca, Alderley Park, Macclesfield SK10 4TG, U.K.
David M SmithEmerging Innovations Unit, Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K.
James C BarrowLieber Institute for Brain Development, 855 North Wolfe Street, Baltimore, Maryland 21205, United States.ORCID https://orcid.org/0000-0001-5115-9300
Lieber Institute for Brain Development · USAstraZeneca (United Kingdom) · GBJohns Hopkins University · USAstraZeneca (Poland) · PLAstraZeneca (United States) · US

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

A high-throughput fragment-based screen has been employed to discover a series of quinazolinone inositol hexakisphosphate kinase (IP6K) inhibitors. IP6Ks have been studied for their role in glucose homeostasis, metabolic disease, fatty liver disease, chronic kidney disease, blood coagulation, neurological development, and psychiatric disease. IP6Ks phosphorylate inositol hexakisphosphate (IP6) to form pyrophosphate 5-diphospho-1,2,3,4,6-pentakisphosphate (IP7). Molecular docking studies and investigation of structure-activity relationships around the quinazolinone core resulted in compounds with submicromolar potency and interesting selectivity for IP6K1 versus the closely related IP6K2 and IP6K3 isoforms.

Identifiers

PMID38116421
PMCPMC10726443
OpenAlexW4389076212

What OpenQuestion holds

Textmetadata
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.