Evidence map›Paper›PMID 26396691›Full record

ArticleACS medicinal chemistry letters2015

Fragment-Based Drug Design of Novel Pyranopyridones as Cell Active and Orally Bioavailable Tankyrase Inhibitors.

Javier de Vicente, Parcharee Tivitmahaisoon, Pamela Berry, David R Bolin, Daisy Carvajal, Wei He, Kuo-Sen Huang, Cheryl Janson, Lena Liang, Christine Lukacs and 5 more

Open access · greenAbstract read
In one paragraph

Article in ACS medicinal chemistry letters, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing papers in PubMed
1.7field-weighted citation impact, top 16% 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

3 citing papers in PubMed, 21 citations in OpenAlex.

  1. Review
  2. Article
  3. Review
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

15 authors.

Javier de VicenteDiscovery Chemistry, Non-clinical Safety, Discovery Technologies, and Discovery Oncology, Small Molecule Research, Pharma Research & Early Development, Hoffmann-La Roche Inc. , pRED, 340 Kingsland Street, Nutley, New Jersey 07110, United States.
Parcharee TivitmahaisoonDiscovery Chemistry, Non-clinical Safety, Discovery Technologies, and Discovery Oncology, Small Molecule Research, Pharma Research & Early Development, Hoffmann-La Roche Inc. , pRED, 340 Kingsland Street, Nutley, New Jersey 07110, United States.
Pamela BerryDiscovery Chemistry, Non-clinical Safety, Discovery Technologies, and Discovery Oncology, Small Molecule Research, Pharma Research & Early Development, Hoffmann-La Roche Inc. , pRED, 340 Kingsland Street, Nutley, New Jersey 07110, United States.
David R BolinDiscovery Chemistry, Non-clinical Safety, Discovery Technologies, and Discovery Oncology, Small Molecule Research, Pharma Research & Early Development, Hoffmann-La Roche Inc. , pRED, 340 Kingsland Street, Nutley, New Jersey 07110, United States.
Daisy CarvajalDiscovery Chemistry, Non-clinical Safety, Discovery Technologies, and Discovery Oncology, Small Molecule Research, Pharma Research & Early Development, Hoffmann-La Roche Inc. , pRED, 340 Kingsland Street, Nutley, New Jersey 07110, United States.
Wei HeDiscovery Chemistry, Non-clinical Safety, Discovery Technologies, and Discovery Oncology, Small Molecule Research, Pharma Research & Early Development, Hoffmann-La Roche Inc. , pRED, 340 Kingsland Street, Nutley, New Jersey 07110, United States.
Kuo-Sen HuangDiscovery Chemistry, Non-clinical Safety, Discovery Technologies, and Discovery Oncology, Small Molecule Research, Pharma Research & Early Development, Hoffmann-La Roche Inc. , pRED, 340 Kingsland Street, Nutley, New Jersey 07110, United States.
Cheryl JansonDiscovery Chemistry, Non-clinical Safety, Discovery Technologies, and Discovery Oncology, Small Molecule Research, Pharma Research & Early Development, Hoffmann-La Roche Inc. , pRED, 340 Kingsland Street, Nutley, New Jersey 07110, United States.
Lena LiangDiscovery Chemistry, Non-clinical Safety, Discovery Technologies, and Discovery Oncology, Small Molecule Research, Pharma Research & Early Development, Hoffmann-La Roche Inc. , pRED, 340 Kingsland Street, Nutley, New Jersey 07110, United States.
Christine LukacsDiscovery Chemistry, Non-clinical Safety, Discovery Technologies, and Discovery Oncology, Small Molecule Research, Pharma Research & Early Development, Hoffmann-La Roche Inc. , pRED, 340 Kingsland Street, Nutley, New Jersey 07110, United States.
Ann PetersenDiscovery Chemistry, Non-clinical Safety, Discovery Technologies, and Discovery Oncology, Small Molecule Research, Pharma Research & Early Development, Hoffmann-La Roche Inc. , pRED, 340 Kingsland Street, Nutley, New Jersey 07110, United States.
Hong QianDiscovery Chemistry, Non-clinical Safety, Discovery Technologies, and Discovery Oncology, Small Molecule Research, Pharma Research & Early Development, Hoffmann-La Roche Inc. , pRED, 340 Kingsland Street, Nutley, New Jersey 07110, United States.
Lin YiDiscovery Chemistry, Non-clinical Safety, Discovery Technologies, and Discovery Oncology, Small Molecule Research, Pharma Research & Early Development, Hoffmann-La Roche Inc. , pRED, 340 Kingsland Street, Nutley, New Jersey 07110, United States.
Yong ZhuangDiscovery Chemistry, Non-clinical Safety, Discovery Technologies, and Discovery Oncology, Small Molecule Research, Pharma Research & Early Development, Hoffmann-La Roche Inc. , pRED, 340 Kingsland Street, Nutley, New Jersey 07110, United States.
Johannes C HermannDiscovery Chemistry, Non-clinical Safety, Discovery Technologies, and Discovery Oncology, Small Molecule Research, Pharma Research & Early Development, Hoffmann-La Roche Inc. , pRED, 340 Kingsland Street, Nutley, New Jersey 07110, United States.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Tankyrase activity has been linked to the regulation of intracellular axin levels, which have been shown to be crucial for the Wnt pathway. Deregulated Wnt signaling is important for the genesis of many diseases including cancer. We describe herein the discovery and development of a new series of tankyrase inhibitors. These pyranopyridones are highly active in various cell-based assays. A fragment/structure based optimization strategy led to a compound with good pharmacokinetic properties that is suitable for in vivo studies and further development.

Indexed as

axinfragment based drug designoncologystructure based drug designTankyrase inhibitorWnt

Identifiers

PMID26396691
PMCPMC4569882
OpenAlexW2198473900

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.