Evidence map›Paper›PMID 32750526›Full record

ArticleBioorganic & medicinal chemistry letters2020

Discovery, synthesis and characterization of a series of 7-aryl-imidazo[1,2-a]pyridine-3-ylquinolines as activin-like kinase (ALK) inhibitors.

Darren W Engers, Sean R Bollinger, Andrew S Felts, Anish K Vadukoot, Charles H Williams, Anna L Blobaum, Craig W Lindsley, Charles C Hong, Corey R Hopkins

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2020. 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
–field-weighted citation impact
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.

  1. Review
  2. Review
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  4. 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

9 authors.

Darren W EngersWarren Center for Neuroscience Drug Discovery, Vanderbilt University, Nashville, TN 37232, USA.
Sean R BollingerWarren Center for Neuroscience Drug Discovery, Vanderbilt University, Nashville, TN 37232, USA.
Andrew S FeltsWarren Center for Neuroscience Drug Discovery, Vanderbilt University, Nashville, TN 37232, USA.
Anish K VadukootDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Nebraska Medical Center, Omaha, NE 68198-6125, USA.
Charles H WilliamsDivision of Cardiovascular Medicine, University of Maryland School of Medicine, Baltimore, MD 21201, USA.
Anna L BlobaumWarren Center for Neuroscience Drug Discovery, Vanderbilt University, Nashville, TN 37232, USA.
Craig W LindsleyWarren Center for Neuroscience Drug Discovery, Vanderbilt University, Nashville, TN 37232, USA; Department of Pharmacology, Vanderbilt University, Nashville, TN 37232, USA; Department of Chemistry, Vanderbilt University, Nashville, TN 37232, USA; Department of Biochemistry, Vanderbilt University, Nashville, TN 37232, USA.
Charles C HongDivision of Cardiovascular Medicine, University of Maryland School of Medicine, Baltimore, MD 21201, USA.
Corey R HopkinsDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Nebraska Medical Center, Omaha, NE 68198-6125, USA. Electronic address: corey.hopkins@unmc.edu.

Funding

Chemical Genetic Analysis of Vertebrate DevelopmentR01GM118557 · NIGMS · VANDERBILT UNIVERSITY MEDICAL CENTER · PI HONG, CHARLES C · 2016 to 2019
$2.0M
NIGMS NIH HHS R01 GM118557
6 · The paper itself

Abstract

The activin-like kinases are a family of kinases that play important roles in a variety of disease states. Of this class of kinases, ALK2, has been shown by a gain-of-function to be the primary driver of the childhood skeletal disease fibrodysplasia ossificans progressiva (FOP) and more recently the pediatric cancer diffuse intrinsic pontine glioma (DIPG). Herein, we report our efforts to identify a novel imidazo[1,2-a]pyridine scaffold as potent inhibitors of ALK2 with good in vivo pharmacokinetic properties suitable for future animal studies.

Indexed as

Activin Receptors, Type IAnimalsChildDiffuse Intrinsic Pontine GliomaDrug DiscoveryHumansImidazolinesMicrosomes, LiverMutationMyositis OssificansProtein Kinase InhibitorsPyridinesQuinolinesRatsSignal TransductionStructure-Activity RelationshipActivin Receptors, Type IACVR1 protein, humanImidazolinesProtein Kinase InhibitorsPyridinesQuinolinesActivin-like kinase inhibitorsALK2ALK3BMP inhibitors

Identifiers

PMID32750526
PMCPMC7494637

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Registered trials

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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.