Evidence map›Paper›PMID 25765758›Full record

ArticleEuropean journal of medicinal chemistry2015

Computer aided drug discovery of highly ligand efficient, low molecular weight imidazopyridine analogs as FLT3 inhibitors.

Brendan Frett, Nick McConnell, Catherine C Smith, Yuanxiang Wang, Neil P Shah, Hong-yu Li

Abstract read
In one paragraph

Article in European journal of medicinal chemistry, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.

0numbers the graph read from it
0cells of the map it votes in
10citing 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

10 citing papers in PubMed.

  1. Article
  2. Synthesis of imidazopyridinesRSC advances · 2025
    Article
  3. Article
  4. Article
  5. Article
  6. Article
  7. Article
  8. Article
  9. A practical and efficient approach to imidazo[1,2-Beilstein journal of organic chemistry · 2017
    Article
  10. 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

6 authors.

Brendan FrettCollege of Pharmacy, Department of Pharmacology and Toxicology, The University of Arizona, Tucson, AZ 85721, USA.
Nick McConnellCollege of Pharmacy, Department of Pharmacology and Toxicology, The University of Arizona, Tucson, AZ 85721, USA.
Catherine C SmithDivision of Hematology/Oncology, University of California, San Francisco, CA, USA.
Yuanxiang WangCollege of Pharmacy, Department of Pharmacology and Toxicology, The University of Arizona, Tucson, AZ 85721, USA.
Neil P ShahDivision of Hematology/Oncology, University of California, San Francisco, CA, USA; Helen Diller Family Comprehensive Cancer Center, University of California, San Francisco, CA, USA.
Hong-yu LiCollege of Pharmacy, Department of Pharmacology and Toxicology, The University of Arizona, Tucson, AZ 85721, USA; The University of Arizona Cancer Center, 1515 N Campbell Ave, Tucson, AZ 85724, USA. Electronic address: hongyuli@pharmacy.arizona.edu.

Funding

CHEMISTRY-BIOLOGY INTERFACE TRAINING PROGRAMT32GM008804 · NIGMS · UNIVERSITY OF ARIZONA · PI MONTFORT, WILLIAM R. · 2003 to 2023
$3.9M
Mechanisms of resistance to clinically-effective FLT3 kinase inhibitors in AMLR01CA166616 · NCI · UNIVERSITY OF CALIFORNIA, SAN FRANCISCO · PI SHAH, NEIL P · 2012 to 2016
$1.6M
Investigating Resistance to FLT3 Inhibitors in AMLK08CA187577 · NCI · UNIVERSITY OF CALIFORNIA, SAN FRANCISCO · PI SMITH, CATHERINE CHOY · 2014 to 2017
$703k
NCI NIH HHS 5R01 CA166616-01NCI NIH HHS K08 CA187577NCI NIH HHS R01 CA166616NIGMS NIH HHS 3T32GM008804-10S1NIGMS NIH HHS T32 GM008804
6 · The paper itself

Abstract

The FLT3 kinase represents an attractive target to effectively treat AML. Unfortunately, no FLT3 targeted therapeutic is currently approved. In line with our continued interests in treating kinase related disease for anti-FLT3 mutant activity, we utilized pioneering synthetic methodology in combination with computer aided drug discovery and identified low molecular weight, highly ligand efficient, FLT3 kinase inhibitors. Compounds were analyzed for biochemical inhibition, their ability to selectively inhibit cell proliferation, for FLT3 mutant activity, and preliminary aqueous solubility. Validated hits were discovered that can serve as starting platforms for lead candidates.

Indexed as

Computer-Aided DesignAnimalsCell LineChemistry Techniques, SyntheticDrug DiscoveryDrug Evaluation, Preclinicalfms-Like Tyrosine Kinase 3Libraries, DigitalLigandsMiceMolecular WeightProtein Kinase InhibitorsPyridinesSmall Molecule LibrariesFLT3 protein, humanfms-Like Tyrosine Kinase 3LigandsProtein Kinase InhibitorsPyridinesSmall Molecule LibrariesAMLComputer aided drug discoveryFLT3Kinase inhibitorLigand efficiency

Identifiers

PMID25765758
PMCPMC4666306

What OpenQuestion holds

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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.