Evidence map›Paper›PMID 29466002›Full record

ArticleJournal of medicinal chemistry2018

Development of Potent Inhibitors of Receptor Tyrosine Kinases by Ligand-Based Drug Design and Target-Biased Phenotypic Screening.

Samuel H Myers, Carolin Temps, Douglas R Houston, Valerie G Brunton, Asier Unciti-Broceta

Abstract read
In one paragraph

Article in Journal of medicinal chemistry, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.

0numbers the graph read from it
0cells of the map it votes in
9citing 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

9 citing papers in PubMed.

  1. Novel 6-aryl-1-(3,4,5-trimethoxyphenyl)-1Journal of enzyme inhibition and medicinal chemistry · 2026
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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

5 authors.

Samuel H MyersCancer Research UK Edinburgh Centre, MRC Institute of Genetics and Molecular Medicine , University of Edinburgh , Crewe Road South , Edinburgh EH4 2XR , U.K.
Carolin TempsCancer Research UK Edinburgh Centre, MRC Institute of Genetics and Molecular Medicine , University of Edinburgh , Crewe Road South , Edinburgh EH4 2XR , U.K.
Douglas R HoustonInstitute of Quantitative Biology, Biochemistry and Biotechnology , University of Edinburgh , Edinburgh EH9 3BF , U.K.
Valerie G BruntonCancer Research UK Edinburgh Centre, MRC Institute of Genetics and Molecular Medicine , University of Edinburgh , Crewe Road South , Edinburgh EH4 2XR , U.K.
Asier Unciti-BrocetaCancer Research UK Edinburgh Centre, MRC Institute of Genetics and Molecular Medicine , University of Edinburgh , Crewe Road South , Edinburgh EH4 2XR , U.K.ORCID 0000-0003-1029-2855

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Pyrazolopyrimidines with potent antiproliferative properties were developed by an adaptive strategy that applies ligand-based design and phenotypic screening iteratively and is informed by biochemical assays. To drive development toward specific oncopathways, compounds were tested against cancer cells that overexpress, or not, AXL kinase. Identified phenotypic hits were found to inhibit oncotargets AXL, RET, and FLT3. Subsequent optimization generated antiproliferative lead compounds with unique selectivity profiles, including selective AXL inhibitors and a highly potent inhibitor of FLT3.

Indexed as

Antineoplastic AgentsAxl Receptor Tyrosine KinaseCell Line, TumorCell SurvivalDrug DesignDrug Evaluation, Preclinicalfms-Like Tyrosine Kinase 3HumansLigandsProtein Kinase InhibitorsProto-Oncogene ProteinsPyrazolesPyrimidinesReceptor Protein-Tyrosine KinasesAntineoplastic AgentsAXL protein, humanAxl Receptor Tyrosine Kinasefms-Like Tyrosine Kinase 3LigandsProtein Kinase InhibitorsProto-Oncogene ProteinsPyrazolespyrazolylpyrimidinePyrimidinesReceptor Protein-Tyrosine Kinases

Identifiers

PMID29466002
PMCPMC5851644

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.