Evidence map›Paper›PMID 20512140›Full record

ArticleNature chemical biology2010

A predictive model for drug bioaccumulation and bioactivity in Caenorhabditis elegans.

Andrew R Burns, Iain M Wallace, Jan Wildenhain, Mike Tyers, Guri Giaever, Gary D Bader, Corey Nislow, Sean R Cutler, Peter J Roy

Abstract read
PubMed Publisher
In one paragraph

Article in Nature chemical biology, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 100 papers.

0numbers the graph read from it
0cells of the map it votes in
100citing papers in PubMed
4.4field-weighted citation impact, top 3% 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

100 citing papers in PubMed, 189 citations in OpenAlex.

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  11. Chemical Genetics inACS chemical biology · 2024
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  19. Article
  20. Article

40 more citing papers are in PubMed but not listed here.

4 · The record

Corrections and comments

5 · Who and what money

Authors and funding

9 authors at 3 institutions in 3 countries.

Andrew R BurnsDepartment of Molecular Genetics, University of Toronto, Toronto, Ontario, Canada.
Iain M Wallace
Jan Wildenhain
Mike Tyers
Guri Giaever
Gary D Bader
Corey Nislow
Sean R Cutler
Peter J Roy
University of Toronto · CAMount Sinai Hospital · CAUniversity of California, Riverside · US

Funding

Canadian Institutes of Health Research 68813Canadian Institutes of Health Research MOP-81340
6 · The paper itself

Abstract

The resistance of Caenorhabditis elegans to pharmacological perturbation limits its use as a screening tool for novel small bioactive molecules. One strategy to improve the hit rate of small-molecule screens is to preselect molecules that have an increased likelihood of reaching their target in the worm. To learn which structures evade the worm's defenses, we performed the first survey of the accumulation and metabolism of over 1,000 commercially available drug-like small molecules in the worm. We discovered that fewer than 10% of these molecules accumulate to concentrations greater than 50% of that present in the worm's environment. Using our dataset, we developed a structure-based accumulation model that identifies compounds with an increased likelihood of bioavailability and bioactivity, and we describe structural features that facilitate small-molecule accumulation in the worm. Preselecting molecules that are more likely to reach a target by first applying our model to the tens of millions of commercially available compounds will undoubtedly increase the success of future small-molecule screens with C. elegans.

Indexed as

AnimalsCaenorhabditis elegansChromatography, High Pressure LiquidDrug Evaluation, PreclinicalModels, BiologicalMolecular StructurePharmaceutical PreparationsStructure-Activity RelationshipPharmaceutical Preparations

Identifiers

PMID20512140
OpenAlexW1997680903

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.