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Discovery of a Novel Class of Orally Active Trypanocidal N-Myristoyltransferase Inhibitors

Overview of attention for article published in Journal of Medicinal Chemistry, December 2011
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About this Attention Score

  • In the top 25% of all research outputs scored by Altmetric
  • High Attention Score compared to outputs of the same age (86th percentile)
  • Above-average Attention Score compared to outputs of the same age and source (64th percentile)

Mentioned by

blogs
1 blog
patent
2 patents

Citations

dimensions_citation
95 Dimensions

Readers on

mendeley
112 Mendeley
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Title
Discovery of a Novel Class of Orally Active Trypanocidal N-Myristoyltransferase Inhibitors
Published in
Journal of Medicinal Chemistry, December 2011
DOI 10.1021/jm201091t
Pubmed ID
Authors

Stephen Brand, Laura A. T. Cleghorn, Stuart P. McElroy, David A. Robinson, Victoria C. Smith, Irene Hallyburton, Justin R. Harrison, Neil R. Norcross, Daniel Spinks, Tracy Bayliss, Suzanne Norval, Laste Stojanovski, Leah S. Torrie, Julie A. Frearson, Ruth Brenk, Alan H. Fairlamb, Michael A. J. Ferguson, Kevin D. Read, Paul G. Wyatt, Ian H. Gilbert

Abstract

N-Myristoyltransferase (NMT) represents a promising drug target for human African trypanosomiasis (HAT), which is caused by the parasitic protozoa Trypanosoma brucei. We report the optimization of a high throughput screening hit (1) to give a lead molecule DDD85646 (63), which has potent activity against the enzyme (IC(50) = 2 nM) and T. brucei (EC(50) = 2 nM) in culture. The compound has good oral pharmacokinetics and cures rodent models of peripheral HAT infection. This compound provides an excellent tool for validation of T. brucei NMT as a drug target for HAT as well as a valuable lead for further optimization.

Mendeley readers

Mendeley readers

The data shown below were compiled from readership statistics for 112 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
United Kingdom 1 <1%
India 1 <1%
Argentina 1 <1%
Brazil 1 <1%
Unknown 108 96%

Demographic breakdown

Readers by professional status Count As %
Researcher 27 24%
Student > Ph. D. Student 25 22%
Student > Bachelor 11 10%
Student > Master 9 8%
Professor 5 4%
Other 18 16%
Unknown 17 15%
Readers by discipline Count As %
Chemistry 43 38%
Agricultural and Biological Sciences 22 20%
Pharmacology, Toxicology and Pharmaceutical Science 10 9%
Biochemistry, Genetics and Molecular Biology 8 7%
Medicine and Dentistry 3 3%
Other 7 6%
Unknown 19 17%
Attention Score in Context

Attention Score in Context

This research output has an Altmetric Attention Score of 8. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 11 October 2022.
All research outputs
#3,930,571
of 23,506,079 outputs
Outputs from Journal of Medicinal Chemistry
#6,126
of 22,347 outputs
Outputs of similar age
#32,229
of 244,370 outputs
Outputs of similar age from Journal of Medicinal Chemistry
#42
of 118 outputs
Altmetric has tracked 23,506,079 research outputs across all sources so far. Compared to these this one has done well and is in the 82nd percentile: it's in the top 25% of all research outputs ever tracked by Altmetric.
So far Altmetric has tracked 22,347 research outputs from this source. They typically receive a little more attention than average, with a mean Attention Score of 6.7. This one has gotten more attention than average, scoring higher than 72% of its peers.
Older research outputs will score higher simply because they've had more time to accumulate mentions. To account for age we can compare this Altmetric Attention Score to the 244,370 tracked outputs that were published within six weeks on either side of this one in any source. This one has done well, scoring higher than 86% of its contemporaries.
We're also able to compare this research output to 118 others from the same source and published within six weeks on either side of this one. This one has gotten more attention than average, scoring higher than 64% of its contemporaries.