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Potent Heterocyclic Ligands for Human Complement C3a Receptor

Overview of attention for article published in Journal of Medicinal Chemistry, October 2014
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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 (83rd percentile)
  • Good Attention Score compared to outputs of the same age and source (72nd percentile)

Mentioned by

patent
4 patents

Citations

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21 Dimensions

Readers on

mendeley
38 Mendeley
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Title
Potent Heterocyclic Ligands for Human Complement C3a Receptor
Published in
Journal of Medicinal Chemistry, October 2014
DOI 10.1021/jm500956p
Pubmed ID
Authors

Robert C. Reid, Mei-Kwan Yau, Ranee Singh, Johan K. Hamidon, Junxian Lim, Martin J. Stoermer, David P. Fairlie

Abstract

The G-protein coupled receptor (C3aR) for human inflammatory protein complement C3a is an important component of immune, inflammatory, and metabolic diseases. A flexible compound (N2-[(2,2-diphenylethoxy)acetyl]-l-arginine, 4), known as a weak C3aR antagonist (IC50 μM), was transformed here into potent agonists (EC50 nM) of human macrophages (Ca(2+) release in HMDM) by incorporating aromatic heterocycles. Antagonists were also identified. A linear correlation between binding affinity for C3aR and calculated hydrogen-bond interaction energy of the heteroatom indicated that its hydrogen-bonding capacity influenced ligand affinity and function mediated by C3aR. Hydrogen-bond accepting heterocycles (e.g., imidazole) conferred the highest affinity and agonist potency (e.g., 21, EC50 24 nM, Ca(2+), HMDM) with comparable efficacy and immunostimulatory activity as that of C3a in activating human macrophages (Ca(2+), IL1β, TNFα, CCL3). These potent and selective modulators of C3aR, inactivated by a C3aR antagonist, are stable C3a surrogates for interrogating roles for C3aR in physiology and disease.

Mendeley readers

Mendeley readers

The data shown below were compiled from readership statistics for 38 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Japan 1 3%
Germany 1 3%
Unknown 36 95%

Demographic breakdown

Readers by professional status Count As %
Researcher 19 50%
Student > Ph. D. Student 5 13%
Student > Master 4 11%
Other 2 5%
Lecturer > Senior Lecturer 1 3%
Other 1 3%
Unknown 6 16%
Readers by discipline Count As %
Chemistry 24 63%
Medicine and Dentistry 3 8%
Pharmacology, Toxicology and Pharmaceutical Science 2 5%
Neuroscience 2 5%
Psychology 1 3%
Other 2 5%
Unknown 4 11%
Attention Score in Context

Attention Score in Context

This research output has an Altmetric Attention Score of 9. 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 22 February 2024.
All research outputs
#3,520,573
of 23,989,432 outputs
Outputs from Journal of Medicinal Chemistry
#3,336
of 22,557 outputs
Outputs of similar age
#39,959
of 258,785 outputs
Outputs of similar age from Journal of Medicinal Chemistry
#34
of 147 outputs
Altmetric has tracked 23,989,432 research outputs across all sources so far. Compared to these this one has done well and is in the 84th percentile: it's in the top 25% of all research outputs ever tracked by Altmetric.
So far Altmetric has tracked 22,557 research outputs from this source. They typically receive a little more attention than average, with a mean Attention Score of 6.8. This one has gotten more attention than average, scoring higher than 73% 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 258,785 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 83% of its contemporaries.
We're also able to compare this research output to 147 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 72% of its contemporaries.