Identification of MCHR1 antagonists with a preclinical safety profile to support clinical evaluation as anti-obesity agents has been a challenge. Our finding that a basic moiety is not required for MCHR1 antagonists to achieve high-affinity allowed us to explore structures less prone to off-target activities such as hERG inhibition. We report the SAR evolution of hydroxylated thienopyrimidinone ethers culminating in the identification of 27 which entered clinical trials as the phosphate ester pro-drug 35 (BMS-830216).
This research output has an Altmetric Attention Score of 16. 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 April 2025.
All research outputs
#2,782,403
of 33,493,714 outputs
Outputs from Journal of Medicinal Chemistry
#1,991
of 27,334 outputs
Outputs of similar age
#24,336
of 275,693 outputs
Outputs of similar age from Journal of Medicinal Chemistry
#18
of 150 outputs
Altmetric has tracked 33,493,714 research outputs across all sources so far. Compared to these this one has done particularly well and is in the 91st percentile: it's in the top 10% of all research outputs ever tracked by Altmetric.
So far Altmetric has tracked 27,334 research outputs from this source. They typically receive more attention than average, with a mean Attention Score of 8.1. This one has done particularly well, scoring higher than 92% 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 275,693 tracked outputs that were published within six weeks on either side of this one in any source. This one has done particularly well, scoring higher than 91% of its contemporaries.
We're also able to compare this research output to 150 others from the same source and published within six weeks on either side of this one. This one has done well, scoring higher than 86% of its contemporaries.
