AI Article Synopsis
- A high-throughput screen identified a non-acidic glycine sulfonamide derivative (2a) that targets the EP(1) receptor with a pK(i) of 6.2.
- Synthesis of analogues enabled a detailed study of how changes in structure affected the activity of the compound.
- This research resulted in a significant improvement in potency, with a 100-fold increase for the recombinant version of the compound.
Article Abstract
A high-throughput screen targeting the EP(1) receptor identified non-acidic glycine sulfonamide derivative 2a with a pK(i) of 6.2. Analogue synthesis allowed a thorough investigation of the structure-activity relationship (SAR) and led to a 100-fold increase in recombinant potency.
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| http://dx.doi.org/10.1016/j.bmcl.2006.12.060 | DOI Listing |
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