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- Review: Bioisosteres in Drug Design
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- Improved PK profile through fluorine and deuterium incorporation
- Discovery of LX2931 (Sphingosine 1-Phosphate Lyase Inhibitor) & Phase IIa Data
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Tag Archives: CGRP
Discovery of MK-2918 (CGRP Antagonist)
The triptan drugs have been highly successful in the treatment of migraine, but adverse effects and low responder rates in some patients have provided the impetus to develop alternative therapies. Blockers of the calcitonin gene-related peptide (CGRP) receptor have … Continue reading
Posted in GPCR ligands
Tagged ALT, CGRP, hERG, isostere, Merck, migraine, MK-0974, MK-2918, MK-3207, telcagepant, triptan
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Working with Ion Channels
Two recent publications highlight the challenges inherent in the targeting of voltage-gated and ion-gated ion channels. It is only in relatively recent times that technological advances (e.g. higher throughput patch-clamping) have opened up many of these targets to drug discovery … Continue reading
