Discovery and hit-to-lead evaluation of piperazine amides as selective, state-dependent NaV1.7 inhibitors
Author:
Affiliation:
1. Department of Medicinal Chemistry
2. Amgen Inc.
3. Cambridge
4. USA
5. Department of Neuroscience
6. Thousand Oaks
7. Department of Pharmacokinetics and Drug Metabolism
8. Department of Molecular Engineering, Amgen Inc.
Abstract
Optimization of a screening hit led to the identification of NaV1.7 inhibitors with a desirable balance of properties.
Publisher
Royal Society of Chemistry (RSC)
Subject
Pharmaceutical Science,Biochemistry,Drug Discovery,Molecular Medicine,Pharmacology,Organic Chemistry
Link
http://pubs.rsc.org/en/content/articlepdf/2017/MD/C6MD00578K
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1. Voltage-Gated Sodium Channels: Structure, Function, Pharmacology, and Clinical Indications
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2. Correlation of Optical and Automated Patch Clamp Electrophysiology for Identification of NaV1.7 Inhibitors;SLAS DISCOVERY: Advancing the Science of Drug Discovery;2020-04-15
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