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Related Experiment Video

Updated: Jun 27, 2026

High-throughput Screening for Small-molecule Modulators of Inward Rectifier Potassium Channels

High-throughput Screening for Small-molecule Modulators of Inward Rectifier Potassium Channels

Published on: January 27, 2013

Identification of Kir2.1 Inhibitors from a High-Throughput Screen.

Jacob L Bouchard^1,2, Pedro de Andrade Horn^1,2, Yu Nishio^1,2

¹Warren Center for Neuroscience Drug Discovery, Vanderbilt University, Franklin, Tennessee, USA.

Assay and Drug Development Technologies

|February 17, 2026

Summary

This summary is machine-generated.

Researchers screened over 20,000 compounds to find new inward-rectifier potassium channel (Kir) 2.x modulators. They identified novel chemical scaffolds and optimized compounds for improved properties, leading to VU6073995.

Keywords:

Andersen-Tawil syndrome high-throughput screening inward-rectifier potassium channel neuropathic pain

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Last Updated: Jun 27, 2026

High-throughput Screening for Small-molecule Modulators of Inward Rectifier Potassium Channels

High-throughput Screening for Small-molecule Modulators of Inward Rectifier Potassium Channels

Published on: January 27, 2013

Identification of Kinase-substrate Pairs Using High Throughput Screening

Identification of Kinase-substrate Pairs Using High Throughput Screening

Published on: August 29, 2015

Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays

Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays

Published on: October 23, 2019

Area of Science:

Biochemistry
Pharmacology
Molecular Biology

Background:

Inward-rectifier potassium channels (Kir) 2.x are crucial for human health, regulating cardiac action potential, muscle formation, bone development, vasodilation, and neuronal activity.
The high structural similarity among Kir family members presents a significant challenge for developing isoform-selective compounds.
Kir channels are attractive targets for therapeutic intervention, necessitating the development of selective tool compounds.

Purpose of the Study:

To discover novel chemical matter targeting the Kir 2.x channel family.
To identify potent and isoform-selective modulators of Kir 2.x channels.
To optimize initial hits for improved potency and pharmacokinetic properties.

Main Methods:

Conducted a high-throughput screen of over 20,000 compounds from the Vanderbilt Institute of Chemical Biology Discovery Collection.
Verified hits and identified six novel chemical scaffolds.
Performed medicinal chemistry optimization on selected hits (VU0523203, VU0606851) to enhance potency and DMPK properties.

Main Results:

The screen yielded 48 verified hits, including six distinct chemical scaffolds.
Medicinal chemistry efforts led to the identification of VU6073995.
VU6073995 demonstrated modest potency at Kir2.1 and exhibited improved distribution, metabolism, and pharmacokinetic (DMPK) properties compared to ML133.

Conclusions:

Novel chemical scaffolds targeting Kir 2.x channels were discovered through high-throughput screening.
Medicinal chemistry optimization successfully improved the properties of initial hits.
VU6073995 represents a promising starting point for further development of Kir 2.x channel modulators.