Discovery of potent T-type calcium channel blocker.

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Seo HN, Choi JY, Choe YJ, Kim Y, Rhim H, Lee SH, Kim J, Joo DJ, Lee JY

Discovery of potent T-type calcium channel blocker.

Bioorg Med Chem Lett. 2007 Nov 1;17(21):5740-3. Epub 2007 Sep 1.

PubMed ID

17869104 [ View in PubMed

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Abstract

The intensive SAR study of 3,4-dihydroquinazoline series led to the most potent compound 10 (KYS05090: IC(50)=41+/-1 nM) against T-type calcium channel and its potency is nearly comparable to that of Kurtoxin. As a small organic molecule, this compound showed the highest blocking activity reported to date.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Mibefradil	Voltage-dependent T-type calcium channel subunit alpha-1G	IC 50 (nM)	1340	N/A	N/A	Details