Synthesis and biological evaluation of 1,4-diazepane derivatives as T-type calcium channel blockers.
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Gu SJ, Lee JK, Pae AN, Chung HJ, Rhim H, Han SY, Min SJ, Cho YS
Synthesis and biological evaluation of 1,4-diazepane derivatives as T-type calcium channel blockers.
Bioorg Med Chem Lett. 2010 May 1;20(9):2705-8. doi: 10.1016/j.bmcl.2010.03.084. Epub 2010 Mar 28.
- PubMed ID
- 20382529 [ View in PubMed]
- Abstract
We have synthesized and biologically evaluated 1,4-diazepane derivatives as T-type calcium channel blockers. In this study, we discovered compound 4s, a potential T-type calcium channel blocker with good selectivity over hERG and N-type calcium channels. In addition, it exhibited favorable pharmacokinetic characteristics for further investigation of T-type calcium channel related diseases.
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- 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