GS-462808 is a late sodium current inhibitor of the cardiac Nav1.5 channel. GS-462808 had lower brain penetration and serendipitously lower activity at the brain isoforms.
PXS-4681A is a powerful, specific, and irreversible inhibitor of semicarbazide-sensitive amine oxidase (SSAO; VAP-1), with an oral activity and a Ki value of 37 nM. It exhibits exceptional selectivity towards related amine oxidases, ion channels, and seven-transmembrane domain receptors. Additionally, PXS-4681A demonstrates potent anti-inflammatory properties.
Chaetomellic acid A is a potent inhibitor of farnesyltransferase in isolated enzyme assays (IC50=55nM) but is inactive in whole cells. Inhibition of farnesyltransferase is selective over geranylgeranyltransferase I and II (IC50=92µM and 34µM respectively).