Membrane channels span the cellular lipid bilayers to transport ions and molecules into cells with sophisticated properties including high efficiency and selectivity. It is of particular biological importance in developing biomimetic transmembrane channels with unique functions by means of chemically synthetic strategies. An artificial unimolecular transmembrane channel using pore‐containing helical macromolecules is reported. The self‐folding, shape‐persistent, pore‐containing helical macromolecules are able to span the lipid bilayer, and thus result in extraordinary channel stability and high transporting efficiency for protons and cations. The lifetime of this artificial unimolecular channel in the lipid bilayer membrane is impressively long, rivaling those of natural protein channels. Natural channel mimics designed by helically folded polymeric scaffolds will display robust and versatile transport‐related properties at single‐molecule level.

Potassium ion channels specifically transport K ions over Na ions across a cell membrane. A queue of four binding sites in the K channel pore plays significant roles during highly selective conduction. A kind of aromatic helical oligomer was synthesized that can selectively bind K over Na . By aromatic stacking of helical oligomers, a type of artificial K channels with contiguous K binding sites was constructed. Such artificial channels exhibited exceptionally high K /Na selectivity ratios during transmembrane ion conduction.

Semithiobambus[6]uril is shown to be an efficient transmembrane anion transporter. Although all bambusuril analogs (having either O, S or N atoms in their portals) are excellent anion binders, only the sulfur analog is also an effective anion transporter capable of polarizing lipid membranes through selective anion uniport. This notable divergence reflects significant differences in the lipophilic character of the bambusuril analogs.

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