<p>The
spatiotemporally resolved monitoring of membrane translocation, <i>e.g.,</i> of drugs or toxins, has been a
long-standing goal. Herein, we introduce the fluorescent artificial
receptor-based membrane assay (FARMA), a facile, label-free method. With FARMA,
the permeation of more than hundred organic compounds (drugs, toxins,
pesticides, neurotransmitters, peptides, etc.) through vesicular phospholipid
bilayer membranes has been monitored in real time (µs-h time scale) and with
high sensitivity (nM-µM concentration), affording permeability coefficients
across an exceptionally large range from 10<sup>–9</sup>‑10<sup>–3</sup> cm s<sup>–1</sup>.
From a fundamental point of view, FARMA constitutes a powerful tool to assess
structure-permeability relationships and to test biophysical models for
membrane passage. From an applied perspective, FARMA can be extended to
high-throughput screening by adaption of the microplate reader format, to
spatial monitoring of membrane permeation by microscopy imaging, and to the compartmentalized
monitoring of enzymatic activity.<b></b></p>