Fig. 1. Discovery and characterization of pan-lysyl oxidase inhibitors, PXS-4787 and PXS-6302.

a Analog generation en route to the discovery of PXS-4787 and PXS-6302. b The measurement of enzymatic inhibitory activity was measured using an Amplex Red oxidation assay, as described previously¹⁶. For compound oxidation assays, the amount of hydrogen peroxide generated at a single concentration (30 µM) of compound relative to DMSO was measured. Minimum of n = 2 for each experiment. *Bovine (aorta) LOX used for analog screening due to ready availability and pharmacological similarity to native human LOX. **Human recombinant LOXL2. ***Human recombinant SSAO. c Jump dilution assay used to measure the irreversible nature of LOXL1 inhibition (LOXL1 was used as a surrogate for LOX owing to similar pharmacology (data are presented as mean ± standard deviation (n = 17 independent experiments for reversible inhibitor, n = 3 for cpd 3, 4 and 8 and n = 22 and 4 for PXS-4787 and PXS-6302 respectively)). Source data are provided as a Source Data file.