Although these crizotinib–GnRH conjugates had potent inhibitory potential on recombinant c-Met kinase and they were able to bind to GnRH-R, the benefit of GnRHR targeting was not clearly proven on the MET-amplified and GnRHR-overexpressing EBC-1 NSCLC cells in vitro. Here, GNRHR is linked to non-small cell lung carcinoma.