We performed a high throughput screening (HTS) aimed at assessing the efficacy and potency of a large panel of drugs/compounds targeting various GPCRs for the growth rate inhibition in the following models: two TNBC cell lines (MDA-MB-231 and MDA-MB-468) and two HER2+ BC cell lines (BT474 and SKBR3), sensitive or resistant to lapatinib + trastuzumab, an effective combination of anti-HER2 therapies. This evidence concerns the gene ERBB2 and breast cancer.